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首页> 外文期刊>American Journal of Drug Discovery and Development >Formulation and In vitro / In vivo Evaluation of Buccoadhesive Discs for Controlled Release of Calcium Channel Antagonist
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Formulation and In vitro / In vivo Evaluation of Buccoadhesive Discs for Controlled Release of Calcium Channel Antagonist

机译：钙通道拮抗剂的控释颊黏膜片的配制及体外/体内评价

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Diltiazem hydrochloride (DTZ HCl) buccoadhesive discs were developed to control the drug release and enhance its bioavailability by evading the first pass metabolism. Buccoadhesive discs were prepared by direct compression of mucoadhesive polymers, namely; polyvinylpyrrolidone (PVP K-30), Sodium Carboxymethyl Cellulose (SCMC) and Carbopol 934 (CP934) in combination with Eudragit L100-55, or Sodium Alginate (SA), as matrix polymers to control the drug release. In vitro characterization showed that drug release, swelling capacity, surface pH and mucoadhesion depended on the type of polymers used and their ratios. In vivo testing in human volunteers showed that most of the formulae had suitable mucoadhesion and controlled drug release, however those containing SA and SCMC mixtures showed optimum drug release and greater mucoadhesion values. Relative bioavailability of a selected DTZ HCl buccoadhesive formulation (SA/SCMC, 3:1) was determined and compared with that of a commercial sustained release oral tablet (Altiazem? SR) as a reference in rabbits. The percentage relative bioavailability of DTZ HCl from the selected buccoadhesive disc was found to be 197.7%. The estimated tmax and AUC0-∞ values were also significantly higher after buccal administration (p<0.05). The proposed buccoadhesive formulation of DTZ HCl could be an alternative for the currently available oral therapy.
机译：开发了盐酸地尔硫卓（DTZ HCl）口腔粘膜粘膜片，以通过逃避首过代谢来控制药物的释放并提高其生物利用度。颊粘膜圆盘是通过直接压粘粘膜聚合物制备的。聚乙烯吡咯烷酮（PVP K-30），羧甲基纤维素钠（SCMC）和Carbopol 934（CP934）与Eudragit L100-55或海藻酸钠（SA）组合作为基质聚合物来控制药物的释放。体外表征显示，药物释放，溶胀能力，表面pH和粘膜粘附取决于所用聚合物的类型及其比例。在人类志愿者中进行的体内测试表明，大多数配方具有合适的粘膜粘附力和可控的药物释放，但是含有SA和SCMC混合物的那些配方表现出最佳的药物释放和更大的粘膜粘附力。确定了选定的DTZ HCl口腔粘膜粘附制剂（SA / SCMC，3：1）的相对生物利用度，并将其与作为参考的商业缓释口服片剂（Altiazem？SR）进行了比较。发现来自选定的颊粘膜圆片的DTZ HCl的相对生物利用度百分比为197.7％。经颊给药后，估计的tmax和AUC0-∞值也显着更高（p <0.05）。提议的DTZ HCl口腔粘膜粘连制剂可以替代当前可用的口服疗法。

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