TENOXICAM-TROMETHAMINE MULTICOMPONENT CRYSTAL: PHYSICOCHEMICAL CHARACTERISTICS, SOLUBILITY, AND DISSOLUTION EVALUATION

Q2 Pharmacology, Toxicology and Pharmaceutics

International Journal of Applied Pharmaceutics Pub Date : 2024-02-15 DOI:10.22159/ijap.2024.v16s1.04

Uswatul Hasanah, Yesica Azfitri, L. Fitriani, Erizal Zaini

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引用次数: 0

Abstract

Objective: Tenoxicam is classified as a nonsteroidal anti-inflammatory drug employed for managing musculoskeletal conditions. However, its effectiveness is obstructed by its restricted ability to dissolve in water. This investigation aims to create a multicomponent crystal involving tenoxicam and tromethamine to augment tenoxicam's solubility and dissolution rate. Methods: Using the solvent drop grinding technique, the multicomponent crystal was synthesized by combining tenoxicam and tromethamine in equimolar proportions. The physicochemical properties of multicomponent crystal were assessed through powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and FT-IR spectroscopy. Solubility test and dissolution rate profile were conducted to evaluate the effectiveness of multicomponent crystal formation in compared to intact tenoxicam. The solubility test occurred in CO2-free distilled water over 48 h and was quantified using UV spectrophotometry at 368 nm. Dissolution rate profiles were conducted using a USP type II dissolution apparatus in HCl 0.1 N, and CO2-free distilled water as the dissolution media. Results: The multicomponent crystal displayed distinctive characteristics in the diffractogram, including altered melting points, and shifts in the FT-IR spectrum peaks. Within the multicomponent crystal system, the solubility of tenoxicam exhibited a notable increase, specifically by a factor of 11.130. Moreover, the dissolution efficiency of tenoxicam in HCl 0.1 N solution and CO2-free distilled water showed substantial enhancements, with respective increases of 2.600-fold and 8.605-fold observed at the 60-minute mark. Conclusion: In conclusion, the tenoxicam and tromethamine multicomponent crystal formation using a solvent drop grinding technique resulted in a novel crystalline structure, enhancing the solubility and dissolution of tenoxicam both in CO2-free distilled water and HCl 0.1 N.

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替诺昔康-三甲胺多组分晶体：理化特性、溶解性和溶解评估

目的：替诺昔康是一种用于治疗肌肉骨骼疾病的非甾体抗炎药。然而，由于其溶解于水的能力有限，其有效性受到了阻碍。本研究旨在创建一种包含替诺昔康和三甲胺的多组分晶体，以提高替诺昔康的溶解度和溶解速率。研究方法采用溶剂滴磨技术，将替诺昔康和氨基丁三醇以等摩尔比例混合，合成多组分晶体。通过粉末 X 射线衍射 (PXRD)、差示扫描量热 (DSC) 和傅立叶变换红外光谱评估了多组分晶体的理化性质。为了评估多组分晶体与完整的替诺昔康相比的有效性，还进行了溶解度测试和溶解速率曲线测试。溶解度测试在无二氧化碳的蒸馏水中进行，历时 48 小时，采用 368 纳米紫外分光光度法进行定量。使用美国药典 II 型溶解仪，以 0.1 N 盐酸和不含二氧化碳的蒸馏水作为溶解介质，进行溶解速率曲线测试。结果多组分晶体在衍射图中显示出独特的特征，包括熔点的改变和傅立叶变换红外光谱峰的移动。在多组分晶体体系中，替诺昔康的溶解度明显增加，特别是增加了 11.130 倍。此外，替诺昔康在 0.1 N 盐酸溶液和无二氧化碳蒸馏水中的溶解效率也有大幅提高，在 60 分钟时分别提高了 2.600 倍和 8.605 倍。结论总之，利用溶剂滴磨技术形成的替诺昔康和氨丁三醇多组分晶体具有新颖的晶体结构，可提高替诺昔康在无二氧化碳蒸馏水和 0.1 N 盐酸中的溶解度和溶解效率。

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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.