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Kinds of Tablets Terms modified by Tablets Selected AbstractsScreening Tablets for DOB Using Surface-Enhanced Raman Spectroscopy,JOURNAL OF FORENSIC SCIENCES, Issue 5 2007Steven E. J. Bell Ph.D. Abstract:, 2,5,-Dimethoxy-4-bromoamphetamine (DOB) is of particular interest among the various "ecstasy" variants because there is an unusually long delay between consumption and effect, which dramatically increases the danger of accidental overdose in users. Screening for DOB in tablets is problematic because it is pharmacologically active at 0.2,3 mg, which is c. 50 times less than 3,4-methylenedioxy-N-methylamphetamine (MDMA) and makes it more difficult to detect in seized tablets using conventional spot tests. The normal Raman spectra of seized DOB tablets are dominated by the bands of the excipient with no evidence of the drug component. Here we report the first use of on-tablet surface-enhanced Raman spectroscopy (SERS) to enhance the signal from a low concentration drug. Raman studies (785-nm excitation) were carried on series of model DOB/lactose tablets (total mass c. 400 mg) containing between 1 mg and 15 ,g of DOB and on seized DOB tablets. To generate surface-enhanced spectra, 5 ,L of centrifuged silver colloid was dispensed onto the upper surface of the tablets, followed by 5 ,L of 1.0 mol/dm3 NaCl. The probe laser was directed onto the treated area and spectra accumulated for c. 20 sec (10 sec × 2). It was found that the enhancement of the DOB component in the model tablets containing 1 mg DOB/tablet and in the seized tablets tested was so large that their spectra were completely dominated by the vibrational bands of DOB with little or no contribution from the unenhanced lactose excipient. Indeed, the most intense DOB band was visible even in tablets containing just 15 ,g of the drug. On-tablet surface-enhanced Raman spectroscopy is a simple method to distinguish between low dose DOB tablets and those with no active constituent. The fact that unique spectra are obtained allows identification of the drug while the lack of sample preparation and short signal accumulation times mean that the entire test can be carried out in <1 min. [source] A randomised comparison of oral desmopressin lyophilisate (MELT) and tablet formulations in children and adolescents with primary nocturnal enuresisINTERNATIONAL JOURNAL OF CLINICAL PRACTICE, Issue 9 2007H. Lottmann Summary Aims:, Desmopressin is a useful treatment for primary nocturnal enuresis (PNE), a common childhood condition that can persist into adolescence. This open-label, randomised, cross-over study evaluated the preference of children and adolescents with PNE for sublingual desmopressin oral lyophilisate (MELT) vs. tablet treatment, and the efficacy, safety, compliance and ease of use associated with each formulation. In total, 221 patients aged 5,15 years who were already receiving desmopressin tablets were randomised 1 : 1 to receive desmopressin treatment in the order MELT/tablet (n = 110) or tablet/MELT (n = 111) for 3 weeks each. Each formulation was administered in bioequivalent doses (0.2/0.4 mg tablets , 120/240 ,g MELT). Following treatment, patients were questioned regarding treatment preference. Diary card data and 100 mm Visual Analogue Scale scores were also recorded. Results:, Overall, patients preferred the MELT formulation to the tablet (56% vs. 44%; p = 0.112). This preference was age dependent (p = 0.006); patients aged < 12 years had a statistically significant preference for desmopressin MELT (p = 0.0089). Efficacy was similar for both formulations (MELT: 1.88 ± 1.94 bedwetting episodes/week; tablet: 1.90 ± 1.85 episodes/week). Ease of use of both formulations was high. Compliance (, 80%) was 94.5% for MELT patients vs. 88.9% for the tablet (p = 0.059). No serious/severe adverse events were reported. Conclusions:, There was an overall preference for the MELT, and a statistically significant preference for desmopressin MELT in children aged 5,11 years. Desmopressin MELT had similar levels of efficacy and safety at lower dosing levels than the tablet, and therefore facilitates early initiation of PNE treatment in children aged 5,6 years. [source] SOY ISOFLAVONE TABLETS REDUCE OSTEOPOROSIS RISK FACTORS AND OBESITY IN MIDDLE-AGED JAPANESE WOMENCLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, Issue 2004Mari Mori Summary 1.,This study examines whether the supplementation of isoflavones (ISO) exerts beneficial effects on the bone mineral density (BMD) measured by dual energy X-ray absorptiometry (DEXA). 2.,Eighty-one healthy Japanese pre- and postmenopausal women were randomly assigned to the following two groups taking either ISO (100 mg) tablets (ISO group) or placebo tablets (P group) containing vitamins C (25 mg) and E (5 mg) daily for 24 weeks in a double-blind placebo controlled parallel design. 3.,Seventy women completed the intervention study (34 on ISO, 36 on P), only ISO group was proven to increase significantly BMD (P < 0.05 vs before) and to significantly decrease body fat measured by the DEXA (P < 0.0001 vs before and P < 0.05 vs P group), while BMI was maintained in ISO group despite significant BMI increase in P group. Thus, percent changes in BMI were significantly different between ISO and P groups (P < 0.05) 24 weeks after the intervention. 