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Published on:August 2020
Indian Journal of Pharmaceutical Education and Research, 2020; 54(3):602-609
Original Article | doi:10.5530/ijper.54.3.109

Solvent Drop Grinding Approach Assisted Development of Glimepiride Co-crystals: Solubility Enhancement Journey of BCS Class-II Product


Authors and affiliation (s):

Santosh Subhash Chhajed1,*, Yatish Rajendra Rajderkar1, Anjali Baburao Tajanpure2, Jaiprakash Navnath Sangshetti3, Debarshi Kar Mahapatra4, Sanjay Jayprakash Kshirsagar5

1Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Nashik, Maharashtra, INDIA.

2Department of Pharmacology, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Nashik, Maharashtra, INDIA.

3Department of Pharmaceutical Chemistry, Y. B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Aurangabad, Maharashtra, INDIA.

4Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur, Maharashtra, INDIA.

5Department of Pharmaceutics, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Nashik, Maharashtra, INDIA.

Abstract:

Background: Glimepiride has limited aqueous solubility and majorly suffers from bioavailability issues that eventually reduce the pharmacotherapeutic potentials of the moiety. Materials and Methods: For the possible augmentation of all the crucial factors, co-crystals were developed using a Generally Recognized As Safe (GRAS) co-former (caffeine) in the presence of few drops of solvent (acetone) by employing a very simple green approach (solvent drop grinding method). The pharmacokinetic study of the co- crystals was performed in Wistar albino rats, the data was compared with free drug form and pharmacokinetic parameters were determined. The fabricated co-crystal product was comprehensively characterized through sophisticated analytical techniques that ascertained the complete product formation. Results: The formation of the glimepiride crystal with the co-former was confirmed through FTIR, DSC, XRD and SEM. From the pharmacokinetic study in rats, the procured data expressed several-folds higher plasma drug concentration which can be correlated with increased bioavailability of glimepiride. Conclusion: This study will positively inspire researchers working in the field of solubility/ bioavailability enhancement due to the simplicity of the method, green approach and positive results which will open several future avenues of drug applications.

Key words: Glimepiride, Caffeine, Co-crystal, Bioavailability, Solubility, Green technique.

 




 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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