论文部分内容阅读
目的制备利多卡因微乳凝胶剂,并考察其含量、理化性质和体外透皮特性。方法以油酸乙酯为油相,吐温-80为表面活性剂,无水乙醇为助表面活性剂,蒸馏水为水相,卡波姆940为凝胶骨架制备利多卡因微乳凝胶。采用NDJ-5S型数字式黏度计和PHS-3TC数显p H计分别测定微乳凝胶的黏度和p H。采用改良的Franz扩散池,比较利多卡因微乳、微乳凝胶及饱和水溶液中利多卡因的透皮特性。结果利多卡因微乳凝胶外观为白色透明凝胶态且稳定性良好,p H均值为6.71,绝对黏度均值为45.4 Pa·s。利多卡因饱和水溶液、微乳、微乳凝胶的稳态渗透速率分别为0.24、1.50、0.47 mg·cm~(-2)·h~(-1)。结论利多卡因微乳、微乳凝胶的稳态渗透速率均优于利多卡因饱和水溶液,可为利多卡因经皮给药提供一种新的剂型。
Objective To prepare lidocaine microemulsion gels and investigate its content, physicochemical properties and in vitro transdermal properties. Methods Ethyl oleate as the oily phase, Tween-80 as surfactant, ethanol as co-surfactant, distilled water as water phase, carbomer 940 as a gel matrix for the preparation of lidocaine microemulsion. The viscosity and p H of microemulsion gel were determined by NDJ-5S digital viscometer and PHS-3TC digital display p H meter, respectively. A modified Franz diffusion cell was used to compare the transdermal properties of lidocaine in lidocaine microemulsion, microemulsion gel and saturated aqueous solutions. Results The appearance of lidocaine microemulsion gel was white and transparent gel with good p H value of 6.71 and mean absolute viscosity of 45.4 Pa · s. The steady state permeation rates of saturated aqueous solution, microemulsion and microemulsion of lidocaine were 0.24, 1.50 and 0.47 mg · cm -2 · h -1, respectively. Conclusion The steady-state permeation rates of lidocaine microemulsion and microemulsion gel are better than that of lidocaine saturated solution, which may provide a new dosage form for transdermal administration of lidocaine.