4.,This prospective DEXA study confirmed a long-term ISO supplementation, 100 mg/day could not only prevent menopausal bone resorption but also increase BMD and decrease body fat concomitantly with BMI reduction. Enough ISO supplementation may contribute to the risk reduction of osteoporosis and obesity and, thus to overall health promotion in menopausal women. [source] A Biomimetic Potentiometric Sensor Using Molecularly Imprinted Polymer for the Cetirizine Assay in Tablets and Biological FluidsELECTROANALYSIS, Issue 18 2008Mehran Javanbakht Abstract Despite the increasing number of applications of molecularly imprinted polymers (MIPs) in analytical chemistry, the construction of a biomimetic potentiometric sensor remains still challenging. In this work, a biomimetic potentiometric sensor, based on a non-covalent imprinted polymer was fabricated for the recognition and determination of cetirizine. The MIP was synthesized by precipitation polymerization, using cetirizine dihydrochloride as a template molecule, methacrylic acid (MAA) as a functional monomer and ethylene glycol dimethacrylate (EGDMA) as a cross linking agent. The sensor showed high selectivity and a sensitive response to the template in aqueous system. The MIP-modified electrode exhibited Nernstian response (28.0±0.9 mV/decade) in a wide concentration range of 1.0×10,6 to 1.0×10,2 M with a lower detection limit of 7.0×10,7 M. The electrode has response time of ca. 20,s, high performance, high sensitivity, and good long term stability (more than 5,months). The method was satisfactory and used to the cetirizine assay in tablets and biological fluids. [source] Rectal Absorption of Lamotrigine Compressed TabletsEPILEPSIA, Issue 7 2000Angela K. Birnbaum Summary: Purpose: Interruption of oral drug administration poses a significant clinical problem for antiepileptic drugs that have no parenteral formulation. If a drug is absorbed rectally, rectal administration can be a useful alternative when the oral route of administration is not possible. The purpose of this study was to compare the single-dose pharmacokinetics of la-motrigine (LTG) compressed tablets after rectal and oral administration in healthy volunteers. Methods: A single LTG compressed tablet (100 mg) was administered orally and rectally to 12 volunteers in this single-dose, two-period, crossover study with a 2-week washout between doses. For rectal administration, tablets were crushed and suspended in 10 mL of water. Plasma samples were collected from 0 to 120 hr after each dose and analyzed for LTG by an HPLC method developed for this investigation. Results: LTG plasma concentrations were lower after rectal administration versus oral administration. The average area under the curve was 28.90 ± 9.5 ,g/mL/hr after rectal administration and 51.71 ± 19.2 ,g/mL/hr after oral administration. The average maximum LTG concentration was 0.53 ± 0.14 ,g/mL after rectal administration and 1.45 ± 0.35 ,g/mL after oral administration. The relative bioavailability for LTG compressed tablets was 0.63 ± 0.33 for rectal administration. There were no drug-related rashes or serious side effects. Conclusions: LTG suspension prepared from LTG compressed tablets is absorbed rectally, although not to the same extent or rate as when given orally. [source] Capillary Zone Electrophoresis and Micellar Electrokinetic Capillary Chromatography for Determining Water-Soluble Vitamins in Commercial Capsules and TabletsJOURNAL OF FOOD SCIENCE, Issue 1 2001S-C. Su ABSTRACT: A rapid method was developed for simultaneously determining thiamine, riboflavin, pyridoxine, nicotinamide, nicotinic acid, and ascorbic acid. It was tested on 15 samples. The peaks of all components were cleanly separated with good resolution by capillary zone electrophoresis (CZE) and micellar electrokinetic chromatography (MECC). CZE was performed with 0.02 M borate buffer, and MECC was performed with 4% acetonitrile in 0.02 M borate/phosphate buffer containing 0.1 M sodium dodecyl sulfate. Average recoveries for all components were 80.3% to 103.7% with coefficients of variation being less than 5%. Thiamine, nicotinic acid, and pyridoxine contents were consistent with those labeled on the packages, but nicotinamide, riboflavin, and ascorbic acid contents of some samples were less. [source] Screening Tablets for DOB Using Surface-Enhanced Raman Spectroscopy,JOURNAL OF FORENSIC SCIENCES, Issue 5 2007Steven E. J. Bell Ph.D. Abstract:, 2,5,-Dimethoxy-4-bromoamphetamine (DOB) is of particular interest among the various "ecstasy" variants because there is an unusually long delay between consumption and effect, which dramatically increases the danger of accidental overdose in users. Screening for DOB in tablets is problematic because it is pharmacologically active at 0.2,3 mg, which is c. 50 times less than 3,4-methylenedioxy-N-methylamphetamine (MDMA) and makes it more difficult to detect in seized tablets using conventional spot tests. The normal Raman spectra of seized DOB tablets are dominated by the bands of the excipient with no evidence of the drug component. Here we report the first use of on-tablet surface-enhanced Raman spectroscopy (SERS) to enhance the signal from a low concentration drug. Raman studies (785-nm excitation) were carried on series of model DOB/lactose tablets (total mass c. 400 mg) containing between 1 mg and 15 ,g of DOB and on seized DOB tablets. To generate surface-enhanced spectra, 5 ,L of centrifuged silver colloid was dispensed onto the upper surface of the tablets, followed by 5 ,L of 1.0 mol/dm3 NaCl. The probe laser was directed onto the treated area and spectra accumulated for c. 20 sec (10 sec × 2). It was found that the enhancement of the DOB component in the model tablets containing 1 mg DOB/tablet and in the seized tablets tested was so large that their spectra were completely dominated by the vibrational bands of DOB with little or no contribution from the unenhanced lactose excipient. Indeed, the most intense DOB band was visible even in tablets containing just 15 ,g of the drug. On-tablet surface-enhanced Raman spectroscopy is a simple method to distinguish between low dose DOB tablets and those with no active constituent. The fact that unique spectra are obtained allows identification of the drug while the lack of sample preparation and short signal accumulation times mean that the entire test can be carried out in <1 min. [source] Crushed Clopidogrel Administered via Nasogastric Tube Has Faster and Greater Absorption than Oral Whole TabletsJOURNAL OF INTERVENTIONAL CARDIOLOGY, Issue 4 2009M. UROOJ ZAFAR M.B.B.S. Objectives: To compare the absorption of 300 mg clopidogrel administered crushed via nasogastric (NG) tube versus whole tablets taken orally in healthy volunteers. Background: Earlier antiplatelet therapy has proven benefits in treatment of myocardial infarction and in patients undergoing PCI. Aspirin can be delivered early in crushed form via NG tube after CABG surgery to prevent graft occlusion. If clopidogrel given crushed via NG tube provides faster absorption, it could allow earlier clopidogrel loading. Methods: Nine healthy human subjects (34.7 ± 11.1 years, 5 males) were given 300 mg clopidogrel in crushed form via NG tube with 30 mL water after 8 hours of fasting. Plasma levels of the primary circulating inactive clopidogrel metabolite SR26334 were measured after 20 minutes, 40 minutes, 1, 2, 4, 8, 12, and 24 hours of dosing. Following ,2 week washout, same subjects swallowed 300 mg clopidogrel (four 75 mg tablets) after an 8-hour fasting and SR26334 levels were measured at the same time points. Results: Plasma SR26334 concentrations peaked earlier after crushed delivery than after oral intake (44 vs. 70 minutes, P = 0.023) and the median peak was 80% higher (13,083 vs. 7,255 ng/mL, respectively, P = 0.021). At 40 minutes, area under the curve was almost twofold greater with NG administration than oral administration (geometric means ratio = 0.5299, 95% CI = 0.28,0.99, P = 0.048), but was similar over the 24-hour period with both administration methods (geometric means ratio = 1.05, 95% CI = 0.84,1.32, P = 0.646). Conclusions: A 300 mg loading dose of crushed clopidogrel administered via NG tube provides faster and greater bioavailability than an equal dose taken orally as whole tablets. The clinical benefits of this strategy need to be investigated. [source] Development and in vitro evaluation of a mucoadhesive vaginal delivery system for nystatinJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 2 2009Juliane Hombach Abstract The purpose of the present study was to design and evaluate a novel vaginal delivery system for nystatin based on mucoadhesive polymers. L -Cysteine and cysteamine, respectively, were covalently attached to poly(acrylic acid), and the two different thiolated polymers were evaluated in vitro regarding their swelling behavior, mucoadhesive properties and release behavior. Tablets comprising these thiolated polymers and nystatin demonstrated a high stability in vaginal fluid simulant pH 4.2 and an increase in weight by swelling whereas control tablets comprising unmodified poly(acrylic acid) disintegrated and dissolved. The mucoadhesion time of tablets on freshly excised bovine vaginal mucosa on a rotating cylinder and the total work of adhesion of gels and tablets increased significantly due to the formation of disulfide bonds between the thiolated polymer and cysteine rich subdomaines of the mucus layer. The drug nystatin was released more slowly out of thiomer tablets and gels than out of PAA control tablets and gels. Therefore these thiolated polymers are promising delivery systems for nystatin providing a prolonged residence time and a sustained drug release in vitro under physiological relevant conditions. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:555,564, 2009 [source] Formulation and food effects on the oral absorption of a poorly water soluble, highly permeable antiretroviral agentJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 6 2002Bruce J. Aungst Abstract DPC 961 is a low-solubility, high-permeability, second-generation non-nucleoside reverse transcriptase inhibitor. The purpose of these studies was to evaluate the effects of drug substance and formulation variables on DPC 961 oral absorption, and to compare fed and fasted state oral absorption. To accomplish this, groups of four to six dogs were dosed with various formulations of DPC 961 under fasted or fed conditions, and DPC 961 pharmacokinetics were examined. Absolute oral bioavailability, based on i.v. AUC in the same dogs, was 24% after a suspension dose in fasted dogs and was 51% in fed dogs. Bioavailability with an unoptimized tablet formulation was 30% in fasted dogs and 86% in fed dogs. DPC 961 oral absorption was shown to be dependent on drug substance particle size in fasted dogs, after dosing with a tablet formulation where only the drug substance particle size was varied, but there was no difference in fed dogs. AUC and Cmax increased in proportion with increases in tablet strength from 100 to 400 mg, using tablets manufactured from a common granulation. Tablets made with 50 and 66% drug loadings showed similar relative oral bioavailabilities. Tablets prepared with two different polymorphic forms of DPC 961 were also compared, and these were found to be equivalent. These studies provided a useful component of the formulation development process, to help identify and control the variables affecting oral absorption of this potential new therapeutic agent. © 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:1390,1395, 2002 [source] Controlled and complete release of a model poorly water-soluble drug, prednisolone, from hydroxypropyl methylcellulose matrix tablets using (SBE)7m -,-cyclodextrin as a solubilizing agentJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 7 2001Venkatramana M. Rao Abstract Sustained-release formulations such as hydroxypropyl methylcellulose (HPMC)-based hydrophilic matrix tablets of poorly water-soluble drugs often result in incomplete release because of the poor solubility and dissolution rate of the drug in the hydrophilic matrix. Sulfobutylether-,-cyclodextrins ((SBE)7M -,-CDs) have been known to improve the solubility of such drugs by forming inclusion complexes. The present paper deals with the modification of drug release from an HPMC-based matrix tablet of a sparingly water-soluble drug, prednisolone (PDL), using (SBE)7M -,-CD as a solubilizing agent. Tablets were prepared by direct compression of a physically mixed PDL, (SBE)7M -,-CD, and polymer. On exposure to water, an in situ PDL:(SBE)7M -,-CD complex was formed in the gel layer, and enhanced drug release relative to a control formulation was observed (lactose used as the excipient instead of (SBE)7M -,-CD ). Other possible changes due to the incorporation of (SBE)7M -,-CD in the formulation were also probed. Incorporation of (SBE)7M -,-CD lead to a higher water uptake relative to the control (lactose) formulation. For a fixed total tablet weight, polymer type, and loading, the drug release rate appeared to depend on the molar ratio of (SBE)7M -,-CD to PDL and not the absolute amount of (SBE)7M -,-CD present in the matrix tablet. This work shows that incorporation of (SBE)7M -,-CD into the matrix tablets could be considered in designing a sustained-release tablet of poorly water-soluble