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Excipients Used (excipient + used)
Selected AbstractsEffect of moisture and pressure on tablet compaction studied with FTIR spectroscopic imagingJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 2 2007Noha Elkhider Abstract FTIR spectroscopic imaging using a diamond ATR accessory has been applied to examine the influence of moisture and compression pressure on the density and components distribution of compacted pharmaceutical tablets. The model drug and excipient used within this study are ibuprofen and hydroxypropylmethylcellulose (HPMC). Chemical images of these compacted tablets were captured in situ without removing the tablet between measurements. A powder mixture of both, drug and excipient, prior to compaction, were subjected to a controlled environment, using a controlled humidity cell. Histograms were plotted to assess the density distribution quantitatively. This FTIR spectroscopic imaging approach enabled both measurement of water sorption and enhanced visualization of the density distribution of the compacted tablets. ©2006 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 96:351,360, 2007 [source] Quantifying the ,hidden' lactose in drugs used for the treatment of gastrointestinal conditionsALIMENTARY PHARMACOLOGY & THERAPEUTICS, Issue 6 2009P. EADALA Summary Background, Lactose intolerance affects 70% of the world population and may result in abdominal and systemic symptoms. Treatment focuses predominantly on the dietary restriction of food products containing lactose. Lactose is the most common form of excipient used in drug formulations and may be overlooked when advising these patients. Aim, To identify and quantify the amount of lactose in medications used for the treatment of gastrointestinal disorders and to identify ,lactose-free' preparations. Methods, Medications used for the treatment of gastrointestinal disorders were identified from the British National Formulary (BNF). Their formulation including excipients was obtained from the Medicines Compendium. The lactose content and quantity in selected medications was measured using high-performance liquid chromatography (HPLC). Results, A wide range of medications prescribed for the treatment of gastrointestinal conditions contain lactose. We have quantified the lactose content in a selection of medications using HPLC. Lactose is present in amounts that may contribute towards symptoms. Lactose-free alternatives were also identified. Conclusions, Lactose is present in a range of medications and may contribute towards symptoms. This may not be recognized by the prescribing doctor as excipients are not listed in the BNF, and the quantity of lactose is not listed on the label or in the accompanying manufacturer's leaflet. [source] Arbutin determination in medicinal plants and creamsINTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 2 2009W. Thongchai Synopsis A simple flow injection (FI) manifold with spectrophotometric detection was fabricated and tested for arbutin determination. It is based on the measurement of a red-coloured product at 514 nm formed by the complexation reaction between arbutin and 4-aminoantipyrine (4-AP) in the presence of hexacyanoferrate (III) in an alkaline medium. On injecting 300 ,L standard solutions at various concentrations of arbutin into the FI system under optimum conditions, a linear calibration graph over the range of 1.0,30.0 ,g mL,1 arbutin was established. It is expressed by the regression equation y = 0.2188 ± 0.0036x + 0.1019 ± 0.0366 (r2 = 0.9990, n = 5). The detection limit (3,) and the limit of quantitation (10,) were 0.04 ,g mL,1 and 0.13 ,g mL,1, respectively. The RSD of intraday and interday precisions were found to be 1.2,1.4% and 1.7,2.7%, respectively. The method was successfully applied in the determination of arbutin in four selected fruits and three commercial whitening cream extracts with the mean recoveries of the added arbutin over the range of 96.2,99.0%. No interference effects from some common excipients used in commercial whitening creams were observed. The method is simple, rapid, selective, accurate, reproducible and relatively inexpensive. Résumé Un collecteur simple pour injection en flux (FI) avec détection spectrométrique a été fabriqué et testé pour le dosage de l'arbutine. Son principe repose sur la mesure à 514 nm du produit rouge formé par la réaction de complexation entre l'arbutine et le 4-aminoantipyrine (4-AP) en présence d'hexacyanoferrate (III) en milieu alcalin. On procède à une injection de 300 ,L des solutions standards à diverses concentrations d'arbutine dans le système FI aux conditions optimales, puis on réalise un graphe de calibration linéaire dans l'intervalle de 1,0 à 30,0 ,g mL,1 d'arbutine. Le graphe correspond à l'équation de régression y = 0.2188 ± 0.0036x + 0.1019 ± 0.0366 (r2 = 0.9990, n = 5). La limite de détection (3,) et la limite de quantification (10,) sont respectivement de 0.04 ,g mL,1 et 0.13 ,g mL,1. La RSD des précisions intra et inter jours sont respectivement de 1.2,1.4% et 1.7,2.7%. La méthode a été appliquée avec succès à la mesure de l'arbutine dans 4 fruits sélectionnés et 3 extraits de crèmes de blanchiment commercialisées avec une recouvrance moyenne de l'arbutine ajoutée de 96.2 à 99%. Aucune interférence avec les excipients communément utilisés dans les crèmes de blanchiment commerciales n'a été observée. La méthode est simple, rapide, sélective, précise, reproductible et relativement bon marché. [source] Technological strategies to improve photostability of a sunscreen agentINTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 2 2006P. Perugini Due to the reduction of the ozone layer, there is an increasing need of effective UV protection systems with minimized side-effects. Trans-2-ethylhexyl- p -methoxycinnamate (trans -EHMC) represents one of the most widely used sunscreen compound. Several studies demonstrated that trans -EHMC is unstable following UV irradiation both in solution and in emulsion formulations. Moreover, various reports of photocontact sensitization induced by trans -EHMC have appeared in the literature. Consequently, in order to ensure adequate efficacy and safety for this sunscreen agent, there is a need for new carrier systems to enhance trans -EHMC photostability. In the present study the photostability of the filter in different formulation types (emulsion,gel, gel and emulsion) with various ingredients is evaluated. In