Formulation development, optimization and study on drug release kinetics of Eudragit® L100-HPMC E15 LV mixed film-coated colon- targeted Mesalamine tablets

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A Maria John Newton
L Prabakaran
KN Jayaveera


The study was designed to evaluate the in vitro dissolution characteristics of pH-sensitive polymer - HPMC E 15 LV-coated tablets - in various simulated fluids (pH range 1.2, 6, 7.2). The Mesalamine tablets were fabricated by mixing
the drug with microcrystalline cellulose and other ingredients.The fabricated Mesalamine tablets were coated with Eudragit L100 polymer and HPMC E 15 LV. The fluctuation in colonic pH conditions during inflammatory bowel disease and the nature of less fluid content in the colon may limit the expected drug release in the colon. Addition of HPMC E 15 LV may control this problem by hydrophilic nature and excellent film-forming characteristics like ductility and elasticity.
The different batches of Mesalamine tablets (FM1-FM5) were coated with increasing concentration of Eudragit L100 and HPMC E 15 LV. The coating was given up to 8% TWG(Total weight gain) of the uncoated tablet. Drug release studies were conducted in different pH conditions in the presence of rat ceaecal contents. The different buffer conditions were chosen to mimic the pH changes in the terminal part of the ileum as well as in the colon. The drug release profile was analyzed for colon-targeting performance in vitro. The release profile of the tablets indicates that the drug release was retarded in the tablet by film coating. The addition of HPMC E 15 LV ensures the channels for allowing colonic fluids to penetrate into the core and subsequent drug release at the target site. The kinetics of the drug release also evaluated the release pattern that was best fitted with Higuchian release. The results of the mechanism of release revealed that drug release was found to be a complex one with diffusion, erosion and swelling.


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Newton, A. M. J., Prabakaran, L., & Jayaveera, K. (2014). Formulation development, optimization and study on drug release kinetics of Eudragit® L100-HPMC E15 LV mixed film-coated colon- targeted Mesalamine tablets. Asian Journal of Pharmaceutics (AJP), 6(3).


James S Chu. Advances in colon-specific drug delivery system employingthe CODES TM. The drug delivery companies report autumn/winter ©Pharma ventures Ltd 2003:39-40.

Drossman DA, Li Z, Andruzzi E, Temple RD, Talley NJ, Thompson WG,et al. U. S householder survey of functional gastrointestinal disorder.

prevalence, sociodemography, and health impact. Dig Dis Sci


Podolsky DK. Inflammatory bowel disease. N Engl J Med 2002;347:417- 29.

Khan MZ, Prebeg Z, Kurjaković N. A pH-dependent colon targeted oral drug delivery system using methacrylic acid copolymers I. Manipulation Of drug release using Eudragit L100-55 and Eudragit S100 combinations.J Control Release 1999;58:215-22.

Yang L, Chu J, Fix JA. Colon-specific drug delivery: New approaches and in vitro/in vivo evaluation. Int J Pharm 2002;235:1-15.

Ardizzone S, Bianchi Porro G. A practical guide to management of distal ulcerative colitis. Drugs 1998;55:519-42.

Singh BN. Modified-release solid formulations for colonic delivery.

Recent Pat Drug Deliv Formul 2007;1:53-63.

Singh BN, Kim KH, Swarbrick J, Boylan JC. Encylopedia of Phrmaceutical

Technology, New York: Marcel Dekker, Inc; 2002. p. 886-909.

Follonier N, Cole ET. Evolution of hot melt extrusion as a new technique for the production of polymer based pellets for sustained release

capsule containing high loadings freely soluble drugs. Drug Dev Ind

Pharm 1994;20:1323-39.

Saffarin M, Kumar GS, Savariar C, BurnhamJC, Williams F,

Neckers DC. A New approach to the oral administration of insulin and

other peptide drugs. Science 1986;233:1081-4.

Ashford M, Fell JT. Targeting drugs to the colon: Delivery systems for

oral administration. J Drug Target 1994;2:241-57.

Wakerly Z, Fell JT, Attwood D. Parkins. Studies on drug release from

pectin/ethylcellulose film-coated tablets: A potential colonic delivery

systems. Int J Pharm 1997;153:219-24.

Evans DF, Pye G, Bramley R, Clark AG, Dyson TJ, Hardcastle JD. Measurement of gastrointestinal pH profiles in normal ambulant human subjects. Gut 1988;29:1035-41.

Ashford, M, Fell, JT, Attwood D, Sharma H. Woodhead P. An in vitro

investigation into the suitability of pH- dependent polymers for colon

targeting. Int J Pharm 1993;91:241-5.

Nugent SG, Kumar D, Rampton DS, Evans DF. Intestinal luminal pH in inflammatory bowel disease: Possible determination and implications

for therapy with aminosalicylates and other drugs. Gut 2001;48:571-7.

Takaya T, Niwa K, Muraka M, Ogita I, Nagai N, Yano R, et al. Importance of dissolution process on systemic availability of drugs delivered by colon delivery system. J Control Release 1998;50:111-22.

Basit A, Bloor J. Perspective on colonic drug delivery. Business briefing. Pharma tech 2003:185-90.

Khan MZ. Dissolution testing for sustained or controlled release

Oral dosage forms and correlation with in vivo data: Challenges and

opportunities. Int J Pharm 1996;140:131-4.

Dressman JB, Amidon GL, Reppas C, Shah VP. Dissolution testing as aprognostic tool for oral drug absorption: Immediate release dosage

forms. Pharm Res 1998;15:11-22.

Ramusen SN, Binder V, Maier K, Bondesen S, Fischer C, Klotz U, et al.Treatment of Crohn’s disease with peroral 5-amiino salicylic acid.

Gastroenterology 1983;85:1350-3.

Stolk LM, Rietbroek R, Wiltink EH, Tukker JJ. Dissolution profile of

mesalazine formuations in vitro. Pharm Weekbl Sci 1990:200-4.

Fallingborg J, Christensen LA, Jacobsen BA, Ramusen SN. Very low

intraluminal colonic pH in patients with active ulcerative colitis. Dig.

Dis Sci 1993;38:1989-93.

Ofori-Kwakye K, Fell JT. Biphasic drug release: The permeability of film containing pectin, chitosan and HPMC. Int J Pharm 2001;226:139-45.

Yuen KH, Deshmukh AA, Newton JM. Development and in-vitro

evaluation of a multiparticulate sustained release theophylline

formulation. Drug Dev Ind Pharm 1993;19:855-74.

Frohoff–Hulsmann MA, Schmitz A, Lippold BC. Aqueous ethyl cellulose dispersion containing plasticizers of different water solubility and

hydroxylpropyl methyl-cellulose as coating material for diffusion

pellets. I. Drug release rates from coated pellets. IntJ Pharm 1999;177:69-82.

Chan LW, Ong KT, Heng PW, Novel film modifiers to alter the physical

properties of composite ethylcellulose films. Pharm Res 2005;22:476- 89.