drugs. © 2001 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 90:807,816, 2001 [source] Oral colonization by Lactobacillus reuteri ATCC 55730 after exposure to probioticsINTERNATIONAL JOURNAL OF PAEDIATRIC DENTISTRY, Issue 5 2009ESBER ÇAGLAR Objective., The aim of this study was to investigate whether Lactobacillus reuteri ATCC 55730 can be detected in the oral cavity after discontinuation of administration of a product prepared with this bacterium. Materials and Methods., The study consisted of three 2-week periods: clearance period, intervention period, and post-treatment period. Twenty-five volunteers consumed a chewable tablet of L. reuteri ATCC 55730 (108 cfu/tablet) during a 14-day trial period. Saliva samples were collected and cultured onto MRS agar after a clearance period of 2 weeks and then daily after a 2-week intervention period for as long as L. reuteri was found. Lactobacillus reuteri colonies were analysed in saliva samples. The analysis was performed using selective media for L. reuteri followed by confirmation using the specific detection of reuterin produced by L. reuteri. Results., The number of L. reuteri carriers decreased gradually, and after 1 week only 8% of the subjects harboured the bacterium. After 5 weeks, L. reuteri was not detected in any of the subjects. Conclusion., Consuming L. reuteri for 2 weeks does not seem to be sufficient for permanent colonization of L. reuteri in the oral cavity. [source] Clinical trial: ulcerative colitis maintenance treatment with 5-ASA: a 1-year, randomized multicentre study comparing MMX® with Asacol®ALIMENTARY PHARMACOLOGY & THERAPEUTICS, Issue 9 2009C. PRANTERA Summary Background, 5-ASA-MMX® (1.2 g/tablet) is a 5-aminosalicylic acid formulation, designed for once-daily dosing in the treatment of ulcerative colitis. Aim, To evaluate the efficacy and safety of 5-ASA-MMX (2.4 g/day, once daily), compared with Asacol® (2.4 g/day, twice daily) in the maintenance of left-sided UC, through a double-blind, double-dummy, parallel-group, randomized, comparator study. Methods, In all, 331 patients with UC were randomized to receive either 5-ASA-MMX 2.4 g/day, once daily, or Asacol 2.4 g/day, twice daily, for 12 months. All patients were in remission for ,1 month prior to the trial, with ,1 documented relapse in the previous year. The co-primary endpoints of this study were the proportion of patients in clinical, and clinical and endoscopic remission following 12 months' treatment. Results, In the intent-to-treat population, excluding those with major protocol deviations, 68.0 and 65.9% patients in the 5-ASA-MMX and Asacol groups, respectively, were in clinical remission (P = 0.69), and 60.9 and 61.7% of patients, respectively, were in clinical and endoscopic remission (P = 0.89). Diary card data revealed statistically significant treatment differences favouring 5-ASA-MMX. Both treatments were similarly tolerated. Conclusions, Once-daily 5-ASA-MMX is similarly effective with a comparable safety profile to Asacol administered twice daily, for the maintenance treatment of ulcerative colitis. [source] Improved glycaemic control with metformin,glibenclamide combined tablet therapy (Glucovance®) in Type 2 diabetic patients inadequately controlled on metforminDIABETIC MEDICINE, Issue 8 2002M. Marre Abstract Aims To evaluate the efficacy and safety of two dosage strengths of a single-tablet metformin,glibenclamide (glyburide) combination, compared with the respective monotherapies, in patients with Type 2 diabetes mellitus (DM) inadequately controlled by metformin monotherapy. Methods In this 16-week, double-blind, multicentre, parallel-group trial, 411 patients were randomized to receive metformin 500 mg, glibenclamide 5 mg, metformin,glibenclamide 500 mg/2.5 mg or metformin,glibenclamide 500 mg/5 mg, titrated with the intention to achieve fasting plasma glucose (FPG) , 7 mmol/l. Results Decreases in glycated haemoglobin (HbA1c) and FPG were greater (P < 0.05) for metformin,glibenclamide 500 mg/2.5 mg (,1.20% and ,2.62 mmol/l) and 500 mg/5 mg (,0.91% and ,2.34 mmol/l), compared with metformin (,0.19% and ,0.57 mmol/l) or glibenclamide (,0.33% and ,0.73 mmol/l). HbA1c < 7% was achieved by 75% and 64% of patients receiving metformin,glibenclamide 500 mg/2.5 mg and 500 mg/5 mg, respectively, compared with 42% for glibenclamide and 38% for metformin (P = 0.001). These benefits were achieved at lower mean doses of metformin or glibenclamide with metformin,glibenclamide 500 mg/2.5 mg and 500 mg/5 mg (1225 mg/6.1 mg and 1170 mg/11.7 mg) than with glibenclamide (13.4 mg) or metformin (1660 mg). Treatment-related serious adverse events occurred in two patients receiving glibenclamide. Plasma lipid profiles were unaffected and mean changes in body weight were , 1.0 kg. Conclusions Intensive management of Type 2 DM with a new metformin,glibenclamide combination tablet improved glycaemic control and facilitated the attainment of glycaemic targets at lower doses of metformin or glibenclamide compared with the respective monotherapies, without compromising tolerability. Diabet. Med. 19, 673,680 (2002) [source] Content of ecstasy in the Netherlands: 1993,2008ADDICTION, Issue 12 2009Neeltje Vogels ABSTRACT Aims The present paper outlines the results of analyses carried out on the content of tablets sold as ecstasy, collected in the Netherlands by the Drugs Information Monitoring System (DIMS) from January 1993 to December 2008. Methods During a period of 16 years, the DIMS analysed the content of 33 006 tablets sold as ecstasy that were handed in by numerous individual (potential) substance users. The DIMS results were compared with the results from various seized tablets to determine whether the DIMS is a monitor of the ecstasy consumer market. Results The DIMS system appears to be a market monitor that gives an accurate reflection of what is actually available on the hidden Dutch ecstasy market. During 16 years of monitoring, the purity [tablets containing only 3,4-methylenedioxymethamphetamine (MDMA)] was lowest around 1997. During this time-period many tablets contained other substances in addition to or instead of MDMA [e.g. 3,4-methylene-dioxyamphetamine (MDA), 3,4-methylene-dioxyethylamphetamine (MDEA) and