Deshpande Radni D, Shah Devanshi S, Gurram Sharda, Jha Durgesh K, Batabyal Paramita, Amin Purnima D, Sathaye Sadhana
Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, India.
DBT-ICT Centre for Energy Biosciences, Institute of Chemical Technology, Mumbai, India.
Int J Pharm. 2023 Oct 15;645:123386. doi: 10.1016/j.ijpharm.2023.123386. Epub 2023 Sep 9.
Phloretin (PHL), a flavonoid of the dihydrogen chalcone class, is reported to have low oral bioavailability due to its poor solubility and absorption. A common approach to enhance the solubility of such flavonoids is solubilization in a polymeric or lipidic matrix which would help in enhance dissolution rate and solubility. Accordingly, in the current study PHL was dissolved in Gelucire® 44/14 by melt-fusion technique and the viscous semisolid melt was adsorbed on a solid carrier to obtain free flowing granules. SeDeM-SLA (Solid-Liquid Adsorption) expert system was employed to select the most suitable carrier. This study achieved positive outcomes through the successful development of formulated oral PHL granules. The granules exhibited good stability, and favourable pharmacokinetic properties. In addition, the selected carrier effectively retained the antioxidant properties of PHL.
根皮素(PHL)是一种二氢查耳酮类黄酮,据报道,由于其溶解性和吸收性差,口服生物利用度较低。提高此类黄酮溶解度的常用方法是将其溶解在聚合物或脂质基质中,这有助于提高溶解速率和溶解度。因此,在本研究中,通过熔融技术将PHL溶解在Gelucire® 44/14中,并将粘性半固体熔体吸附在固体载体上,以获得自由流动的颗粒。采用SeDeM-SLA(固液吸附)专家系统选择最合适的载体。本研究通过成功开发口服PHL制剂颗粒取得了积极成果。这些颗粒表现出良好的稳定性和有利的药代动力学性质。此外,所选载体有效地保留了PHL的抗氧化特性。