Design and Characterization of Colon-specific Drug Delivery System Containing Paracetamol Microsponges

다국어 초록 (Multilingual Abstract)

The present work was aimed at designing microsponge based colon specific drug delivery system containing paracetamol. Eudragit S-100 based microsponges containing drug in varying amounts were prepared using quasi-emulsion solvent diffusion method. The microsponges were prepared by optimizing various process parameters. DSC and FTIR studies indicated compatibility of the drug in various formulations. Shape and surface morphology of the microsponges were examined using scanning electron microscopy. The formulations were subjected to in vitro release studies and the results were evaluated kinetically and statistically. The in vitro release data showed a bi-phasic pattern with an initial burst effect. In the first hour drug release from microsponges was found to be between 18-30%. The cumulative percent release at the end of 12th hour was noted to be between 74-98%. The release kinetics showed that the data followed Higuchi model and the main mechanism of drug release was diffusion. The colon specific tablets were prepared by compressing the microsponges followed by coating with pectin: hydroxypropylmethyl cellulose (HPMC) mixture. In vitro release studies exhibited that compression coated colon specific tablet formulations started releasing the drug at 6th hour corresponding to the arrival time at proximal colon. The study presents a new approach for colon specific drug delivery.

참고문헌 (Reference)

• 1 Mastiholimath, V. S., "Time and pH dependent colon specific, pulsatile delivery of theophylline for nocturnal asthma" 328 : 49-56, 2007
• 2 Vandamme, Th. F., "The use of polysaccharides to target drugs to the colon" 48 : 219-231, 2002
• 3 Jelvehgari, M., "The microsponge delivery system of benzoyl peroxide: preparation, characterization and release studies" 308 : 124-132, 2006
• 4 Lamprecht, A., "Size-dependent bioadhesion of micro- and nanoparticulate carriers to the inflamed colonic mucosa" 18 : 788-793, 2001
• 5 Yang, M., "Preparation of sustained-release nitrendipine microspheres with Eudragit RS and Aerosil using quasiemulsion solvent diffusion method" 259 : 103-113, 2003
• 6 Como lu, T., "Preparation and in vitro evaluation of modified release ketoprofen microsponges" 58 : 101-106, 2003
• 7 Devrim, B., "Preparation and evaluation of modified release ibuprofen microspheres with acrylic polymers (Eudragit) by quasi-emulsion solvent diffusion method: effect of variables" 63 : 521-534, 2006
• 8 Asghar, L. F. A., "Multiparticulate formulation approach to colon specific drug delivery: current perspectives" 9 : 327-338, 2006
• 9 Perumal, D., "Microencapsulation of ibuprofen and Eudragit RS 100 by the emulsion solvent diffusion technique" 218 : 1-11, 2001
• 10 Krishnaiah, Y. S. R., "Gamma scintigraphic studies on guar gum matrix tablets for colonic drug delivery in healthy human volunteers" 55 : 245-252, 1998
• 11 Nokhodchi, A., "Factors affecting the morphology of benzoyl peroxide microsponges" 38 : 834-840, 2007
• 12 Kshirsagar, N. A., "Drug delivery systems" 32 : S54-S61, 2000
• 13 Orlu, M., "Design and evaluation of colon specific drug delivery system containing flurbiprofen microsponges" 318 : 103-117, 2006
• 14 Chourasia, M. K., "Design and development of multiparticulate system fort targeted drug delivery to colon" 11 : 201-207, 2004
• 15 Ceschel, G. C., "Degradation of components in drug formulations: a comparison between HPLC and DSC methods" 32 : 1067-1072, 2003
• 16 Sriamornsak, P., "Composite film-coated tablets intended for colon-specific delivery of 5-aminosalicylic acid: using deesterified pectin" 8 : 311-318, 2003
• 17 Varshosaz, J., "Colon-specific delivery of mesalazine chitosan microspheres" 23 : 329-339, 2006
• 18 Kosaraju, S. L., "Colon targeted delivery systems: review of polysaccharides for encapsulation and delivery" 45 : 251-258, 2005
• 19 Sinha, V. R., "Coating polymers for colon specific drug delivery: a comparative in vitro evaluation" 53 : 41-47, 2003
• 20 Mukherjee, B., "A comparison between povidone-ethylcellulose and povidone-eudragit transdermal dexamethasone matrix patches based on in vitro skin permeation" 59 : 475-483, 2005