油包油型辣椒素乳剂的制备与体外透皮研究

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Abstract Objective To prepare oil-in-oil capsaicin emulsion to control the release rate of capsaicin and prolong the latent itching time. Methods The oil-in-oil capsaicin emulsion was prepared by high pressure homogenization using orthogonal test, and transdermal test was conducted in vitro using modified Franz diffusion cell. The optimal formulation was selected by using the steady-state diffusion rate (Js) and centrifugal stability as indexes. The effect of dextran induced pruritus in mice was determined. The experimental group (n=8) and the commercial sale group (n=8) were given oil-in-oil capsaicin emulsion and commercial capsaicin ointment, respectively, and the blank control group (n=8) were given equal volume of normal saline. The latency time and itching times of each group were compared. Results The optimal formula of oil-in-oil capsaicin emulsion was 0.5 phase volume ratio, 500 mPa·s viscosity of silicone oil and 2%dosage of Triton X100. The transdermal rate of oil-in-oil capsaicin emulsion was lower than that of hydrophilic pepper cream. The latency time of the experimental group was longer than that of the blank control group and the commercial sale group, and the itching frequency was less than that of the blank control group and the commercial sale group, the differences were statistically significant (P<0.05). Conclusion The oil-in-oil capsaicin emulsion have good sustained release effect, high drug loading and little irritation. It is hopeful to be used in the treatment of chronic pruritus.

Key words： apsaicin Oil-in-oil-emulsions In vitro transdermal penetration

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