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Mucoadhesive buccal patches based on interpolymer complexes of chitosan-pectin for delivery of carvedilol

机译:基于壳聚糖-果胶互聚物复合物的粘膜粘膜颊贴片可递送卡维地洛

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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+/-0.20g, in vitro release of 98.73% and ex vivo mucoadhesion time of 451min with in a period of 8h. 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.
机译:该研究旨在利用壳聚糖(CH)和果胶(PE)互聚物复合物开发盐酸卡维地洛的生物粘附性贴剂,并系统地评估其体外和体内性能。卡维地洛的粘膜粘膜颊黏膜贴剂采用溶剂流延法制备。通过FTIR和DSC研究了CH和PE之间的理化相互作用。评价贴剂的物理特性,例如质量变化,含量均匀性,耐折性,离体粘膜粘附强度,离体粘膜粘附时间,表面pH,体外药物释放,原位释放研究和体内生物利用度研究。发现贴剂的溶胀指数与PE浓度成正比。发现所有配制的生物粘附贴剂的表面pH都在6.2至7.2之间。优化的生物粘附贴剂(C1,CH:PE 20:80)在8h内显示出22.10 +/- 0.20g的生物粘附强度,98.73%的体外释放和451min的体外粘膜粘附时间。优化的贴剂显示出良好的体外和体内结果。与口服途径相比,卡维地洛在兔的颊部递送显示卡维地洛从贴剂的生物利用度显着提高。

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