Pharmacokinetic evaluation of guar gum-based three-layer matrix tablets for oral controlled delivery of highly soluble metoprolol tartrate as a model drug

被引:38
作者
Al-Saidan, SM
Krishnaiah, YSR
Satyanarayana, V
Bhaskar, P
Karthikeyan, RS
机构
[1] Kuwait Univ, Dept Pharmaceut, Fac Pharm, Safat 13110, Kuwait
[2] Sipra Labs Pvt Ltd, Hyderabad, Andhra Pradesh, India
[3] Andhra Univ, Dept Pharmaceut Sci, Visakhapatnam, Andhra Pradesh, India
关键词
metoprolol tartrate; guar gum; three-layered tablets; oral controlled release; pharmacokinetic; humans;
D O I
10.1016/j.ejpb.2004.04.013
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
The objective of the present study is to carry out pharmacokinetic evaluation of oral controlled release formulation (guar gum-based three-layer matrix tablets) containing highly soluble metoprolol tartrate as a model drug. Six healthy volunteers participated in the study, and a two-way crossover design was followed. The plasma concentration of metoprolol tartrate was estimated by reverse-phase HPLC. The pharmacokinetic parameters were calculated from the plasma concentration of metoprolol tartrate versus time data. The delayed T-max, lower C-max decreased K-a, unaltered bioavailability and prolonged t(1/2) indicated a slow and prolonged release of metoprolot tartrate from guar gum three-layer matrix tablets in comparison with the immediate release tablet dosage form. The results of the study indicated that guar gum three-layer matrix tablets were able to provide oral controlled delivery of highly water-soluble drug such as metoprolol tartrate in humans. (C) 2004 Elsevier B.V. All rights reserved.
引用
收藏
页码:697 / 703
页数:7
相关论文
共 23 条
[1]
THE RELATIONSHIP BETWEEN METOPROLOL PLASMA-CONCENTRATION AND BETA-1-BLOCKADE IN HEALTHY-SUBJECTS - A STUDY ON CONVENTIONAL METOPROLOL AND METOPROLOL CR ZOK FORMULATIONS [J].
ABRAHAMSSON, B ;
LUCKER, P ;
OLOFSSON, B ;
REGARDH, CG ;
SANDBERG, A ;
WIESELGREN, I ;
BERGSTRAND, R .
JOURNAL OF CLINICAL PHARMACOLOGY, 1990, 30 (02) :S46-S54
[2]
Guar gum-based sustained release diltiazem [J].
Altaf, SA ;
Yu, K ;
Parasrampuria, J ;
Friend, DR .
PHARMACEUTICAL RESEARCH, 1998, 15 (08) :1196-1201
[3]
METOPROLOL - AN UPDATED REVIEW OF ITS PHARMACODYNAMIC AND PHARMACOKINETIC PROPERTIES, AND THERAPEUTIC EFFICACY, IN HYPERTENSION, ISCHEMIC-HEART-DISEASE AND RELATED CARDIOVASCULAR DISORDERS [J].
BENFIELD, P ;
CLISSOLD, SP ;
BROGDEN, RN .
DRUGS, 1986, 31 (05) :376-429
[4]
Modulation of the dissolution profiles from Geomatrix(R) multi-layer matrix tablets containing drugs of different solubility [J].
Conte, U ;
Maggi, L .
BIOMATERIALS, 1996, 17 (09) :889-896
[5]
Gibaldi M, 1990, PHARMACOKINETICS
[6]
INVESTIGATION OF DRUG ABSORPTION FROM THE GASTROINTESTINAL-TRACT OF MAN .3. METOPROLOL IN THE COLON [J].
GODBILLON, J ;
EVARD, D ;
VIDON, N ;
DUVAL, M ;
SCHOELLER, JP ;
BERNIER, JJ ;
HIRTZ, J .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1985, 19 :S113-S118
[7]
GRAHNEN A, 1984, PHARM INT, V5, P100
[8]
EFFECTS ON EXERCISE TACHYCARDIA DURING 48 HOURS OF A SERIES OF DOSES OF ATENOLOL, SOTALOL, AND METOPROLOL [J].
HARRON, DWG ;
BALNAVE, K ;
KINNEY, CD ;
WILSON, R ;
RUSSELL, CJ ;
SHANKS, RG .
CLINICAL PHARMACOLOGY & THERAPEUTICS, 1981, 29 (03) :295-302
[9]
JAIN NK, 1992, PHARMAZIE, V47, P277
[10]
JOHNSSON G, 1975, ACTA PHARMACOL TOX, V36, P31