灵芝三萜纳米混悬凝胶剂的制备及其体外透皮研究  

Preparation of nanosuspension-based gel of Ganoderma lucidum triterpenoids and its in vitro transdermal diffusion characteristics

作　　者：沈成英[1,2] 申宝德[2] 徐平华[2] 李晓荣[1,2] 闵红燕[2] 韩晋[2] 袁海龙[2] 

机构地区：[1]成都中医药大学药学院,四川成都611137 [2]中国人民解放军第三0二医院,北京100039

出　　处：《中草药》2014年第19期2770-2775,共6页Chinese Traditional and Herbal Drugs

基　　金：国家新药创制重大专项(2014ZX09J14106-01A);北京市自然科学基金资助项目(7122176)

摘　　要：目的研制灵芝三萜纳米混悬凝胶剂(GT-NS-gel),并进行体外透皮研究。方法采用高压均质法制备灵芝三萜纳米混悬剂(GT-NS),然后进一步制成凝胶剂。以24 h体外累积释放率和24 h后皮肤中的滞留量为指标,通过效应面法优化GT-NS-gel的处方;比较优化后的GT-NS-gel和灵芝三萜凝胶剂(GT-gel)的体外经皮渗透量及滞留量。结果以最优处方:5 mg/g卡波姆940、30 mg/g GT、47.2 mg/g卵磷脂制得的GT-NS-gel在24 h时的体外累积释放率为(56.28±2.16)%,24 h皮肤滞留量为(472.89±8.74)μg/cm2,理论预测值与实测值接近,模型具有良好的预测性;GT-NS-gel 24 h药物累积渗透量和皮肤滞留量分别为(50.73±4.97)和(475.89±10.74)μg/cm2,明显高于GT-gel的(14.79±3.45)和(101.32±7.02)μg/cm2(P<0.05)。结论将灵芝三萜制成纳米混悬凝胶剂,能够增加药物的皮肤滞留量,提高药物在皮肤局部的生物利用度。Objective To prepare the nanosuspension-based gel of Ganoderma lucidum triterpenoids （GT-NS-gel） and investigate the in vitro transdermal diffusion characteristics. Methods GT-NS was prepared by high pressure homogenization and then transformed into gel. The formulation of GT-NS-gel was optimized by response surface method with cumulative release of drug from the GT-NS-gel within 24 h, and the amount of drug in the skin after applying GT-NS-gel for 24 h was used as indexes. In vitro percutaneous permeation and skin deposition of GT-NS-gel were studied and compared with those of GT-gel. Results The GT-NS-gel prepared by optimal formulation （5 mg/g Carbomer 940, 30 mg/g GT, and 47.2 mg/g lecithin） could release in vitro at 24 h to （56.28 ± 2.16）%, and the amount of drug in the skin after applying GT-NS-gel for 24 h was （472.89 ± 8.74） gg/cm2. There was a little deviation between the theoretically predicted value and the measured value. It showed that this model had a good prediction. The amounts of GT penetrating through the skin and in the skin after applying GT-NS-gel for 24 h were （50.73± 4.97） and （475.89± 10.74） gg/cm2, which were significantly higher than GT-gel （P 〈 0.05）. Conclusion The GT-NS-gel has the ability to increase drug concentration in the skin, which can improve the bioavailability of the local skin.

关 键 词：灵芝三萜 纳米混悬剂 凝胶剂 体外释放 经皮渗透 滞留量 效应面法 

分 类 号：R283.6[医药卫生—中药学]