A novel colonic drug delivery system of ibuprofen

M C Gohel, S A Nagori


The present endeavor was directed towards fabrication of the novel colonic drug delivery system of ibuprofen. To begin with, the hydroxypropyl methylcellulose capsules containing adsorbate of eutectic mixture of ibuprofen and menthol
and pregelatinized starch were coated with ethyl cellulose. These ethyl cellulose coated capsules were filled in another capsule and the capsules were coated with a Eudragit® S100. The in vitro drug release study was conducted using sequential
dissolution technique at pH 1.2 (two hour), 6.0 (1hr), 7.2 (two hour) and 6.4 (three hour) mimicking different regions of gastrointestinal tract. The optimized batch with two per cent and 6.5% weight gain of ethyl cellulose and Eudragit® S100 showed less than eight per cent drug release in stomach and intestinal pH. The remaining 92% drug release was obtained thereafter from the optimized batch within two hours in colonic pH. Scanning electron microscopy study of the optimizedbatch confirmed presence of ibuprofen crystals (rod shape) in the formulation. The infrared spectroscopy study of the
optimized batch indicated stability of ibuprofen during processing of the formulation.

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Barbara L, Teresa C, Federica B, Isabella O, Vittorio Z. pH-sensitive

polymeric physical-mixture for possible site-specific delivery of

ibuprofen. Eur J Pharm Biopharm 2003;55:199-202.

Antonin K, Rak R, Beick P, Schenker U, Hastewell J, Fox R, et al. The

absorption of human calcitonin from the transverse colon of man. Int

J Pharm 1996;130:33-9.

Tozaki H, Komoike J, Tada C, Marnyama T, Terabe A, Suzuki T, et al.

Chitosan capsules for colon-specific drug delivery: Improvement of

insulin absorption from the rat colon. J Pharm Sci 1997;86:1016-21.

Van-den M, Kinget R. Oral colon-specific drug delivery: A review. Drug

Delivery 1995;2:81-93.

Rama Prasad Y, Krishnaiah Y, Satyanarayana S. in vitro evaluation of guar gum as a carrier for colon-specific drug delivery. J Control Rel 1998;51:281-7.

Evans D, Pye G, Bramely R, Clark A, Dysoa T. Measurement of gastrointestinal pH profiles in normal ambulant human subjects. Gut 1988;29:1035-41.

Ashford M, Fell J, Attwood D, Sharma H, Woodhead P. An in vivo

investigation into the suitability of pH dependent polymers for colonic

targeting. Int J Pharm 1993;95:193-9.

Davis S, Hardy J, Taylor M, Stockwell A, Whalley D, Wilson C. The in vivo

evaluation of an osmotic device (Osmet) using gamma scintigraphy. J

Pharm Pharmacol 1984;36:740-2.

Marvola M, Aito H, Ponto P, Kanniksoki A, Nykanen S, Kokkonen P.

Gastrointestinal transit and concomitant absorption of verapamil from a

single unit sustained release tablet. Drug Dev Ind Pharm 1987;13:1593-609.

Vyas S, Khar R. Controlled Drug Delivery-Concepts and Advances. New

Delhi: Vallabh Prakashan; 2002. p. 218-56.

Brondsted H, Andersen C, Hovgaard L. Crosslinked dextran-A new

capsule material for colon targeting of drugs. J Control Rel 1998;53:7-13.

Huskisson E. Anti-Rheumatic Drugs. Westport: Praeger Publishers Inc;

p. 244-66.

Wilson C, Washington N, Greaves J, Kamali F, Rees J, Sempik A, et al.

Bimodal release of ibuprofen in a sustained release formulation:

A scintigraphic and pharmacokinetic open study in healthy

volunteers under different conditions of food intake. Int J Pharm


Yao M, Zhou W, Sangha S, Albert A, Chang AJ, Liu TC, et al. Effects of

nonselective cyclooxygenase inhibition with low-dose ibuprofen on

tumor growth, angiogenesis, metastasis, and survival in a mouse model

of colorectal cancer. Clin Cancer Res 2005;11:1618-28.

