Drug Res (Stuttg) 2018; 68(10): 576-583
DOI: 10.1055/a-0591-2506
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Nanocrystalization of Pioglitazone by Precipitation Method

Jaleh Varshosaz
1   Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran
,
Saeedeh Ahmadipour
1   Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran
,
Majid Tabbakhian
1   Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran
,
Shokoufeh Ahmadipour
2   Faculty of medicine, Department of Pediatric, Lorestan University of medical Sciences, Khorramabad, Iran
› Author Affiliations
Further Information

Publication History

received 31 December 2017

accepted 09 March 2018

Publication Date:
09 April 2018 (online)

Abstract

Background Poor solubility in aqueous medium limits the use of many drugs. Different methods have been adopted to promote the rate of dissolution of slightly water soluble drugs. Crystallization improves solubility, and bioavailability by increasing the surface area of slightly water soluble drugs. Pioglitazone (PGZ), which is a class II Biopharmaceutical Classification System drug has a slight solubility in water and a slow rate of dissolution, which may have a negative effect on its metabolism leading to a therapeutic failure.

Aim The aim of this study was to improve the solubility of PGZ-HCl; an antidiabetic drug using precipitation method.

Materials and Methods Formulations were prepared with polyethylene glycol 6000 and isomalt using different speed of homogenizer and quantity of solvent by precipitation method. Drug-polymer interactions were examined using differential scanning calorimetry (DSC), and Powder X-Ray Diffraction (PXRD). Surface structure were shown by SEM photographs.

Results The particle size was significantly decreased and solubility was enhanced with increase speed, ethanol solvent and increase stabilizer, however very high amount of stabilizer resulted in a decrease in solubility.

Conclusion This result however showed that solid dispersion technique is a potential method for increasing dissolution profile of a poorly aqueous soluble agent.

 
  • References

  • 1 Amidon GL, Lennernas H, Shah VP. et al. Basis for a Biopharmaceutic Drug Classification – the Correlation of in-Vitro Drug Product Dissolution and in-Vivo Bioavailability. Pharm Res 1995; 12: 413-420
  • 2 Williams HD, Trevaskis NL, Charman Sa. et al. Strategies to address low drug solubility in discovery and development. Pharmacol Rev 2013; 65: 315-499
  • 3 Krishnaiah YS. Pharmaceutical technologies for enhancing oral bioavailability of poorly soluble drugs. J Bioequiv Availab 2010; 2: 28-36
  • 4 Kawabata Y, Wada K, Nakatani M. et al. Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications. Int J Pharm 2011; 420: 1-10
  • 5 Kumar S, Bhargava D, Thakkar A. et al. Drug carrier systems for solubility enhancement of BCS class II drugs: A critical review. Crit Rev Ther Drug Carrier Syst 2013; 30: 217-256
  • 6 Onoue S, Kojo Y, Aoki Y. et al. Physicochemical and pharmacokinetic characterization of amorphous solid dispersion of tranilast with enhanced solubility in gastric fluid and improved oral bioavailability. Drug Metab. Pharmacokinet. 2012; 27: 379-387
  • 7 Urbanetz NA. Stabilization of solid dispersions of nimodipine and polyethylene glycol 2000. Eur. J Pharm Sci 2006; 28: 67-76
  • 8 Serajuddin ATM. Salt formation to improve drug solubility. Adv Drug Deliv. Rev 2007; 59: 603-616
  • 9 Babu NJ, Nangia A. Solubility advantage of amorphous drugs and pharmaceutical cocrystals. Cryst Growth Des 2011; 11: 2662-2679
  • 10 Li A, Yalkowsky SH. Predicting Cosolvency. 1. Solubility Ratio and Solute log K ow. Ind Eng Chem Res 1998; 37: 4470-4475
  • 11 Kim JY, Kim S, Papp M. et al. Hydrotropic solubilization of poorly water-soluble drugs. J Pharm Sci 2010; 99: 3953-3965
  • 12 Mizuuchi H, Jaitely V, Murdan S. et al. Room temperature ionic liquids and their mixtures: Potential pharmaceutical solvents. Eur J Pharm Sci 2008; 33: 326-331
  • 13 Anton N, Vandamme TF. Nano-emulsions and micro-emulsions: Clarifications of the critical differences. Pharm Res 2011; 28: 978-985
  • 14 Mazzola L. Commercializing nanotechnology. Nat Biotechnol 2003; 21: 1137-1143
  • 15 Chaudhary A, Nagaich U, Gulati N. et al. Enhancement of solubilization and bioavailability of poorly soluble drugs by physical and chemical modifications: A recent review. J Adv Pharm Educ Res 2012; 2: 32-67
  • 16 Pandit V, Gorantla R, Devi K. et al. Preparation and characterization of pioglitazone cyclodextrin inclusion complexes. J Young Pharm 2011; 3: 267-274
  • 17 Sadique Faisal K, Giri A, Hassan R. et al. Solid dispersion formulations of Pioglitazone HCl using five different polymers for enhancing dissolution profile. Int J Pharm Life Sci 2013; 4: 2269-2275
  • 18 Elbary AA, Kassem MA, Abou Samra MM. et al. Formulation and hypoglycemic activity of pioglitazone-cyclodextrin inclusion complexes. Drug Discov Ther 2008; 2: 94-107
  • 19 Shejul AA, Deshmane S, Biyani K. Modified Natural Carrier in Solid Dispersion for Enhancement of Solubility of Poorly Water Soluble Drugs. J Drug Deliv Ther 2014; 4: 111-116
  • 20 Grace XF, Latha S, Shanthi S. et al. Comparative study of different surfactants for solubility enhancement of two class II drugs for type II diabetes mellitus, Int. J Pharm Pharm Sci 2012; 4: 5-7
  • 21 Yoshihashi Y, Iijima H, Yonemochi E. et al. Estimation of physical stability of amorphous solid dispersion using differential scanning calorimetry. In: J Therm Anal Calorim 2006; pp 689-692
  • 22 Razavipour S, Keshmiri K, Vatanara A. et al. Precipitation of Pioglitazone Hydrochloride Microparticles by Supercritical Anti-Solvent (SAS). Br J Pharm Res 2015; 6: 415-422