Bioavailability of Oral Colon-Specific Ketoprofen Microcapsules
Abstract
Oral, colon-specific drug delivery has attracted much interest recently. It is of considerable advantage to have an oral drug delivery system that could be targeted to the colon. This could be either for the local treatment of diseases such ulcerative colitis, irritable bowel syndrome and tumors, or to exploit the colon as a preferred region for systemic drug absorption, possibly as a site for polypeptides absorption. Delivery systems that rely on pH and/or time dependent mechanisms for drug release are less reliable in achieving consistent site-specific drug delivery to the colon. The successful delivery of prodrugs of 5- aminosalicylic acid is an evident of the potential of the bacterial flora. However, it has been less successful in the development of polysaccharide – based dosage forms or synthetic polymer coatings. This work was aimed at the development of ketoprofen microcapsules based on polysaccharide coating. The in-vitro release studies in simulated colonic media showed sensitivity of such dosage form to bacterial enzymes with subsequent increase in dissolution rate. The in -vivo profiles in dogs showed that the tested product exhibited a lag- time prior to commencement of drug absorption. The plasma profiles were not accompanied by a high initial plasma concentration associated with conventional dosage forms.
References
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2. Ashford M, Fell J. Targeting drugs to the colon: delivery systems for oral administration. journal of drug targeting. 1994 Jan 1;2(3):241-57.
3. Chourasia MK, Jain SK. Pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Pharm Sci. 2003 Jan 1;6(1):33-66.
4. Pozzi F, Furlani P, Gazzaniga A, Davis SS, Wilding IR. The time clock system: a new oral dosage form for fast and complete release of drug after a predetermined lag time. Journal of controlled release. 1994 Aug 1;31(1):99-108.
5. Jain A, Gupta Y, Jain SK. Perspectives of biodegradable natural polysaccharides for site- specific drug delivery to the colon. J Pharm Pharm Sci. 2007 Apr;10(1):86-128.
6. Gidwani B, Vyas A, Ahirwar K, Shukla SS, Pandey R, Kaur CD. Factorial Design and a Practical Approach for Gastro-Retentive Drug Delivery System. Research Journal of Pharmacy and Technology. 2016 Jun 20;9(6).
7. Oliveira GF, Ferrari PC, Carvalho LQ, Evangelista RC. Chitosan–pectin multiparticulate systems associated with enteric polymers for colonic drug delivery. Carbohydrate polymers. 2010 Oct 15;82(3):1004-9.
8. Watts PJ, Lllum L. Colonic drug delivery. Drug development and industrial pharmacy. 1997 Jan 1;23(9):893-913.
9. Akhgari A, Heshmati Z, Garekani HA, Sadeghi F, Sabbagh A, Makhmalzadeh BS, Nokhodchi A. Indomethacin Electrospun Nanofibers for Colonic Drug Delivery: In vitro dissolution studies. Colloids and Surfaces B: Biointerfaces. 2016 Dec 23.
10. Krishnaiah YS, Satyanarayana S, Prasad YR, Rao SN. Gamma scintigraphic studies on guar gum matrix tablets for colonic drug delivery in healthy human volunteers. Journal of controlled release. 1998 Nov 13;55(2):245-52.
11. Maestrelli F, Cirri M, Corti G, Mennini N, Mura P. Development of enteric-coated calcium pectinate microspheres intended for colonic drug delivery. European journal of pharmaceutics and biopharmaceutics. 2008 Jun 30;69(2):508-18.
12. Sinha VR, Kumria R. Polysaccharides in colon- specific drug delivery. International journal of pharmaceutics. 2001 Aug 14;224(1):19-38.
13. Liu L, Fishman ML, Kost J, Hicks KB. Pectin-based systems for colon-specific drug delivery via oral route. Biomaterials. 2003 Aug 31;24(19):3333-43.
14. Shah N, Shah T, Amin A. Polysaccharides: a targeting strategy for colonic drug delivery. Expert opinion on drug delivery. 2011 Jun 1;8(6):779-96.
