摘要
目的制备油包油型辣椒素乳剂,以控制辣椒素释放速率,并延长瘙痒潜伏时间。方法采用正交试验,通过高压均质法制备油包油型辣椒素乳剂,采用改良Franz扩散池进行体外透皮试验,以稳态扩散速率(Js)和离心稳定性为指标筛选最优处方。并以右旋糖酐致小鼠瘙痒模型测定其药效,其中受试组(n=8)、市售组小鼠(n=8)背部皮肤分别给予油包油型辣椒素乳剂与市售辣椒素软膏,空白对照组小鼠(n=8)给予等容积生理盐水,比较各组的潜伏时间和瘙痒次数。结果油包油型辣椒素乳剂的最佳处方是相体积比为0.5,硅油黏度为500 mPa·s,Triton X100用量为2%。油包油型辣椒素乳剂的透皮速率低于亲水性辣椒乳膏。受试组的潜伏时间长于空白对照组和市售组,瘙痒次数少于空白对照组和市售组,差异有统计学意义(P<0.05)。结论制备的油包油型辣椒素乳剂具有良好的缓释效果,可用于治疗慢性瘙痒。
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.
作者
钟仲
杨棣华
麦蕴华
ZHONG Zhong;Yang Dihua;MAI Yunhua(Department of Pharmacy and Medical Equipment,Foshan Chancheng People's Hospital,Guangdong Province,Foshan 528000,China;Department of Pharmacy,the First Affiliated Hospital of Guangzhou University of Chinese Medicine,Guangdong Province,Guangzhou 510006,China)
出处
《中国当代医药》
CAS
2022年第8期15-20,共6页
China Modern Medicine
基金
广东省佛山市科技创新项目(医学类科技攻关)(1920001000634)。
关键词
辣椒素
油包油型乳剂
体外透皮
Capsaicin
Oil-in-oil-emulsions
In vitro transdermal penetration
作者简介
钟仲(1984-),男,汉族,硕士,副主任中药师,研究方向:中药学。