具有更好溶解性的酮洛芬-琥珀酸-糖精共晶体的制备及固态表征

Q2 Pharmacology, Toxicology and Pharmaceutics

International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI:10.22159/ijap.2024v16i1.48829

Teguh Imanto, E. R. Wikantyasning, Setyo Nurwaini, Monica Amalia, N. Sambudi, N. Y. Harun

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引用次数: 1

摘要

研究目的本研究旨在通过使用琥珀酸和糖精以 1:1:1 和 2:1:1 的摩尔比共结晶来提高酮洛芬的溶解度，酮洛芬是一种非甾体抗炎药（NSAID），属于生物制药分类系统（BCS）二级：方法：采用浆料法制备酮洛芬共晶体，然后对其进行各种物理化学表征技术，如熔点测定、溶解研究、差示扫描量热法（DSC）、X 射线衍射法（XRD）和傅立叶变换红外光谱法（FTIR）：结果表明，摩尔比为 1:1:1 的酮洛芬-琥珀酸-糖精共晶体（配方 1）的溶解度高于酮洛芬的溶解度标准和摩尔比为 2:1:1 的共晶体（配方 2）。配方 1、配方 2 和标准酮洛芬的溶出曲线（Q30）分别为 96.73±1.77、93.09±1.16 和 70.22±4.72。这些结果表明，采用浆液法与琥珀酸和糖精构象共结晶可显著提高酮洛芬的溶解度：1:1:1摩尔比的酮洛芬-琥珀酸-糖精共晶体（配方1）是测试样品中最有效的配方，显示出最高的溶解度。这项研究可为开发生物利用度和疗效更高的新型药物制剂提供有价值的见解。

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PREPARATION AND SOLID-STATE CHARACTERIZATION OF KETOPROFEN-SUCCINIC ACID-SACCHARIN CO-CRYSTAL WITH IMPROVED SOLUBILITY

Objective: This study aimed to improve the solubility of Ketoprofen, a non-steroidal anti-inflammatory drug (NSAID) that belongs to the Biopharmaceutical Classification System (BCS) Class II, through co-crystallization using succinic acid and saccharin coformers in a 1:1:1 and 2:1:1 molar ratio. Methods: The slurry method was utilized to prepare the ketoprofen co-crystals, which were then subjected to various physical-chemical characterization techniques such as melting point determination, dissolution studies, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared (FTIR) spectroscopy. Results: The results showed that the 1:1:1 molar ratio of ketoprofen-succinic acid-saccharin co-crystal (Formula 1) exhibited higher solubility than the solubility standard of Ketoprofen and the 2:1:1 molar ratio of the co-crystal (Formula 2). The dissolution profile (Q30) of Formula 1, Formula 2, and standard Ketoprofen were 96.73±1.77, 93.09±1.16, and 70.22±4.72, respectively. These findings suggest that co-crystallization with succinic acid and saccharin conformers using the slurry method can significantly enhance the solubility of Ketoprofen. Conclusion: The 1:1:1 molar ratio of ketoprofen-succinic acid-saccharin co-crystal (Formula 1) was the most effective formulation among the tested samples, demonstrating the highest solubility. This research may provide valuable insights for developing novel drug formulations with improved bioavailability and therapeutic efficacy.

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来源期刊

International Journal of Applied Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)

CiteScore

1.40

自引率

0.00%

发文量

219

期刊介绍： International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open access journal devoted to the excellence and research in the pure pharmaceutics. This Journal publishes original research work that contributes significantly to further the scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based drug delivery, nanotechnology, nanocarrier based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions etc. However, the other areas which are related to the pharmaceutics are also entertained includes physical pharmacy and API (active pharmaceutical ingredients) analysis. The Journal publishes original research work either as a Original Article or as a Short Communication. Review Articles on a current topic in the said fields are also considered for publication in the Journal.