Co-crystals: A Novel Approach to Improve the Solubility of Apixaban

被引：1
|
作者：
Asati, Amit, V [1 ,6 ]
Salunkhe, Kishor S. [2 ]
Rajput, Rudra Pratap Singh [3 ]
Chintamani, Sonali R. [4 ]
Khairnar, Akshay U. [5 ]
Patil, Nilesh S. [5 ]
Chintamani, Ravindra N. [5 ]
机构：
[1] Amrutvahini Coll Pharm, Dept Pharmaceut, Ahmednagar, Maharashtra, India
[2] Sanjivani Coll Pharmaceut Educ & Res, Dept Pharmaceut, Kopargaon, Maharashtra, India
[3] Columbia Inst Pharm, Dept Pharmaceut, Raipur, Chhattisgarh, India
[4] MCE Soc Allana Coll Pharm, Dept Pharmaceut, Pune, Maharashtra, India
[5] Inst Pharm, Rajmata Jijau Shikshan Prasarak Mandals, Dept Pharmaceut, Pune, Maharashtra, India
[6] Amrutvahini Coll Pharm, Sangamner 422608, Maharashtra, India
来源：
INTERNATIONAL JOURNAL OF PHARMACEUTICAL INVESTIGATION | 2023年 / 13卷 / 02期
关键词：
Apixaban; Co-crystal; Solubility; Oxalic acid; DRUG;
D O I：
10.5530/ijpi.13.2.033
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Objectives:The current study work was aimed to improve the solubility of Apixaban by forming co-crystals. Materials and Methods: Two solvents mainly Dimethyl Sulphoxide (DMSO) and 2,2,2-trifluoroethanol were tried during the formulation of co-crystals. The other chemicals oxalic acid, adipic acid and L-Tartaric acid were used. Results: From the different trials it was concluded that oxalic acid and DMSO combination with the drug gave the better results for improvement in the solubility. Hence the batch F3 was analysed further. The melting point of F3 was found lower than pure drug. Drug content was found optimum as 95.06 +/- 0.65%. FTIR-spectra demonstrated the combined peaks of drug and oxalic acid. DSC thermogram showed the sharp endothermic peak similar to pure drug. SEM and XRD spectra confirmed the formation of co-crystals. Conclusion: It was found that formation of co-crystals of apixaban and oxalic acid was satisfactory and it was beneficial to improve the solubility of the apixaban.
引用
收藏
页码：243 / 247
页数：5
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