Gohel M, Parikh R, Nagori S, Dabhi M. Design of potential colonic drug

delivery system of mesalamine. Pharm Dev Tech 2008;13:447-56.

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

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

Mariko M, Ayako M, Kozo T, Koichi I, Tsuneji N. Improving insulin

enteral absorption using water-in-oil-in water emulsion. Int J Pharm


Flashner-Barak M, Lerner I, Rosenberger V, Moldavski N. Menthol

solutions of drugs. Patent WO/2004/073686 Sep 2, 2004.

Mckay D, Blumberg J. A review of the bioactivity and potential health

benefits of peppermint tea (Mentha piperita L.). Phytother Res


Nahor H, Chell N, Kamyar H, Carlos K, Osvaldo C, Jenna R, et al. A

multi- cale stochastic drug release model for polymer-coated targeted

s drug delivery systems. J Control Rel 2006;110:314-22.

François L, Louis C, Roch T. New methods characterizing avalanche

behavior to determine powder flow. Pharm Res 2002;19:887-93.

United States Pharmacopoeia, 2006, Asian edition. United States

Pharmacopoeial Convention Inc: 1842.

Indian Pharmacopoeia. Vol. 1. 1996. p. 736.

Sangalli M, Maroni A, Foppoli A, Zema L, Giordano F, Gazzaniga A.

Different HPMC viscosity grades as coating agents for an oral time

and/or site-controlled delivery system: A study on process parameters

and in vitro performances. Eur J Pharm Sci 2004;22:469-76.

British Pharmacopoeia. Vol. 2. 2001. Appendix XII B.

Pawar A, Paradkar, Kadam S, Mahadik K. Agglomeration of ibuprofen

with talc by novel crystallo-co-agglomeration technique. AAPS

Pharm Sci Tech 2004;5:e55.

Garekani H, Sadeghi F, Badiee A, Mostafa S, Ali R, Rajabi Siahboomi A.

Crystal habit modifications of ibuprofen and their physicomechanical

characteristics. Drug Dev Ind Pharm 2001;27:803-9.

Bunyan J, Shankland N, Sheen D. Solvent effects on the morphology

of ibuprofen. AIChe Symp Ser 1991;87:44-57.

Gordon R, Amin S. Crystallization of ibuprofen. U. S. Patent 44, 76, 248

Oct 9, 1984.

Franz R. Stable, high dose, high bulk density ibuprofen granulations for

tablet and capsule manufacturing. U. S. Patent 46, 09, 675 Sep 2, 1986.

Chen J. Process for enhancing the flow characteristics of ibuprofen. U.

S. Patent 5,191,114 March 2, 1993.

Groenewoud P, Facemire J, Jayanth J. Narcotic composition and method

for making same. Patent WO 2005/037192 April 28, 2005.

Raymond R, Paul S. Handbook of Pharmaceutical Excipients. 4th ed.

London: The Pharmaceutical Press; 1994. p. 373-7, 462-8, 609-11.

Vasanthakumar S, Vijaya R. Immediate release tablets of telmisartan

using superdisintegrant-formulation, evaluation and stability studies.

Chem Pharm Bull 2008;56:575-7.

Inactive Ingredient Guide (Redacted). U.S. Food and Drug Administration,

Center for Drug Evaluation and Research. January, 1996; Available from:

http://www.fda.gov/cder/drug/iig/default.htm. [last accessed on 2006

Jun 18].

Meza C, Santos M, Romañach R. Quantitation of drug content in a low

dosage formulation by transmission near infrared spectroscopy. AAPS

Pharm Sci tech 2006;7:E29.

Rees J. Mixing of particulate solids to ensure homogeneity of dosage

forms: Need for a critical approach to pharmaceutical process

development. Boll Chim Farm 1977;116:445-62.

DOI: http://dx.doi.org/10.22377/ajp.v3i3.272


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