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首页> 外文期刊>Open Pharmaceutical Sciences Journal >Hydroxyl Ethyl Cellulose HHX and Polymethyl Methacrylate Based Site Specific Floating Delivery of Prochlorperazine Maleate
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Hydroxyl Ethyl Cellulose HHX and Polymethyl Methacrylate Based Site Specific Floating Delivery of Prochlorperazine Maleate

机译：羟乙基纤维素HHX和聚甲基丙烯酸甲酯基于马来酸氯丙嗪的定点漂浮递送

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Background:Prochlorperazine maleate is a phenothiazine antipsychotic used principally in the treatment of nausea, vomiting and vertigo. Biological half- life of the drug is about 6 to 8 hrs and oral dose is 5 or 10 mg thrice or four times a day. The mean absolute bioavailability for drug is 12.5%. Due to the solubility of drug in acidic pH, it is mainly absorbed from stomach.Objective:Site specific oral floating delivery of prochlorperazine maleate will prolong the gastric retention time, increases the drug bioavailability, reduces frequency of administration and can result in better patient compliance.Method:The tablets were prepared by direct compression technique. Floating drug delivery was developed using gas forming agent and release retarding agent i.e. hydroxyethyl cellulose HHX (Natrosol HHX) and polymethyl methacrylate (PMMA). 3~(2) full factorial design was used for optimization. Prepared tablets were evaluated for pre and post compression parameters.Results:From the factorial batches it was observed that formulation containing 68.5% of hydroxyethyl cellulose HHX and 15% of polymethyl methacrylate had shown a drug release of 91.56 ± 2.7% with floating upto 10 hrs following Korsmeyer Peppas release kinetics.Conclusion:In- vivo placebo X-ray study for optimized batch F6 had shown good gastroretention ability for 6 ± 0.5 hrs. In- vitro and in- vivo study confirmed the site specific floating delivery for drug.
机译：背景：马来酸氯丙嗪是一种吩噻嗪类抗精神病药，主要用于治疗恶心，呕吐和眩晕。该药物的生物半衰期约为6至8小时，口服剂量为每日三次或三次，每次5或10 mg。药物的平均绝对生物利用度为12.5％。由于药物在酸性pH值中具有溶解性，因此主要从胃中吸收。目的：马来酸氯丙嗪的特定部位经口服浮动漂浮可延长胃的保留时间，增加药物的生物利用度，减少给药频率，并可以改善患者的依从性方法：采用直接压片法制备片剂。使用气体形成剂和释放阻滞剂i.e.开发了漂浮药物递送。羟乙基纤维素HHX（Natrosol HHX）和聚甲基丙烯酸甲酯（PMMA）。使用3〜（2）全因子设计进行优化。结果：从因子批次中观察到，含有68.5％羟乙基纤维素HHX和15％聚甲基丙烯酸甲酯的制剂显示出91.56±2.7％的药物释放，漂浮时间长达10个小时。结论：体内安慰剂X射线研究优化了F6批次，在6±0.5小时内具有良好的胃滞留能力。体外和体内研究证实了针对药物的部位特异性漂浮递送。

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