addition, nanoparticles based on poly- D,L -lactide-co-glycolide (PLGA) as carrier for trans -EHMC are investigated. The influence of nanoparticle matrix on the photochemical stability of the sunscreen agent is also presented. The results obtained demonstrated that PLGA nanoparticles are effective in reducing the light-induced degradation of the sunscreen agent. Moreover, the choice of formulation type and the excipients used play an important role in order to obtain a stable cosmetic product containing trans -EHMC. [source] ORIGINAL ARTICLE: Solubilization of vorinostat by cyclodextrinsJOURNAL OF CLINICAL PHARMACY & THERAPEUTICS, Issue 5 2010Y. Y. Cai BSc Summary Background:, Vorinostat (suberoylanilide hydroxamic acid) is the first histone deacetylase inhibitor approved by US FDA for use in oncology. However, as a hydrophobic acid, its limited aqueous solubility poses a problem for parenteral delivery. Such limited solubility may also affect its oral bioavailability. Objective:, The aim of this study was to evaluate whether cyclodextrins (CDs), common excipients used in pharmaceutical industry, could increase the aqueous solubility of vorinostat. Methods:, The actual aqueous solubility of vorinostat was investigated by phase-solubility method. Molecular simulation was employed to predict the interaction energy and preferred orientation of vorinostat in CD cavities. Results:, Phase-solubility studies indicated that the solubility of vorinostat (7·24 × 10,1 mm) was substantially increased when complexed with various CDs, in the following order: randomly methylated-,-cyclodextrin (RM-,-CD) > hydroxypropyl-,-cyclodextrin (HP-,-CD) > ,-cyclodextrin > hydroxypropyl-,-cyclodextrin > Hydroxypropyl-,-cyclodextrin > ,-cyclodextrin. RM-,-CD 300 mm increased vorinostat solubility to 70·8 mm, almost two orders of magnitude higher than the baseline solubility. Such findings were in good agreement with the results obtained from molecular simulation. Conclusion:, CDs, particularly RM-,-CD and HP-,-CD, increased vorinostat's solubility. Future studies could be focused on the application of HP-,-CD in parenteral delivery of vorinostat or using RM-,-CD as an oral absorption enhancer. Molecular simulation appeared to be a useful tool for the selection of appropriate CD as excipient for drug delivery. [source] Biowaiver monographs for immediate release solid oral dosage forms: Amitriptyline hydrochloride,JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 5 2006R.H. Manzo Abstract Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing amitriptyline hydrochloride are reviewed. Its therapeutic uses, its pharmacokinetic properties, the possibility of excipient interactions and reported BE/bioavailability (BA) problems are also taken into consideration. Literature data indicates that amitriptyline hydrochloride is a highly permeable active pharmaceutical ingredient (API). Data on the solubility according to the current Biopharmaceutics Classification System (BCS) were not fully available and consequently amitriptyline hydrochloride could not be definitively assigned to either BCS Class I or BCS Class II. But all evidence taken together, a biowaiver can currently be recommended provided that IR tablets are formulated with excipients used in existing approved products and that the dissolution meets the criteria defined in the Guidances. © 2006 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 95:966,973, 2006 [source] Dodging matrix effects in liquid chromatography tandem mass spectrometric assays,compilation of key learnings and perspectivesBIOMEDICAL CHROMATOGRAPHY, Issue 5 2009Nuggehally R. Srinivas Abstract Triple quad liquid chromatography mass spectrometric assays (LC/MS/MS) have revolutionized the analysis of drug(s)/metabolite(s) with exceptional speed, sensitivity and selectivity features. From inception to date, several new and innovative features have been regularly proposed by researchers to further enhance the value in the applicability of this analytical tool. However, owing to such compressed run times and scanty sample preparation procedures, LC/MS/MS assays that are not fully optimized generally have issues of matrix effects, where ionization potential is either suppressed or enhanced due to the presence of other materials (endogenous/exogenous) in the matrix. By definition, even co-medications, isomeric or isobaric impurities, and drug excipients used in dosing solutions could also potentially contribute to matrix effects. This article captures some of the interesting work carried out by researchers to understand and handle matrix effects. Additionally, it provides perspectives to effectively deal with matrix effects. Copyright © 2008 John Wiley & Sons, Ltd. [source] Epinephrine for the treatment of anaphylaxis: do all 40 mg sublingual epinephrine tablet formulations with similar in vitro characteristics have the same bioavailability?BIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 9 2006Mutasem M. Rawas-Qalaji Abstract Epinephrine autoinjectors are underutilized in the first aid emergency treatment of anaphylaxis in the community; so non-invasive sublingual epinephrine administration is being proposed. In order to determine the effect of changing excipients on the bioavailability of sublingual epinephrine, four distinct fast-disintegrating epinephrine 40 mg tablet formulations, A, B, C and D, were manufactured using direct compression. All formulations were evaluated for tablet hardness (H), disintegration time (DT) and wetting time (WT). In a prospective 5-way crossover study, four sublingual formulations and epinephrine 0.3 mg i.m. as a control were tested sequentially in a validated rabbit model. Blood samples were collected before dosing and at intervals afterwards. Epinephrine plasma concentrations were measured using HPLC-EC. All tablet formulations met USP standards for weight variation and content uniformity, and resulted in similar mean H, DT and WT (n=6). The area under the curve (AUC), maximum concentration (Cmax) and time at which Cmax was achieved (Tmax) did not differ significantly after the sublingual administration of formulation A and epinephrine 0.3 mg i.m. The AUC after B, C and D were significantly lower (p<0.05) than after epinephrine 0.3 mg i.m. These results suggest that the selection of excipients used in these tablet formulations can affect the bioavailability of sublingually administered epinephrine. Copyright © 2006 John Wiley & Sons, Ltd. [source] | |||||||||||||