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Author Ammar, Hussein O. ♦ Ghorab, Mahmoud ♦ Kamel, Rabab ♦ Salama, Alaa H.
Source SpringerLink
Content type Text
Publisher Springer US
File Format PDF
Copyright Year ©2016
Language English
Subject Domain (in DDC) Technology ♦ Medicine & health
Subject Keyword Cinnarizine ♦ Microballoons ♦ Gastro-retentive ♦ Sustained release ♦ Bioavailability ♦ Pharmaceutical Sciences/Technology
Abstract This study is focused on the design of gastro-retentive drug delivery system composed of hollow microspheres (microballoons) for the sustained delivery of cinnarizine (CIN). The microballoons (MBs) were prepared by the emulsion solvent diffusion method using cellulose acetate butyrate (CAB) as the hosting polymer and absolute ethanol (ETH) and dichloromethane (DCM) as solvents. A 3$^{3}$ full factorial experimental design was adopted to study the effect of different variables and to find an optimum formula with desired properties. Prepared microballoons showed high drug loading capacities and controlled release behaviour. The optimum formulation was chosen on the basis of achieving maximum values for both drug loading capacity and release efficiency as well as having suitable size. The optimized MB (MB-F21) was composed of 200 mg CIN and 400 mg CAB with a DCM/ETH ratio of 2:1. Scanning electron microscopy for the optimum formulation showed a spherical outline with internal porous structure. An in vivo study using human volunteers was performed by determination of CIN concentration in the plasma using the liquid chromatography-mass spectrometry (LC-MS) method. Results proved the superiority of the designed formulation over the market product Stuval® tablets in bioavailability parameters comprising T $_{max}$ as well as area under the plasma CIN concentration-time curve (AUC$_{0–24 h}$) and AUC$_{0–∞}$ values. Also, the significantly greater value of mean residence time (MRT) in case of MB-F21 indicates its higher gastric residence time and proves the advantages of micro-multiparticulate dosage forms over conventional one.
ISSN 2190393X
Age Range 18 to 22 years ♦ above 22 year
Educational Use Research
Education Level UG and PG
Learning Resource Type Article
Publisher Date 2016-01-29
Publisher Institution Controlled Release Society
Publisher Place New York
e-ISSN 21903948
Journal Drug Delivery and Translational Research
Volume Number 6
Issue Number 3
Page Count 15
Starting Page 210
Ending Page 224


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Source: SpringerLink