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Inclusion Complex of Hydroxypropyl-β-Cyclodextrin with Carbamazepine: Preparation by Co-Dissolution, Characterization, and In Vivo Comparative Study of the Anticonvulsant Activity
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2021-07-23 , DOI: 10.1007/s11094-021-02425-w
M. N. Antyasova 1 , V. S. Tyukova 1 , D. I. Prokhorov 1 , E. S. Zhavoronok 1 , A. V. Panov 1 , S. A. Kedik 1 , I. G. Kapitsa 2
Affiliation  

The inclusion complex of the antiepileptic drug carbamazepine with hydroxypropyl-β-cyclodextrin was prepared by co-dissolution in practically quantitative yield with losses <1% to increase its solubility and bioavailability. The complex was studied by PMR spectroscopy and differential scanning calorimetry. Acomparison with initial carbamazepine and hydroxypropyl-β-cyclodextrin confirmed that the inclusion complex formed without covalent chemical bonds. The physicochemical properties of the inclusion complex were studied. Its solubility in water was determined as 5・105 mg/L (at 25°C). The anticonvulsant activity of the resulting drug form was assessed after intraperitoneal and intranasal administration to mice. The results indicated that the complex could be used effectively as an anticonvulsant agent at a dose of 20 mg/kg.



中文翻译:

羟丙基-β-环糊精与卡马西平的包合物:共溶解制备、表征和抗惊厥活性的体内比较研究

抗癫痫药物卡马西平与羟丙基-β-环糊精的包合物通过共溶解制备,产量几乎定量,损失<1%,以增加其溶解度和生物利用度。通过PMR光谱和差示扫描量热法研究该配合物。与初始卡马西平和羟丙基-β-环糊精的比较证实包合物形成时没有共价化学键。研究了包合物的理化性质。其在水中的溶解度测定为 5・10 5毫克/升(在 25°C 时)。在对小鼠腹膜内和鼻内给药后评估所得药物形式的抗惊厥活性。结果表明,该复合物在20mg/kg的剂量下可有效用作抗惊厥剂。

更新日期:2021-07-23
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