Gastric floating matrix tablets: Design and optimization using combination of polymers

Abstract

The real challenge in the development of a controlled drug delivery system is not just to sustain the drug release but also to prolong the presence of the dosage form in the stomach or the upper small intestine until all the drug is completely released in the desired period of time (1-2). The residence of a drug delivery system in the upper part of the gastrointestinal tract (GIT) can be accomplished by several drug delivery systems, such as intragastric floating systems (3), swelling and expandable systems (4), bioadhesive systems (5), modified shape systems (6), high density systems (7), delayed gastric emptying systems (8) and low density super porous systems (9).Domperidone is a synthetic benzimidazole compound that acts as a dopamine D2 receptor antagonist. Domperidone is also used as a prokinetic agent for treatment of up- The purpose of the present study was to develop an optimized gastric floating drug delivery system (GFDDS) containing domperidone as a model drug. Box-Behnken design was employed in formulating the GFDDS with three polymers: hydroxypropyl methylcellulose K4M (HPMC K4M) (X 1 ), Carbopol 934P (X 2 ) and sodium alginate (X 3 ), as independent variables. Floating lag time (FLT), total floating time (TFT), time required to release 50% of the drug (t 50 ) and diffusion exponent (n) were selected as dependent variables. Seventeen formulations were prepared, dissolution data obtained was fitted to the power law and floating profiles were analyzed. HPMC loading was found to be significant for floating properties. Carbopol loading had a negative effect on floating properties but was found helpful in controlling the release rate of the drug. No significant effect of sodium alginate on floating properties was observed but it was important for gel formation. The quadratic mathematical model developed could be used to predict formulations with desired release and floating properties.

Characterization and In Vitro Drug Release Studies of a Natural Polysaccharide Terminalia catappa Gum (Badam Gum)

“…The real challenge in the development of an oral controlled release drug delivery system is not only to control the drug release but also to prolong the presence of the dosage form within the gastrointestinal tract (GIT) until complete release of the drug at a desired period of time (17). Indeed, gastric retention has received significant interest in the past few decades.…”

Floating ability and drug release evaluation of gastroretentive microparticles system containing metronidazole obtained by spray drying

“…Gastroretentive systems have received significant interest in the past few decades, because they are able to sustain the drug release and to prolong the presence of the dosage form within the gastrointestinal tract until all the drug is completely released (Prajapati, Patel, Patel, 2008;Rapolu et al, 2012). Besides being able to continually and sustainably deliver drugs to the small intestinal absorption window, the improvements provided from gastroretentive systems include achieving a greater and prolonged therapeutic effect and thus reducing the frequency of administration periods, and providing a more effective treatment of local stomach disorders (Chen et al, 2010).…”

Matrix Tablet Containing Quaternary Inclusion Complex of Domperidone for Treatment of Diabetic Gastroparesis

“…13 DOM, being a weakly basic drug, may exhibit limited solubility leading into precipitation at intestinal pH if formulated as an extended release dosage form. Due to this reason, Prajapati ST et al, (2008) have developed a gastric floating matrix tablet of DOM to obtain its sustained release. 14 In last few years, some works have been reported where sustained release tablets of DOM have been prepared without considering the aforementioned problem associated with DOM.…”

“…Due to this reason, Prajapati ST et al, (2008) have developed a gastric floating matrix tablet of DOM to obtain its sustained release. 14 In last few years, some works have been reported where sustained release tablets of DOM have been prepared without considering the aforementioned problem associated with DOM. 15,16 β-cyclodextrin (βCD) and its derivatives have been used by many authors to improve the solubility of DOM.…”