Abstract
Atorvastatin calcium, a lipid-lowering drug, is much less bioavailable because of reduced solubility in acidic media. Multiple-unit floating microcapsules of Atorvastatin calcium (ATC) were developed to expand the gastric residence time of the drug, as ATC has maximum rate of absorption in the upper GI tract. Floating microcapsules were prepared by Emulsion-solvent evaporation technique through incorporation of dioctyl sodium sulphosuccinate (DSS) as a dissolution enhancer. The microcapsules were assessed for shape, size, drug entrapment efficiency, stability and in-vitro drug dissolution rate and were subjected to SEM, DSC and PXRD studies. The ATC-loaded floating microcapsules were spherical in shape and had the particle size of about 28.10 μm and drug-loading efficiency of about 96.55 %. The floating microspheres containing DSS had significantly higher drug dissolution rates than those without DSS. The best formulation, AT4, consisting of Ethyl cellulose, DSS and Poly Ox®, had a maximum drug dissolution rate of 97.86 %, as compared to Storvas 80 mg (Ranbaxy Ltd, as a reference) which had a rate of only 54% during a period of 12 h in acidic media. A pharmacokinetic study performed on albino rabbits illustrates that the bioavailability of AT4 floating microcapsules significantly increased to nearly 1.7 times that of Storvas 80 mg. The present study indicates that the use of multi-unit floating microcapsules for delivery of ATC can improve its bioavailability.
Highlights
Atorvastatin calcium (ATC) is the treatment of choice in moderate to severe familial or nonfamilial hypercholesterolemia
A self-micro emulsifying drug delivery system (SMEDDS) of ATC consisting of Labrafil, propylene glycol and Cremophor RH40 has been developed [2]
Microcapsules with EC were prepared by dissolving ATC in 2ml methanol; EC and dioctyl sodium sulphosuccinate (DSS) were dissolved in acetone (8ml)
Summary
Atorvastatin calcium (ATC) is the treatment of choice in moderate to severe familial or nonfamilial hypercholesterolemia. A self-micro emulsifying drug delivery system (SMEDDS) of ATC consisting of Labrafil, propylene glycol and Cremophor RH40 has been developed [2] Another self-emulsifying drug delivery system (SEDDS) of ATC in various vehicles such as Captex 355, Captex 355 EP/NF, Ethyl oleate, Capmul MCM, Capmul PG-8, Gelucire 44/14, Tween 80, Tween 20, and PEG 400 has been reported [3]. The negative aspect of formerly reported solo unit systems such as tablets and capsules are the high inconsistency of their GI transfer moment because of their all-ornothing emptying course of action To overcome these limitations, multiple-unit floating microcapsules have been developed to form cost-effective stable ATC formulation with enhanced bioavailability. The focus of this research was to develop solubilized gastro-retentive multi-unit floating microcapsules of ATC to achieve better bioavailability
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
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 callDisclaimer: 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.
