| OBJECTIVE: To prepare a silk compound membrane of lidocaine hydrochloride with silk fibroin.The destination is to prepare a new vehicle for transdermal therapeutic drugs,which is safe and has delayed release effect, and its preparation craft is simple.METHODS: The extraction craft of silk fibroin was screened by the orthogonal experiment. The lidocaine hydrochloride detection method in vitro was established by high performance liquid chromatogram.The prescription of formulation and preparation process were screened by the uniform design for permeation rate.The release characteristics of silk compound membrane and silk monolayer membrane were studied.To invest the biocompatibility and toxicity of silk compound membrane of lidocaine by animal experiment.And its analgesic effect was studied by the hot plate test and twisting reaction.RESULTS:The best extraction condition of silk fibroin was degumming 2h at 121℃,and degrdnning 4h at 80℃. When the ratio of azone and propylene glycol was 1.6% :2.0%,the transdermal absorption reached a maximum.The release mechanism of silk compound membrane of lidocaine in vitro was coincided with Higuchi Equation,and the compound membrane's release characteristics was better than the monolayer one.It has delayed release effect,and the release rate was 0.5984(mg/cm2h1/2).As animal experiment proved ,the silk compound membrane's blood compatibility and anticoagulant property were well.Haemolysis rate was 0.8%,so it had no haemolyticus.Its biodegradation was well, degrdned soundly in 6 weeks.It had no irritation or hypersensibility for skin. In the hot plate test and twisting reaction,compared with diluents bases,silk compound membrane of lidocaine hydrochloride can raise pain threshold and depress writhing times significantly(p<0.05),show it had analgesic effect.CONCLUSION: Slik compound membrane is biocompatibility and safety as a new vehicle for transdermal therapeutic drugs,also has a satisfactory prospect.
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