Formulation and in vivo imaging evaluation of colonic targeting tablets prepared by a simple dry powder coating technique

다국어 초록 (Multilingual Abstract)

Purpose The study aimed firstly to determine the release behavior of the model drug (berberine chloride) from the dry coated tablets. The second objective of this study was to evaluate the exact location of the dry coated tablets in in vivo.
Methods The colon targeting tablets were developed by dry powder coating technique on pan coater. The drug release behavior was determined in the three continuous mediums: pH 1.2; 7.4 and 6.8 plus pectinase. The location of the dry coated tablets in the gastrointestinal tract of human volunteers was observed through the X-ray imaging of the dry coated tablets containing the optimized radiocontrast agents.
Results The release kinetics of berberine chloride from the dry coated tablets was mainly controlled by erosion and enzyme sensitive mechanism. The optimum dry coated tablets having the coating powders of pectin 102:HPMC K4 M (2:1) with the coating level of 200%, and the tablet core with BaSO4 10% and iobitridol 30% as radiocontrast agents were observed in the caecum and ascending colon of human volunteers after 5–6 h of oral administration.
Conclusion The successful development of these dosage forms is believed to have a high potential in precisely monitoring the release of highly potent drugs such as anti-inflammatory drugs in bowel diseases.

참고문헌 (Reference)

1 Makhlof A, "pH-Sensitive nanospheres for colon-specific drug delivery in experimentally induced colitis rat model" 72 : 1-8, 2009

2 Mastiholimath VS, "Time and pH dependent colon specific, pulsatile delivery of theophylline for nocturnal asthma" 328 : 49-56, 2007

3 Klar F, "The role of capillary force promoters in dry coating procedures–evaluation of acetylated monoglyceride, isopropyl myristate and palmitate. Parameters influencing polymer particle layering of the dry coating process" 71 : 124-129, 2009

4 Ma Y, "The in vivo fate of nanoparticles and nanoparticleloaded microcapsules after oral administration in mice : Evaluation of their potential for colon-specific delivery" 94 : 393-403, 2015

5 Krishnaiah YS, "Studies on the development of oral colon targeted drug delivery systems for metronidazole in the treatment of amoebiasis" 236 : 43-55, 2002

6 Bose S, "Solventless pharmaceutical coating processes : a review" 12 : 115-131, 2007

7 Teruel AH, "Smart gated magnetic silica mesoporous particles for targeted colon drug delivery : new approaches for inflammatory bowel diseases treatment" 281 : 58-69, 2018

8 Yehia SA, "Pulsatile systems for colon targeting of budesonide : in vitro and in vivo evaluation" 18 : 620-630, 2011

9 Carbinatto FM, "Physical properties of pectin-high amylose starch mixtures cross-linked with sodium trimetaphosphate" 423 : 281-288, 2012

10 Tung N-T, "Pectin/HPMC dry powder coating formulations for colon specific targeting tablets of metronidazole" 33 : 19-27, 2016

11 Liu L, "Pectin-based systems for colon-specific drug delivery via oral route" 24 : 3333-3343, 2003

12 Kablitz CD, "Parameters influencing polymer particle layering of the dry coating process" 69 : 760-768, 2008

13 Yassin AE, "New targeted-colon delivery system : in vitro and in vivo evaluation using X-ray imaging" 18 : 59-66, 2010

14 Felton LA, "Influence of insoluble excipients on film coating systems" 28 : 225-243, 2002

15 Turkoglu M, "In vitro evaluation of pectin-HPMC compression coated 5-aminosalicylic acid tablets for colonic delivery" 53 : 65-73, 2002

16 Smikalla M, "Impact of excipients on coating efficiency in dry powder coating" 405 : 122-131, 2011

17 Yang C, "Highly specific colon-targeted transformable capsules containing indomethacin immediate-release pellets for colon cancers therapy" 2019

18 Rowe RC, "Handbook of Pharmaceutical Excipients" Pharmaceutical Press 2009

19 Bhavsar MD, "Gastrointestinal distribution and in vivo gene transfection studies with nanoparticles-in-microsphere oral system(NiMOS)" 119 : 339-348, 2007

20 Veerareddy PR, "Formulation, evaluation and pharmacokinetics of colon targeted pulsatile system of flurbiprofen" 20 : 703-714, 2012

21 Potu A, "Formulation and evaluation of fenoprofen calcium compressed coated tablets for colon specific drug delivery" 4 : 88-95, 2011

22 Maroni A, "Film coatings for oral pulsatile release" 457 : 362-371, 2013

23 Sauer D, "Dry powder coating of pharmaceuticals : a review" 457 : 488-502, 2013

24 Pearnchob N, "Dry polymer powder coating and comparison with conventional liquid-based coatings for Eudragit)RS, ethylcellulose and shellac" 56 : 363-369, 2003

25 Luo Y, "Dry coating, a novel coating technology for solid pharmaceutical dosage forms" 358 : 16-22, 2008

26 Teruel AH, "Double drug delivery using capped mesoporous silica microparticles for the effective treatment of inflammatory bowel disease" 16 : 2418-2429, 2019

27 Bharaniraja B, "Different approaches of katira gum formulations for colon targeting" 49 : 305-310, 2011

28 Sinha Roy D, "Comparative evaluation of rate of hydration and matrix erosion of HEC and HPC and study of drug release from their matrices" 16 : 193-199, 2002

29 Ugurlu T, "Colonic delivery of compression coated nisin tablets using pectin/HPMC polymer mixture" 67 : 202-210, 2007

30 Pearnchob N, "Coating of pellets with micronized ethylcellulose particles by a dry powder coating technique" 268 : 1-11, 2003

31 Lanjhiyana SK, "Chitosan-sodium alginate blended polyelectrolyte complexes as potential multiparticulate carrier system : colon-targeted delivery and gamma scintigraphic imaging" 10 : 5-15, 2013

32 Kablitz CD, "Characterization of the film formation of the dry coating process" 67 : 449-457, 2007

33 Fan TY, "An investigation of pulsatile release tablets with ethylcellulose and Eudragit L as film coating materials and cross-linked polyvinylpyrrolidone in the core tablets" 77 : 245-251, 2001

34 Ashford M, "An evaluation of pectin as a carrier for drug targeting to the colon" 26 : 213-220, 1993

35 Qiao M, "A novel electrostatic dry powder coating process for pharmaceutical dosage forms : immediate release coatings for tablets" 76 : 304-310, 2010

36 Singh SK, "A novel dissolution method for evaluation of polysaccharide based colon specific delivery systems : a suitable alternative to animal sacrifice" 73 : 72-80, 2015