Konjac glucomannan and xanthan gum as compression
coat for colonic drug delivery: experimental and theoretical evaluations
Konjac glucomannan and xanthan gum as compression
coat for colonic drug delivery: experimental and theoretical evaluations
Kang WANG,Jiangyang FAN,Yanjun LIU,Zhimin HE,
Enzyme Technology Laboratory,
Chemical Engineering Research Center, School of Chemical Engineering
and Technology, Tianjin University, Tianjin 300072, China;
Abstract:Compression coated tablets for oral colon specific delivery systems were developed with a mixture polysaccharide of konjac glucomannan (KGM) and xanthan gum (XG) as the compression coat. Diffusion of cimetidine from compression coated tablets was investigated by release experiment in Vitro. 0.22U/mL β-mannanase was applied in the mimic colon solution. The structure of the mixture polysaccharide was studied by an atomic force microscope (AFM). The experimental results indicate that a KGM70 tablet with a 0.4g coat is of good design, due to a less than 5% drug loss in the mimic upper gastrointestinal solution by the synergistic interaction between XG and KGM, and due to about 50% cumulative release in the mimic colon solution by degradation after 24 hours. The release mechanism and model are discussed based on different periods of drug release including the delay of the drug, the constant release without an enzyme and the delay of degradation. Under hydrolysis by β-mannanase, drug release from the tablet with KGM coat shows an exponential increase, while that from the dosage with the mixture polysaccharide coat is an approximately zero-order process in which the constant release rate relates to the release velocity of a non-degraded system, the content of KGM within the coat and the average molecular weight ratio of KGM to XG. It was found that XG was the framework of the polysaccharide mixtures by AFM, which is similar to the analysis results from experiments on drug release.
出版日期: 2010-03-05
引用本文:
. Konjac glucomannan and xanthan gum as compression
coat for colonic drug delivery: experimental and theoretical evaluations[J]. Front. Chem. Sci. Eng., 2010, 4(1): 102-108.
Kang WANG, Jiangyang FAN, Yanjun LIU, Zhimin HE, . Konjac glucomannan and xanthan gum as compression
coat for colonic drug delivery: experimental and theoretical evaluations. Front. Chem. Sci. Eng., 2010, 4(1): 102-108.
Kinget R, Kalala W, Vervoort L, Mooter G V. Colonic drug targeting. J Drug Target, 1988, 6(2): 129–149 doi: 10.3109/10611869808997888
Vandamme T F, Lenourry A, Charrueau C, Chaumeil J. Theuse of polysaccharides to target drugs to the colon. Carbohyd Polym, 2000, 48(3): 219–231 doi: 10.1016/S0144-8617(01)00263-6
Alonso-Sande M, Teijeiro-Osorio D, Remunan-Lopez C, Alonso M J. Glucomannan, a promising polysaccharide for biopharmaceuticalpurposes. European Journal of Pharmaceuticsand Biopharmaceutics, 2009, 72: 453–462 doi: 10.1016/j.ejpb.2008.02.005
He Z M, Zhang J, Huang D P. A kinetic correlation for konjac powder hydrolysis by β-mannanase from Bacillus licheniformis. BiotechnolLett, 2001, 23(5): 389–393 doi: 10.1023/A:1005615204340
Huang C Y, Zhang M Y, Peng S S. Effect of konjac food on blood glucose level in patientswith diabetes. Biomed Environ Sci, 1990, 3(2): 123–131
Vuksan V, Jenkins D J, Spadafora P. Konjac-mannan (glucomannan) improves glycemia and otherassociated risk factors for coronary heart disease in type 2 diabetes.A randomized controlled metabolic trial. Diabetes Care, 1999, 22(6): 913–919 doi: 10.2337/diacare.22.6.913
Dave V, Sheth M, McCarthy S P, Ratto J A, Kaplan D L. Liquid crystalline, rheological and thermalproperties of konjac glucomannan. Polymer, 1998, 39(5): 1139–1148 doi: 10.1016/S0032-3861(97)00255-3
