Solid State Characterization of Olmesartan medoximil Solid Dispersion and in-silico Formulation Design using Quality by Design Techniques Engendered by Definitive Screening Design

Abstract

Objectives: Olmesartan medoxomil (OM) is employed for treating patients who are intolerant of ACE inhibitors. The challenge to the researchers is because of its poor oral bioavailability and poor solubility. The approach for this problem is to use a hydrophilic carrier in formulation of oro-dispersible tablet (ODT) which presents a suitable way to improve the bioavailability by using quality by design (QbD) techniques with design of experiments (DoE) using definitive screening design (DSD) which produce a robust and rugged formulation. Methods: The focus of the research was to formulate OM/PVP solid dispersion (SD) and formulation of an Oro dispersible tablet (ODT) by QbD techniques. The main focus of this research is to provide a rugged and robust formulation using QbD concept with the application of Definitive screening design for optimization. Results: The dissolution studies of OM/PVP K30 1:1% w/w showed full release within 30 min which may be attributed due to the hydrogen bond formation between OM and PVP K30 in the FTIR spectra which enhanced the solubility. The disintegration and dissolution results were found to be satisfactory and meeting the desired quality target product profile (QTPP). Conclusion: The present research highlights a thorough understanding of the dosage form development with the knowledge of the critical risks involved in formulation to have an impact on critical quality attributes (CQAs). The critical material attributes (CMAs) were refined by DoE using definitive screening design (DSD) to develop design space. Key words: Critical material attributes (CMAs), Critical quality attributes (CQAs), Definitive screening design (DSD), Quality by design (QbD), Design of experiments (DoE).