N-methyl-a-(1,3-benzodixol-5-yl)-2-butamine (MBDB), amphetamine and caffeine]. From 1998 to 2008, the number of high-dose tablets (,106 mg MDMA per tablet) gradually increased. The same holds true for the proportion of tablets that contained only MDMA, reaching the highest levels in 2000 and 2004. After 2004, the purity of ecstasy tablets decreased again, caused mainly by a growing proportion of tablets containing meta-chlorophenylpiperazine (mCPP). Conclusions The DIMS results provide valuable qualitative information on the content of ecstasy tablets in the Netherlands, and its changes throughout the years. Moreover, the results were used for national and international risk assessments and important warning and prevention activities. [source] Analysis of amphetamine-type substances by capillary zone electrophoresis using capacitively coupled contactless conductivity detectionELECTROPHORESIS, Issue 15 2010Rochelle Epple Abstract CE with capacitively coupled contactless conductivity detection (C4D) was employed for the separation and detection of seven amphetamine analogues as well as amphetamine, dextroamphetamine, methamphetamine and 3,4-methylenedioxymethamphetamine. The separation electrolyte was 30,mM hydroxypropyl-,-cyclodextrin (HP,CD) in a 75,mM acetic acid+25,mM sodium acetate buffer adjusted to pH 4.55. Conductivity detection was compared with UV detection using this same electrolyte. Average detection limits for C4D and UV were 1.3 and 1.0,ppm, respectively. The effects of HP,CD concentration and BGE composition on the selectivity of the separation were also investigated. An illicit, street-grade sample of 3,4-methylenedioxymethamphetamine (Ecstasy) and a prescription dextroamphetamine tablet were also analysed. [source] Rectal Absorption of Lamotrigine Compressed TabletsEPILEPSIA, Issue 7 2000Angela K. Birnbaum Summary: Purpose: Interruption of oral drug administration poses a significant clinical problem for antiepileptic drugs that have no parenteral formulation. If a drug is absorbed rectally, rectal administration can be a useful alternative when the oral route of administration is not possible. The purpose of this study was to compare the single-dose pharmacokinetics of la-motrigine (LTG) compressed tablets after rectal and oral administration in healthy volunteers. Methods: A single LTG compressed tablet (100 mg) was administered orally and rectally to 12 volunteers in this single-dose, two-period, crossover study with a 2-week washout between doses. For rectal administration, tablets were crushed and suspended in 10 mL of water. Plasma samples were collected from 0 to 120 hr after each dose and analyzed for LTG by an HPLC method developed for this investigation. Results: LTG plasma concentrations were lower after rectal administration versus oral administration. The average area under the curve was 28.90 ± 9.5 ,g/mL/hr after rectal administration and 51.71 ± 19.2 ,g/mL/hr after oral administration. The average maximum LTG concentration was 0.53 ± 0.14 ,g/mL after rectal administration and 1.45 ± 0.35 ,g/mL after oral administration. The relative bioavailability for LTG compressed tablets was 0.63 ± 0.33 for rectal administration. There were no drug-related rashes or serious side effects. Conclusions: LTG suspension prepared from LTG compressed tablets is absorbed rectally, although not to the same extent or rate as when given orally. [source] Postprandial interstitial insulin concentrations in type 2 diabetes relativesEUROPEAN JOURNAL OF CLINICAL INVESTIGATION, Issue 6 2006M. Sandqvist Abstract Background, An endothelial barrier for the insulin transport from the circulation to the target tissues of insulin has previously been suggested to contribute to insulin resistance. The interstitial insulin concentration (I-insulin) and insulin kinetics following a mixed meal have, however, previously not been characterized in human adipose tissue. Subjects and methods, Eight nondiabetic first-degree relatives (FDR) of type 2 diabetes patients were recruited. Their I-insulin was measured by microdialysis after a test meal with or without oral administration of the insulin secretagogue nateglinide (120 mg). In parallel, adipose tissue blood flow and lipolysis were measured by xenon-clearance and microdialysis, respectively. Results, The I-insulin increased after the test meal, and this response was more prominent on the day the subjects received the nateglinide tablet when compared with the day the subjects received the placebo tablet [I-insulin incremental area under the curve (IAUC) nateglinide 7612 ± 3032 vs. Plac 4682 ± 2613 pmol L,1 min; P < 0·05, mean ± SE]. However, the postprandial I-insulinmax/P-insulinmax ratio was similar on the two test days (nateglinide: 213 ± 62 vs. 501 ± 92 pmol L,1, I/P-ratio: 0·38 ± 0·06 and placebo: 159 ± 39 vs. 410 ± 74 pmol L,1, I/P-ratio: 0·36 ± 0·05). There was no difference in time of onset of insulin action in situ, or responsiveness, when comparing placebo and nateglinide. Conclusions, Microdialysis can now be used to measure the I-insulin in human adipose tissue following a mixed meal. The data also showed that the transendothelial delivery of insulin occurs rapidly, supporting the concept that transcapillary insulin transfer is a nonsaturable process in nondiabetic first-degree relatives of type 2 diabetes patients. [source] A randomized, double-blind, placebo-controlled clinical evaluation of a nicotine sublingual tablet in smoking cessationADDICTION, Issue 8 2000Mats Wallström Aims. Evaluation of the clinical efficacy and safety of a nicotine 2-mg sublingual tablet in smoking cessation. Design. A randomized, double-blind, placebo-controlled study of smokers using the 2-mg tablet for 3-6 months with follow-up to 12 months. Dosing was established according to baseline nicotine dependence, scored on the Fagerström Tolerance Questionnaire (FTQ): FTQ , 7, two tablets/hour (maximum 40/day); FTQ < 7, one tablet/hour (maximum 20/day). Setting. Smoking cessation programme in a department of oral and maxillofacial surgery. Participants. A total of 247 adult smokers, smoking , 10 cigarettes/day for , 3 years, of whom 123 received active and 124 placebo treatment. The study was powered to detect difference at 6 months. Measurements. Efficacy and