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FORMULATION OF COLON SPECIFIC 5-FLUOROURACIL TABLETS USING NOVEL AZO CONJUGATES
FORMULATION OF COLON SPECIFIC 5-FLUOROURACIL TABLETS USING NOVEL AZO CONJUGATES
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机译:使用新型偶氮缀合物配制结肠特定的5-氟尿嘧啶片剂
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摘要
This invention explores a novel formulation process for designing 5-fluorouracil (5-FU) tablets using azo polymeric conjugates. The polymeric conjugates ofHPMC, sodium CMC, sodium alginate, guar gum and pectin with amino acids were synthesized using azo polymeric complex mechanism. The polymeric conjugates were screened for their topographic structure and presence of azo linkage was confirmed by spectral analysis. The inertness of conjugates with 5-FU was confirmed by compatibility studies. Colon specific 5- FU tablets were formulated by blending 5-FU with co-processing agents like polymeric conjugates, magnesium stearate, microcrystalline cellulose (MCC), talc and starch. Tablets were prepared by direct compression mechanism and subjected to evaluation parameters and /�- vitro release studies in rat faecal matter using simulated gastric fluid (HCI buffer pH 1.2), simulated intestinal fluid (phosphate buffer pH 7.4) and simulated colonic fluid (phosphate buffer pH 6.8 with rat faecal matter). The invention concludes that guar gum polymeric conjugate displayed a significant colon specific property both in-viiro and in-vivo. The best tablet formulation was FG2 (containing 5-FU with guar gum-phenyl alanine polymer conjugate in 1:2 ratio) with an in-vitro release of 98.25�2.19% over 24 hours. In-vivo bioavailability studies of FG2 showed the Cmax, Tmax aid AUC value 12.17 �g/ml, 8 hours and 346.96 �g.h/ml respectively. This conjugate can serve as a novel colon specific polymeric conjugate for delivering APIs to colonic region.
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