Abstract
Captopril has a short elimination half-life and is stable at pH 1.2 and as the pH increases; the drug becomes unstable and undergoes a degradation reaction. The purpose of this study was to develop a gastroretentive controlled release drug delivery system with swelling and floating properties. Seventeen tablet formulations were designed using hydroxyl propyl methyl cellulose (HPMC) K4M, Carbomer 934, Eudragit RS PO as release retarding polymer(s), lactose or Avicel PH 102 as a filler and sodium bicarbonate as a gas former by direct compression. Tablets were evaluated for various physical parameters, floating properties, swelling ability and drug release characteristics in 12 h. Based on the release kinetics, all formulations best fitted the Higuchi, Hixson Crowell model and non-Fickian as the mechanism of drug release. Statistical analyses of data revealed that formulation containing HPMC K4M (42%, w/w), NaHCO3 (8%, w/w) and Avicel PH 102 (32.35%, w/w) was the promising system exhibiting excellent floating properties and sustained drug release (12 h) characteristics. Key words: Floating drug delivery system, captopril, HPMC K4M, Carbomer 934, Eudragit RS PO.
Highlights
The drug bioavailability of pharmaceutical dosage forms is influenced by various factors
It is useful for drugs that act locally in the proximal part of GI tract such as antibiotic administration for Helicobacter pylori eradication in the treatment of peptic ulcer, for drugs that exhibit poor solubility in the intestinal tract such as diazepam and verapamil HCl, and for drugs that are unstable in the intestinal fluid such as Captopril (Sungthongjeen et al, 2008; Gambhire et al, 2007; Singh and kim, 2000)
All batches were produced under similar conditions
Summary
The drug bioavailability of pharmaceutical dosage forms is influenced by various factors. One of the important factors is the gastric residence time (GRT) of these dosage forms. Variable and short gastric emptying time can result in an incomplete release of drug and diminished efficacy of the administered dose. Floating drug delivery system (FDDS) is one of the gastroretentive dosage forms that could prolong GRT to obtain sufficient drug bioavailability (Sungthongjeen et al, 2008; Strubing et al, 2008a,b; Gambhire et al, 2007). It is useful for drugs that act locally in the proximal part of GI tract such as antibiotic administration for Helicobacter pylori eradication in the treatment of peptic ulcer, for drugs that exhibit poor solubility in the intestinal tract such as diazepam and verapamil HCl, and for drugs that are unstable in the intestinal fluid such as Captopril (Sungthongjeen et al, 2008; Gambhire et al, 2007; Singh and kim, 2000)
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