Abstract
<p><strong>Objective: </strong>The objective of this study was to formulate an oral sustained release delivery system of ezetimibe mucoadhesive beads by ionic gelation technique based on sodium alginate used as a hydrophilic carrier in combination with carbopol 934P which acts as a rate modifier.</p><p><strong>Methods: </strong>Microbeads of ezetimibe were prepared using an easy method of ionotropic gelation by little modification while in addition of drug. The prepared beads were characterised for mean particle size, entrapment efficiency, swelling capacity, and <em>in vitro</em> release. They were also subjected to various studies such as Fourier Transform Infrared Spectrophotometer (FTIR) Spectroscopy for drug polymer reaction, Scanning Electron Microscopy for surface morphology, and Differential Scanning Calorimetric Analysis to determine the physical state of the drug in the beads.</p><p><strong>Results</strong>:<strong> </strong>The microspheres of ezetimibe were formulated successfully. The addition of drug concentration gives higher drug loading and higher conc. of Alcl<sub>+3</sub> yields small diameter beads and lower drug entrapment. Analysis of the release profiles showed that the data corresponds to zero order release and the diffusion-controlled mechanism as suggested by Higuchi concept.</p><p><strong>Conclusion</strong>:<strong> </strong>It can be concluded that beads produced by the sequential method had higher drug entrapment. Beads produced by simultaneous yields larger beads in diameter. The concept was cleared that drug release was dependent upon the quantity of polymer and increase in conc. of. aluminium chloride retarded the drug release in the sequential method. Prepared beads enhance the dissolution of ezetimibe and the oral bioavailability and also reduce the fluctuations in the oral bioavailability.</p>
Highlights
Controlled release systems have been extensively developed and advised to superior due to their extensive therapeutic advantages over conventional forms [1]
In Simulated gastric fluids, alginate beads prepared by the sequential method, ezetimibe releases about less than 21% drug in the first 2 h
Ezetimibe was entrapped in aluminium alginate beads prepared with hydrophilic polymer sodium alginate and retarding material carbopol 934P by the using ionotropic gelation method
Summary
Controlled release systems have been extensively developed and advised to superior due to their extensive therapeutic advantages over conventional forms [1]. The versatility of polymeric materials allows ease fabrication of the drug delivery devices with a desirable degree of swelling and of the release of the drug. This microparticulate material as in the form of microbeads may be dispensed as filled in hard gelatin capsules or they can be compressed into a suitable dosage form like tablets or hard gelatin capsule [2]. The numbers of the apparent cross-linking sites within the formed aluminium alginate gel beads increased with increasing sodium alginate concentration in the formulation This increase in the apparent crosslinking density delayed the alginate gel disintegration in phosphate buffer due to the retardation of Al+3 exchange with Na+and eventually increasing lag time. Increased alginate gel density per unit volume was thought to affect the decreased pore size within the gels, and ezetimibe release becomes slow
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callMore From: International Journal of Pharmacy and Pharmaceutical Sciences
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
