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目的阐明喘平缓释片的释药机制。方法采用转篮法结合HPLC测定喘平缓释片的累计释放率,用零级、一级、Higuchi方程、Peppas方程等释药模型对喘平缓释片的释放曲线进行拟合,从溶出过程中各规定时间点取样测定其溶胀率、溶蚀度,体视显微镜观察缓释片的形态变化。结果喘平缓释片指标成分盐酸麻黄碱和盐酸伪麻黄碱在8 h的累计释放率均达到了80%,基本实现了均衡释放,用Peppas方程进行拟合后的方程分别为lg(Mt/M肄)=0.5108 lgt-0.5562,R2=0.9991,n=0.5108和lg(Mt/M肄)=0.5150 lgt-0.5386,R2=0.9989,n=0.5150。喘平缓释片的溶胀率在药物约释放60%时达到了最大值,其后逐渐下降,而溶蚀度则随着药物累计释放率的增加而增加。从体视显微镜观察到遇水膨胀后的缓释片凝胶层和浸润层在一定时间内是逐渐增厚的。结论喘平缓释片的体外释放机制为药物扩散及骨架溶蚀两种作用。在喘平缓释片的体外溶出实验中,有众多颗粒从片剂表面脱落,提示喘平缓释片释药可能存在着新的释放模式-溶蚀-溶散-扩散机制。
Objective To clarify the release mechanism of Chuan-Ping sustained-release tablets. Methods The cumulative release rate of asthma sustained release tablets was determined by rotary basket method and HPLC. The release profiles of asthma sustained release tablets were fitted by release models such as zero order, first order, Higuchi equation and Peppas equation, In each of the provisions of the sample point of time to determine the swelling rate, dissolution, microscope observation of morphological changes of sustained-release tablets. Results The cumulative release rates of ephedrine hydrochloride and pseudoephedrine hydrochloride were all 80% at 8 h, and the equilibrium release was basically achieved. The equation after Peppas equation fitting was lg (Mt / M 肄) = 0.5108 lgt-0.5562, R2 = 0.9991, n = 0.5108 and lg (Mt / M 肄) = 0.5150 lgt-0.5386, R2 = 0.9989, n = 0.5150. The swelling rate of asthmatic sustained-release tablets reached its maximum at about 60% drug release, then decreased gradually, while the dissolution increased with the cumulative drug release rate. It is observed from the stereomicroscope that the gel layer and the infiltrated layer of the sustained-release tablets after water swelling gradually thicken in a certain period of time. Conclusion The release mechanism of Chuan-Ping sustained-release tablets in vitro is two effects of drug diffusion and skeleton erosion. In the in vitro dissolution test of the sustained-release tablets, there are a large number of particles detaching from the surface of the tablets, suggesting that there may be a new release mode - dissolution-dissolution-diffusion mechanism.