Abstract
The aim of the present study is to formulate floating effervescent microsponge tablet of the narrow absorption window drug, Baclofen (BFN) for controlling drug release and thereby decrease the side effect of the drug. The microsponges of BFN were prepared by non-aqueous emulsion solvent diffusion method (oil in oil emulsion method). The effects of drug: polymer ratio, stirring time and type of Eudragit polymer on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selected microsponge formula was incorporated into the floating effervescent gastro-retentive tablet. The prepared floating microsponge tablet was evaluated for tablet hardness, friability, swelling in addition to in vitro drug release. The results showed that the microsponge formula with Eudragit RS100 had optimum physical properties and controlled drug release (75% of drug release in 8 hr.) when compared with other formulas and pure baclofen. The oil in oil emulsion method is a promising method to produce baclofen microsponge.
Highlights
Conventional tablet dosage form is administered several times a day
Microsponge could encapsulate a wide range of hydrophilic and hydrophobic drugs [5]
Gave the highest peak of absorbance at 220 nm as shown in figure 1; this result was with an agreement with that previously recorded [24] [25]
Summary
These dosage forms are designed to release medication continuously over a long period of time [1]. One of the new ways of a gastroretentive dosage form is the floating microsponge. It significantly increases the residence time of medication in stomach, improve bioavailability, improve patient compliance by reducing frequency doses, reduce drug waste [4]. The solubility of BFN decreases with increase pH, having maximum solubility at pH 1.2 which equal to 26mg/ml. It has short plasma half-life which is about 2–4 hr. It is stable and well absorbed within pH range 1-4 [9]
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Schedule a callMore From: Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
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