Paper Information

Journal:   IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES   DECEMBER 2013 , Volume 16 , Number 12; Page(s) 1223 To 1231.
 
Paper: 

ARIPIPRAZOLE-CYCLODEXTRIN BINARY SYSTEMS FOR DISSOLUTION ENHANCEMENT: EFFECT OF PREPARATION TECHNIQUE, CYCLODEXTRIN TYPE AND MOLAR RATIO

 
 
Author(s):  BADR ELDIN SHAIMAA M., AHMED TAREK A.*, ISMAIL HATEM R.
 
* DEPARTMENT OF PHARMACEUTICS AND INDUSTRIAL PHARMACY, FACULTY OF PHARMACY, KING ABDULAZIZ UNIVERSITY, JEDDAH, KSA, 21589
 
Abstract: 

Objective (s): The aim of this work was to investigate the effect of the natural and the chemically modified form of cyclodextrins namely; b -cyclodextrin (?-CD) and hydroxypropyl-b-cyclodextrin (HP- b -CD) respectively on the solubility and dissolution rate of aripiprazole; an antipsychotic medication showing poor aqueous solubility.
Materials and Methods: Phase solubility of aripiprazole with the studied CDs and the complexation efficiency values (CE) which reflect the solubilizing power of the CDs towards the drug was performed. Solid binary systems of aripiprazole with CDs were prepared by kneading, microwave irradiation and freeze-drying techniques at 1: 1 and 1: 2 (drug to CD) molar ratios. Drug-CD physical mixtures were also prepared in the same molar ratios for comparison. The dissolution of aripiprazole-binary systems was carried out to select the most appropriate CD type, molar ratio and preparation technique.
Results: Phase solubility study indicated formation of higher order complexes and the complexation efficiency values was higher for HP-
b -CD compared to b -CD. Drug dissolution study revealed that aripiprazole dissolution was increased upon increasing the CD molar ratio and, the freeze-drying technique was superior to the other studied methods especially when combined with the HP- b -CD. The cyclodextrin type, preparation technique and molar ratio exhibited statistically significant effect on the drug dissolution at P?0.05.
Conclusion: The freeze-dried system prepared at molar ratio 1: 2 (drug: CD) can be considered as efficient tool for enhancing aripiprazole dissolution with the possibility of improving its bioavailability.

 
Keyword(s): ARIPIPRAZOLE, BINARY SYSTEMS, CYCLODEXTRIN, IN VITRO DISSOLUTION PHASE-SOLUBILITY
 
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