Preparation and Characterization of Pioglitazone Cyclodextrin Inclusion Complexes

Abstract

Pioglitazone, a class II Biopharmaceutical Classification System drug having poor water solubility and slow dissolution rate may have a negative impact on its subtherapeutic plasma drug levels leading to therapeutic failure. In order to improve its water solubility and thus dissolution, cyclodextrin complexation technique was followed. The phase solubility studies were carried using three different types of cyclodextrins viz., β, methyl-β and γ-cyclodextrins. The Gibbs free energy was calculated in order to determine ease of the complexation. Binary systems of pioglitazone with cyclodextrins were prepared by kneading method and spray drying method. The phase solubility profiles with all the three cyclodextrins were classified as AL-type, indicating the formation of 1:1 stoichiometric inclusion complexes. The complexation capability of cyclodextrins with pioglitazone increased in the order of methyl-β > β > γ-cyclodextrin. The Gibbs free energy was found to be in the order γ > methyl-β > β cyclodextrin. Characterization of inclusion complexes was done by solubility studies, in vitro dissolution studies, Fourier transformation-infrared spectroscopy, scanning electron microscopy, differential scanning calorimetry and X-ray powder diffractometry studies. Inclusion complexes exhibited higher rates of dissolution than the corresponding physical mixtures and pure drug. Greater solubility was observed with spray-dried methyl-β cyclodextrin complexes (2.29 ± 0.001 mg/ml) in comparison to the kneaded methyl-β cyclodextrin complexes (1.584 ± 0.053 mg/ml) and pure drug (0.0714 ± 0.0018 mg/ml).

Development and evaluation of orally disintegrating tablets of cilostazol-β-cyclodextrin inclusion complexes

“…Various techniques like kneading, anti-solvent, co-precipitation and spray drying were used for the preparation of ICs. Spray-drying technique was found to be most feasible amongst these in terms of powder characteristics and solubility enhancement 10 . Hydro-alcoholic solution containing methanol and water in the ratio of 80:20 was used as solvent for spray drying.…”

“…Drug Dev Ind Pharm, Early Online:[1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19] …”

Untitled

“…[32] A reduction in the stability constant of DOM/βCD system was observed in mannitol solution which may be due to competition of mannitol with DOM to form hydrogen bonds with βCD.…”

UPLCMS Method Development and Validation of Tablet Dosage form Containing Glimepiride, Metformin and Pioglitazone Using Internal Standard

“…Thus, combination regimens which include drugs with different and complementary mechanisms of action are recommended. The combinational therapy for type II diabetes [4][5] is frequently prescribed when mono therapy fails. The combination of metformin (MET), pioglitazone (PIO), and glimepiride (GLIMP) is approved by FDA for treatment of type II diabetes [6].…”