safety were evaluated at 6 weeks and 3, 6 and 12 months. Self-reported abstinence was verified by exhaled CO < 10 p.p.m. Findings. Success rates for complete abstinence (no slips after 2 weeks) for active vs. placebo were 50% vs. 29% at 6 weeks, 42% vs. 23% at 3 months, 33% vs. 18% at 6 months and 23% vs. 15% at 12 months ( p < 0.001, 0.001, 0.005 and p = 0.14), respectively. Craving during the first 8 days was significantly reduced among highly dependent smokers on active treatment compared to placebo. Baseline mucosal lesions among abstinent subjects were reduced during the treatment period and at the non-treatment follow-up. Adverse events were mild and tolerable, the most common being irritation and soreness in the mouth and throat. Conclusion. The nicotine sublingual tablet increased the smoking cessation rate compared to placebo, reduced craving in highly dependent smokers and was well tolerated. [source] Upper limb movement interruptions are correlated to freezing of gait in Parkinson's diseaseEUROPEAN JOURNAL OF NEUROSCIENCE, Issue 7 2009Alice Nieuwboer Abstract Freezing of gait (FOG) in patients with Parkinson's disease (PD) is a common problem of unknown origin, which possibly reflects a general motor control deficit. We investigated the relationship between the frequency of freezing episodes during gait and during a bimanual task in control and subjects with PD with and without FOG. Group differences in spatiotemporal characteristics were also examined as well as the effects of visual cueing. Twenty patients with PD in the off-phase of the medication cycle and five age-matched controls performed a repetitive drawing task in an anti-phase pattern on a digitizer tablet. The task was offered at two different speeds (comfortable and maximal) and two different amplitudes (small and large) with and without visual cueing. The results showed that freezing episodes in the upper limbs occurred in only 10.4% of patient trials and that their occurrence was correlated with FOG scores (Spearman's rho = 0.64). Overall, few spatiotemporal differences were found between freezers, non-freezers and controls, except for an overshooting of the target amplitude in controls. Effects of visual cueing were largely similar in all groups, except for the variability of relative phase, which decreased in non-freezers and controls, and was unaffected in freezers. Despite the fact that general motor differences between subgroups were small, freezing episodes were manifest during a bimanual repetitive upper limb task and were correlated to FOG. Further study into upper limb movement breakdown is warranted to understand the parallel deficits that lead up to FOG. [source] Flame retardant performance of various UL94 classified materials exposed to external ignition sourcesFIRE AND MATERIALS, Issue 1 2004Sanghyun Hong Abstract The flammability of eight halogen-free styrene resins and one halogen-containing styrene resin was characterized by UL 94 VB, LOI and cone calorimeter tests. Their burning behaviour was also measured when exposed to three external ignition sources (methenamine tablet, candle, paper ball). Five resins were used for 19, monitor housings and the others for 25, TV. The LOI values of UL 94 V-2, V-1 and V-0 rated resins were higher than that of HB. The heat release rate decreased as the UL 94 ratings increased from HB to V-0. When these resins were exposed to three external ignition sources, UL 94 V-1 and V-0 rated resins showed a self-extinguishing property after removal of the fire and did not cause fire growth in either 19, monitor or the 25, TV housings in all cases. However, UL 94 V-2 and HB rated resins were easily ignited and spread fire by dripping burning trickles. The burning rate of V-2 resin was slower than that of HB. Copyright © 2004 John Wiley & Sons, Ltd. [source] Combined therapy of silymarin and desferrioxamine in patients with ,-thalassemia major: a randomized double-blind clinical trialFUNDAMENTAL & CLINICAL PHARMACOLOGY, Issue 3 2009Marjan Gharagozloo Abstract Silymarin, a flavonolignan complex isolated from Silybum marianum, has a strong antioxidant, hepatoprotective, and iron chelating activities. The present study was designed to investigate the therapeutic activity of orally administered silymarin in patients with thalassemia major under conventional iron chelation therapy. A 3-month randomized, double-blind, clinical trial was conducted in 59 ,-thalassemia major patients in two well-matched groups. Patients were randomized to receive a silymarin tablet (140 mg) three times a day plus conventional desferrioxamine therapy. The second group received the same therapy but a placebo tablet instead of silymarin. Clinical laboratory tests were assessed at the beginning and the end of the trial, except for serum ferritin level that was assessed at the middle of the trial as well. Results of this study revealed that the combined therapy was well tolerated and more effective than desferrioxamine in reducing serum ferritin level. Significant improvement in liver alkaline phosphatase and glutathione levels of red blood cells was also observed in silymarin-treated ,-thalassemia patients. However, no significant difference in serum ferritin levels was detected between silymarin and placebo groups after 1.5 and 3 months treatment, probably because of insufficient sample size to detect subtle changes in ferritin levels between groups. This is the first report showing the beneficial effects of silymarin in thalassemia patients and suggests that silymarin in combination with desferrioxamine can be safely and effectively used in the treatment of iron-loaded patients. [source] TRIZAL study: switching from successful HAART to TrizivirTM (abacavir-lamivudine-zidovudine combination tablet): 48 weeks efficacy, safety and adherence resultsHIV MEDICINE, Issue 2 2003C Katlama Objective To assess the antiviral efficacy, safety, and adherence in subjects who switched to TrizivirÔ following long-term HIV-1 RNA suppression. Study design A randomized, open-label, multicentre, 48-week comparative study in subjects who have received two nucleoside reverse transcriptase inhibitors plus a protease inhibitor or an nonnucleoside reverse transcriptase inhibitor or three nucleoside reverse