Formulation and evaluation of buccal film of an antihypertensive drug

Ashinaa Benedict, Irin Rose Paul, Manju Maria Mathews, B. R
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Abstract

The aim of the study was to formulate and evaluate Losartan potassium buccal films, an angiotensin receptor blocker and is used to treat hypertension. Losartan potassium is having less bioavailability (33%), so the buccal films are expected to increase the bioavailability by avoiding hepatic metabolism. Ten formulations of buccal films were prepared by solvent casting method using HPMC K15 M as the main film-forming polymer in various proportions with various co-polymers such as Eudragit RL. 100, Carbopol 940, Ethyl cellulose. Physicochemical characteristics,in vitro buccal permeation, in vitro release study and residence time were evaluated. In vitro studies revealed that the release rate of Losartan potassium was higher for films containing HPMC K15 M and Eudragit RL100 in 3:1 ratio. The result of stability study indicated that no significant changes have occurredduring the period of study.
抗高血压药物口腔胶片的配制与评估
洛沙坦钾是一种血管紧张素受体阻滞剂,用于治疗高血压。洛沙坦钾的生物利用度较低(33%),因此口腔黏膜有望通过避免肝脏代谢来提高生物利用度。我们采用溶剂浇铸法制备了十种配方的口腔胶片,以 HPMC K15 M 为主要成膜聚合物,并以不同比例添加了各种共聚物,如 Eudragit RL.100、Carbopol 940、乙基纤维素。对其理化特性、体外口腔渗透性、体外释放研究和停留时间进行了评估。体外研究表明,含有 HPMC K15 M 和 Eudragit RL100(比例为 3:1)的薄膜的洛沙坦钾释放率更高。稳定性研究结果表明,在研究期间没有发生重大变化。
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