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. 2018 Mar;13(2):120-130.
doi: 10.1016/j.ajps.2017.10.003. Epub 2017 Oct 26.

Two kinds of ketoprofen enteric gel beads (CA and CS-SA) using biopolymer alginate

Bingchao Cheng  1 , Dongyang Li  1 , Qiye Huo  1 , Qianqian Zhao  1 , Qi Lan  1 , Mengsuo Cui  1 , Weisan Pan  1 , Xinggang Yang  1   2
Affiliations

Two kinds of ketoprofen enteric gel beads (CA and CS-SA) using biopolymer alginate

Bingchao Cheng et al. Asian J Pharm Sci. 2018 Mar.

Abstract

To obtain expected rapid-release and sustained-release of ketoprofen gel beads, this paper adopted biopolymer alginate to prepare alginate beads and chitosan-alginate gel beads. Formulation factors were investigated and optimized by the single factor test. The release of ketoprofen from calcium alginate gel beads in pH 1.0 hydrochloric acid solution was less than 10% during 2 h, then in pH6.8 was about 95% during 45 min, which met the requirements of rapid-release preparations. However, the drug release of chitosan-alginate gel beads in pH1.0 was less than 5% during 2 h, then in pH6.8 was about 50% during 6 h and reached more than 95% during 12 h, which had a good sustained-release behavior. In addition, the release kinetics of keteprofen from the calcium alginate gel beads fitted well with the Korsmeyer-Peppas model and followed a case-II transport mechanism. However, the release of keteprofen from the chitosan-alginate gel beads exhibited a non-Fickian mechanism and based on the mixed mechanisms of diffusion and polymer relaxation from chitosan-alginate beads. In a word, alginate gel beads of ketoprofen were instant analgesic, while chitosan-alginate gel beads could control the release of ketoprofen during gastro-intestinal tract and prolong the drug's action time.

Keywords: Enteric rapid-release; Enteric sustained-release; Gel beads; Ketoprofen.

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Figures

Unlabelled image
Graphical abstract
Fig. 1
Fig. 1
Influence on release from CS-SA beads in the artificial gastric and intestinal juice: (A) molecular weights of SA, (B) concentrations of SA, (C) the ratio of the SA:drug, (D) the concentrations of CaCl2 and (E) the concentrations of CS.
Fig. 2
Fig. 2
Scanning electron micrographs of (A) the SA gel beads and (B) the CS-SA gel beads, the scale bar was 0.25 mm and 50 μm, respectively.
Fig. 3
Fig. 3
The swelling ration of (A) CA gel beads and (B) CS-SA gel beads in different mediums.
Fig. 4
Fig. 4
The release profile of Ketoprofen from (A) CA gel beads and (B) CS-SA gel beads in different media.
Fig. 5
Fig. 5
The release profile of CA and CS-SA gel beads in the artificial gastric and intestinal juice.
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