Establishment of In Vitro Dissolution Based on Similarity with In Vivo Dissolution: A Case Study on Aripiprazole

Abstract

In vitro dissolution that predicts the in vivo performance of solid preparations is extremely important in formulation optimization. Fraction absorbed (F a ) has been used to screen in vitro dissolution protocols based on the idea of in vitro−in vivo correlation (IVIVC) but failed to increase the success rate due to the inaccuracy of the F a . The essence of IVIVC is the correlation between in vitro dissolution and in vivo dissolution. We tried to establish in vitro dissolution protocol via similarity with in vivo dissolution using aripiprazole (APZ) as a model drug. Hybrid APZ crystals (APZ-HCs) were prepared by physically embedding aggregation-caused quenching (ACQ) fluorophores inside the lattice to measure the in vivo dissolution. The process did not change the physicochemical properties and crystallinity of APZ. The fluorophore illuminated APZ crystals but was quenched upon dissolution of APZ-HCs in aqueous media, enabling monitoring intact APZ-HCs in real-time. The good correlation between fluorescent quenching and dissolution of APZ-HCs justified reliable quantification of intact APZ crystals. The residual percentage of fluorescence intensity in rats treated by APZ-HCs was recorded with time, which was converted to in vivo dissolution by the difference from 100%. The in vivo dissolution was validated with the F a . The in vitro dissolution profile of APZ was set up via a similarity factor larger than 50 in comparison with the in vivo dissolution. The study provides a novel idea and method to establish in vitro dissolution protocol.

Electrosprayed Eudragit RL100 nanoparticles with Janus polyvinylpyrrolidone patches for multiphase release of paracetamol

“…The blood drug concentration is viewed as a key parameter to evaluate their therapeutic effects. 77–79 The pharmacokinetic profiles of the plasma drug concentration vs. time after oral administration through gavage are depicted in Fig. 9.…”

Electrosprayed Stearic-Acid-Coated Ethylcellulose Microparticles for an Improved Sustained Release of Anticancer Drug

“…The solutes TC, EC, and also SA were solidified together, with few chances to escape from the working processes to the environment. The fate of a drug molecule from the preparation of its dosage form to its final clinical application is influenced by many factors [ 60 , 61 , 62 , 63 , 64 ]. Compared with many “bottom–up” nanofabrication methods, EHDA has its advantages to create drug-loaded micro/nano products with a higher EE % value.…”

A combined electrohydrodynamic atomization method for preparing nanofiber/microparticle hybrid medicines

“…Therefore, pharmaceutical excipients that enhance drug penetration across the blood-prostate barrier could be loaded into the shell coating of ES100 to improve drug delivery. By the way, the fate of drug molecules is influenced by many factors ( Wu and Li, 2022 ; Dong et al, 2023 ; Man et al, 2023 ; Zhang et al, 2023 ), the in vivo / in vitro drug delivery relationships and the final clinic results would be the most useful demonstrations for the applications of new methods of creating medicated materials, which will be further investigated.…”