Preparation Of Liposomal Harmine Hydrochloride Cream

Objective: To prepare a liposomal harmi ne hydrochloride cream with quick and lacol prolonged effect, study on transdermal absorption of the cream, and probe into application rules of liposomal technology of transdermal delivery system. Methods: 1)A comprehensive score system was established as optimization index.Then uniform design was used for selecting the prescription of harmine hydrochloride cream; 2)To confirm the anti-itching pharmacodynamics basic by pruritus model; 3)To screen the method of liposome abstraction through studying the recovery rate to select the best abstraction method; 4)Uniform design was used for selecting the prescription of harmine hydrochloride liposomes through studying the encapsulation efficiency; 5)Compare anti-itching pharmacodynamics of the liposomal and non-liposomal cream through studying the itching time; 6)To study on the transdermal delivery of the liposomal and non-liposomal cream through studying the transdermal abstraction rate and the drug content in intra. Result: 1) the optimized prescription is as follows: monostearin 8%, Vaseline 5%, beeswax 6.1%, Span -60 1.1%, Tween -80 1.9 %; 2) The local application of harmine hydrochloride cream can alleviate the itching induced by histamine phosphate and 5-hydroxytryptamine (5-HT) respectively. And the anti-itching effect of harmine hydrochloride cream is stronger than the effect of the positive control group; 3)Column chromatography was used to separate the free drug and liposomes, the eluant is PBS,and the average recovery rate is 100.04%,102.20%,97.38%; 4)pH-gradients method was the best method to prepare the harmine hydrochloride liposomes, the average encapsulation efficiency was 85.32%; 5)Liposomal harming hydrochloride cream can alleviate the itching induced by histamine phosphate and 5-hydroxytryptamine (5-HT) respectively. And the anti-itching effect of 30%liposomal harmine hydrochloride cream is stranger than the non-liposomal cream; 6)The transdermal abstraction rate of 30% liposomal cream is lower than the non-liposomal cream, and the drug content in intra of liposomal cream is higher than the non-liposomal cream. Conclusion: The prescription of the 30% liposomal harmine hydrochloride cream is available, reasonable, and reproducible. The 30% liposomal harmine hydrochloride cream has the quick and lacol prolonged anti-itching effect.