Clopidogrel is a medication to reduce the risk of heart disease and taken orally. Quality of drug characterizes the production process and every phamaceutical company strives for it but often it is very difficult to achieve. This study was to investigate quality control parameters of some marketed Clopidogrel tablets. To assess the quality, eight different marketed brands of Clopidogrel 75 mg tablets available in Yemeni market collected from different pharmacies in Hodeida city. Different quality parameters like weight variation, hardness, thickness and friability were determined according to established protocols. Then the in-vitro dissolution test, potency, disintegration time were also carried out. UV-spectrophotometer was used to determine the percentage released and assay at 218 nm. All the brands comply the requirements of Pharmacopoeia as they showed acceptable weight variation range. Friability of all brands was less than 1% and no significant differences in disintegration times as they disintegrated within 15 minutes. In case of dissolution profile, all brands except C6 showed acceptable dissolution time as they released more than 60% of drug in 45 minute. The hardness of only two brands was within the range. All brands also meet the potency specifications. This study suggested that most commercially Clopidogrel tablets in Yemen maintain the quality and comply with the pharmacopeia specifications.
Aim: The aim of this study to compare the relative bioavailability of baclofen as a peroral tablet with the new formulations (transdermal and buccal films). Materials and Methods: Rapid and simple high-performance liquid chromatography/ultraviolet method has been adopted and validated for the determination of baclofen in human plasma with acceptable linearity, precision and accuracy. The study was performed on six human volunteers divided into three groups each contained two individuals. The first group was dosed with 20 mg of baclofen tablet (Lioraz ® ) as a reference, the second group received 40 mg baclofen transdermal film, and the third group received 20 mg baclofen buccal film. Transdermal and buccal films were subjected to in vivo study to evaluate the bioavailability parameters and then compared to the reference. Results and Discussion: Following Lioraz ® tablet, the maximum concentration was achieved after 3.0 h unlike, after transdermal film with a double dose, it was at 6.0 h whereas, following buccal film, maximum time was 3.0 h post-dosing. Thus absorption from buccal films was faster, whereas transdermal spent longer times to reach the maximum concentration in systemic circulation. The mean values of pharmacokinetic parameters were significantly higher from transdermal than oral, demonstrating prolongation of baclofen action, whereas with buccal was lower. Taking Lioraz ® as a reference, the % relative bioavailability from transdermal and buccal film was 78.99% and 89.22%, respectively. Conclusion: Study indicates that the absorption from buccal films was faster, whereas the transdermal spent longer times to reach the maximum drug concentration. Transdermal film of baclofen was successful in all the established studies by improving the prolongation of action and increasing the half-life of baclofen.
Aim: The aim of this study is to formulate and evaluate of baclofen transdermal patches using different polymers, penetration enhancers, and plasticizers. A drug with different film forming polymers was subjected to compatibility study. In addition, in-vitro permeation across animal skin for the best formulation was investigated. Materials and Methods: After studying the incompatibility of baclofen and other polymers used, the pure drug baclofen was formulated as transdermal patches composed of different polymers by solvent evaporation method and the formulations were 16. Then, the physicochemical properties of formulated patches were evaluated to determine the best optimum formula to be examined in-vitro release. Results and Discussion: The drug excipient compatibility study revealed no interaction between baclofen and polymers used. All the physicochemical studies of formulated patches were satisfactory except the formulation. The best-chosen formula was F13 that composed of polyvinyl alcohol as film-forming polymer and Carbopol 940 as bioadhesive polymer with propylene glycol as plasticizer and dimethyl sulfoxide as penetration enhancer. Conclusion: Study indicates that baclofen can be formulated as transdermal patches of acceptable appearance and suitable drug release through 24 h.
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