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. 2013:2013:495319.
doi: 10.1155/2013/495319. Epub 2013 Oct 29.

Preparation and characterization of a gastric floating dosage form of capecitabine

Ehsan Taghizadeh Davoudi  1 , Mohamed Ibrahim Noordin, Ali Kadivar, Behnam Kamalidehghan, Abdoreza Soleimani Farjam, Hamid Akbari Javar
Affiliations

Preparation and characterization of a gastric floating dosage form of capecitabine

Ehsan Taghizadeh Davoudi et al. Biomed Res Int. 2013.

Abstract

Gastrointestinal disturbances, such as nausea and vomiting, are considered amongst the main adverse effects associated with oral anticancer drugs due to their fast release in the gastrointestinal tract (GIT). Sustained release formulations with proper release profiles can overcome some side effects of conventional formulations. The current study was designed to prepare sustained release tablets of Capecitabine, which is approved by the Food and Drug Administration (FDA) for the treatment of advanced breast cancer, using hydroxypropyl methylcellulose (HPMC), carbomer934P, sodium alginate, and sodium bicarbonate. Tablets were prepared using the wet granulation method and characterized such that floating lag time, total floating time, hardness, friability, drug content, weight uniformity, and in vitro drug release were investigated. The sustained release tablets showed good hardness and passed the friability test. The tablets' floating lag time was determined to be 30-200 seconds, and it floated more than 24 hours and released the drug for 24 hours. Then, the stability test was done and compared with the initial samples. In conclusion, by adjusting the right ratios of the excipients including release-retarding gel-forming polymers like HPMC K4M, Na alginate, carbomer934P, and sodium bicarbonate, sustained release Capecitabine floating tablet was formulated.

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Figures

Figure 1
Figure 1
Calibration curve of Capecitabine in HCL 0.1 N.
Figure 2
Figure 2
In vitro release profiles of various Capecitabine floating formulations in 0.1 N HCl (pH 1.2) at 37 ± 0.5°C (n = 4).
Figure 3
Figure 3
The influence of carbomer934P on the release of Capecitabine from the SR tablets in 0.1 N HCl (pH 1.2) at 37 ± 0.5°C (n = 4).
Figure 4
Figure 4
The influence of HPMC K4M in F4, F7, and F10 on the release of Capecitabine from the SR tablets in 0.1 N HCl (pH 1.2) at 37 ± 0.5°C (n = 4).
Figure 5
Figure 5
The influence of Na alginate in F4, F5, and F6 on the release of Capecitabine from the SR tablets in 0.1 N HCl (pH 1.2) at 37 ± 0.5°C (n = 4).
Figure 6
Figure 6
The influence of Na alginate in F7, F8, and F9 on the release of Capecitabine from the SR tablets in 0.1 N HCl (pH 1.2) at 37 ± 0.5°C (n = 4).
Figure 7
Figure 7
Release profiles of a commercial brand of Capecitabine and F7 (n = 4).
Figure 8
Figure 8
Comparison of the release profiles of F7 and stored tablets (n = 4).
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