Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis

The objective of this work was to formulate co-loaded bilayer tablets containing ezetimibe (EZB) and atorvastatin (ATC). ATC loaded in the immediate-release (IR) layer is an HMG CoA reductase inhibitor, while EZB, added in the sustained-release (SR) layer, is a lipid-lowering agent. This study was c...

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Published in:Polymers 2022-09, Vol.14 (18), p.3770
Main Authors: Mubeen, Iqra, Zaman, Muhammad, Farooq, Muhammad, Mehmood, Asim, Azeez, Fahad Khan, Rehman, Wajiha, Akhtar, Sohail, Chaudhry, Mueen Ahmad, Butt, Muhammad Hammad, Shamim, Qurat-Ul-Ain, Adnan, Sherjeel, Khan, Muhammad Rizwan, Atta-Ur-Rehman
Format: Article
Language:English
Subjects:
Aluminum
Animals
Atherosclerosis
atorvastatin
bilayer tablets
Bioavailability
Buffer solutions
Cardiovascular disease
Cholesterol
Diet
Drug delivery systems
Drug dosages
Drugs
Ethanol
ezetimibe
HPMC K-100
In vivo methods and tests
Lipids
Polymers
Reductases
Statins
Tablets
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Summary:The objective of this work was to formulate co-loaded bilayer tablets containing ezetimibe (EZB) and atorvastatin (ATC). ATC loaded in the immediate-release (IR) layer is an HMG CoA reductase inhibitor, while EZB, added in the sustained-release (SR) layer, is a lipid-lowering agent. This study was conducted to evaluate the effects of polymer on the formulation and characterization of bilayer tablets, as well as the therapeutic impact of the concurrent use of both drugs having a sequential release pattern. To obtain the optimized results, four different formulations with variable compositions were developed and evaluated for different parameters. The drug release studies were carried out using a type II dissolution apparatus, using phosphate buffer solution (PBS) of 1.2 pH for IR of EZB for an initial 2 h, followed by 24 h studies for ATC in PBS 6.8 pH. The IR layer showed rapid drug release (96%) in 2 h, while 80% of the ATC was released in 24 h from the SR layer. Locally obtained, 6-week-old female albino rats were selected for in vivo studies. Both preventive and curative models were applied to check the effects of the drug combination on the lipid profile, atherosclerosis and physiology of different organs. Studies have shown that the administration of both drugs with different release patterns has a better therapeutic effect (p < 0.05), both in preventing and in curing hyperlipidemia. Conclusively, through the sequential release of ATC and EZB, a better therapeutic response could be obtained.
ISSN:2073-4360
2073-4360
DOI:10.3390/polym14183770