Oral sustained delivery of atenolol from floating matrix tablets - Formulation and in vitro evaluation

被引:42
作者
Srivastava, AK [1 ]
Wadhwa, S [1 ]
Ridhurkar, D [1 ]
Mishra, B [1 ]
机构
[1] Banaras Hindu Univ, Inst Technol, Dept Pharmaceut, Varanasi 221005, Uttar Pradesh, India
关键词
atenolol; swelling index; floating matrix; guargum; HPMC;
D O I
10.1081/DDC-200054313
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Floating matrix tablets of atenolol were developed to prolong gastric residence time and increase drug bioavailability. Atenolol was chosen as a model drug because it is poorly absorbed from the lower gastrointestinal tract. The tablets were prepared by direct compression technique, using polymers such as hydroxypropyl methylcellulose ( HPMC K15M, K4M), guargum (GG), and sodium carboxymethylcellulose ( SCMC), alone or in combination, and other standard excipients. Tablets were evaluated for physical characteristics viz. hardness, swelling index, floating capacity, thickness, and weight variation. Further, tablets were evaluated for in vitro release characteristics for 8 hr. The effect of effervescent on buoyancy and drug release pattern was also studied. In vitro release mechanism was evaluated by linear regression analysis. GG- and SCMC-based matrix tablets showed significantly greater swelling indices compared with other batches. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium.
引用
收藏
页码:367 / 374
页数:8
相关论文
共 17 条
[1]   A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY [J].
AMIDON, GL ;
LENNERNAS, H ;
SHAH, VP ;
CRISON, JR .
PHARMACEUTICAL RESEARCH, 1995, 12 (03) :413-420
[2]   Optimisation of floating matrix tablets and evaluation of their gastric residence time [J].
Baumgartner, S ;
Kristl, J ;
Vrecer, F ;
Vodopivec, P ;
Zorko, B .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 195 (1-2) :125-135
[3]  
Baumgartner S, 1998, STP PHARMA SCI, V8, P285
[4]  
Davis D.W., 1968, U.S. Patent, Patent No. [3,418,999, 3418999]
[5]   A FLOATING CONTROLLED-RELEASE DRUG-DELIVERY SYSTEM - IN-VITRO IN-VIVO EVALUATION [J].
DESAI, S ;
BOLTON, S .
PHARMACEUTICAL RESEARCH, 1993, 10 (09) :1321-1325
[6]   Controlled-release drug delivery systems for prolonged gastric residence: An overview [J].
Deshpande, AA ;
Rhodes, CT ;
Shah, NH ;
Malick, AW .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1996, 22 (06) :531-539
[7]  
Hwang SJ, 1998, CRIT REV THER DRUG, V15, P243
[8]   FOOD-INDUCED REDUCTION IN BIOAVAILABILITY OF ATENOLOL [J].
MELANDER, A ;
STENBERG, P ;
LIEDHOLM, H ;
SCHERSTEN, B ;
WAHLINBOLL, E .
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, 1979, 16 (05) :327-330
[9]  
MICHAELS AS, 1979, Patent No. 3786813
[10]   THE BILAYER FLOATING CAPSULE - A STOMACH-DIRECTED DRUG DELIVERY SYSTEM FOR MISOPROSTOL [J].
OTH, M ;
FRANZ, M ;
TIMMERMANS, J ;
MOES, A .
PHARMACEUTICAL RESEARCH, 1992, 9 (03) :298-302