摘要
目的通过制备碘化钾醇质体,观察其经皮渗透性能及口服药代动力学特点。方法采用乙醇注入法制备碘化钾醇质体,以正交法筛选碘化钾醇质体最佳处方,以粒径、聚合物分散性指数(PDI)、Zeta电位、稳定性为主要评价指标,采用超滤离心法测定碘化钾醇质体包封率。采用Franz扩散池法,以碘化钾的稳态透皮速率(Js)、累积透过率(An)、增渗比(ER)作为主要指标,评价碘化钾醇质体经皮渗透性能。利用大鼠灌胃给药,采用电感耦合等离子体-质谱法(ICP-MS)检测不同时间血碘浓度,考察碘化钾醇质体药代动力学特点。结果碘化钾醇质体最佳处方为:药脂比为2:3,卵磷脂与胆固醇比为15:2,乙醇浓度为35%(v/v),碘化钾浓度为2%(g/100mL)。碘化钾醇质体在4h和8h的累积透过率分别为(9.08±0.69)%和(20.82±1.73)%,均明显高于碘化钾溶液组(P<0.01)。大鼠灌胃后,碘化钾醇质体组的峰浓度(C_(max))、药时曲线下面积(AUC)均明显高于碘片组,且表观清除率(CLz/F)低于碘片组(P<0.05)。结论碘化钾醇质体具有良好的经皮渗透特性和口服生物利用度。
Objective To prepare potassium iodide ethosomes and investigate their percutaneous permeability and oral pharmacokinetics.Methods Potassium iodide ethosomes were prepared by ethanol injection method.Orthogonal method was used to select the best formulation of potassium iodide ethosomes.Particle size,polymer dispersity index(PDI),Zeta potential and stability were used as evaluation indicators.The encapsulation efficiency of potassium iodide ethosomes was determined by ultrafiltration centrifugal method.The percutaneous permeability of potassium iodide ethosomes was evaluated using Franz diffusion cell method,with the steady permeation rate(Js),cumulative permeability rate(An)and enhancing ratio(ER)as the main indicators.Using intragastrical administration in rats,the plasma iodine concentration at different time was measured by inductively coupled plasma-Mass spectrometry(ICP-MS)to investigate the pharmacokinetic characteristics of potassium iodide ethosomes.Results The optimal formulation of potassium iodide ethosomes was as follows:the drug-to-lipid ratio was 2:3,the lecithin-tocholesterol ratio was 15:2,the concentration of ethanol was 35%(v/v),and the concentration of potassium iodide was 2%(g/100mL).The cumulative permeability rate of potassium iodide ethosomes at 4h and 8h was(9.08±0.69)%and(20.82±1.73)%,respectively,which were significantly higher than those of potassium iodide solution group(P<0.01).After intragastrical administration in rats,the peak concentration(C_(max))and area under the curve(AUC)of potassium iodide ethosomes group were significantly higher than those of iodine tablet group,and the apparent clearance(CLz/F)was lower than that of iodine tablet group(P<0.05).Conclusion Potassium iodide ethosomes have good percutaneous permeability and oral bioavailability.
作者
陈双景
刘全斌
柳彦君
李玉星
高琪琛
刘波
朱征
王萌
王志鑫
苏璞
Chen Shuangjing;Liu Quanbin;Liu Yanjun;Li Yuxing;Gao Qichen;Liu Bo;Zhu Zheng;Wang Meng;Wang Zhixin;Su Pu(PLA Rocket Force Characteristic Medical Center,Beijing 100088)
出处
《中国现代医药杂志》
2025年第3期37-43,共7页
Modern Medicine Journal of China
关键词
碘化钾
醇质体
经皮渗透
药代动力学
Potassium iodide
Ethosomes
Percutaneous penetration
Pharmacokinetics
