Abstract:
Colorectal cancer as the common malignant tumor in digestive tract is seriously
threatening the health of human beings. With the development of medicine, current
treatment for colorectal cancer has gradually diversified. Targeted therapy is a kind
of therapy that combines therapy drug with drug carrier system, delivering the drug to
specific target organs to play the curative effect under the function of specificoriented
mechanism. Capecitabine is an orally-administered chemotherapeutic agent
used in the treatment of numerous cancers. It has been used in the treatment of
colorectal, breast, gastric and oespphageal cancer. The purpose of present
investigation was to develop colon targeting tablet of capecitabine for colorectal cancer
targeting. Capecitabine is anti-metabolite which enzymatically convert to 5-
flurouracil by two step in present of enzyme cytidine deaminase and thymidine
phosphorylase. Fourier transform infrared spectroscopy (FTIR) and Differential
scanning calorimetry had employed to study drug-excipients incompatibility.
Capecitabine colon targeted tablets were prepared using wet granulation method.
Optimization of formulation was done by 32 full factorial design using Design Expert
software. The pre-formulation study shows that neither drug nor any excipients interact
with each other. Different pre-compression and post compression parameters had been carried out to optimize the formulation. In-Vitro drug dissolution and bio-relevant drug
dissolution study were carried out which shows 98.835 ±0.390% and 97.650±0.652%
after 345 min. drug release at colonic pH. Bio-relevant drug dissolution study was
carried out for comparison with marketed product which demonstrates that colon
targeting tablet had good drug dissolution compared to marketed product. Stability
study shows Colon targeted capecitabine tablet was stable at accelerated condition. The
present study demonstrated that Colon targeted capecitabine tablet is suitable for colon
targeting drug delivery and had great potential for targeting colorectal cancer.
