Dr. B.C. Roy College of Pharmacy & AHS., Formulation Development Research Unit, Pharmaceutics, Durgapur-06, West Bengal, India.
Curr Drug Deliv. 2021;18(1):44-53. doi: 10.2174/1567201817666200804110837.
The sole purpose of this study is to improve the solubility and dissolution of telmisartan by cocrystallization technique and apply a computational simulation approach to assess the nature of chemical interactions between telmisartan and coformer as well as the solvent contribution to the molecules for furnishing cocrystallization.
The effects of various concentrations of coformer . oxalic acid on physicochemical parameters and drug release were investigated.
Solubility studies suggested that cocrystallization technique with oxalic acid helps to increase the solubility of pure telmisartan of about 7 folds and drug release study revealed that telmisartan-oxalic acid cocrystals showed greater dissolution as compared to pure telmisartan. SEM study suggested that prepared telmisartan cocrystals showed rhomboid-shaped crystals with sharp edges and smooth surface. FTIR study revealed that shifting in the vibrational frequencies of C=O group of telmisartan in telmisartan- oxalic acid cocrystal indicates the formation of supra molecular hetero synthon of the cocrystal. DSC and XRD studies confirmed the formation of telmisartan-oxalic acid cocrystals. Computational simulation approach revealed that telmisartan and oxalic acid can interact with each other in the presence of methanol and water where oxalic acid can form interactions principally with the others. The interactions, thereof, may form several associations or bondings in between the drug and carrier modifying the planarity, bond energy, bond angles of both which subsequently lead to cocrystallization.
So, the present research concluded that prepared telmisartan-oxalic acid cocrystal is a successful application of crystal engineering approach to improve the physicochemical properties as well as to enhance the solubility and dissolution of telmisartan.
本研究的唯一目的是通过共晶技术提高替米沙坦的溶解度和溶解率，并应用计算模拟方法来评估替米沙坦与共晶形成剂之间的化学相互作用的性质以及溶剂对形成共晶的分子的贡献。
考察了不同浓度的共晶形成剂草酸对替米沙坦物理化学参数和药物释放的影响。
溶解度研究表明，与草酸共晶化技术有助于将纯替米沙坦的溶解度提高约 7 倍，药物释放研究表明，替米沙坦-草酸共晶比纯替米沙坦具有更大的溶解能力。SEM 研究表明，所制备的替米沙坦共晶呈现出具有锐边和光滑表面的菱形晶体。FTIR 研究表明，替米沙坦-草酸共晶中替米沙坦的 C=O 基团振动频率的移动表明共晶形成了超分子杂同晶。DSC 和 XRD 研究证实了替米沙坦-草酸共晶的形成。计算模拟方法表明，替米沙坦和草酸可以在甲醇和水的存在下相互作用，其中草酸可以与其他物质形成相互作用。这些相互作用可能在药物和载体之间形成若干种关联或键合，从而改变两者的平面性、键能和键角，进而导致共晶化。
因此，本研究得出结论，所制备的替米沙坦-草酸共晶是晶体工程方法成功应用的一个例子，可改善替米沙坦的物理化学性质，提高其溶解度和溶解率。
