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Published on:June 2022
Indian Journal of Pharmaceutical Education and Research, 2022; 56(3):697-705
Original Article | doi:10.5530/ijper.56.3.118

Novel Glibenclamide–Phospholipid Complex for Diabetic Treatment: Formulation, Physicochemical Characterization, and in-vivo Evaluation


Authors and affiliation (s):

Sandeep Rathor1,2,*, DC Bhatt1

1Department of Pharmaceutical Sciences, Guru Jambheswar University of Sciences and Technology, Hisar, Haryana, INDIA.

2Department of Pharmaceutics, School of Medical and Allied Sciences, K.R. Mangalam University, Sohna Road, Gurugram, Haryana, INDIA.

Abstract:

Introduction: Formulation of phospholipid complex is an ideal approach to improve the solubility of poorly soluble drugs. Objectives: This study has been aimed to prepare a novel glibenclamide-phospholipid complex by using the solvent evaporation technique. Materials and Methods: Because glibenclamide is a weakly soluble medication, complexing it with phospholipids is an excellent way to enhance its solubility. The phospholipid complex of Glibenclamide was produced using the solvent-evaporation technique to enhance its oral efficacy. The formulation was characterized and evaluated by various parameters including FTIR, DSC, PXRD, SEM, TEM, in vitro drug release, and in vivo pharmacokinetic studies in Wistar rats plasma. According to studies, the Glibenclamide phosphates combination is significantly more water-soluble than the physical combination and pure Glibenclamide. The oral bioavailability of the glibenclamide-phospholipids complex was measured by using HPLC in Wistar rats’ plasma. Results: There was no substantial interaction between the medication and the phospholipid in the formulation, according to the FTIR and PXRD findings. The morphology of the formulation was verified by SEM and TEM investigations, indicating that the crystalline form had been converted to an amorphous form. The glibenclamide-phospholipids complex had a greater peak plasma concentration (5.1 vs. 3.8 g/mL), its AUC was higher (14.65 vs. 11.81 μgh/L), and its T1/2 was longer (2.4 vs. 3.1 hr), showing that it enhanced drug dissolution rate. Conclusion: The findings showed that increasing the oral bioavailability of waterinsoluble medicines by phospholipid-complexation is a potential approach. The results showed that phospholipid-complexation may be used to enhance the oral bioavailability of water-insoluble drugs.

Keywords: Glibenclamide, Glibenclamide–phospholipid complex, Pharmacokinetic, Oral bioavailability.

 




 

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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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