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. 2013 Dec 13;14(12):24305-19.
doi: 10.3390/ijms141224305.

The preparation of capsaicin-chitosan microspheres (CCMS) enteric coated tablets

Jian Chen, Gui-Dong Huang, Si-Rong Tan, Jiao Guo  1 , Zheng-Quan Su  2
Affiliations

The preparation of capsaicin-chitosan microspheres (CCMS) enteric coated tablets

Jian Chen et al. Int J Mol Sci. .

Abstract

This study aimed to research the preparation and content determination of capsaicin-chitosan microspheres (CCMS) enteric coated tablets. The core tablets were prepared with the method of wet granulation. Nine formulae were designed to determine the optimal formula of the core tablet. Eudragit L100 was used to prepare the CCMS enteric-coated tablets. The effect of enteric coated formulation variables such as content of talc (10%, 25% and 40%), plasticisers (TEC and DBS), dosage of plasticiser (10%, 20% and 30%) and coating weight (2%, 3% and 5%) were evaluated for drug release characteristics. The in vitro release was studied using 0.1 N HCl and pH 6.8 phosphate buffer. Enteric coated tablets without ruptures or swelling behaviour over 2 h in 0.1 N HCl indicated that these tablets showed acid resistance. The accumulated release rate in phosphate buffer (pH 6.8) revealed that the prepared tablets were able to sustain drug release into the intestine and a first-order release was obtained for capsaicin. This research is the first report of the preparation and content determination of CCMS enteric coated tablets. The sustained release behavior of enteric coated formulations in pH 6.8 phosphate buffer demonstrated that it would be a potential drug delivery platform for sustained delivery of gastric irritant drugs.

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Figures

Figure 1.
Figure 1.
The determination curve of capsaicin equilibrium solubility. Abbreviations: S0, equilibrium solubility; A, the intersection of two lines.
Figure 2.
Figure 2.
HPLC chromatogram of specificity investigation; 1: the negative control (an enteric coated tablet without CAP); 2: standard substance of CAP; 3: sample of CAP. Abbreviations: CAP, capsaicin.
Figure 3.
Figure 3.
The dissolution property of CAP from the CCMS core tablet. Each point represents the mean ± SD. Abbreviations: CCMS, capsaicin-chitosan microspheres; CAP, capsaicin.
Figure 4.
Figure 4.
The effect of various plasticisers on the release of CAP from CCMS enteric coated tablets. Each point represents the mean ± SD. Abbreviations: TEC, triethyl citrate; DBS, dibutyl sebacate.
Figure 5.
Figure 5.
The effect of TEC dosage on the release of CAP from CCMS enteric coated tablets. Each point represents the mean ± SD. Abbreviations: TEC, triethyl citrate.
Figure 6.
Figure 6.
The effect of coating weight on the release of CAP from CCMS enteric coated tablets. Each point represents the mean ± SD.
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