Pokharkar Varsha, Dhar Sheetal, Mandpe Leenata
Department of Pharmaceutics, Bharati Vidyapeeth University Poona College of Pharmacy, Erandwane, Pune 411038.
Hindustan Antibiot Bull. 2007;49-50(1-4):21-8.
Carvedilol a poorly water soluble drug undergoes extensive first pass metabolism, which reduces its bioavailability to 25-30%. Mouth dissolving tablets of Carvedilol were prepared with the purpose of delivering the drug directly into the systemic circulation and bypassing the hepatic first pass metabolism with a concomitant increase in bioavailability. The solubility of Carvedilol was improved by forming inclusion complex with cyclodextrin which was then further used for the formulation of mouth dissolving tablet. Differential scanning calorimetry and Infrared spectroscopy results indicated no incompatibilities between drug-excipient mixtures. Effect of three different superdisintegrants on disintegration was studied. The formulations were evaluated for drug content, content uniformity, friability, disintegration time and in-vitro dissolution. Tablets containing Carvedilol-beta-cyclodextrin complex exhibited good tablet properties, with 90% drug dissolved within 5 min. This demonstrated the effectiveness of using various superdisintegrants and Carvedilol-beta-cyclodextrin complex in formulation of mouth dissolving tablet.
卡维地洛是一种水溶性差的药物,会经历广泛的首过代谢,这使其生物利用度降低至25 - 30%。制备卡维地洛口腔崩解片的目的是将药物直接输送到体循环中,绕过肝脏首过代谢,同时提高生物利用度。通过与环糊精形成包合物来提高卡维地洛的溶解度,然后将其进一步用于制备口腔崩解片。差示扫描量热法和红外光谱结果表明药物 - 辅料混合物之间不存在不相容性。研究了三种不同超级崩解剂对崩解的影响。对制剂进行了药物含量、含量均匀度、脆碎度、崩解时间和体外溶出度的评估。含有卡维地洛 - β - 环糊精复合物的片剂表现出良好的片剂性能,90%的药物在5分钟内溶解。这证明了在口腔崩解片制剂中使用各种超级崩解剂和卡维地洛 - β - 环糊精复合物的有效性。