Siraprapa Chansatidkosol,
Praneet Opanasopit,
Tanasait Ngawhirunpat,
Sontaya Limmatvapirat,
Prasert Akkaramongkolporn
Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand;
For correspondence:- Prasert Akkaramongkolporn
Email: akkaramongkol_p@su.ac.th
Accepted: 22 July 2018
Published: 31 August 2018
Citation:
Chansatidkosol S, Opanasopit P, Ngawhirunpat T, Limmatvapirat S, Akkaramongkolporn P.
Preparation and assessment of poly(methacrylic acid-co-ethylene glycol dimethacrylate) as a novel disintegrant. Trop J Pharm Res 2018; 17(8):1475-1482
doi:
10.4314/tjpr.v17i8.3
© 2018 The authors.
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Abstract
Purpose: To prepare and evaluate poly(methacrylic acid (MAA)-co-ethylene glycol dimethacrylate (EGD)) as a tablet disintegrant.
Methods: Poly(MAA-co-EGD) in acid (H) and sodium (Na) forms at cross-linker (EGD) levels of 0.25 - 16 % were synthesized and subjected to Fourier transform infrared spectroscopy. Swelling capacity, disintegration efficiency and cytotoxicity to Caco-2 cells were determined using standard procedures.
Results: Poly(MAA-co-EGD) in acid (H) and sodium (Na) forms were successfully prepared. In contact with water, the polymers in Na form swelled more than those in H form. The swelling capacities of polymers in H and Na forms decreased with increasing amounts of cross-linker. Incorporation of the polymers accelerated the disintegration of microcrystalline cellulose tablets (placebo), and the disintegration efficiency depended on the salt form and amount of cross-linker. The Na salt form of the polymer crosslinked at 16 % EGD was the best candidate disintegrant. When used at 2.5 and 10 %, the selected polymer effectively promoted the disintegration and drug release of propranolol hydrochloride tablets. Moreover, cytotoxicity tests showed that it was non-toxic to Caco-2 cells.
Conclusion: The developed poly(MAA-co-EGD) possesses good disintegration and dissolution functionalities. Thus, it may be adopted as a new super-disintegrant for fast-release tablets
Keywords: Tablet disintegrant, Methacrylic acid, Ethylene glycol dimethacrylate, Propranolol hydrochloride