Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Development, optimization, and in vitro/in vivo evaluation of ranitidine hydrochloride- resinate sustained-release suspension

Meiping Han¹, Yi Du¹, Xiaowen Wu¹, Xin Zhang¹, Quanzhu Yang¹, Caleb Kesse Firempong¹, Hongfei Liu^1,2 , Dongli Li²

¹School of Biotechnology and Health Sciences, Wuyi University, Jiangmen 529020, China; ²International Healthcare Innovation Institute (Jiangmen), Jiangmen 529040, PR China.

For correspondence:- Hongfei Liu Email: articlepharmacyliu@163.com Tel:+867503299391

Accepted: 25 February 2023 Published: 31 March 2023

Citation: Han M, Du Y, Wu X, Zhang X, Yang Q, Firempong CK, et al. Development, optimization, and in vitro/in vivo evaluation of ranitidine hydrochloride- resinate sustained-release suspension. Trop J Pharm Res 2023; 22(3):457-467 doi: 10.4314/tjpr.v22i3.1

© 2023 The authors.
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Abstract

Purpose: To prepare ranitidine hydrochloride (RH) sustained-release suspension aimed at improving its safety, effectiveness and convenience of administration.

Methods: The RH resinate suspension was prepared using bath method, with a cation- exchange resin as carrier. To obtain an ideal sustained release effect, RH resinates were coated with Eudragit®RS100 using the surface coating method, followed by optimization through a single-factor experiment and response surface analysis. The optimized RH suspension was characterized using accelerated stability test. Moreover, it was pharmacokinetically evaluated in vivo.

Results: The optimized RH resin microcapsules showed relative mean deviation between the predicted and measured release values that was < 10 %, (p < 0.05) and demonstrated good reproducibility. Accelerated stability test results showed that the optimized RH suspension exhibited good stability over a period of 6 months (F > 0.9; drug content: 97 – 100 %, drug release: f₂ > 50; drug leakage < 0.5 %), with good redispersibility. Results from pharmacokinetics showed that values of T_max for RH sustained-release suspension and RH common tablet were 4.00 and 2.5 h, respectively (p < 0.05), while the corresponding C_max values were 2545.78 and 3245.97 ng/mL, respectively (p < 0.05). Results of analysis of AUC_0-24 showed that they were equivalent in terms of AUC_0-24 (p < 0.05) and bioavailability of 101.05%.

Conclusion: The optimized ranitidine hydrochloride (RH) sustained-release suspension has been successfully prepared using ion-exchange resin as a carrier and Eudragit® RS100 as a coating material.

Keywords: Ion exchange resins, Ranitidine hydrochloride (RH), Surface coating method, Sustained-release suspension, Pharmacokinetics, Bioavailabilityv