雪上一枝蒿生物碱可溶性微针制备

Preparation of soluble microneedles of Aconitum brachypodum alkaloids

目的 制备雪上一枝蒿生物碱可溶性微针。方法 离心注模法制备可溶性微针。在单因素试验基础上,以硫酸软骨素用量、PVP K120用量、40%乙醇用量为影响因素,刺孔率为评价指标,Box-Behnken响应面法优化处方,考察形态、穿刺性能、含药量、体外透皮性能。结果 最优处方为硫酸软骨素用量123 mg, PVP K120用量298 mg, 40%乙醇用量2.4 mL,刺孔率为98.3%。可溶性微针为黄色正方形贴片,针体呈圆锥形,可刺穿铝箔和大鼠皮肤,含药量为(0.94±0.025)mg。可溶性微针组24 h内累积渗透率为91.4%,明显高于凝胶膏剂组,渗透符合Higuchi方程。结论 雪上一枝蒿可溶性微针机械强度较好,可实现药物的有效经皮递送。

AIM To prepare the soluble microneedles of Aconitum brachypodum Diels alkaloids.METHODS Centrifugal molding method was adopted in the preparation of soluble microneedles.With chondroitin sulfate consumption,PVP K120 consumption and 40%ethanol consumption as influencing factors,piercing rate as an evaluation index,the formulation was optimized by Box-Behnken response surface method,after which the morphology,piercing performance,drug content and in vitro transdermal performance were investigated.RESULTS The optimal formulation was determined to be 123 mg for chondroitin sulfate consumption,298 mg for PVP K120 consumption,and 2.4 mL for 40%ethanol consumption,the piercing rate was 98.3%.The soluble microneedles were yellow and square patch with conoid needle,which could pierce aluminum foil and rat skin,along with the drug content of(0.94±0.025)mg.The soluble microneedle group demonstrated the accumulative permeability rate of 91.4%within 24 h,which was higher than that in the gel ointment group,and the permeability accorded with Higuchi equation.CONCLUSION The soluble microneedles of A.brachypodum alkaloids exhibit good mechanical strength,which can achieve effective transdermal delivery of drugs.