Abdullah Monahi Albogami,
Mustafa E Omer,
Abdulkareem M Al Bekairy,
Abdulmalik Alkatheri,
Alaa Eldeen B Yassin
College of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, King Abdullah International Medical Research Center, and King Abdulaziz Medical City, Ministry of National Guard, Health Affairs, Riyadh, Saudi Arabia;
For correspondence:- Alaa Yassin
Email: yassina@ksau-hs.edu.sa Tel:+966509426323
Received: 7 April 2017
Accepted: 25 July 2017
Published: 31 August 2017
Citation:
Albogami AM, Omer ME, Bekairy AM, Alkatheri A, Yassin AE.
Modified geometry three-layered tablet as a platform for class II drugs zero-order release system. Trop J Pharm Res 2017; 16(8):1773-1778
doi:
10.4314/tjpr.v16i8.4
© 2017 The authors.
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Abstract
Purpose: To optimize a geometrical design of three-layered tablets for controlling the release of indomethacin (Ind) as a BCS class II model.
Methods: The core formulation was optimized to ensure non-disintegrating tablet with a slow release behavior. Three-layered tablets were prepared by a single-step direct compression method by manual feeding of a hydrophobic layer in the bottom followed by Ind core layer and another hydrophobic layer at the top using 6 and 12 mm round compression sets. Four batches were prepared, differing only in either thickness of the drug layer or tablet diameter. A number of factors were studied, including tablet thickness to diameter ratio and drug layer surface area. The rate of Ind released was determined using USP dissolution apparatus I.
Results: The optimum drug layer formulation contained Ind (40%), polyvinylpyrolidone K30 (40 %), and ethyl cellulose (20 %). The t50% (time taken for 50 % drug release) for the four three-layered tablet batches with varying diameter to thickness ratios were in the range of 1.5 to 3.7 h. The diameter to thickness ratios were in good correlation with % Ind release after 4 h (R2 = 0.94). It was found that all batches complied with zero order kinetic model.
Conclusion: The new one-compression phase applied in this study is successful in producing three-layered tablets in a single-step with very good mechanical attributes. The approach of designing a controlled release tablet via control of the surface area of drug release is feasible for non-swelling matrices.
Keywords: Controlled release, Indomethacin, BCS class II drugs, Ethyl cellulose, Release kinetics, Direct compression