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Research Article
Effect of Additives
on the Physicochemical and Drug Release Properties of
Pioglitazone Hydrochloride Spherical Agglomerates
Sachinkumar Patil1,2*, Atmaram Pawar3
and Sunit Kumar Sahoo1
1Department
of Pharmaceutics, University Department of
Pharmaceutical Sciences, Utkal University, Bhubaneswar,
Orissa, 2Department of Pharmaceutics, Shree
Santkrupa College of Pharmacy, Ghogaon, Maharashtra,
3Department of Pharmaceutics, Poona College
of Pharmacy, Erandwane, Pune, Maharashtra, India.
*For correspondence:
Email:
sachinpatil79@rediffmail.com Tel: +91
06742586152
Received: 31 May
2011 Revised
accepted: 14 December 2011
Tropical
Journal of Pharmaceutical Research, February 2012;
11(1): 18-27
http://dx.doi.org/10.4314/tjpr.v11i1.3
Abstract
Purpose: To prepare and evaluate spherical
agglomerates of pioglitazone hydrochloride (PGH) for
direct compression with different additives.
Methods :
Spherical agglomerates of pioglitazone hydrochloride
were prepared by emulsion solvent diffusion method with
and without additives (polyethylene glycol 6000,
polyvinyl pyrrolidone, β cyclodextrin, Eudragit RS100,
low acyl gellan gum and xanthan gum) using methanol,
chloroform and water as good solvent, bridging liquid
and poor solvent respectively. The agglomerates were
evaluated for compressibility, solubility and
dissolution rate and also by scanning electron
microscopy (SEM), X-ray powder diffraction (XRPD),
differential scanning calorimetry (DSC) and fourier
transforms infrared spectroscopy (FTIR).
Results :
The particle size, flowability, compactibility,
packability, solubility and dissolution rate of plain
agglomerates and agglomerates with additives, except
polyvinyl pyrrolidone, were enhanced compared with the
original crystals of pioglitazone hydrochloride. This
might be attributed to their large size (10 x original
PGH crystals), spherical shape, enhanced fragmentation
during compaction (yield pressure increased from 22.6 to
29.3 MPa) and reduced elastic recovery of compacts (from
8.1 to 5.5 %) compared to the original drug crystals.
XRPD and DSC studies indicate polymorphic transition of
PGH in all agglomerates from form II to I during
recrystallization; FTIR spectra show that this was not
associated with any chemical transition.
Conclusion :
The findings indicate that spherical crystallization by
emulsion solvent diffusion method to produce
agglomerates containing selected additives is a
satisfactory approach for the formulation of directly
compressed pioglitazone hydrochloride tablets.
Keywords: S pherical
crystallization, Agglomerates, Compressibility,
Pioglitazone, Emulsion solvent diffusion. |
