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Improved compressibility, flowability, dissolution and bioavailability of pioglitazone hydrochloride by emulsion solvent diffusion with additives.

Abstract

Spherical agglomerates of pioglitazone hydrochloride were prepared by the emulsion solvent diffusion method with additives (polyethylene glycol 6000, polyvinyl pyrrolidone, beta cyclodextrin, eudragit RS100, low acyl gellan gum and xanthan gum) using methanol, chloroform and water as a good solvent, bridging liquid and poor solvent respectively. Prepared agglomerates were evaluated for compressibility, solubility, dissolution rate and bioavailability, and characterized by SEM, XRPD, DSC and FTIR spectroscopy. Particle size, flowability, compactibility, packability, solubility, dissolution rate and bioavailability of plain agglomerates and agglomerates with additives (except with polyvinyl pyrrolidone) were advantageously improved compared with raw crystalline pioglitazone hydrochloride. These improved properties for direct compression were due to their large-spherical shape and enhanced fragmentation during compaction, together with increased tensile strength and reduced elastic recovery of the compacts. XRPD and DSC studies indicated polymorphic transition of pioglitazone hydrochloride from form II to I during recrystallization but this was not associated with any chemical transition, as indicated by FTIR spectra, well supported by stability studies. Thus spherical crystallization by the emulsion solvent diffusion method with selected additives is a satisfactory method for direct tableting of pioglitazone hydrochloride giving improved bioavailability.

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  • Publisher Full Text

    • Authors

    Patil SV, Pawar AP, Sahoo SK

    Institution

    Patil S. V., Department of Pharmaceutics, Utkal University, Bhubaneswar, Orissa, India. sachinpatil79@rediffmail.com

    Source

    Die Pharmazie 67:3 2012 Mar pg 215-23

    MeSH

    Animals
    Biological Availability
    Calibration
    Calorimetry, Differential Scanning
    Chromatography, Thin Layer
    Crystallization
    Diffusion
    Drug Compounding
    Drug Stability
    Emulsions
    Hypoglycemic Agents
    Male
    Microscopy, Electron, Scanning
    Microspheres
    Particle Size
    Rats
    Rats, Wistar
    Solubility
    Solvents
    Spectroscopy, Fourier Transform Infrared
    Thiazolidinediones
    X-Ray Diffraction

    Pub Type(s)

    Journal Article

    Language

    eng

    PubMed ID

    22530302