Colon Specific Delivery of Indomethacin: Effect of Incorporating pH Sensitive Polymers in Xanthan Gum Matrix Bases

被引:41
作者
Asghar, Laila F. A. [1 ]
Chure, Chetan B. [1 ]
Chandran, Sajeev [1 ,2 ]
机构
[1] Birla Inst Technol & Sci, Pharm Grp, Formulat Dev & Pharmacokinet Lab, Pilani 333031, Rajasthan, India
[2] Lupin Ltd, Pharma Res, Innovat Cell, Pune 411042, Maharashtra, India
关键词
colon specific delivery; controlled release; Eudragits; matrix; pH sensitive polymers; xanthan gum; IN-VITRO EVALUATION; TRIGGERED DRUG-DELIVERY; CONTROLLED-RELEASE; SUSTAINED-RELEASE; DICLOFENAC SODIUM; RESPONSIVE POLYMERS; SOLID DISPERSIONS; VIVO PERFORMANCE; CANCER CELLS; GUAR GUM;
D O I
10.1208/s12249-009-9223-4
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
In the present study, an attempt has been made to design controlled release colon-specific formulations of indomethacin by employing pH responsive polymers Eudragit (L100 or S100) in matrix bases comprised of xanthan gum. The prepared tablets were found to be of acceptable quality with low-weight variation and uniform drug content. In vitro release studies indicated rapid swelling and release of significant percentage of drug in the initial period from matrix tablets composed of xanthan gum alone. Addition of pH responsive polymers Eudragit (L100 or S100) to xanthan gum matrix resulted in negligible to very low drug release in the initial period in acidic to weakly acidic medium. Furthermore, with increase in pH of the dissolution medium due to dissolution of Eudragit L100/Eudragit S100 that resulted in the formation of a porous matrix, faster but controlled drug release pattern was observed. Thus, a sigmoidal release pattern was observed from the designed formulations suitable for colonic delivery. Drug release mechanism in all cases was found to be of super case II type, indicating erosion to be the primary cause of drug release. Since the drug release from almost all the matrix bases in the initial phase was negligibly low and followed with controlled release for about 14-16 h, it was concluded that a matrix design of this composition could have potential applications as a colon-specific drug delivery device with additional advantage of easy scale-up and avoidance of all-or-none phenomenon associated with coated colon-specific systems.
引用
收藏
页码:418 / 429
页数:12
相关论文
共 56 条
[1]
Combination of time-dependent and pH-dependent polymethacrylates as a single coating formulation for colonic delivery of indomethacin pellets [J].
Akhgari, A. ;
Sadeghi, F. ;
Garekani, H. Afrasiabi .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2006, 320 (1-2) :137-142
[2]
Statistical optimization of indomethacin pellets coated with pH-dependent methacrylic polymers for possible colonic drug delivery [J].
Akhgari, A ;
Garekani, HA ;
Sadeghi, E ;
Azimaie, A .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2005, 305 (1-2) :22-30
[3]
PH-INDEPENDENT CONTROLLED-RELEASE MICROSPHERES USING POLYGLYCEROL ESTERS OF FATTY-ACIDS [J].
AKIYAMA, Y ;
YOSHIOKA, M ;
HORIBE, H ;
HIRAI, S ;
KITAMORI, N ;
TOGUCHI, H .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1994, 83 (11) :1600-1607
[4]
Development of enteric-coated timed-release matrix tablets for colon targeting [J].
Alvarez-Fuentes, J ;
Fernández-Arévalo, M ;
González-Rodríguez, ML ;
Cirri, M ;
Mura, P .
JOURNAL OF DRUG TARGETING, 2004, 12 (9-10) :607-612
[5]
Preparation and evaluation of sustained-release solid dispersions of drugs with Eudragit polymers [J].
Ammar, HO ;
Khalil, RM .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1997, 23 (11) :1043-1054
[6]
Xanthan gum as a carrier for controlled release of drugs [J].
Andreopoulos, AG ;
Tarantili, PA .
JOURNAL OF BIOMATERIALS APPLICATIONS, 2001, 16 (01) :34-46
[7]
Design and evaluation of pH modulated controlled release matrix systems for colon specific delivery of indomethacin [J].
Asghar, L. F. A. ;
Chandran, S. .
PHARMAZIE, 2008, 63 (10) :736-742
[8]
Asghar LFA, 2008, J DRUG TARGET, V16, P741, DOI [10.1080/10611860802473345, 10.1080/10611860802473345 ]
[9]
5-aminosalicylic acid release from a new controlled-release mesalazine formulation during gastrointestinal transit in healthy volunteers [J].
Brunner, M ;
Lackner, E ;
Exler, PS ;
De Fluiter, HC ;
Kletter, K ;
Tschurlovits, M ;
Dudczak, R ;
Eichler, HG ;
Müller, M .
ALIMENTARY PHARMACOLOGY & THERAPEUTICS, 2006, 23 (01) :137-144
[10]
Value and advocacy in conservation biology:: Crisis discipline or discipline in crisis? [J].
Chan, Kai M. A. .
CONSERVATION BIOLOGY, 2008, 22 (01) :1-3