Standard

Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes. / Kong, Ruiping; Zhu, Xingyi; Meteleva, Elizaveta S. и др.

в: International Journal of Pharmaceutics, Том 534, № 1-2, 20.12.2017, стр. 108-118.

Результаты исследований: Научные публикации в периодических изданияхстатьяРецензирование

Harvard

Kong, R, Zhu, X, Meteleva, ES, Chistyachenko, YS, Suntsova, LP, Polyakov, NE, Khvostov, MV, Baev, DS, Tolstikova, TG, Yu, J, Dushkin, AV & Su, W 2017, 'Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes', International Journal of Pharmaceutics, Том. 534, № 1-2, стр. 108-118. https://doi.org/10.1016/j.ijpharm.2017.10.011

APA

Kong, R., Zhu, X., Meteleva, E. S., Chistyachenko, Y. S., Suntsova, L. P., Polyakov, N. E., Khvostov, M. V., Baev, D. S., Tolstikova, T. G., Yu, J., Dushkin, A. V., & Su, W. (2017). Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes. International Journal of Pharmaceutics, 534(1-2), 108-118. https://doi.org/10.1016/j.ijpharm.2017.10.011

Vancouver

Kong R, Zhu X, Meteleva ES, Chistyachenko YS, Suntsova LP, Polyakov NE и др. Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes. International Journal of Pharmaceutics. 2017 дек. 20;534(1-2):108-118. doi: 10.1016/j.ijpharm.2017.10.011

Author

Kong, Ruiping ; Zhu, Xingyi ; Meteleva, Elizaveta S. и др. / Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes. в: International Journal of Pharmaceutics. 2017 ; Том 534, № 1-2. стр. 108-118.

BibTeX

@article{219329e81bd34ed3a00197d8f2ee2ae9,
title = "Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes",
abstract = "In the present work, complexes of simvastatin (SIM) with polysaccharide arabinogalactan (AG) or disodium salt of glycyrrhizin acid (Na2GA) have been prepared using mechanochemical technique to improve the solubility of SIM and enhance its oral bioavailability. The interactions of SIM with AG or Na2GA were investigated by FTIR, DSC, XRD and SEM. Self-association of SIM in various solvents was investigated by UV/Vis and NMR techniques. The molecular masses of supramolecular systems–inclusion complexes and micelles, which are the “hosts” for SIM molecules were measured. The parallel artificial membrane permeability assay (PAMPA) revealed a strong increasing of SIM permeability in the presence of Na2GA in comparison with pure SIM used as a control. On the other hand, the rapid storage assay (+40 °C for 3 months) showed that the chemical stability of SIM/AG complexes was similar to pure SIM, but SIM/Na2GA complexes had an enhanced stability. Pharmacokinetic tests in vivo on laboratory animals showed a significant increase in SIM's bioavailability after its introduction as a complex with Na2GA or AG. Moreover, SIM/AG inclusion complex performed better than SIM in reducing total cholesterol level. Therefore, the mechanochemically synthesized complexes of SIM with AG or Na2GA might have a promising future as novel formulations for hyper-cholesterolemia treatment.",
keywords = "Mechanochemistry, Pharmacokinetics, Simvastatin, Solubility, Supramolecular complexes, DRUG-DELIVERY-SYSTEM, PERMEABILITY, SOLUBLE INTERMOLECULAR COMPLEXES, GLYCYRRHIZIC ACID, SOLID DISPERSIONS, BETA-CYCLODEXTRIN, ARTIFICIAL MEMBRANE, DISSOLUTION RATE, POLYSACCHARIDE ARABINOGALACTAN, INCLUSION COMPLEX, Glycyrrhizic Acid/chemistry, Biological Availability, Male, Drug Carriers/chemistry, Micelles, Galactans/chemistry, Administration, Oral, Solvents/chemistry, Simvastatin/chemistry, Polysaccharides/chemistry, Permeability/drug effects, Animals, Solubility/drug effects, Mice",
author = "Ruiping Kong and Xingyi Zhu and Meteleva, {Elizaveta S.} and Chistyachenko, {Yulia S.} and Suntsova, {Lyubov P.} and Polyakov, {Nikolay E.} and Khvostov, {Mikhail V.} and Baev, {Dmitry S.} and Tolstikova, {Tatjana G.} and Jianming Yu and Dushkin, {Alexander V.} and Weike Su",
note = "Copyright {\textcopyright} 2017 Elsevier B.V. All rights reserved.",
year = "2017",
month = dec,
day = "20",
doi = "10.1016/j.ijpharm.2017.10.011",
language = "English",
volume = "534",
pages = "108--118",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

RIS

TY - JOUR

T1 - Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes

AU - Kong, Ruiping

AU - Zhu, Xingyi

AU - Meteleva, Elizaveta S.

