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Design and optimization of gastric floating sustained-release mini-tablets of alfuzosin hydrochloride based on a factorial design: in vitro/in vivo evaluation.
Drug Dev Ind Pharm. 2018 Dec; 44(12):1990-1999.DD

Abstract

The purpose of this research was to develop multiple-unit gastric floating mini-tablets and to evaluate the possibility of using these mini-tablets as a delivery system to improve the drug absorption for drugs with a narrow absorption window. Mini-tablets were prepared using hydroxypropyl methylcellulose (HPMC K100M) and carbopol 971P as release retarding agents and sodium bicarbonate (NaHCO3) as gas-forming agent. The properties of the prepared mini-tablets in terms of floating characteristic parameters and in vitro release were evaluated. Furthermore, in vivo gastric retention study in rats and in vivo pharmacokinetic study in rabbits of the optimized formulation were performed. The optimized mini-tablets containing 45% HPMC K100M, 15% stearyl alcohol, 13% carbopol 971P, and 12% NaHCO3 were found to float immediately within 1 min and duration more than 9 h. The in vivo gastric retention study results indicated that the mini-tablets could retain in the stomach for more than 6.67 h. Furthermore, the AUC0-t of the floating mini-tablets (6849.83 ± 753.80 h ng·mL-1) was significantly higher than that of marketed sustained-release tablets XATRAL®XL (4970.16 ± 924.60 h ng·mL-1). All these results illustrated that the gastric floating mini-tablets might be a promising drug delivery system for drugs with a narrow absorption window.

Authors+Show Affiliations

a Department of Pharmaceutics, School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , China.a Department of Pharmaceutics, School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , China.a Department of Pharmaceutics, School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , China.a Department of Pharmaceutics, School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , China.a Department of Pharmaceutics, School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , China.a Department of Pharmaceutics, School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , China.a Department of Pharmaceutics, School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , China.

Pub Type(s)

Journal Article
Validation Study

Language

eng

PubMed ID

30058391

Citation

Gong, Ling, et al. "Design and Optimization of Gastric Floating Sustained-release Mini-tablets of Alfuzosin Hydrochloride Based On a Factorial Design: in Vitro/in Vivo Evaluation." Drug Development and Industrial Pharmacy, vol. 44, no. 12, 2018, pp. 1990-1999.
Gong L, Yu M, Sun Y, et al. Design and optimization of gastric floating sustained-release mini-tablets of alfuzosin hydrochloride based on a factorial design: in vitro/in vivo evaluation. Drug Dev Ind Pharm. 2018;44(12):1990-1999.
Gong, L., Yu, M., Sun, Y., Gao, Y., An, T., Zou, M., & Cheng, G. (2018). Design and optimization of gastric floating sustained-release mini-tablets of alfuzosin hydrochloride based on a factorial design: in vitro/in vivo evaluation. Drug Development and Industrial Pharmacy, 44(12), 1990-1999. https://doi.org/10.1080/03639045.2018.1506473
Gong L, et al. Design and Optimization of Gastric Floating Sustained-release Mini-tablets of Alfuzosin Hydrochloride Based On a Factorial Design: in Vitro/in Vivo Evaluation. Drug Dev Ind Pharm. 2018;44(12):1990-1999. PubMed PMID: 30058391.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design and optimization of gastric floating sustained-release mini-tablets of alfuzosin hydrochloride based on a factorial design: in vitro/in vivo evaluation. AU - Gong,Ling, AU - Yu,Miao, AU - Sun,Yanyan, AU - Gao,Ying, AU - An,Tong, AU - Zou,Meijuan, AU - Cheng,Gang, Y1 - 2018/09/17/ PY - 2018/7/31/pubmed PY - 2019/2/20/medline PY - 2018/7/31/entrez KW - Alfuzosin hydrochloride KW - factorial design KW - floating mini-tablets KW - near-infrared fluorescence imaging KW - pharmacokinetics SP - 1990 EP - 1999 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 44 IS - 12 N2 - The purpose of this research was to develop multiple-unit gastric floating mini-tablets and to evaluate the possibility of using these mini-tablets as a delivery system to improve the drug absorption for drugs with a narrow absorption window. Mini-tablets were prepared using hydroxypropyl methylcellulose (HPMC K100M) and carbopol 971P as release retarding agents and sodium bicarbonate (NaHCO3) as gas-forming agent. The properties of the prepared mini-tablets in terms of floating characteristic parameters and in vitro release were evaluated. Furthermore, in vivo gastric retention study in rats and in vivo pharmacokinetic study in rabbits of the optimized formulation were performed. The optimized mini-tablets containing 45% HPMC K100M, 15% stearyl alcohol, 13% carbopol 971P, and 12% NaHCO3 were found to float immediately within 1 min and duration more than 9 h. The in vivo gastric retention study results indicated that the mini-tablets could retain in the stomach for more than 6.67 h. Furthermore, the AUC0-t of the floating mini-tablets (6849.83 ± 753.80 h ng·mL-1) was significantly higher than that of marketed sustained-release tablets XATRAL®XL (4970.16 ± 924.60 h ng·mL-1). All these results illustrated that the gastric floating mini-tablets might be a promising drug delivery system for drugs with a narrow absorption window. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/30058391/Design_and_optimization_of_gastric_floating_sustained-release_mini-tablets_of_alfuzosin_hydrochloride_based_on_a_factorial_design:_in_vitro/in_vivo_evaluation L2 - http://www.tandfonline.com/doi/full/10.1080/03639045.2018.1506473 DB - PRIME DP - Unbound Medicine ER -