Formulation And In Vitro/In Vivo Evaluation Of Olmesartan Medoxomil Solid Dispersions Incorporated E/R Trilayer Matrix Tablets By Geomatrix

M. Balakrishnaiah, V. Gupta
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Abstract

An attempt has been made to develop and optimize an novel anti hypertensive trilayered controlled release matrix tablets incorporated with Olmesartan medoxomil solid dispersion prepared by direct compression and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), guar gum, ethyl cellulose. Upper and lower layers are prepared with Carnauba wax, guar gum and sodium CMC. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF14) was described by the Zero-order and Higuchi model. In-vivo bioavailability studies were carried out with the optimized formulation (HF14) and reference standard A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a trilayer extended release formulation up to 24h. These results also demonstrated that the Olmesartan solid dispersion incorporated trilayer tablets shown more bioavailability because of its conversion from crystalline to amorphous form.
奥美沙坦美多沙米固体分散体含E/R三层基质片的制备及体外/体内评价
采用直接压缩法制备了由不同等级羟丙基甲基纤维素(HPMC)、瓜尔胶、乙基纤维素组成中间活性层的奥美沙坦-美多索米固体分散体,制备并优化了新型抗高血压三层控释片。上下两层由巴西棕榈蜡、瓜尔胶和CMC钠配制而成。该给药系统具有24 h的缓释时间。优化后的配方(HF14)的释放曲线采用零阶和Higuchi模型描述。采用优化后的配方(HF14)和参比标准进行体内生物利用度研究,发现其溶出度与生物利用度之间存在良好的相关性。结果表明,所采用的方法可以成功地开发出长达24小时的三层缓释制剂。这些结果还表明,奥美沙坦固体分散体含有三层片剂,由于其从晶体到无定形的转化,具有更高的生物利用度。
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