15. Klotz U. Clinical pharmacokinetics of sulphasalazine, its metabolites and other prodrugs of 5- aminosalicylic acid. Clinical pharmacokinetics. 1985 Apr 1;10(4):285-302.
16. Sinha VR, Kumria R. Binders for colon specific drug delivery: an in vitro evaluation. International journal of pharmaceutics. 2002 Dec 5;249(1):23-31.
17. El-Mahdi IM, Deasy PB. Tableting of coated ketoprofen pellets. Journal of microencapsulation. 2000 Jan 1;17(2):133-44.
18. El-Mahdi IM, El-Shehebia TA. Three-Dimensional Presentations of Factorial Experimentation Data of Extrusion–Spheronization. Lebda Medical Journal. 2016 Oct 26;2(1). 89.
19. Brøndsted H, Kopeček J. Hydrogels for site-specific drug delivery to the colon: in vitro and in vivo degradation. Pharmaceutical research. 1992 Dec 1;9(12):1540-5.
20. Sinha VR, Mittal BR, Bhutani KK, Kumria R. Colonic drug delivery of 5-fluorouracil: an in vitro evaluation. International Journal of Pharmaceutics. 2004 Jan 9;269(1):101-8.
21. Akimoto M, Furuya A, Nakamura M, Maki T, Yamada K, Suwa T, Ogata H. Release and absorption characteristics of chlorphenesin carbamate sustained- release formulations: In vitro-in vivo and in vivo dog-human correlations. International journal of pharmaceutics. 1995 Apr 4;117(1):31-9.
22. Lui CY, Amidon GL, Berardi RR, Fleisher D, Youngberg C, Dressman JB. Comparison of gastrointestinal pH in dogs and humans: implications on the use of the beagle dog as a model for oral absorption in humans. Journal of pharmaceutical sciences. 1986 Mar 1;75(3):271-4.
23. Dar MJ, Ali H, Khan A, Khan GM. Polymer based drug delivery: The quest for local targeting of inflamed intestinal mucosa. Journal of Drug Targeting. 2017 Feb 23(just-accepted):1-44.
24. Sugito K, Ogata H, Goto H, Noguchi M, Kogure T, Takano M, Maruyama Y, Sasaki Y. Gastrointestinal transit of non-disintegrating solid formulations in humans. International Journal of Pharmaceutics. 1990 Apr 30;60(2):89-97.
25. Yang L, Chu JS, Fix JA. Colon-specific drug delivery: new approaches and in vitro/in vivo evaluation. International Journal of Pharmaceutics. 2002 Mar 20;235(1):1-5.
26. Khosla R, Davis SS. Gastric emptying and small and large bowel transit of non-disintegrating tablets in fasted subjects. International journal of pharmaceutics. 1989 May 15;52(1):1-0.
27. Asghar LF, Chandran S. Multiparticulate formulation approach to colon specific drug delivery: current perspectives. J Pharm Pharm Sci. 2006 Sep 1;9(3):327-38.
28. Deasy PB. Microencapsulation of drugs by pan and air suspension techniques. Critical reviews in therapeutic drug carrier systems. 1990 Dec;8(1):39-89
29. Gibaldi, M., (1991). Biopharmaceutics and Clinical pharmacokinetics, 4 th Ed ., Lea & Febiger , USA
30. Ibekwe VC, Liu F, Fadda HM, Khela MK, Evans DF,
Parsons GE, Basit AW. An investigation into the in vivo performance variability of pH responsive polymers for ileo- colonic drug delivery using gamma scintigraphy in humans. Journal of pharmaceutical sciences. 2006 Dec 1;95(12):2760-6.
Additional Files
Published
2017-10-02
How to Cite
Bioavailability of Oral Colon-Specific Ketoprofen Microcapsules. (2017). Lebda Medical Journal, 3(1), 101–105. Retrieved from https://lebmedj.elmergib.edu.ly/index.php/LMJ/article/view/78
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Section
Pharmacy
