Virtual screening of coformers and solubility test for glibenclamide cocrystallization
Journal Title: National Journal of Physiology, Pharmacy and Pharmacology - Year 2018, Vol 8, Issue 1
Abstract
Background: The therapeutic effectiveness of active pharmaceutical ingredients (API) depends on their solubility. API, which has poorly soluble drugs, can cause low bioavailability. According to the biopharmaceutical classification system (BCS), glibenclamide is classified under BCS Class II drugs), which has low solubility and high permeability. Cocrystallization is one method to enhance the physical properties of drugs, especially the solubility. Aims and Objectives: In this study, we apply the approach to the solid state to estimate the probability of cocrystal formation using virtual screening, and then, study the solubility and dissolution test of one of the best coformers. Materials and Methods: We used virtual screening of coformers for glibenclamide by employing the molecular docking method. AutoDock was used for docking, and the type and energy (Ei) of interaction were observed. The work was continued by the cocrystallization process using dry grinding. Solubility and dissolution tests have referred to the Higuchi and Connor methods using the ultraviolet spectrophotometer. Results: Based on molecular docking, the best of three from coformers were oxalic acid (Ei = −1.6 kcal/mol), benzoic acid (Ei = −2.6 kcal/mol), and ascorbic acid (Ei = −2.1 kcal/mol). The result of the solubility test showed that glibenclamide oxalic acid increases by 81.6% compared to pure glibenclamide at 24 h. The result of the dissolution test showed that glibenclamide oxalic acid has a better curve (77.3% in 60 min) that pures glibenclamide (44.52% in 60 min). Conclusion: This study indicated that oxalic acid as a coformer can increase the dissolution profile of glibenclamide by the approach cocrystalization method.
Authors and Affiliations
Arif Budiman, Sandra Megantara, Ayu Apriliani
Keywords
Related Articles
- EP ID EP449762
- DOI 10.5455/njppp.2017.7.0833229092017
- Views 77
- Downloads 0
Fructose-1,6-diphosphate and vitamin C combination increases seizure threshold in chemical kindling models
Background: Fructose-1,6-diphosphate (FDP), through its activity in glucose metabolism, has anticonvulsant efficacy whereas vitamin C acts as neuromodulator. Aims and Objectives: To assess the antiepileptic effects of FD...
Evaluation of diuretic, saluretic and natriuretic activity of hydrochlorothiazide in combination with misoprostol in Wistar rats
Background: Renal vasodilatation by prostaglandins is well proven facts. Furosemide is better diuretics due to their additional effect on intrarenal hemodynamic changes brought about by increase in local prostaglandin sy...
Lower esophageal sphincter pressures in gastroesophageal reflux disease: Where do they stand?
Background: Esophageal manometry is mandatory for localization of lower esophageal sphincter (LES) in patients undergoing ambulatory esophageal pH-metry for proper positioning of the pH-sensing catheter. Manometry not...
Attitude and perceptions of fifth term medical students of Gulbarga Institute of Medical Sciences, Kalaburagi, regarding teaching methods and their learning in pharmacology
Background: Pharmacology, like any other branch of medicine, is progressing by leaps and bounds. Consequently, reforms in undergraduate teaching are the need of the hour. Aims and Objectives: To determine the medical stu...
Learning styles and approaches toward pharmacology curriculum among medical undergraduates
Background: Learning styles (LSs) and learning approaches (LAs) of each medical student vary to a great extent. If LSs and LAs of the students are known, the teaching-learning programs can be developed in an appropriate...