Development And Evaluation Of Amoxicillin Formulations By Direct Compression: Influence Of The Adjuvants On Physicomechanical And Biopharmaceutical Properties Of The Tablets

The amoxicillin 500 mg formulations were developed by direct compression using a 23 factorial design. Eight different formulations were carried out and they were analyzed considering three levels: the type of microcrystalline cellulose (Avicel® PH-102 or Avicel® PH-200), the presence or absence of spray-dried lactose, and the presence or absence of the superdisintegrant agent, croscarmellose sodium. Average weight, thickness and diameter, hardness, friability, amoxicillin concentration (iodometric assay), disintegration time, and dissolution profile were the parameters used for the tablets evaluation. Considering all evaluated parameters, a suitable amoxicillin 500 mg tablet formulation should present the microcrystalline cellulose type Avicel® PH-102 and the superdisintegrant agent, croscarmellose sodium (Ac-disol® SD-711), in its composition.2413947Korolkovas, A., (1988) Essentials of Medicinal Chemistry, 2nd Ed., p. 1216. , New York: Wiley-InterscienceDevani, M.B., Patel, I.T., Patel, T.M., (1992) J. Pharm. Biomed. Anal., 10, pp. 355-358Bird, A.E., (1994) Analytical Profiles of Drug Substances and Excipients, 23, pp. 1-52Carceles, C.M., Escudero, E., Vicente, M.S., Serrano, J.M., Carli, S., (1995) Vet. Quart., 17, pp. 134-138Chogle, P., Gudsoorkar, V.R., Shete, J.S., (1996) East Pharm., 39, pp. 121-123Westphal, J.F., Deslandes, A., Brogard, J.M., Carbon, C., (1991) J. Antimicrob. Chemother., 27, pp. 647-654Sanchez, M.A.C., Pastor, R.M.S., Suarez, A.I.T., (1991) An. Real Acad. Farm., 57, pp. 553-561Enézian, G.M., (1972) Pharm. Acta Helv., 47, pp. 321-363Banker, G.S., Anderson, N.R., (1986) The Theory and Pratice of Industrial Pharmacy, , New York: Lea & FebigerShangraw, R.F., (1989) Pharmaceutical Dosage Forms: Tablets, 1. , New York: Marcel Dekker IncBauer-Brandl, A., Becker, D., (1996) Drug Dev. Ind. Pharm., 22, pp. 417-430Sheth, B.B., Bandelin, F.J., Shangraw, R.F., (1980) Pharmaceutical Dosage Forms: Tablets, 1. , New York: Marcel Dekker IncAnsel, H.C., Popovich, N.G., Allen Jr., L.V., (1995) Pharmaceutical Dosage Forms and Drug Delivery Systems, , Philadelphia: Lea & FebigerDoelker, E., (1993) Drug Dev. Ind. Pharm., 19, pp. 2399-2471Ferrero, C., Muñoz, N., Velasco, M.V., Muñoz-Ruiz, A., Jiménez-Castellano, S.R., (1997) Int. J. Pharm., 144, pp. 11-21(2004) DMS Anti-Infectives - Amoxicillin Trihydrate, Compacted for Direct Compression, , www.dsm.com/en_US/html/dai/amoxicillinfordirectcompression.htmNeto, B.B., Scarminio, I.S., Bruns, R.E., (1995) Planejamento e Otimização de Experimentos, 2 Ed., pp. 61-100. , Editora da UNICAMP(1988) Brazilian Pharmacopoeia, , Part I. General Methods, 4th ed., São Paulo: AtheneuFood and Drug Administration, HHS (1996). Code of Federal. Washington: Office of the Federal regulations. Pp 21, págs. 387-535(1995) Pharmacopoeia of United States of America, , 23th ed., Rockville: United States Pharmacopoeial ConventionDoelker, E., Massuelle, D., Veuillez, F., Humbert-Droz, P., (1995) Drug Dev. Ind. Pharm., 21, pp. 643-661Gordon, M.S., Chatterjee, B., Chowhan, Z.T., (1990) J. Pharm. Sci., 79, pp. 43-47Roberts, R.J., Rowe, R.C., (1986) J. Pharm. Pharmacol., 38, pp. 567-571Martin, A., Swarbrick, J., Cammarata, A., (1993) Physical Pharmacy, , Philadelphia: Lea & FebigerHassan, M.A., Kaloustian, J., Prinderre, P., Ramsi, S.H., Khaled, K.A., El-Faham, T.H., Tous, S.S., Joachim, J., (1996) Pharmazie, 51, pp. 400-403Gordon, M.S., Chowhan, Z.T., (1987) J. Pharm. Sci., 76, pp. 907-90