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Atorvastatin calcium inclusion complexation with polysaccharide arabinogalactan and saponin disodium glycyrrhizate for increasing of solubility and bioavailability.
Kong, Ruiping; Zhu, Xingyi; Meteleva, Elizaveta S; Polyakov, Nikolay E; Khvostov, Mikhail V; Baev, Dmitry S; Tolstikova, Tatjana G; Dushkin, Alexander V; Su, Weike.
Afiliação
  • Kong R; Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou, 310014, People's Republic of China.
  • Zhu X; Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou, 310014, People's Republic of China.
  • Meteleva ES; Institute of Solid State Chemistry and Mechanochemistry, SB RAS, Novosibirsk, Russia, 630128.
  • Polyakov NE; Institute of Chemical Kinetics and Combustion, SB RAS, Novosibirsk, Russia.
  • Khvostov MV; N.N. Vorozhtsov Institute of Organic Chemistry, SB RAS, Novosibirsk, Russia.
  • Baev DS; Novosibirsk State University, Novosibirsk, Russia.
  • Tolstikova TG; N.N. Vorozhtsov Institute of Organic Chemistry, SB RAS, Novosibirsk, Russia.
  • Dushkin AV; Novosibirsk State University, Novosibirsk, Russia.
  • Su W; N.N. Vorozhtsov Institute of Organic Chemistry, SB RAS, Novosibirsk, Russia.
Drug Deliv Transl Res ; 8(5): 1200-1213, 2018 10.
Article em En | MEDLINE | ID: mdl-30039497
The aim of the present investigation was to enhance the solubility and dissolution of atorvastatin calcium (ATV), a poorly water-soluble drug with larch polysaccharide arabinogalactan (AG) and disodium glycyrrhizate (Na2GA) as carriers of drug delivery systems for improving its bioavailability. The interactions of ATV with AG or Na2GA were investigated by DSC, XRD, SEM, and NMR techniques. The molecular weights of supramolecular systems-inclusion complexes and micelles-which are the hosts for ATV molecules were measured. On the other hand, the rapid storage assay (+ 40 °C for 3 months) showed that the chemical stability of ATV/AG and ATV/Na2GA complexes had been enhanced compared with pure ATV. In vitro drug release showed a significant increase in ATV's dissolution rate after formation of a complex with Na2GA or AG. Pharmacokinetic tests in vivo on laboratory animals showed a significant increase in ATV's bioavailability after its introduction as a complex with Na2GA or AG. Moreover, ATV/AG and ATV/Na2GA complexes showed a more prominent decrease of total cholesterol (TC) level compared to net ATV. Therefore, the novel mechanochemically synthesized complexes of ATV with AG or Na2GA as drug delivery systems might be potential and promising candidates for hypercholesterolemia treatment and deserved further researches.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Ácido Glicirrízico / Atorvastatina / Galactanos / Hipercolesterolemia Idioma: En Ano de publicação: 2018 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Ácido Glicirrízico / Atorvastatina / Galactanos / Hipercolesterolemia Idioma: En Ano de publicação: 2018 Tipo de documento: Article