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

被引:2
|
作者
Mubeen, Iqra [1 ]
Zaman, Muhammad [2 ]
Farooq, Muhammad [1 ]
Mehmood, Asim [3 ]
Azeez, Fahad Khan [3 ]
Rehman, Wajiha [3 ]
Akhtar, Sohail [4 ]
Chaudhry, Mueen Ahmad [5 ]
Butt, Muhammad Hammad [6 ]
Shamim, Qurat-Ul-Ain [2 ]
Adnan, Sherjeel [1 ]
Khan, Muhammad Rizwan [7 ]
Atta-Ur-Rehman [8 ]
机构
[1] Univ Lahore, Fac Pharm, Dept Pharmaceut, Lahore 54000, Pakistan
[2] Univ Cent Punjab, Fac Pharm, Lahore 54000, Pakistan
[3] Jazan Univ, Fac Publ Hlth & Trop Med, Dept Hlth Informat, Jazan 45142, Saudi Arabia
[4] Qassim Univ, Coll Publ Hlth & Hlth Informat, Hlth Informat Dept, Buraydah 52385, Saudi Arabia
[5] Allied Coll Hlth Sci, Multan 59300, Pakistan
[6] Uppsala Univ, Fac Pharm, Dept Med Chem, S-75123 Uppsala, Sweden
[7] Imran Idrees Coll Pharm, Dept Pharm, Sialkot 51040, Pakistan
[8] Forman Christian Coll, Dept Pharm, Lahore 54000, Pakistan
关键词
bilayer tablets; ezetimibe; atorvastatin; HPMC K-100;
D O I
10.3390/polym14183770
中图分类号
O63 [高分子化学(高聚物)];
学科分类号
070305 ; 080501 ; 081704 ;
摘要
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.
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页数:15
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