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 effect of hydroxypropyl-β-cyclodextrin (HP-β-CD) on pharmaceutical properties of brucine hydrogel emplastrum (BHE). MethodsThe brucine-HP-β-CD inclusion complex (B-HIC) was prepared by the freeze-dry method and the brucine content was determined. The formation of inclusion complex was confirmed by X-ray diffraction (XRD) and differential scanning calorimetry (DSC). The three kinds of emplastrums, BHE, brucine + HP-β-CD physical mixture hydrogel emplastrum (B + HPMHE), and brucine + HP-β-CD inclusion complex hydrogel emplastrum (B + HICHE) were prepared and their pharmaceutical properties, such as drug loading, early adhesion, held adhesion, peel strength, and in vitropercutaneous absorption, were measured and compared. Results The average content of brucine in B-HIC was (59.34 ± 0.68) mg/g and the average inclusion ratio was (98.76 ± 0.51)%. The formation ofinclusion complex was verified by XRD. The adhesion ability of BHE was significantly enhanced by the addition of HP-β-CD. The results of in vitropercutaneous absorption demonstrated that the absorption rate of B+HICHE was the most constant. The cumulative percutaneous absorption percentages of BHE, B + HPMHE, and B + HICHE were (80.16 ± 1.36)%, (85.47 ± 1.89)%, and (92.67 ± 5.88)%,respectively. Conclusion The inclusion of HP-β-CD could dramatically improve the pharmaceutical properties of BHE.

科技部“十一五”重大新药创制项目（2009ZX09103-342）