Document Type: Research(Original) Article
Department of Medicinal Chemistry, School of Pharmacy, Hamedan University of Medical Sciences, Hamedan, Iran.
Department of Pharmaceutics, School of Pharmacy, Hamedan University of Medical Sciences, Hamedan, Iran.
Lansoprazole degrades rapidly in an aqueous solution at low pH values. Degradation rate increases at pH values below 4 .The aim of this study was development of enteric coated pellets containing Lansoprazole by an extrusion/ spheronization technique. Eight different formulations based on lactose and six different formulations based on mannitol, consisting of different portions of other excipients including sucrose, hydroxy propyl methyl cellulose, magnesium carbonate, and sodium lauryl sulfate have been prepared. Feret diameter, shape factor, and amount of drug released were determined for each formulation. Among different formulations, F14, which consists of mannitol, sucrose, HPMC, talc, magnesium carbonate, and lansoprazole, is considered to be the best formulation. Six other different formulations for the preparation of enteric coatings based on Eudragit S100, Eudragit L100, triethyl citrate, and talc were prepared and coating procedure on pellets (F14) was performed using coating pan. In vitro drug release tests in acidic media (pH=1.2) and buffer media (pH=6.8) were performed for pellets, coated with each coating formulation and dissolution profile for each formulation was prepared. The pellets coated by formulation F.C 4, consisting of Eudragit L 100, triethylcitrate, and talc, showed a proper in vitro drug release profile. Accelerated stability tests were performed on coated pellets according to USP, and data suggested that pellets will be stable for 2 years
- Koo OM, Heng PW. The Influence of Microcrystalline Cellulose Grade on Shape and Shape Distributions of Pellets Produced by Extrusion-Spheronization. Chem Pharm Bull (Tokyo). 2001;49:1383-7.
- Abbaspour MR, Sadeghi F, Afrasiabi Gharekani H. Design and study of ibuprofen disintegrating sustained-release tablets comprising coated pellets. Eur J Pharm Biopharm. 2008;68:747-59.
- Podczeck F, Knight P. The Evaluation of Formulations for the Preparation of Pellets with High Drug Loading by Extrusion/Spheronization. Pharm Dev Technol. 2006;11:263-74.
- Tomer G, Podczeck F, Newton JM. The influence of model drugs on the preparation of pellets by extrusion/spheronization: II. Spheronization parameters. Int J Pharm. 2002;231:107-19.
- Gherbre Sellasie Issac. (2005).Pharmaceutical pelletization technology. New York, US: Marcel Dekker.
- Fielden KE, Newton JM, Rowe RC. Movement of liquids throw powder beds. Int J Pharm.1992;79:47-60.
- Piao J, Lee JE, Weon KY, Kim DW, Lee JS, Park JD, Nishiyama Y, Fukui I, Kim JS. Development of Novel Mucoadhesive Pellets of Metformin Hydrochloride. Arch Pharm Res. 2009;32:391-97.
- Dietrich R, Brausse R. Validation of the pellet coating process used for a new sustained-release theophylline formulation. Arzneimittelforschung. 1988;38:1210-9.
- Kramar A, Turk S, Verecer F. Statistical optimisation of diclofenac sustained release pellets coated with polymethacrylic films. Int J Pharm. 2003;256:43-52.
- Kablitz CD, Harder K, Urbanetz NA. Dry coating in a rotary fluid bed. Eur J Pharm Sci. 2006;27:212-19.
- el-Mahdi IM, Deasy PB. Tableting of coated ketoprofen pellets. J Microencapsul. 2000;17:133-44.
- Ganesan M, Pal TK, Jayakumar M. Pellet coating by air suspension technique using a mini-model coating unit. Boll Chim Farm. 2003;142:290-4.
- Sachs G, Shin JM, Howden CW. Review article: The clinical pharmacology of proton pump inhibitors. Aliment Pharmacol Ther. 2006;23:2-8.
- Michael R. Riley. 2000). Drug facts and comparisons. Missouri, US: facts and comparisonsÂ®
- Tabata T, Makino T, Kikuta J, et al. Manufacturing method of stable enteric granules of a new antiulcer drug (Lansoprazole). Drug Dev Ind Pharm. 1994;20:1661-72.
- Tutunji MF, Qaisi AM, El-Eswed B, Tutunji LF. An in vitro investigation on acid catalyzed reactions of proton pump inhibitors in the absence of an electrophile. Int J pharm. 2006;323:110-16.
- Deasy PB, Law FML. Use of extrusion-spheronization to develop an improved oral dosage form of indomethacin. Int J Pharm. 1997; 148:201-9.
- Sheng JJ, Kasim NA, Chandrasekharan R, Amidon GL. Solubilization and dissolution of insoluble weak acid, ketoprofen: effects of pH combined with surfactant. Eur J Pharm Sci. 2006;29: 306-14.
- Shah VP, Konecny JJ, Everett RL, McCullough B, Noorizadeh AC, Skelly JP. In vitro dissolution profile of water-insoluble drug dosage forms in the presence of surfactants. Pharm Res. 1989; 6:612-8.
- Balaxi M, Nikolakakis I, Kachrimanis K, Malamataris S. Combined effects of wetting, drying, and microcrystalline cellulose type on the mechanical strength and disintegration of pellets. J Pharm Sci. 2009;98:676-89.
- Balogh E, Kallai N, Dredan J, Lengyel M, Klebovich I, Antal I. Application of computer image analysis for characterization of pellets. Acta Pharm Hung. 2007;77:123-31.
- Jin Y, Wang YF, Wang CR, et al. Preparation of sustained-release and enteric coated pellets of pantoprazole. Chinese Pharmaceutical Journal. 2009;44:997-1001
- Zhang SQ, Rahman Z, Thumma S, Repka MA, Chen GH, Li SM. Development and evaluation of a pH-dependent sustained release tablet for irritable bowel syndrome. Drug Dev Ind Pharm. 2009;35:57-64
- Sinchaipanid N, Chitropas P, Mitrevej A. Influences of Layering on Theophylline Pellet Characteristics. Pharm Dev Technol. 2004;9:163-70.
- Kleinebudde P, SchrÃ¶der M, Schultz P, MÃ¼ller BW, Waaler T, Nymo L. Importance of the Fraction of Microcrystalline Cellulose and Spheronization Speed on the Properties of Extruded Pellets Made from Binary Mixtures. Pharm Dev Technol. 1999;4:397-404.
- Chatchawalsaisin J, Podczeck F, Newton JM. The preparation by extrusion/spheronization and the properties of pellets containing drugs, microcrystalline cellulose and glyceryl monostearate. Eur J Pharm. 2005;24:35-48.
- Asghar LF, Chure CB, Chandran S. Colon specific delivery of indomethacin: Effect of incorporating pH sensitive polymers in xanthan gum matrix bases. AAPS PharmSciTech. 2009;10:335-45.