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目的考察加入羟丙基-β-环糊精(HP-β-CD)对马钱子碱贴膏剂药剂学性质的影响。方法采用冷冻干燥法制备了马钱子碱HP-β-CD包合物并测定其量,采用X射线衍射和DSC分析验证了包合物的形成。制备了马钱子碱贴膏剂、马钱子碱与HP-β-CD物理混合物贴膏剂以及马钱子碱包合物贴膏剂,并比较了3种贴膏剂的载药量、初黏力、持黏力、剥离强度、体外透皮吸收性质等药剂学性质。结果制得的马钱子碱HP-β-CD包合物中马钱子碱的平均质量分数为(59.34±0.68)mg/g,平均包合率为(98.76±0.51)%,X射线衍射测定结果验证了包合物的形成。HP-β-CD的加入显著提高了马钱子碱贴膏剂的黏附力。马钱子碱包合物贴膏剂的体外透皮吸收速度最为平稳;马钱子碱贴膏剂、物理混合物贴膏剂和包合物贴膏剂的24 h累积透过率分别为(80.16±1.36)%、(85.47±1.89)%和(92.67±5.88)%。结论 HP-β-CD包合有助于改善马钱子碱贴膏剂的药剂学性质。
Objective To investigate the effects of hydroxypropyl-β-cyclodextrin (HP-β-CD) on the pharmacological properties of brucine paste. Methods The strychnine HP-β-CD inclusion complex was prepared by freeze-drying method and its content was determined. The formation of inclusion complex was confirmed by X-ray diffraction and DSC. Strychnine patch, strychnine and HP-β-CD physical mixture patch and strychnine inclusion patch were prepared, and the drug loading, initial viscosity, Holding sticky, peel strength, transdermal absorption in vitro and other pharmacological properties. Results The average mass fraction of brucine in strychnine HP-β-CD inclusion complex was (59.34 ± 0.68) mg / g and the average inclusion rate was (98.76 ± 0.51)%. The results of X-ray diffraction The results confirmed the formation of inclusion complex. Addition of HP-β-CD significantly increased the adhesion of brucine paste. The transdermal absorption rate of strychnine inclusion complex was the most stable in vitro. The cumulative transmission rates of brucine, physical mixture and inclusion complex were (80.16 ± 1.36)% , (85.47 ± 1.89)% and (92.67 ± 5.88)%, respectively. Conclusion Inclusion of HP-β-CD helps to improve the pharmacological properties of brucine paste.