aripiprazole-cyclodextrin binary systems for dissolution enhancement: effect of preparation technique, cyclodextrin type and molar ratio
نویسندگان
چکیده
objective(s): the aim of this work was to investigate the effect of the natural and the chemically modified form of cyclodextrins namely; β-cyclodextrin (β-cd) and hydroxypropyl-β-cyclodextrin (hp-β-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-β-cd compared to β-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-β-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
منابع مشابه
Aripiprazole-Cyclodextrin Binary Systems for Dissolution Enhancement: Effect of Preparation Technique, Cyclodextrin Type and Molar Ratio
Objective(s): The aim of this work was to investigate the effect of the natural and the chemically modified form of cyclodextrins namely; β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) respectively on the solubility and dissolution rate of aripiprazole; an antipsychotic medication showing poor aqueous solubility. Materials and Methods: Phase solubility of ar...
متن کاملAripiprazole-Cyclodextrin Binary Systems for Dissolution Enhancement: Effect of Preparation Technique, Cyclodextrin Type and Molar Ratio
OBJECTIVE(S) The aim of this work was to investigate the effect of the natural and the chemically modified form of cyclodextrins namely; β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-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...
متن کاملPhysicochemical Characterization and Dissolution Enhancement of Loratadine–Hydroxypropyl-β-cyclodextrin Binary Systems
Loratadine, a Class II drug is a second generation antihistaminic agent, which is poorly water soluble with low bioavailability. Loratadine is practically insoluble in water and as such it exhibits poor variable oral bioavailability. Loratadine needs enhancement of solubility and dissolution rate to improve its oral bioavailability and therapeutic efficacy. In the present investigation, studies...
متن کاملPreparation, Physicochemical Characterization and In-vitro Dissolution Studies of Diosmin-cyclodextrin Inclusion Complexes
Diosmin, a vascular-protecting agent, is practically insoluble in water, and its oral absorption is limited by its extremely low dissolution rate. In this study, β-cyclodextrin (βCD) and 2-hydroxypropyl-β-cyclodextrin (HPβCD) were obtained to improve the solubility and dissolution rate of diosmin. Phase solubility studies of diosmin with βCD and HPβCD in distilled water were conducted to charac...
متن کاملPreparation, Physicochemical Characterization and In-vitro Dissolution Studies of Diosmin-cyclodextrin Inclusion Complexes
Diosmin, a vascular-protecting agent, is practically insoluble in water, and its oral absorption is limited by its extremely low dissolution rate. In this study, β-cyclodextrin (βCD) and 2-hydroxypropyl-β-cyclodextrin (HPβCD) were obtained to improve the solubility and dissolution rate of diosmin. Phase solubility studies of diosmin with βCD and HPβCD in distilled water were conducted to charac...
متن کاملSolid-state Characterization of Bifonazole – beta-cyclodextrin Binary Systems. II
CRISTINA TRANDAFIRESCU1, STEFANA AVRAM1*, CODRUTA SOICA1, ZOLTÁN AIGNER2, GYÉRESI ÁRPÁD3, MIHALY KATA2, CRISTINA DEHELEAN1, ZOLTÁN SZABADAI1, FLORIN BORCAN1 1Faculty of Pharmacy, Victor Babe’ University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., 300041, Timisoara, Romania 2Faculty of Pharmacy, University of Szeged, 6th Eötvös Str., Szeged, Hungary 3Faculty of Pharmacy, University of Medic...
متن کاملمنابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
iranian journal of basic medical sciencesجلد ۱۶، شماره ۱۲، صفحات ۱۲۲۳-۱۲۳۱
میزبانی شده توسط پلتفرم ابری doprax.com
copyright © 2015-2023