Tags

Type your tag names separated by a space and hit enter

Floating matrix dosage form for phenoporlamine hydrochloride based on gas forming agent: in vitro and in vivo evaluation in healthy volunteers.
Int J Pharm. 2006 Mar 09; 310(1-2):139-45.IJ

Abstract

Phenoporlamine hydrochloride is a novel compound that is used for the treatment of hypertension. The purpose of this study was to develop a sustained release tablet for phenoporlamine hydrochloride because of its short biological half-life. Three floating matrix formulations of phenoporlamine hydrochloride based on gas forming agent were prepared. Hydroxypropyl methylcellulose K4M and Carbopol 971P NF were used in formulating the hydrogel drug delivery system. Incorporation sodium bicarbonate into matrix resulted in the tablet floating over simulated gastric fluid for more than 6h. The dissolution profiles of all tablets showed non-Fickian diffusion in simulated gastric fluid. Moreover, release of the drug from these tablets was pH-dependent. In vivo evaluations of these formulations of phenoporlamine hydrochloride were conducted in six healthy male human volunteers to compare the sustained release tablets with immediate release tablets. Data obtained in these studies demonstrated that the floating matrix tablet containing more Carbopol was capable of sustained delivery of the drug for longer periods with increased bioavailability and the relative bioavailability of formulation (containing 25% Carbopol 971P NF, 8.3% HPMC K4M) showed the best bioequivalency to the reference tablet (the relative bioavailability was 1.11+/-0.19).

Authors+Show Affiliations

State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, China.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Comparative Study
Journal Article

Language

eng

PubMed ID

16413710

Citation

Xu, Xiaoqiang, et al. "Floating Matrix Dosage Form for Phenoporlamine Hydrochloride Based On Gas Forming Agent: in Vitro and in Vivo Evaluation in Healthy Volunteers." International Journal of Pharmaceutics, vol. 310, no. 1-2, 2006, pp. 139-45.
Xu X, Sun M, Zhi F, et al. Floating matrix dosage form for phenoporlamine hydrochloride based on gas forming agent: in vitro and in vivo evaluation in healthy volunteers. Int J Pharm. 2006;310(1-2):139-45.
Xu, X., Sun, M., Zhi, F., & Hu, Y. (2006). Floating matrix dosage form for phenoporlamine hydrochloride based on gas forming agent: in vitro and in vivo evaluation in healthy volunteers. International Journal of Pharmaceutics, 310(1-2), 139-45.
Xu X, et al. Floating Matrix Dosage Form for Phenoporlamine Hydrochloride Based On Gas Forming Agent: in Vitro and in Vivo Evaluation in Healthy Volunteers. Int J Pharm. 2006 Mar 9;310(1-2):139-45. PubMed PMID: 16413710.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Floating matrix dosage form for phenoporlamine hydrochloride based on gas forming agent: in vitro and in vivo evaluation in healthy volunteers. AU - Xu,Xiaoqiang, AU - Sun,Minjie, AU - Zhi,Feng, AU - Hu,Yiqiao, Y1 - 2006/01/18/ PY - 2005/08/04/received PY - 2005/11/17/revised PY - 2005/12/03/accepted PY - 2006/1/18/pubmed PY - 2006/6/3/medline PY - 2006/1/18/entrez SP - 139 EP - 45 JF - International journal of pharmaceutics JO - Int J Pharm VL - 310 IS - 1-2 N2 - Phenoporlamine hydrochloride is a novel compound that is used for the treatment of hypertension. The purpose of this study was to develop a sustained release tablet for phenoporlamine hydrochloride because of its short biological half-life. Three floating matrix formulations of phenoporlamine hydrochloride based on gas forming agent were prepared. Hydroxypropyl methylcellulose K4M and Carbopol 971P NF were used in formulating the hydrogel drug delivery system. Incorporation sodium bicarbonate into matrix resulted in the tablet floating over simulated gastric fluid for more than 6h. The dissolution profiles of all tablets showed non-Fickian diffusion in simulated gastric fluid. Moreover, release of the drug from these tablets was pH-dependent. In vivo evaluations of these formulations of phenoporlamine hydrochloride were conducted in six healthy male human volunteers to compare the sustained release tablets with immediate release tablets. Data obtained in these studies demonstrated that the floating matrix tablet containing more Carbopol was capable of sustained delivery of the drug for longer periods with increased bioavailability and the relative bioavailability of formulation (containing 25% Carbopol 971P NF, 8.3% HPMC K4M) showed the best bioequivalency to the reference tablet (the relative bioavailability was 1.11+/-0.19). SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/16413710/Floating_matrix_dosage_form_for_phenoporlamine_hydrochloride_based_on_gas_forming_agent:_in_vitro_and_in_vivo_evaluation_in_healthy_volunteers_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(05)00816-1 DB - PRIME DP - Unbound Medicine ER -