<p>a drug delivery system based on <b>k</b>anemite/carvedilo (Ka/CV) composite for sustained release of carvedilol (CV) has been constructed by protonation, intercalation, and ionic exchange process. Structure and compositional analyses revealed that the initial Na-kanemite (Na-Ka) was an orthorhombic structure with chemical formula of NaHSi<sub>2</sub>O<sub>4</sub>(OH)<sub>2</sub>·2.52H<sub>2</sub>O. When the Na-Ka was protonated with HCl solution, the yielding H-kanemite (H-Ka) was also an orthorhombic structure with chemical formula of be H<sub>2</sub>Si<sub>2</sub>O<sub>4</sub>(OH)<sub>2</sub>·0.60H<sub>2</sub>O. After the H-Ka was reacted with tetrabutylammonium hydroxide (TBAOH) solution, a colloid suspension consisting of TBA<sup>+</sup> and Ka (TBA-Ka) formed, and the TBA-Ka sediment exhibited amorphous state. Further, while the TBA-Ka colloid suspension was reacted with carvedilo hydrochloride solution, the Ka/CV composite formed, and its chemical formula was estimated to be H<sub>1.08</sub>[(C<sub>24</sub>H<sub>27</sub>N<sub>2</sub>O<sub>4</sub>)<sup>+</sup><sub>0.92</sub>]·Si<sub>2</sub>O<sub>4</sub>(OH)<sub>2</sub>·6.70H<sub>2</sub>O. The loading capacity of Ka/CV for CV was about 57.60%. Drug release revealed that the Ka/CV composite showed extremely slow and sustained release of CV in phosphate buffer solution (PBS, pH = 7.40), and the releasing percentages of CV were 4.09, 5.81, 7.06, 7.62, and 7.64% after 6, 12, 24, 48, and 96&#xa0;h, respectively. This extremely slow and sustained release of CV may be important in maintaining effective drug concentrations in the bloodstream with a single administration, thereby enhancing therapeutic efficacy and improving drug availability.</p>

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A novel drug delivery system based on kaemite/carvedilol composite for sustained release of carvedilol

  • Yu Zhong,
  • Hao Yang,
  • Wanyun Feng,
  • Fang Guo,
  • Xiaoqiang Shang,
  • Yufeng Chen

摘要

a drug delivery system based on kanemite/carvedilo (Ka/CV) composite for sustained release of carvedilol (CV) has been constructed by protonation, intercalation, and ionic exchange process. Structure and compositional analyses revealed that the initial Na-kanemite (Na-Ka) was an orthorhombic structure with chemical formula of NaHSi2O4(OH)2·2.52H2O. When the Na-Ka was protonated with HCl solution, the yielding H-kanemite (H-Ka) was also an orthorhombic structure with chemical formula of be H2Si2O4(OH)2·0.60H2O. After the H-Ka was reacted with tetrabutylammonium hydroxide (TBAOH) solution, a colloid suspension consisting of TBA+ and Ka (TBA-Ka) formed, and the TBA-Ka sediment exhibited amorphous state. Further, while the TBA-Ka colloid suspension was reacted with carvedilo hydrochloride solution, the Ka/CV composite formed, and its chemical formula was estimated to be H1.08[(C24H27N2O4)+0.92]·Si2O4(OH)2·6.70H2O. The loading capacity of Ka/CV for CV was about 57.60%. Drug release revealed that the Ka/CV composite showed extremely slow and sustained release of CV in phosphate buffer solution (PBS, pH = 7.40), and the releasing percentages of CV were 4.09, 5.81, 7.06, 7.62, and 7.64% after 6, 12, 24, 48, and 96 h, respectively. This extremely slow and sustained release of CV may be important in maintaining effective drug concentrations in the bloodstream with a single administration, thereby enhancing therapeutic efficacy and improving drug availability.