PREPARATION OF SPRAY-DRIED MULTICOMPONENT CRYSTALS OF TRIMETHOPRIM-MANDELIC ACID AND ITS PHYSICOCHEMICAL CHARACTERIZATION

Q2 Pharmacology, Toxicology and Pharmaceutics

International Journal of Applied Pharmaceutics Pub Date : 2024-02-15 DOI:10.22159/ijap.2024.v16s1.03

L. Fitriani, Denanda Shintania, Hendrizal Usman, Uswatul Hasanah, Erizal Zaini

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Abstract

Objective: Trimethoprim is a wide-spectrum antimicrobial compound belonging to Class II of the Biopharmaceutics Classification System (BCS), with high permeability but low solubility. This study aimed to prepare a multicomponent crystal (MCC) of trimethoprim-mandelic acid to enhance the solubility of trimethoprim. Methods: MCC trimethoprim–mandelic acid was prepared by spray drying technique. Solid-state characterizations were performed by using PowX-ray diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier-transform infrared (FT IR) spectroscopy, Scanning Electron Microscopy (SEM), and polarized microscopy. The solubility test was performed in distilled water. The amount of dissolved trimethoprim was analyzed by High-Performance Liquid Chromatography (HPLC) using acetonitrile and phosphoric acid 1 % (10:90 v/v) as the mobile phase. Results: MCC characterizations showed a different diffraction pattern from its intact materials according to PXRD analysis, a decrease in the melting point in the DSC thermogram, a shift of the wave number in the FT-IR spectra, and a new crystalline habit compared to the intact materials was presented by SEM analysis. The MCC also showed the color of interference under polarized microscopy, indicating the crystalline phase. The solubility of trimethoprim in MCC increased significantly by 3.98 times in comparison to intact trimethoprim. Conclusion: The MCC trimethoprim-mandelic acid by spray drying technique enhanced the solubility of trimethoprim.

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三甲氧苄啶-扁桃酸喷雾干燥多组分晶体的制备及其理化性质分析

目的：甲氧苄啶是一种广谱抗菌化合物，属于生物制药分类系统（BCS）的第二类，具有高渗透性，但溶解度较低。本研究旨在制备甲氧苄啶-扁桃酸的多组分晶体（MCC），以提高甲氧苄啶的溶解度。制备方法采用喷雾干燥技术制备了 MCC 三甲双胍-扁桃酸。采用粉末 X 射线衍射（PXRD）、差示扫描量热法（DSC）、傅立叶变换红外光谱（FT IR）、扫描电子显微镜（SEM）和偏光显微镜进行固态表征。溶解度测试在蒸馏水中进行。以乙腈和 1 % 磷酸（10:90 v/v）为流动相，采用高效液相色谱法（HPLC）分析溶解的三甲氧苄啶的量。结果显示根据 PXRD 分析，MCC 的衍射图样与完整材料不同，DSC 热图中的熔点降低，傅立叶变换红外光谱中的波数移动，SEM 分析显示出与完整材料相比新的结晶习性。在偏光显微镜下，MCC 还显示出干涉色，表明其为结晶相。与完整的三甲氧苄啶相比，三甲氧苄啶在 MCC 中的溶解度显著增加了 3.98 倍。结论：通过喷雾干燥技术制备的 MCC 三甲氧苄啶-扁桃酸提高了三甲氧苄啶的溶解度。

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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.