Surface Solid Dispersion and Solid Dispersion of Meloxicam: Comparison and Product Development.

Mayank Chaturvedi,Vipin Saini,Manish Kumar,Kamla Pathak,Shailendra Bhatt

doi:10.15171/apb.2017.068

Abstract

Purpose: A comparative study was carried out between surface solid dispersion (SSD) and solid dispersion (SD) of meloxicam (MLX) to assess the solubility and dissolution enhancement approach and thereafter develop as patient friendly orodispersible tablet.Methods: Crospovidone (CPV), a hydrophilic carrier was selected for SSD preparation on the basis of 89% in- vitro MLX adsorption, 19% hydration capacity and high swelling index. SD on the other hand was made with PEG4000. Both were prepared by co-grinding and solvent evaporation method using drug: carrier ratios of 1:1, 1:4, and 1:8. Formulation SSDS3 (MLX: CPV in 1:8 ratio) made by solvent evaporation method showed t50% of 28 min and 80.9% DE50min which was higher in comparison to the corresponding solid dispersion, SDS3 (t50% of 35min and 76.4% DE50min). Both SSDS3 and SDS3 were developed as orodispersible tablets and evaluated.Results: Tablet formulation F3 made with SSD3 with a disintegration time of 11 secs, by wetting time= 6 sec, high water absorption of 78%by wt and cumulative drug release of 97% proved to be superior than the tablet made with SD3.Conclusion: Conclusively, the SSD of meloxicam has the potential to be developed as fast acing formulation that can ensure almost complete release of drug.

Highlights

Dissolution of solid dosage forms in gastrointestinal fluids is a precondition for the delivery of the drug to the systemic circulation following oral administration
At high concentrations such carriers may decrease dissolution due to high viscosity in the boundary layer close to the dissolving surface.[5]. These problems can be mitigated by surface solid dispersion that uses water insoluble hydrophilic carriers and the drug is deposited on the surface of carrier.[6]
The drug content of solid dispersion (SD) prepared by co-grinding method (SDC1 – SDC3) varied from 89.2 - 96.6 and those prepared by solvent evaporation method (SDS1 – SDS3) varied from 90.2 – 96.3 respectively while the drug content of prepared surface solid dispersion (SSD) by co-grinding method (SSDC1 – SSDC3) varied from 91.9 - 96.0 and that prepared from solvent evaporation (SSDS1 – SSDS3) varied from 89.1 – 97.9 respectively

Summary

Introduction

Dissolution of solid dosage forms in gastrointestinal fluids is a precondition for the delivery of the drug to the systemic circulation following oral administration. Amorphization of drug, improved wettability and decrease in particle size are the main mechanisms for enhanced dissolution.[2] In spite of several advantages of solid dispersions, the water soluble carriers used for their preparation produce soft and tacky mass which is difficult to handle especially in tablet making.[3,4] at high concentrations such carriers may decrease dissolution due to high viscosity in the boundary layer close to the dissolving surface.[5] These problems can be mitigated by surface solid dispersion that uses water insoluble hydrophilic carriers and the drug is deposited on the surface of carrier.[6] Such excipients include sodium starch glycolate, crospovidone, potato starch, silicon dioxide, croscarmellose sodium, pre-gelatinized starch and microcrystalline cellulose Drug release from these carriers depends on the porosity, particle size and surface area of the carrier.

Results

Discussion

Conclusion