Forni F, Coppi G, Iannuccelli V, Bernabei M T
Department of Pharmaceutical Sciences, University of Modena, Italy.
J Microencapsul. 1988 Apr-Jun;5(2):139-46. doi: 10.3109/02652048809056477.
The mechanism of papaverine hydrochloride release from ethyl cellulose-walled microcapsules in both simulated gastric and intestinal fluid is discussed. The microcapsules were prepared by coacervation using different core: wall ratios. The rupture of the thin-walled microcapsules after release in simulated gastric fluid was shown and attributed to the internal osmotic pressure, supporting a mechanism for drug dissolution. The internal osmotic pressure produced only a few small holes in the thin-walled microcapsules after release in simulated intestinal fluid. No rupture of the thick-walled microcapsules after release in either medium was shown. Therefore these release data fitted diffusion-type kinetics. It is suggested that the internal osmotic pressure developed after penetration of the medium is affected by the ratio between the core dissolution rate and the drug diffusion rate through the wall.
讨论了盐酸罂粟碱从乙基纤维素壁微囊中在模拟胃液和肠液中的释放机制。微囊通过凝聚法制备,使用不同的芯壁比。展示了薄壁微囊在模拟胃液中释放后破裂的情况,并归因于内部渗透压,这支持了药物溶解的机制。薄壁微囊在模拟肠液中释放后,内部渗透压仅产生了一些小孔。在两种介质中释放后,厚壁微囊均未显示破裂。因此,这些释放数据符合扩散型动力学。有人提出,介质渗透后产生的内部渗透压受芯溶解速率与药物通过壁的扩散速率之比的影响。