盐酸利多卡因凝胶剂的制备工艺研究

Study on preparation of Lidocaine Hydrochloride Gelatin

目的制备并优化盐酸利多卡因凝胶剂。方法以盐酸利多卡因为主药,卡波姆-941、PEG-400和azone等为基质,制备凝胶剂;以离体皮肤渗透速率为指标,采用正交实验优化处方。结果最优处方为:盐酸利多卡因8.8g,卡波姆-941 3.5g,1,2-丙二醇62.5g;azone 6.5g,PEG-400 13.0g,蒸馏水加至200g。该凝胶剂的盐酸利多卡因离体皮肤渗透速率为744.45μg.h-1.cm-2,稳定性好。结论制备的盐酸利多卡因凝胶剂符合药典要求,质量稳定。

Objective To optimize the preparation procedure of Lidocaine Hydrochloride Gelatin.Method Gelatin was prepared by using lidocaine hydrochloride as the main component and carbomer-941,PEG-400 and azone as the matrix.The permeation rate of skin in vitro was used as an indicator in orthogonal design tests.Results The optimized conditions were as follows:lidocaine hydrochloride 8.8 g,carbomer-941 3.5 g,1,2-propanediol 62.5 g,azone 6.5 g,PEG-400 13.0 g,distilled water to 200 g.The gel permeation rate of lidocaine was 744.45 μg·h-1·cm-2.Conclusion The proposed procedure could obtain Lidocaine Hydrochloride Gelatin which can attain the requirement of Chinese Pharmacopoeia.