Study on the solubilization of telmisartan by forming cocrystals with aromatic carboxylic acids

Study on the solubilization of telmisartan by forming cocrystals with aromatic carboxylic acids
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芳香族羧酸共晶增溶替米沙坦的研究

DOI:
10.1039/d1ce00551k
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发表时间:
2021-05
期刊:
影响因子:
3.1
通讯作者:
Ren Zhongqi
Ren Zhongqi
中科院分区:
化学3区
文献类型:
--
作者:
Yu Guojia;Chen Xinjian;He Lichao;Li Xiangrong;Zhou Zhiyong;Ren Zhongqi

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通过与几种芳香羧酸形成新的共晶形式,提高了不溶性替米沙坦(TEL)的溶解度。所有固体剂型均表现出3种溶出模式:TEL-HBA在30 min内达到最大释放平衡,在6 h内保持稳定高效的溶出水平。TEL-3 HBA和TEL-2,5DHBA随时间缓慢下降,直至6 h。TEL-3、5DHBA符合“弹簧-降落伞”模型。TEL-HBA混合物是最稳定的,并被选择用于进一步的热力学研究,其发现与HCl(0.1M)溶液的1:1络合。
The solubility of insoluble telmisartan (TEL) was improved by forming new cocrystal forms with several aromatic carboxylic acids. All solid forms showed three dissolution modes: TEL-HBA achieved maximum release equilibrium within 30 min and maintained stable and efficient dissolution level within 6 h. TEL-3HBA and TEL-2,5DHBA showed declining trend slowly over time up to 6 h. TEL-3,5DHBA conformed to the 'spring and parachute' model. The TEL-HBA mixture was most stable and selected for further thermodynamic study, which found a 1:1 complexation with HCl (0.1 M) solution.
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期刊: CrystEngComm
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