中国临床药学杂志

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。

AIM To prepare the microemulsion-based gel of lidocaine,and to study its content,physicochemical properties and transdermal diffusion characteristics in vitro. METHODS To use ethylis oleate as oil phase,Tween 80 as surfactant,ethanol as cosurfactant,distilled water as aqueous phase,Carbopol 940 as substrate,the microemulsion-based gel of lidocaine was prepared by direct swelling method. The viscosity of microemulsion-based gel was measured with NDJ-5S rotating viscometer,and the p H value was detected with PHS-3TC p H meter. The transdermal characteristics of lidocaine in microemulsion,microemulsion-based gel and saturated aqueous solution were compared by modified Franz diffusion cell. RESULTS With good stability,the appearance of microemulsion-based gel of lidocaine was transparent white gel. The p H was about 6. 71,and the average absolute viscosity was 45. 4 Pa·s. The steady-state infiltration rates of lidocaine saturated aqueous solution,microemulsion,microemulsion-based gel were 0. 24,1. 50,0. 47 mg·cm^-2·h^-1respectively. CONCLUSION The infiltration rates of lidocaine in mieroemulsion and microemulsion-based gel are superior to those of saturated aqueous solution,which will supply evidence for the new selection for the transdermal formulations of lidocaine.