AU - Chistyachenko, Yulia S.

AU - Suntsova, Lyubov P.

AU - Polyakov, Nikolay E.

AU - Khvostov, Mikhail V.

AU - Baev, Dmitry S.

AU - Tolstikova, Tatjana G.

AU - Yu, Jianming

AU - Dushkin, Alexander V.

AU - Su, Weike

N1 - Copyright © 2017 Elsevier B.V. All rights reserved.

PY - 2017/12/20

Y1 - 2017/12/20

N2 - In the present work, complexes of simvastatin (SIM) with polysaccharide arabinogalactan (AG) or disodium salt of glycyrrhizin acid (Na2GA) have been prepared using mechanochemical technique to improve the solubility of SIM and enhance its oral bioavailability. The interactions of SIM with AG or Na2GA were investigated by FTIR, DSC, XRD and SEM. Self-association of SIM in various solvents was investigated by UV/Vis and NMR techniques. The molecular masses of supramolecular systems–inclusion complexes and micelles, which are the “hosts” for SIM molecules were measured. The parallel artificial membrane permeability assay (PAMPA) revealed a strong increasing of SIM permeability in the presence of Na2GA in comparison with pure SIM used as a control. On the other hand, the rapid storage assay (+40 °C for 3 months) showed that the chemical stability of SIM/AG complexes was similar to pure SIM, but SIM/Na2GA complexes had an enhanced stability. Pharmacokinetic tests in vivo on laboratory animals showed a significant increase in SIM's bioavailability after its introduction as a complex with Na2GA or AG. Moreover, SIM/AG inclusion complex performed better than SIM in reducing total cholesterol level. Therefore, the mechanochemically synthesized complexes of SIM with AG or Na2GA might have a promising future as novel formulations for hyper-cholesterolemia treatment.

AB - In the present work, complexes of simvastatin (SIM) with polysaccharide arabinogalactan (AG) or disodium salt of glycyrrhizin acid (Na2GA) have been prepared using mechanochemical technique to improve the solubility of SIM and enhance its oral bioavailability. The interactions of SIM with AG or Na2GA were investigated by FTIR, DSC, XRD and SEM. Self-association of SIM in various solvents was investigated by UV/Vis and NMR techniques. The molecular masses of supramolecular systems–inclusion complexes and micelles, which are the “hosts” for SIM molecules were measured. The parallel artificial membrane permeability assay (PAMPA) revealed a strong increasing of SIM permeability in the presence of Na2GA in comparison with pure SIM used as a control. On the other hand, the rapid storage assay (+40 °C for 3 months) showed that the chemical stability of SIM/AG complexes was similar to pure SIM, but SIM/Na2GA complexes had an enhanced stability. Pharmacokinetic tests in vivo on laboratory animals showed a significant increase in SIM's bioavailability after its introduction as a complex with Na2GA or AG. Moreover, SIM/AG inclusion complex performed better than SIM in reducing total cholesterol level. Therefore, the mechanochemically synthesized complexes of SIM with AG or Na2GA might have a promising future as novel formulations for hyper-cholesterolemia treatment.

KW - Mechanochemistry

KW - Pharmacokinetics

KW - Simvastatin

KW - Solubility

KW - Supramolecular complexes

KW - DRUG-DELIVERY-SYSTEM

KW - PERMEABILITY

KW - SOLUBLE INTERMOLECULAR COMPLEXES

KW - GLYCYRRHIZIC ACID

KW - SOLID DISPERSIONS

KW - BETA-CYCLODEXTRIN

KW - ARTIFICIAL MEMBRANE

KW - DISSOLUTION RATE

KW - POLYSACCHARIDE ARABINOGALACTAN

KW - INCLUSION COMPLEX

KW - Glycyrrhizic Acid/chemistry

KW - Biological Availability

KW - Male

KW - Drug Carriers/chemistry

KW - Micelles

KW - Galactans/chemistry

KW - Administration, Oral

KW - Solvents/chemistry

KW - Simvastatin/chemistry

KW - Polysaccharides/chemistry

KW - Permeability/drug effects

KW - Animals

KW - Solubility/drug effects

KW - Mice

UR - http://www.scopus.com/inward/record.url?scp=85031112386&partnerID=8YFLogxK

U2 - 10.1016/j.ijpharm.2017.10.011

DO - 10.1016/j.ijpharm.2017.10.011

M3 - Article

C2 - 28993167

AN - SCOPUS:85031112386

VL - 534

SP - 108

EP - 118

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -

ID: 9429088