transcriptase inhibitors for at least 6 months, with a history of undetectable plasma HIV-1 RNA since initiation of therapy and plasma viral load of < 50 HIV-1 RNA copies/mL at screening. Methods Subjects were randomized 1:1 to continue their current treatment or to switch to a simplified treatment with TrizivirÔ administered twice daily. Assessments included plasma HIV-1 RNA, lymphocyte counts, clinical laboratory evaluations, adverse events, and adherence to treatment (obtained via subject self-report). Treatment failure was defined as a plasma viral load of , 400 HIV-1 RNA copies/mL on two consecutive occasions or premature discontinuation of randomized treatment. Results At week 48, the proportion of treatment failures in TrizivirÔ arm (23/106, 22%) was noninferior to that observed in continued arm (23/103, 22%) with a treatment difference stratified by prior ART of 1.2%[-10.1; 12.5]. Incidence of adverse events was similar in both treatment groups. The incidence of possible hypersensitivity reaction in the TrizivirÔ arm was 10%. Significant reductions in cholesterol and triglyceride plasma levels were observed in the TrizivirÔ arm (P < 0.001 and P = 0.006, respectively). Conclusion Switching to TrizivirÔ offers a potent and simplified regimen with equivalent efficacy and significant improvement in lipid abnormalities compared to continued triple therapy. [source] Scintigraphy can be used to compare delivery of sore throat formulationsINTERNATIONAL JOURNAL OF CLINICAL PRACTICE, Issue 4 2009M. Limb Summary Aims:, Sore throat (pharyngitis) is commonly treated with over-the-counter lozenges, tablets, sprays and gargles. While the efficacy of the active ingredients has been examined, less is known about the comparative efficacy of the different delivery formats. Methods:, A pilot study was initially performed, followed by an open-label, four-way crossover study in healthy volunteers to quantitatively assess the delivery efficacy of a lozenge, tablet, spray and gargle, using technetium-99m and scintigraphy as a marker of deposition and clearance of the active ingredients. Results:, Initial deposition in the mouth and throat combined was significantly greater for the solid dose forms (lozenge and tablet) than for the spray or gargle. Rates of clearance were initially similar for the tablet and lozenge with low levels of radioactivity present at up to 2 h. At 10 and 20 min, significantly more of the dose remained for the lozenge than for the tablet. The mouth appeared to act as a reservoir for continued clearance to the throat. Discussion and Conclusion:, Scintigraphy is an effective means of quantifying the delivery efficiency, and hence availability, of sore throat medications. The results presented here suggest that both lozenges and tablets offer considerable advantages over sprays or gargles, both in terms of proportion of the dose delivered to the mouth and throat, combined, and clearance from these regions. These delivery formats provide fast, effective and prolonged delivery of active ingredients, highlighting their potential benefits for sore throat medication. [source] A randomised comparison of oral desmopressin lyophilisate (MELT) and tablet formulations in children and adolescents with primary nocturnal enuresisINTERNATIONAL JOURNAL OF CLINICAL PRACTICE, Issue 9 2007H. Lottmann Summary Aims:, Desmopressin is a useful treatment for primary nocturnal enuresis (PNE), a common childhood condition that can persist into adolescence. This open-label, randomised, cross-over study evaluated the preference of children and adolescents with PNE for sublingual desmopressin oral lyophilisate (MELT) vs. tablet treatment, and the efficacy, safety, compliance and ease of use associated with each formulation. In total, 221 patients aged 5,15 years who were already receiving desmopressin tablets were randomised 1 : 1 to receive desmopressin treatment in the order MELT/tablet (n = 110) or tablet/MELT (n = 111) for 3 weeks each. Each formulation was administered in bioequivalent doses (0.2/0.4 mg tablets , 120/240 ,g MELT). Following treatment, patients were questioned regarding treatment preference. Diary card data and 100 mm Visual Analogue Scale scores were also recorded. Results:, Overall, patients preferred the MELT formulation to the tablet (56% vs. 44%; p = 0.112). This preference was age dependent (p = 0.006); patients aged < 12 years had a statistically significant preference for desmopressin MELT (p = 0.0089). Efficacy was similar for both formulations (MELT: 1.88 ± 1.94 bedwetting episodes/week; tablet: 1.90 ± 1.85 episodes/week). Ease of use of both formulations was high. Compliance (, 80%) was 94.5% for MELT patients vs. 88.9% for the tablet (p = 0.059). No serious/severe adverse events were reported. Conclusions:, There was an overall preference for the MELT, and a statistically significant preference for desmopressin MELT in children aged 5,11 years. Desmopressin MELT had similar levels of efficacy and safety at lower dosing levels than the tablet, and therefore facilitates early initiation of PNE treatment in children aged 5,6 years. [source] StriantÔ SR: a novel, effective and convenient testosterone therapy for male hypogonadismINTERNATIONAL JOURNAL OF CLINICAL PRACTICE, Issue 11 2004M. Korbonits Summary StriantÔ SR (marketed as Striant® in the US) is a novel sustained-release mucoadhesive buccal testosterone tablet for the treatment of male hypogonadism. StriantÔ SR restores serum testosterone concentrations to the physiological range within 4 h of application, and steady-state concentrations are achieved within 24 h of twice-daily dosing. In phase III clinical trials, 87,97% of patients using StriantÔ SR achieved 24-h-averaged serum testosterone concentrations within the normal range. In a comparative study, StriantÔ SR was more likely to restore testosterone concentrations to the physiological range than Andropatch®. In a small study, StriantÔ SR produced steady-state testosterone concentrations comparable with those achieved with a testosterone gel (50 mg testosterone). StriantÔ SR was well tolerated, with a low incidence of adverse events and a low discontinuation rate (3.5%) due to adverse events in phase III studies. StriantÔ SR is an