Abstract

Meloxicam (MLX) is non-steroidal anti -inflammatory, poorly water soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Solid dispersion (SD) is an effective technique for enhancing the solubility and dissolution rate of such drug.
 The present study aims to enhance the solubility and the dissolution rate of MLX by SD technique by solvent evaporation method using sodium alginate (SA), hyaluronic acid (HA), collagen and xyloglucan (XG) as gastro-protective hydrophilic natural polymers.
 Twelve formulas were prepared in different drug: polymer ratios and evaluated for their, percentage yield, drug content, water solubility, dissolution, crystal lattice using powder X-ray diffraction (PXRD) and studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-polymer interaction.
 All the prepared showed improvement of drug solubility except that prepared with HA. The best result was obtained with formula SD1 (MLX: SA 1:1) that showed a high percentage yield (97), high drug content (97.4±0.05) and increase in solubility compared to solubility of pure MLX with improved dissolution rate. the PXRD study revealed the conversion of the drug to amorphous form without chemical interaction according to FTIR results

Highlights

  • Drug product solubility can be defined as being both quantitative and qualitative

  • While qualitative solubility is defined as where two phases are mixed together to form a homogeneous solution ( 1)

  • The polymers were dispersed in 20 ml of 20% v/v of methanol separately by utilizing a magnetic stirrer, until a clear solution was obtained, MLX was added and stirring was continued for 10 min

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Summary

Introduction

Drug product solubility can be defined as being both quantitative and qualitative. The concept of quantitative solubility is the number of gram of solute particles required to make a saturated solution at certain temperature. While qualitative solubility is defined as where two phases are mixed together to form a homogeneous solution ( 1). It is one of the essential parameters for achieving desired drug concentration in systemic circulation for the desired pharmacological response. Low aqueous solubility is the main problem associated with the development of formulations of new chemical entities. Solubility is a major challenge for formulation scientist. Any drug to be absorbed must be present in the form of solution at the site of absorption [2]

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