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
Highlights
The rapid disintegration of tablets and dissolution of drugs are generally assisted by disintegrants, which are categorized into traditional disintegrants and super-disintegrants
The traditional disintegrants are hydrophilic, linear or branch polymeric substances such as starch, gum and un-crosslinked cellulose, while the super-disintegrants, some of which are modified from the traditional disintegrants, are hydrophilic crosslinked polymeric substances such as croscarmellose sodium, sodium starch glycolate, crospovidone, and polacrilin potassium
Polymers in Na salt form were prepared by placing the ground polymers in H form in aqueous NaOH
Summary
The rapid disintegration of tablets and dissolution of drugs are generally assisted by disintegrants, which are categorized into traditional disintegrants and super-disintegrants. The super-disintegrants have superior disintegrating efficiency, and require lower amounts (2 - 10 %) for tablet disintegration than the traditional disintegrants. Previous works showed that acidhydrolyzed yam and breadfruit starches enhanced the disintegration of paracetamol tablets [2,3]. Hydrochlorothiazide tablets containing the mucilage obtained from Mimosa pudica showed rapid disintegration capacity [5]. The disintegration property of crosslinked polyalkylammonium polymers was evaluated using hydrochlorothaizide and aspirin tablets as the model formulations. The results showed that the crosslinked polyalkylammonium polymer was a powerful disintegrant for both drug tablets [6]. Other developed novel disintegrants with improved efficiency were reported in recent publications [7,8]
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