In vitro and in vivo quality consistency evaluation of loxoprofen sodium hot-melt adhesive patch and its reference preparation

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Affiliation: 1. College of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou 311402, China 2. Shijiazhuang Discovery Pharmaceutical Technology Co., Ltd, Shijiazhuang 052165, China

Keywords: Loxoprofen sodium patch In vivo and in vitro evaluation In vitro release In vitro permeation Bioequivalence

DOI: 10.12173/j.issn.2097-4922.202504052

Reference: YANG Yang, LIU Hui. In vitro and in vivo quality consistency evaluation of loxoprofen sodium hot-melt adhesive patch and its reference preparation[J]. Yaoxue QianYan Zazhi, 2025, 29(8): 1296-1302. DOI: 10.12173/j.issn.2097-4922.202504052 .[Article in Chinese]  Copied

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Abstract

Objective To evaluate the quality consistency of self-prepared loxoprofen sodium patch and reference preparation in vivo and in vitro.

Methods The consistency of the self-prepared patch and the reference preparation was evaluated through in vitro tests, including initial adhesion, in vitro release, and in vitro permeation. Initial adhesion was measured using the rolling ball method, while in vitro release and in vitro permeation were assessed using the Franz diffusion cell method. Additionally, a pharmacokinetic-bioequivalence human clinical trial was conducted to analyze the pharmacokinetic parameters of both formulations, including the peak plasma concentration (C_max), area under the concentration-time curve from 0 to t (AUC_0-t), and AUC from 0 to infinity (AUC_0-∞). The geometric mean ratio (GMR) and its 90% confidence interval (CI) were calculated to assess bioequivalence.

Results The self-prepared patch and the reference preparation exhibited consistent initial adhesion, in vitro release, and in vitro permeation. For loxoprofen, the 90%CI of C_max, AUC_0-t, and AUC_0-∞ were 101.59% (97.70%, 105.63%), 100.67% (96.51%, 105.01%), and 100.40% (96.37%, 104.60%), respectively. For the trans-hydroxy metabolite, the 90%CI of C_max, AUC_0-t, and AUC_0-∞ were 101.55% (97.72%, 105.53%), 101.79% (97.63%, 106.13%), and 101.43% (97.42%, 105.61%), respectively. All GMR values fell within the equivalence range of 80%-125%.

Conclusion The self-prepared loxoprofen sodium patch demonstrated consistent quality with the reference preparation both in vitro and in vivo.

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