Abstract
Solid dispersion is an attractive tool of pharmaceutical technology used to improve the physical properties of drugs. Among these properties is to enhance the solubility of the drugs.Rebamipide is a poorly soluble drug of class IV of biopharmaceutical classification system (BCS).Rebamipide is used as potent antiulcer, mucoprotective drug, by stimulating the generation of prostoglandine enhanced mucosal protection.Rebamipide was formulated as a solid dispersion using different polymers such as pluronic F-127, PEG6000, PVP K30, and TPGS by using different preparation methods solvent evaporation, fusion, and kneading methods.It was seen that rebamipide was successfully dispersed in a homogenous solid dispersion matrix by solvent evaporation method using TPGS (1:15) drug carrier ratio.Moreover, the results revealed that the solubility of rebamipide (23.9µg/ml) increased significantly (p?0.05) by 36.4 x fold to obtain 874µg/ml solubility in rebamipide matrix. On the other hand, characterization of rebamipide solid dispersion using FTIR, DSC, SEM and x-ray diffraction demonstrated no drug polymer interaction, and converting the rebamipide from crystal to amorphous state lattice.
Highlights
Rebamipide has a chemical formula of [2 - ( 4 – chlorobenzoylamino ) – 3 – [ 2 ( 1H ) – Quinolinon – 4 – yl ] proponic acid], (REM) as shown in Figure [1]
The results indicate that the used polymer show improvement in drug solubility in the following descending order; Tocopheryl polyethylene Glycol Succinate (TPGS)>PVP K30>polyethelen glycol (PEG) 6000 > pluronic F-127 and the best drug: polymer ratio was 1:15 while best method was solvent evaporation
The results revealed that the solubility of REM is very poor in 0.1 N HCl pH (1.2), which may be attributed to it is acidic nature of the drug, so increasing the pH of the solvent using phosphate buffer lead to increase the solubility from 1.8μg/ml to 1320 μg/ml at pH6.8 (730 x fold)
Summary
Rebamipide has a chemical formula of [2 - ( 4 – chlorobenzoylamino ) – 3 – [ 2 ( 1H ) – Quinolinon – 4 – yl ] proponic acid], (REM) as shown in Figure [1]. REM is an amino acid analog of 2(1H) – Quinolinone It is a new mucoprotactive drug which was developed in Japan for the treatment of peptic ulcer disease (PUD) [1]. To increase the low solubility of poor water soluble drug and improve its bioavailability, several strategies can be employed, such as size reduction, use of surfactants, pH adjustment, and complexation with cyclodextrines, emulsions and solid dispersion[4]. When the solid dispersion interacts with gastrointestinal fluid, the carrier or polymer which enhances solubility of drug it first dissolves and the drug release as fine colloidal particles. This result in enhanced surface area produces higher dissolution rate and bioavailability of poor water soluble drug[5]. To enhance the solubility and the dissolution of the drugs [6]
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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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