Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar- Delhi, Phagwara (Punjab) 144411, India.
School of Pharmaceutical Education and Research, Jamia Hamdard University, Hamdard Nagar, New Delhi, Delhi, 110062, India.
Curr Drug Deliv. 2021;18(5):596-606. doi: 10.2174/1567201817666200902151528.
To develop a co-crytsal of Telmisartan for enhancing its solubility in water.
Intermolecular interaction happens in crystal packing; it utilizes and helps to understand the design of new solid with their respective chemical and physical properties called crystal engineering. It is a blueprint of molecular solids with specific chemical and physical properties through an understanding and handling of intermolecular interaction for increasing the solubility, in case of poor water-soluble drugs.
The study was taken under consideration with an aim to generate and synthesize a cocrystal form of Telmisartan (TEL) with L-lysine to improve its water solubility, dissolution, and micrometric properties.
Using dry grinding technique, solvent evaporation and cooling crystallization, the results revealed a generation of co-crystals with enhanced solubility by liquid drop grinding method. Hence, this process was further explored to investigate various formulations and process parameters that could significantly affect the crystal solubility, dissolution, and micrometric properties.
The solubility of TEL co-crystals was enhanced by L-lysine. Further, the optimized batch was subjected to its micrometric evaluation and physiochemical characterization like FT-IR, NMR, PXRD. The result of the micrometric evaluation showed better results as compared to standards. The dissolution studies also showed a better dissolution rate for TEL co-crystal tablets than TEL tablets formulation.
Co-crystals of TEL with L-lysine showed better solubility and dissolution rate.
开发替米沙坦共晶以提高其在水中的溶解度。
分子间相互作用发生在晶体堆积中；它利用并有助于理解新的固体的设计及其各自的化学和物理性质，称为晶体工程。它是通过理解和处理分子间相互作用来增加溶解度的蓝图，对于水溶性差的药物而言。
本研究旨在生成和合成替米沙坦（TEL）与 L-赖氨酸的共晶形式，以提高其水溶解度、溶解率和微观性质。
使用干法研磨技术、溶剂蒸发和冷却结晶，结果表明通过液滴研磨法生成了溶解度提高的共晶。因此，进一步探索了该过程以研究可能显著影响晶体溶解度、溶解率和微观性质的各种配方和工艺参数。
L-赖氨酸提高了替米沙坦共晶的溶解度。此外，优化的批次还进行了微观评价和物理化学特性分析，如 FT-IR、NMR、PXRD。微观评价的结果显示出比标准更好的结果。溶出度研究也表明替米沙坦共晶片剂的溶出率比替米沙坦片剂配方更好。
替米沙坦与 L-赖氨酸的共晶显示出更好的溶解度和溶解速率。
