Preparation and Evaluation of '3 Cap' Pulsatile Drug Delivery System of Ramipril.

Priyanka Kriplani, Kamla Pathak, Anil Philip
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引用次数: 1

Abstract

Background: Chronotherapeutics, the drug delivery based on circadian rhythm, is recently gaining much attention worldwide. Various diseases like asthma, hypertension, and arthritis show the circadian variation that demands time scheduled drug release for effective drug action. Therefore, the pulsatile drug delivery system has been designed to confer preprogrammed drug delivery.

Objective: In the present study, a '3 Cap' pulsatile drug delivery system has been developed, optimized, and characterized in order to achieve the floating and pulsatile release of ramipril.

Methods: An optimal response surface design was employed to investigate the effect of isopropanol: formaldehyde vapors for varying time on drug release from the capsules. '3 Cap' pulsatile drug delivery system was evaluated in terms of floating time, density, the effect of gastric flow rate, and type of dissolution apparatus on drug release.

Results: Independent variables exhibited a significant effect on the drug release of the prepared formulations. Results showed that time between the release of fractions of dose increased with an increase in formaldehyde: isopropanol ratio and duration of exposure to formaldehyde vapors with no effect of gastric flow rate.

Conclusion: The results of the designed system revealed that an optimum exposure of 1:2 of isopropanol: formaldehyde vapors for sixty minutes resulted in the desired release of second pulse of dose after a predetermined lag time of 5 hours as desired. '3Cap' system was successful in achieving floating and pulsed release of hypertensive drug opening a 'new lease of life' to the existing drug molecule.

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雷米普利“3帽”脉动给药系统的制备与评价。
背景:时间疗法是一种基于昼夜节律的给药方法,近年来在世界范围内受到广泛关注。各种疾病,如哮喘、高血压和关节炎,都表现出昼夜变化,需要定时释放药物以达到有效的药物作用。因此,脉动给药系统已被设计为赋予预编程给药。目的:为实现雷米普利的漂浮脉动释放,建立了“3帽”脉动给药系统,并对其进行了优化和表征。方法:采用最佳响应面设计,考察不同时间异丙醇甲醛蒸汽对胶囊释药的影响。从漂浮时间、密度、胃流速率、溶出器类型对药物释放的影响等方面评价“3 Cap”脉动给药系统。结果:自变量对制剂的释药效果有显著影响。结果表明,随着甲醛与异丙醇比例的增加,各剂量组分释放间隔时间增加,甲醛蒸气暴露时间增加,胃流率不受影响。结论:所设计的系统结果表明,异丙醇:甲醛蒸气1:2的最佳暴露时间为60分钟,在预定的延迟时间为5小时后,可获得所需的第二脉冲剂量释放。“3Cap”系统成功地实现了高血压药物的浮动和脉冲释放,为现有的药物分子打开了“新的生命”。
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来源期刊
Cardiovascular and Hematological Agents in Medicinal Chemistry
Cardiovascular and Hematological Agents in Medicinal Chemistry Medicine-Cardiology and Cardiovascular Medicine
CiteScore
2.70
自引率
0.00%
发文量
34
期刊介绍: Cardiovascular & Hematological Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new Cardiovascular & Hematological Agents. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of current topics in Cardiovascular & Hematological medicinal chemistry. Cardiovascular & Hematological Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cardiovascular & hematological drug discovery.
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