Dissolution of Poorly Water-soluble Drugs: Proof of Concept Based on Fluorescence Bioimaging

Overview

Journal Acta Pharm Sin B

Publisher Elsevier

Specialty Pharmacology

Date 2021 May 17

PMID 33996417

Citations 10

Authors

Yinqian Yang

Yongjiu Lv

Chengying Shen

Tingting Shi

Haisheng He

Jianping Qi

Xiaochun Dong

Weili Zhao

Yi Lu

Wei Wu

Affiliations

Soon will be listed here.

Abstract

‒ correlation (IVIVC) of solid dosage forms should be established basically between and dissolution of active pharmaceutical ingredients. Nevertheless, dissolution profiles have never been accurately portrayed. The current practice of IVIVC has to resort to absorption fractions ( ). In this proof-of-concept study, dissolution of a model poorly water-soluble drug fenofibrate (FNB) was investigated by fluorescence bioimaging. FNB crystals were first labeled by near-infrared fluorophores with aggregation-caused quenching properties. The dyes illuminated FNB crystals but quenched immediately and absolutely once been released into aqueous media, enabling accurate monitoring of residual drug crystals. The linearity established between fluorescence and crystal concentration justified reliable quantification of FNB crystals. dissolution was first measured following pharmacopoeia monograph protocols with well-documented IVIVC. The synchronicity between fluorescence and dissolution of FNB supported using fluorescence as a measure for determination of dissolution. dissolution correlated well with dissolution, acquired by either live or imaging. The newly established IVIVC was further validated by correlating both and dissolution with obtained from pharmacokinetic data.

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