effective, well-tolerated, convenient and discreet treatment for male hypogonadism. [source] Oral colonization by Lactobacillus reuteri ATCC 55730 after exposure to probioticsINTERNATIONAL JOURNAL OF PAEDIATRIC DENTISTRY, Issue 5 2009ESBER ÇAGLAR Objective., The aim of this study was to investigate whether Lactobacillus reuteri ATCC 55730 can be detected in the oral cavity after discontinuation of administration of a product prepared with this bacterium. Materials and Methods., The study consisted of three 2-week periods: clearance period, intervention period, and post-treatment period. Twenty-five volunteers consumed a chewable tablet of L. reuteri ATCC 55730 (108 cfu/tablet) during a 14-day trial period. Saliva samples were collected and cultured onto MRS agar after a clearance period of 2 weeks and then daily after a 2-week intervention period for as long as L. reuteri was found. Lactobacillus reuteri colonies were analysed in saliva samples. The analysis was performed using selective media for L. reuteri followed by confirmation using the specific detection of reuterin produced by L. reuteri. Results., The number of L. reuteri carriers decreased gradually, and after 1 week only 8% of the subjects harboured the bacterium. After 5 weeks, L. reuteri was not detected in any of the subjects. Conclusion., Consuming L. reuteri for 2 weeks does not seem to be sufficient for permanent colonization of L. reuteri in the oral cavity. [source] Urinary fluoride excretion in children drinking fluoridated school milkINTERNATIONAL JOURNAL OF PAEDIATRIC DENTISTRY, Issue 4 2000C.E. Ketley Summary.Objective. To determine fluoride excretion under various conditions of fluoride intake and to estimate the fractional urinary excretion of fluoride in individual children participating in a school milk fluoridation scheme. Design. In the first part of the study, individual urine samples were collected from each of eight 4 to 5-year-old children for a continuous period of 55 h. For each child (n = 8) and for each day (n = 3) the maximum urinary fluoride concentration (p.p.m.F), the maximum fluoride excretion rate (,gF/h) and the total daily fluoride excretion (mg) were calculated. The second part of the study was carried out to determine the 24 h fractional percentage of fluoride excreted following administration of a known dose of fluoride in the absence of other sources. Results. Under usual conditions of fluoride intake (i.e. milk containing 0·5 mg fluoride, customary diet and toothbrushing with fluoride toothpaste) the children's daily fluoride excretion was 0·33 mg. The fractional urinary fluoride excretion of a 0·5-mg fluoride tablet was 30%. Conclusions. It is concluded that the children's mean 24 h fluoride excretion was somewhere between that reported in low fluoride conditions and that reported in optimally fluoridated areas. The fractional urinary fluoride excretion was found to be in agreement with the findings of other workers. [source] Use of software to facilitate pharmaceutical formulation,experiences from a tablet formulationJOURNAL OF CHEMOMETRICS, Issue 3-4 2004Nils-Olof Lindberg Abstract This paper exemplifies the benefits of using experimental design together with software to facilitate the formulation of a tablet for specific purposes, from screening to robustness testing. By applying a multivariate design for the screening experiments, many excipients were evaluated in comparatively few experiments. The formulation work was generally based on designed experiments. Most of the experiments were fractional or full factorial designs, generated and evaluated in Modde with the centre point replicated. The robustness of the formulation was evaluated with experimental designs on two different occasions. Tested flavours were found to have limited influence on the important responses, which was key information in order to proceed with that particular composition. The formulation was also robust towards normal batch-to-batch variation of the excipients and the active pharmaceutical ingredient. A process step was investigated and, by applying experimental design and keeping in mind previous findings, important information could be gained from the study. The different studies yielded good and very useful models. Established relationships between design factors and responses provided information that was vital for the project. In cases of poor models, essential information regarding robustness was obtained. Copyright © 2004 John Wiley & Sons, Ltd. [source] Multivariate methods in pharmaceutical applicationsJOURNAL OF CHEMOMETRICS, Issue 3 2002Jon Gabrielsson Abstract This review covers material published within the field of pharmacy in the last five years. Articles concerning experimental design, optimization and applications of multivariate techniques have been published, from factorial designs to multivariate data analysis, and the combination of the two in multivariate design. The number of publications on this topic testifies to the good results obtained in the studies. Much of the published material highlights the usefulness of experimental design, with many articles dealing with optimization, where much effort is spent on getting useful results. Examples of multivariate data analysis are comparatively few, but these methods are gaining in use. The employment of multivariate techniques in different applications has been reviewed. The examples in this review represent just a few of the possible applications with different aims within pharmaceutical applications. A number of companies are using experimental design as a standard tool in preformulation and in combination with response surface modeling. The properties of e.g. a tablet can be optimized to fulfill a well-specified aim such as a specific release profile, hardness, disintegration time etc. However, none of the companies apply multivariate methods in all steps of the drug development process. As this is still very much a growing field, it is only a question of time before experimental design, optimization and multivariate data analysis are implemented throughout the entire formulation process, from performulation to multivariate process control. Copyright ©,2002 John Wiley & Sons, Ltd. [source] | ||||||||||||||||||||||||||||||||||||||||