Nakano M, Takikawa K, Arita T. Release characteristics of dibucaine dispersed in konjacgels. J Biomed Mater Res,1979, 13: 811–819 doi: 10.1002/jbm.820130511
Wang K, He Z M. Alginate-konjac glucomannan-chitosanbeads as controlled release matrix. IntJ Pharm, 2002, 244(2): 117–126 doi: 10.1016/S0378-5173(02)00324-1
Liu M M, Fan J Y, Wang K, He Z M. Synthesis,characterization, and evaluation of phosphated cross-linked konjacglucomannan hydrogels for colon-targeted drug delivery. Drug Delivery, 2007, 14(6): 397–402 doi: 10.1080/10717540701202887
Sinha V R, Mittal B R, Bhutani K K, Kumria R. Colonicdrug delivery of 5-fluorouracil: an in vitro evaluation. Int J Pharm, 2004, 269(1): 101–108 doi: 10.1016/j.ijpharm.2003.09.036
Fan J Y, Wang K, Liu M M, He Z M. In vitroevaluations of konjac glucomannan and xanthan gum mixture as the sustainedrelease material of matrix tablet. CarbohydratePolymers, 2008, (73): 241–247 doi: 10.1016/j.carbpol.2007.11.027
Paradossi G, Chiessi E, Barbiroli A, Fessas D. Xanthanand glucomannan mixtures: synergistic interactions and gelation. Biomacromolecules, 2002, 3(3) : 498–504 doi: 10.1021/bm010163v
Alvarez-Mancenido F, Landin M, Martinez-Pacheco R. Konjac glucomannan/xanthan gum enzymesensitive binary mixtures for colonic drug delivery. European Journal of Pharmaceutics and Biopharmaceutics, 2008, 69: 573–581 doi: 10.1016/j.ejpb.2008.01.004
Sinha V R, Mittal B R, Kumria R. In vivo evaluation of time and site of disintegrationof polysaccharide tablet prepared for colon-specific drug delivery. Int J Pharm, 2005, 289(1—2): 79–85 doi: 10.1016/j.ijpharm.2004.10.019
Zhang Y, Hou S X, Lu Y, Chen G, Ju J H. Study on preparation of konjac glucomannan-hydroxypropylmethyl cellulose compression coated tablets for colonic delivery andin vitro release. China Journal of ChineseMateria Medica (Zhongguo Zhong Yao Za Zhi), 2006, 31(8): 642–645 (in Chinese)
Hodgesa L A, Connollya S M, Banda J. Scintigraphic evaluation of colon targeting pectin-HPMCtablets in healthy volunteers. InternationalJournal of Pharmaceutics, 2009, 370: 144–150 doi: 10.1016/j.ijpharm.2008.12.002
Rief M, Oesterhelt F, Heymann B, Gaub H E. AFM, a toolfor single-molecule experiments. Science, 1997, 275(21): 1295–1297 doi: 10.1126/science.275.5304.1295
Feng Y Y, He Z M, Ong S L, Hu J Y, Zhang Z G, Ng W J. Optimization of agitation, aeration, and temperature conditions formaximum β-mannanase production. Enzyme Microb Tech, 2003, 32(2): 282–289 doi: 10.1016/S0141-0229(02)00287-9
Krishnaiah Y S R, Satyanarayana V, Dinesh Kumar B, Karthikeyan R S. In vitro drug release studies on guar gum-based colon targeted oraldrug delivery systems of 5-fluorouracil. Eur J Pharm Sci, 2002, 16(3): 185–192 doi: 10.1016/S0928-0987(02)00081-7
Kirby A R, Gunning A P, Morris V J. Imaging xanthan gum by atomic force microscopy. Carbohyd Res, 1995, 267(1): 161–166 doi: 10.1016/0008-6215(94)00294-P
Alvarez-Manceñido F, Landin M, Lacik I, Martínez-Pacheco R. Konjacglucomannan and konjac glucomannan/xanthan gum mixtures as excipientsfor controlled drug delivery systems. Diffusionof small drugs. International Journal of Pharmaceutics, 2008, 349:11–18 doi: 10.1016/j.ijpharm.2007.07.015
Whistler R L, Bemiller J N. Xanthan, Gellan, Welan, andRhamsan. In: Whistler R L, Bemiller J N, eds. Industrial Gums.Polysaccharides and Their Derivatives. 3rd ed. New York: Academic Press, 1993, 341–371
Charlier A, Leclerc B, Couarraze G. Release of mifepristone from biodegradable matrices:experimental and theoretical evaluations. Int J Pharm, 2000, 200(2): 115–120 doi: 10.1016/S0378-5173(00)00356-2
Li B, Xie B J, John F K. Studies on the molecular chain morphology of kongjacglucomannan. Carbohydr Polym, 2006, 64(4): 510–515 doi: 10.1016/j.carbpol.2005.11.001