INCREASED DISSOLUTION RATE OF ACECLOFENAC BY FORMATION OF MULTICOMPONENT CRYSTALS WITH L-GLUTAMINE

Q2 Pharmacology, Toxicology and Pharmaceutics

International Journal of Applied Pharmaceutics Pub Date : 2024-02-15 DOI:10.22159/ijap.2024.v16s1.09

Adhitya Jessica, S. W. N. Yasa, Erizal Zaini, L. Fitriani

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引用次数: 0

Abstract

Objective: The objectives of this research were to improve the solubility as well as the rate of dissolution of aceclofenac (ACF) through the formation of multicomponent crystals (MCC) with L-glutamine (LGLN) as a coformer and following the liquid-assisted grinding (LAG) technique. Methods: MCC of ACF and LGLN was formed by Liquid Assisted Grinding (LAG) technique. Powder X-ray Diffractometer (PXRD), Differential Scanning Calorimeter (DSC), Fourier Transform Infrared (FT-IR) spectrometer, Particle Size Analyzer (PSA), and Scanning Electron Microscope (SEM) were used for MCC characterization. Solubility and dissolution test were determined using ultraviolet-visible (Uv-Vis( spectrophotometer. Results: The results showed a decrease in the diffraction peak intensity, melting point, and enthalpy of fusion. FT-IR analysis showed a non-significant wavenumber shift compared to intact components. These characterizations showed that MCC formed a eutectic mixture. SEM and particle size analysis showed a homogeneous particle rod shape and decreased particle size. ACF's solubility in MCC increased 2.21 times more than intact form. MCC's dissolution rate increased by 5.34 times and 5.56 times, respectively, after 60 min in phosphate buffer pH 6.8 and CO2-free distilled water. Conclusion: The formation of MCC of ACF and LGLN considerably enhances ACF's solubility and dissolution rate.

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通过与 l-谷氨酰胺形成多组分晶体提高醋氯芬酸的溶解率

研究目的本研究的目的是以 L-谷氨酰胺（LGLN）为辅剂，通过液体辅助研磨（LAG）技术形成多组分晶体（MCC），从而提高醋氯芬酸（ACF）的溶解度和溶解速率。方法：采用液体辅助研磨（LAG）技术形成 ACF 和 LGLN 的多晶体（MCC）。使用粉末 X 射线衍射仪（PXRD）、差示扫描量热仪（DSC）、傅立叶变换红外光谱仪（FT-IR）、粒度分析仪（PSA）和扫描电子显微镜（SEM）对 MCC 进行表征。使用紫外可见分光光度计测定了溶解度和溶解试验。结果显示结果表明，衍射峰强度、熔点和熔焓均有所下降。傅立叶变换红外分析表明，与完整成分相比，其波长位移并不明显。这些分析表明 MCC 形成了共晶混合物。扫描电子显微镜和粒度分析表明，颗粒呈均匀的棒状，粒度减小。ACF 在 MCC 中的溶解度是完整形态的 2.21 倍。在 pH 值为 6.8 的磷酸盐缓冲液和不含二氧化碳的蒸馏水中溶解 60 分钟后，MCC 的溶解速率分别增加了 5.34 倍和 5.56 倍。结论ACF 和 LGLN 形成的 MCC 大大提高了 ACF 的溶解度和溶解速率。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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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.