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Indian Journal of Pharmaceutical Education and ResearchNOW IN
Article

Formulation and Evaluation of Nano Co-Crystal Based Oral Disintegrating Tablet of Ezetimibe

J Puneeth1, Preethi Sudheer1★, Shiji John2, Darshan PR1, Jyothi Y3★ Corresponding author

  1. 1Department of Pharmaceutics, Krupanidhi College of Pharmacy, Bengaluru, Karnataka, INDIA.
  2. 2Department of Pharmacy Practice, Krupanidhi College of Pharmacy, Bengaluru, Karnataka, INDIA.
  3. 3Department of Pharmacology, Krupanidhi College of Pharmacy, Bengaluru, Karnataka, INDIA.

CORRESPONDENCE

Preethi Sudheer

Professor, Department of Pharmaceutics, Krupanidhi College of Pharmacy, #12/1, Chikkabellandur, Varthur, Hobli, Bangalore-35, Karnataka, INDIA.

preetisudheer@gmail.com

Received: 02-06-2022; Revised: 28-01-2023; Accepted: 23-06-2023.

Volume 57, Issue 3S · pp. s587–s598 · PUBLISHED 2023 · DOI: 10.5530/ijper.57.3s.67

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ABSTRACT

Background: Low solubility, poor permeability, and hepatic drug degradation are the primary factors responsible for the poor bioavailability issues of orally administered drugs. Ezetimibe, a biopharmaceutics classification system (BCS) Class II anti-cholesteremic drug, has a bioavailability between 35% and 65% due to its substantial intestinal and first-pass metabolism. Objectives: An alternative method for drug administration is to be attempted on an orally disintegrating Ezetimibe tablet to avoid low bioavailability, as mentioned earlier. Materials and Methods: The solubility issues of the drug were tackled by converting the drug into nano co-crystals using nicotinamide as a coformer utilizing the solvent anti-solvent method, followed by spray drying. The formulations were optimized using a custom experimental design. The optimum nano co-crystal formulation was converted into an orally disintegrating tablet using crospovidone as a super disintegrating agent and evaluated. Results: Nano co-crystals solubility was 0.030 to 0.049mg/mL. The release of the drug in a pH of 6.8 phosphate buffer was found to be 027.100.011 to 30.02;0.003%. Compatibility studies by FTIR confirm the absence of the drug's reaction with the excipients. X-ray, as well as DSC, indicated reduced Ezetimibe's crystalline nature. The disintegration time of ODT was marked down as 28 sec. ODT's in vitro release profile in PBS p 6.8 reveal a 20-fold increase in drug release compared to the pure drug. Conclusion: Therefore, ODTs containing nano co-crystals of Ezetimibe could provide a better alternative to improve solubility and the dissolution rate, which may enhance the bioavailability.

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    Puneeth, J., Sudheer, P., John, S., PR, D., & Y, J. (2023). Formulation and Evaluation of Nano Co-Crystal Based Oral Disintegrating Tablet of Ezetimibe. Indian Journal of Pharmaceutical Education and Research, 57(3S), s587–s598. https://doi.org/10.5530/ijper.57.3s.67