一种新的环丙贝特钙盐，其溶解度和内在溶解速率均有所提高。

IF 3.7 3区医学 Q2 CHEMISTRY, MEDICINAL

Journal of pharmaceutical sciences Pub Date : 2024-11-01 DOI:10.1016/j.xphs.2024.08.025

Bruno Arantes Borges , Kassius de Souza Reis , Camila Batista Pinto , Javier Ellena , Antônio Carlos Doriguetto , Rudy Bonfilio

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引用次数: 0

摘要

环丙贝特（CIP）是一种活性药物成分（API），根据生物制药分类系统（BCS）被归为第二类，这表明它在水性溶剂中的溶解度较低。由于原料药盐具有更好的溶解性、耐受性、更高的吸收率和吸收范围以及更快的治疗效果，其使用已引起人们的关注。在这项研究中，我们成功获得了一种新型结晶的 CIP 一水钙盐 (Ca(CIP)2.H2O)，并通过单晶 X 射线衍射分析 (SCXRD) 确定了其晶体结构。此外，还通过粉末 X 射线衍射 (PXRD)、傅立叶变换红外光谱 (FTIR)、差示扫描量热法 (DSC)、热重分析 (TGA) 对 Ca(CIP)2.H2O 进行了广泛表征，并对其进行了溶解度、内在溶解度和加速稳定性研究。与不含 CIP 的形式相比，Ca(CIP)2.H2O 表现出更高的溶解度和溶解速率，并且在 40°C （75%RH）条件下可稳定长达 6 个月。因此，Ca(CIP)2.H2O 可以作为固体制剂的一种可行替代品。

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A new ciprofibrate calcium salt with improved solubility and intrinsic dissolution rate

Ciprofibrate (CIP) is an active pharmaceutical ingredient (API) classified as class II on the basis of biopharmaceutical classification system (BCS), what indicates that it has low solubility in aqueous solvents. The use of API salts has attracted attention due to their improvements in solubility, tolerability, higher rate and extent of absorption, and faster onset of the therapeutic effect. In this work, a new crystalline CIP monohydrated calcium salt (Ca(CIP)₂.H₂O) was successfully obtained and its crystal structure determined by single crystal X-ray diffraction analysis (SCXRD). Additionally, Ca(CIP)₂.H₂O was widely characterized by powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and submitted to solubility, intrinsic dissolution and accelerated stability studies. Ca(CIP)₂.H₂O exhibited higher solubility and dissolution rate than CIP-free form and was stable up to 6 months at 40 °C (75 %RH). Therefore, Ca(CIP)₂.H₂O may be a viable alternative for use in solid dosage forms.

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来源期刊

Journal of pharmaceutical sciences 医学-化学综合

CiteScore

7.30

自引率

13.20%

发文量

367

审稿时长

33 days

期刊介绍： The Journal of Pharmaceutical Sciences will publish original research papers, original research notes, invited topical reviews (including Minireviews), and editorial commentary and news. The area of focus shall be concepts in basic pharmaceutical science and such topics as chemical processing of pharmaceuticals, including crystallization, lyophilization, chemical stability of drugs, pharmacokinetics, biopharmaceutics, pharmacodynamics, pro-drug developments, metabolic disposition of bioactive agents, dosage form design, protein-peptide chemistry and biotechnology specifically as these relate to pharmaceutical technology, and targeted drug delivery.