Rayat and Bahra Institute of Pharmacy, Sahauran, Mohali, Punjab, India.
Saudi Pharm J. 2012 Jan;20(1):21-7. doi: 10.1016/j.jsps.2011.04.005. Epub 2011 Apr 30.
The study was designed to develop bioadhesive patches of carvedilol hydrochloride using chitosan (CH) and pectin (PE) interpolymer complexes and to systematically evaluate their in vitro and in vivo performances. Mucoadhesive buccal patches of carvedilol were prepared using solvent casting method. The physicochemical interaction between CH and PE was investigated by FTIR and DSC studies. The patches were evaluated for their physical characteristics like mass variation, content uniformity, folding endurance, ex vivo mucoadhesion strength, ex vivo mucoadhesion time, surface pH, in vitro drug release, in situ release study, and in vivo bioavailability study. The swelling index of the patches was found to be proportional to the PE concentration. The surface pH of all the formulated bioadhesive patches was found to lie between 6.2 and 7.2. The optimized bioadhesive patch (C1, CH:PE 20:80) showed bioadhesive strength of 22.10 ± 0.20 g, in vitro release of 98.73% and ex vivo mucoadhesion time of 451 min with in a period of 8 h. The optimized patch demonstrated good in vitro and in vivo results. The buccal delivery of carvedilol in rabbits showed a significant improvement in bioavailability of carvedilol from patches when compared to oral route.
本研究旨在开发盐酸卡维地洛的生物粘附贴片,使用壳聚糖(CH)和果胶(PE)的聚合物复合物,并系统地评估其体外和体内性能。采用溶剂浇铸法制备盐酸卡维地洛的粘膜粘附颊贴片。通过傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)研究了 CH 和 PE 之间的物理化学相互作用。对贴片进行了物理特性评估,如质量变化、含量均匀性、折叠耐力、体外粘膜粘附强度、体外粘膜粘附时间、表面 pH 值、体外药物释放、原位释放研究和体内生物利用度研究。贴片的溶胀指数与 PE 浓度成正比。所有配方的生物粘附贴片的表面 pH 值均在 6.2 至 7.2 之间。优化的生物粘附贴片(C1,CH:PE 20:80)表现出 22.10±0.20g 的生物粘附强度、98.73%的体外释放和 451 分钟的体外粘膜粘附时间,在 8 小时内。优化的贴片表现出良好的体外和体内结果。与口服途径相比,兔口腔给予卡维地洛贴片后,卡维地洛的生物利用度有显著提高。