复合物微针的制备及其对盐酸青藤碱透皮性能的影响  

Preparation of compound microneedles and its influence on transdermal delivery of sinomenine hydrochloride

作　　者：陈磊[1] 桂双英[1,2] 钱珊珊[1] 方慧慧[1] 

机构地区：[1]安徽中医药大学,安徽合肥230031 [2]安徽省中药制剂工程技术中心,安徽合肥230031

出　　处：《中国医院药学杂志》2014年第4期255-259,共5页Chinese Journal of Hospital Pharmacy

基　　金：国家自然基金项目(编号:81274099);安徽省自然基金(编号:11040606M219);安徽省高校省级自然科学研究基金重点项目(编号:KJ2011A194)

摘　　要：目的:优选复合物微针的处方工艺,并探讨微针对盐酸青藤碱透皮性能的影响。方法:采用浇铸法制备复合物微针,采用单因素法优选处方,并对微针进行表征。采用改良Franz扩散池考察微针处理皮肤对盐酸青藤碱微乳凝胶、盐酸青藤碱凝胶经皮吸收的影响。结果:优选出微针的处方工艺为:质量分数90%麦芽糖与10%聚乳酸-羟基乙酸共聚物(PLGA)在160℃混合均匀作为微针基质,并向其中加入重量比10%的聚乙二醇(PEG-4 000)作为脱模剂,在65℃脱模;制备出的微针,形貌学考察与机械强度考察均符合要求。微针预处理皮肤后分别使得盐酸青藤碱微乳凝胶、盐酸青藤碱凝胶的累积渗透量增加了15.50倍和22.13倍。结论:复合物微针的制备工艺简单、可行;使用复合物微针对大鼠皮肤进行穿刺后与单纯的被动扩散比较,能显著增加盐酸青藤碱透皮给药的累积渗透量,微针为盐酸青藤碱透皮给药系统提供一种新型、高效、无痛的透皮给药新技术,具有广泛的应用前景。OBJECTIVE To optimize the optimal preparation process of compound microneedles and prepare compound mi- croneedles for investigating its effect on transdermal delivery of sinomenine hydrochloride. METHODS Casting method was ap- plied to fabricating microneedles. Preparation technology was optimized by single factor method and the characterization of the microneedles was also investigated. With Franz diffusion cell as apparatus, the effect of the microneedles on transdermal deliv- ery of sinomenine hydrochloride mieroemulsion-based hydrogel and sinomenine hydrochloride hydrogd were investigated through pretreating rat＇s skins with microneedles. RESULTS The optimized preparation was as follows., maltose （90~）and 10~//00 poly lactic acid glycolic acid copolymer （PLGA） were blended evenly at 165 ~C as ground substance. PEG-4000（weight ratio： 10 %0） was chosen to be stripping compound and be added in ground substance. The temperature of stripping was at 65~C. Microneedles made by above technology conformed to the requirements of the morphology inspection and the mechanical strength inspection. After preproeessing skin by mieroneedies, the cumulative permeation quantity of sinomenine hydrochloride microemulsion-based hydrogel and sinomenine hydrochloride hydrogel increased 15.50 times and 22. 13 times, respectively. CONCLUSION The preparation technology of compound microneedles is simple and reliable. Compared with the pure passive diffusion group, puncturing the rat＇s skin by compound microneedles can increase the cumulative permeation quantity of trans- dermal drug delivery of sinomenine hydrochloride markedly. Microneedles provide an efficient and promising technology for transdermal drug delivery of sinomenine hydrochloride.

关 键 词：微针 盐酸青藤碱 经皮给药 

分 类 号：R28[医药卫生—中药学]