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Design and Characterization of Buccoadhesive Liquisolid System of an Antihypertensive Drug

机译:降压药物的口腔粘膜粘固液体系的设计与表征

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摘要

Nifedipine is an antihypertensive BCS class II drug which has poor bioavailability when given orally. The objective of the present study was to increase the bioavailability of nifedipine, by formulation and evaluation of a buccoadhesive liquisolid system using magnesium aluminium silicate (Neusilin) as both carrier and coating material and dissolution media were selected based on the solubility studies. A mixture of carboxymethylcellulose sodium and carbomer was used as mucoadhesive polymers. Buccoadhesive tablets were prepared by direct compression. FTIR studies confirmed no interaction between drug and excipients. XRD studies indicated change/reduction in crystallinity of drug. The powder characteristics were evaluated by different flow parameters to comply with pharmacopoeial specifications. The dissolution studies for liquisolid compacts and tablet formulations were carried out and it was found that nifedipine liquisolid tablets formulated from bioadhesive polymers containing 49% liquisolid system, 17.5% carbomer, and 7.5% carboxymethylcellulose sodium showed the best results in terms of dissolution properties. Prepared formulation batches were evaluated for swelling, bioadhesion strength, ex vivo residence time, and permeability studies. The optimized batch was showing promising features of the system. Formulating nifedipine as a buccoadhesive tablet allows reduction in dose and offers better control over the plasma levels.
机译:硝苯地平是一种降压的BCS II类降压药,口服时生物利用度较差。本研究的目的是通过使用硅酸铝镁(Neusilin)作为载体和包衣材料配制和评估颊黏膜粘液固液系统,从而提高硝苯地平的生物利用度,并根据溶解度研究选择溶出介质。羧甲基纤维素钠和卡波姆的混合物用作粘膜粘附聚合物。通过直接压制制备口腔粘膜片剂。 FTIR研究证实药物和赋形剂之间没有相互作用。 XRD研究表明药物结晶度的改变/降低。通过不同的流动参数评估粉末特性,以符合药典规范。进行了液体固体压片和片剂制剂的溶解研究,发现硝苯地平液体片剂由含有49%液体固体系统,17.5%卡波姆和7.5%羧甲基纤维素钠的生物粘附性聚合物配制而成,显示出最佳的溶出性能。对制备的制剂批次进行溶胀,生物粘附强度,离体停留时间和渗透性研究。优化的批次显示出该系统很有希望的功能。将硝苯地平配制成粘膜粘附片剂可以减少剂量,并更好地控制血浆水平。

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