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目的:构建黄芩苷壳聚糖微粒,并与黄芩苷乳膏体外经皮扩散行为进行比较。方法:采用中和法构建微粒,正交试验法优化构建条件;利用Franz扩散池进行微粒与乳膏体外经皮扩散行为的比较。结果:微粒的最佳构建条件为:药物/材料比(1∶3),壳聚糖浓度2 mg/mL,反应10 min,包封率与载药量均达60%以上;微粒与乳膏经皮扩散36 h后,药物累积扩散百分率分别为4.04%和30%,皮层药物百分含量分别为0.11%和0.14%(n=3)且无统计学差异(W=7,P=0.127)。结论:采用中和法构建黄芩苷壳聚糖微粒,简便易行;且皮肤给药时具有局部药物贮库和一定的缓释的作用。
Objective: To construct the baicalin chitosan microparticles and compare with the in vitro proliferation of baicalin cream. Methods: The neutralization method was used to construct the microparticles. The orthogonal experimental method was used to optimize the construction conditions. The Franz diffusion cells were used to compare the in vitro diffusion behaviors of microparticles and creams. Results: The optimal conditions for the preparation of the particles were as follows: drug / material ratio (1: 3), chitosan concentration 2 mg / mL, reaction time 10 min, encapsulation efficiency and drug loading reached more than 60% After 36 h of transdermal diffusion, the cumulative drug diffusion rates were 4.04% and 30%, respectively. The percentage of drug in the cortex was 0.11% and 0.14% respectively (n = 3) and there was no significant difference (W = 7, P = 0.127) . CONCLUSION: The baicalin chitosan microparticle is prepared by neutralization method, which is simple and easy to operate. It also has the function of local drug depot and sustained release in the skin.