20(S)-原人参二醇4种剂型在体透皮实验的初步研究  

The preliminary study on in vivo transdermal experiments of 20(S)-protopanaxadiol(PPD)of four formulations

作　　者：陈婧[1,2] 韩美华[1] 王键[3] 季宇彬 王向涛[1] 

机构地区：[1]中国医学科学院药用植物研究所,北京100193 [2]国家教育部抗肿瘤天然药物工程研究中心哈尔滨商业大学生命科学与环境科学研究中心药物研究所博士后科研工作站,黑龙江哈尔滨150076 [3]黑龙江中医药大学,黑龙江哈尔滨150040

出　　处：《现代药物与临床》2009年第6期354-358,共5页Drugs & Clinic

摘　　要：目的研究20(S)-原人参二醇(PPD)4种剂型的制备及大鼠在体PPD透皮吸收情况。方法用薄膜超声法制备PPD药质体和醇质体,用超声法制备环糊精包合物,用增溶法制备PPD溶液;建立在体透皮试验中PPD的HPLC测定方法;利用皮肤剩余量法计算PPD4种剂型透皮18h后残留在皮肤内的药量。色谱条件:COSMO-SIL5C18-MS-Ⅱ色谱柱(250mm×4.6mm,5μm);流动相为甲醇-水(90∶10);体积流量1.0mL/min;检测波长203nm;柱温25℃;进样量50μL。结果豆磷脂、羟丙基-β-环糊精(HP-β-CD)空白皮肤洗液和试剂对药物的测定无干扰,PPD质量浓度在0.1～0.5mg/mL与峰面积的线性关系良好(r=0.9999),回收率均在96.93%～104.78%,日内及日间RSD均小于1.54%(n=3)。PPD药质体、PPD醇质体、PPDβ-环糊精包合物、PPD原药液的皮肤剩余量分别为69.6%、86.36%、100%、73.55%。结论RP-HPLC法能很好地测定PPD的量,且回归方程线性均较好,表明建立的在体透皮试验方法准确、稳定,适用于PPD经皮给药系统制剂的在体透皮试验研究。Objective To study the preparation of 20（S）-protopanaxadiol （PPD） in four formulations and the in vivo percutaneous absorption in rats. Methods PPD pharmacosomes and PPD plastid alcohol were prepared by means of film ultrasound, β-cyelodextrin inclusion were prepared by using ultrasound, and original liquid by solubilization. The RP-HPLC method was studied for determining PPD in vivo transdermal test. The remaining skin method was adopted to calculate the remaining volume of the four formulations after 18 h. The HPLC separation was performed with a COSMOSIL 5 C18-MS-Ⅱ column （250 mm×4.6 mm, 5 μm）, with methanol-water （90 ： 10） as the mobile phase and the detection wave-length at 203 nm. The column temperature was 25 ℃. The flow rate was 1.0 mL/min, and 50 vL sample solution was injected. Results Under the above-mentioned chromatographic conditions, soybean phospholipid, HP-β-CD, blank skin lotion and reagents did not interfere the determination of the drug. The calibration curve was linear within the range 0.1-0.5 mg/mL （r=0. 999 9）, and the average recovery was between 96.93%-104.78%. Both the intra-day and inter-day RSD were less than 1.54% （n=3）. The remaining volumes of PPD pharmacosomes, PPD plastid alcohol, PPD β-cyclodextrin inclusion and PPD original liquid were respectively 69.6%, 86.36%, 100%, and 73.55%. Conclusion The RP-HPLC method can be well applied to the determination of PPD. The in vivo transdermal test method is accurate, stable, and applicable for the study of in vivo transdermal experiments of PPD.

关 键 词：20(S)-原人参二醇 在体透皮实验 皮肤剩余量法 反相高效液相色谱法 

分 类 号：R943[医药卫生—药剂学]