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罗望子胶、壳聚糖和秋葵胶控释结肠靶向直接压片盐酸普萘洛尔基质片的时辰治疗药物递送及体外评价

Chronotherapeutic drug delivery of Tamarind gum, Chitosan and Okra gum controlled release colon targeted directly compressed Propranolol HCl matrix tablets and in-vitro evaluation.

作者信息

Newton A M J, Indana V L, Kumar Jatinder

机构信息

Rayat Bahra Institute of Pharmacy, Rayat Bahra University, Punjab, India; Research and Development Department, Jawaharlal Nehru Technological University, Hyderabad, India.

Nirmala College of Pharmacy, Andhra Pradesh, India.

出版信息

Int J Biol Macromol. 2015 Aug;79:290-9. doi: 10.1016/j.ijbiomac.2015.03.031. Epub 2015 May 1.

DOI:10.1016/j.ijbiomac.2015.03.031
PMID:25936283
Abstract

The main objective of this investigation is to develop a chronotherapeutic drug delivery of various natural polymers based colon targeted drug delivery systems to treat early morning sign in BP. The polymers such as Tamarind gum, Okra gum and Chitosan were used in the formulation design. A model drug Propranolol HCl was incorporated in the formulation in order to assess the controlled release and time dependent release potential of various natural polymers. A novel polymer Tamarind gum was extracted and used as a prime polymer in this study to prove the superiority of this polymer over other leading natural polymer. Propranolol HCl was used as a model drug which undergoes hepatic metabolism and witnesses the poor bioavailability. The matrix tablets of Propranolol HCl were prepared by direct compression. The tablets were evaluated for various quality control parameters and found to be within the limits. Carbopol 940 was used as an auxiliary polymer to modify the drug release and physicochemical characteristics of the tablets. The in vitro release studies were performed in 0.1N HCl for 1.5h, followed by pH 6.8 phosphate buffer for 2h and pH 7.4 phosphate buffer till maximum amount of drug release. The in vitro release profile of the formulations were fitted with various pharmacokinetic mathematical models and analyzed for release profile. The formulations prepared with Tamarind gum prolonged the release for an extended period of time compared to other polymer based formulation and showed an excellent compression characteristic.

摘要

本研究的主要目的是开发一种基于多种天然聚合物的结肠靶向给药系统的时辰治疗性药物递送方法,以治疗血压的清晨症状。在制剂设计中使用了罗望子胶、秋葵胶和壳聚糖等聚合物。为了评估各种天然聚合物的控释和时间依赖性释放潜力,在制剂中加入了模型药物盐酸普萘洛尔。提取了一种新型聚合物罗望子胶并将其用作本研究中的主要聚合物,以证明该聚合物优于其他主要天然聚合物。盐酸普萘洛尔用作经历肝脏代谢且生物利用度差的模型药物。盐酸普萘洛尔的骨架片通过直接压片法制备。对片剂进行了各种质量控制参数评估,结果发现均在限度范围内。使用卡波姆940作为辅助聚合物来改变片剂的药物释放和理化特性。体外释放研究在0.1N盐酸中进行1.5小时,然后在pH 6.8磷酸盐缓冲液中进行2小时,再在pH 7.4磷酸盐缓冲液中进行直至药物最大量释放。将制剂的体外释放曲线与各种药代动力学数学模型拟合,并对释放曲线进行分析。与其他基于聚合物的制剂相比,用罗望子胶制备的制剂延长了释放时间,并显示出优异的压缩特性。

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