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Selected AbstractsTreatment of nicotine dependence with bupropion SR: review of its efficacy, safety and pharmacological profileADDICTION BIOLOGY, Issue 1 2003JOSÉ MARTÍNEZ-RAGA Bupropion hydrochloride, an atypical antidepressant, is the first non-nicotine product that, in its sustained release form (bupropion SR), has been licensed as an aid for smoking cessation. The specialized literature on bupropion SR and smoking cessation is critically reviewed. The pharmacological profile, dosage and administration, contraindications, as well as the clinical efficacy, safety and tolerability data of bupropion are discussed. Recent reports suggest that its mode of actions might be different to what had originally been proposed. When prescribed appropriately, it appears to be a safe, well-tolerated and effective medication in combination with smoking cessation counselling,for a wide range of smokers, as shown in several multicentre double-blind, placebo-controlled clinical trials. Further research is needed on aspects such as the optimal duration of treatment, the potential role of combination therapy with NRT and psychological interventions, and to establish its effectiveness in smokers with other psychiatric disorders or when used with only minimal support by general practitioners. [source] Bioavailability of modified-release methylphenidate: influence of high-fat breakfast when administered intact and when capsule content sprinkled on applesauceBIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 6 2003Lucy Lee Abstract Ritalin®, an immediate release form of racemic methylphenidate hydrochloride, has been available in the USA since 1955 and is used for the treatment of ADHD. The objective of this study was to evaluate the pharmacokinetics of modified-release methylphenidate (highest single dose), Ritalin® LA, when administered under fasting condition, with a high-fat breakfast, and when sprinkled on applesauce in healthy adult subjects. Blood samples were drawn for 24 h following a 40 mg oral administration. Most subjects appeared to produce a bimodal methylphenidate plasma concentration profile. In all three treatment groups, methylphenidate was rapidly absorbed with an initial average tmax(0,4) of 1.3,2.4 h and an average peak plasma concentration [Cmax(abs)] of 14.4,15.2 ng/ml. On average, both the rate [Cmax(abs) and tmax(abs)] and the extent of absorption (AUC0,,) of methylphenidate were similar when the capsule was given with a high fat breakfast and when the capsule contents were sprinkled onto applesauce, compared with the fasting state. No dose dumping was observed when the capsule was given with a high fat breakfast or when sprinkled onto applesauce. The dose was safe and generally well tolerated. Coadministration of a single oral dose of 40 mg methylphenidate capsule whether administered intact with a high-fat breakfast or sprinkled on applesauce did not affect the overall rate or extent of absorption of methylphenidate compared with the fasted condition. Copyright © 2003 John Wiley & Sons, Ltd. [source] Neurocognitive effects of switching from methylphenidate-IR to OROS-methylphenidate in children with ADHDHUMAN PSYCHOPHARMACOLOGY: CLINICAL AND EXPERIMENTAL, Issue 2 2009Yeni Kim Abstract Objectives This study evaluated neurocognitive changes after switching from immediate release forms of methylphenidate (MPH-IR) to osmotic release oral system methylphenidate (OROS-MPH). Methods 102 children with attention-deficit/hyperactivity disorder (ADHD) participated in an open label, 28,day trial, performing neurocognitive test at baseline and at 28 days after the switch from MPH-IR to OROS-MPH. Results There were significant improvements in the commission error and the reaction time of both visual and auditory continuous performance tests (CPTs) at 28 days after switching from MPH-IR to OROS-MPH. A positive correlation was observed between the improvement in parent/caregiver-rated IOWA Conners total score (, IOWA) and the reduction in commission error (r,=,0.3, p,=,0.001) and reduction in reaction time variability (r,=,0.3, p,=,0.006) of visual CPT. In a linear regression model, the change in parent/caregiver-rated IOWA Conners scale total scores were significant predictors of change in commission error (,,=,0.3, p,=,0.005, CI,=,0.4,2.3, adjusted R2,=,0.12) and RT variability (,,=,0.3, p,=,0.004, CI,=,0.5,2.4, adjusted R2,=,0.09) of visual CPT. Conclusions These data suggest that MPH-IR may be successfully switched to OROS-MPH treatment with associated improvements in neurocognitive performance. Large-scale controlled trials are needed to replicate these findings. Copyright © 2009 John Wiley & Sons, Ltd. [source] Colloidal soft matter as drug delivery systemJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 1 2009Giulia Bonacucina Abstract Growing interest is being dedicated to soft matter because of its potential in delivering any type of drugs. Since hydrophilic, lipophilic, small and big molecules can be loaded into these colloidal systems and administered through the parenteral or nonparenteral route, soft matter systems have been used to solve many biomedical and pharmaceutical problems. In fact, they make possible to overcome difficulties in the formulation and delivery of poorly water-soluble drug molecules, settle some stability issues typical of biological drug molecules, design parenteral sustained release forms and provide functionalized soft particles that are very effective in drug targeting. This review deals with the important role that colloids play in the drug delivery and targeting, with particular attention to the more currently used systems such as microemulsions, organogels, liposomes, micelles, and dendrimers. Though significant progress has been made in drug targeting, some challenges still remain. Further efforts will be required to better understand the characteristics of targets and to discover new ones. In-depth knowledge of the physico-chemical structure and properties of the systems used for targeting is fundamental for understanding the mechanism of interaction with the biological substrate and the consequent drug release. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:1,42, 2009 [source] |