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Tytuł pozycji:

[Effects of HPMCAS MF on absorption of silybin from supersaturable self-nanoemulsifying drug delivery system].

Tytuł:
[Effects of HPMCAS MF on absorption of silybin from supersaturable self-nanoemulsifying drug delivery system].
Autorzy:
Lai ZT; Key Laboratory of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Traditional Chinese Medicine Nanchang 330004,China Medical Device Testing Center of Jiangxi Provinice Nanchang 330029,China.
Ding HB; Key Laboratory of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Traditional Chinese Medicine Nanchang 330004,China.
Jiang QY; Experimental Animal Center of Traditional Chinese Medicine,Jiangxi University of Traditional Chinese Medicine Nanchang 330004,China.
Yuan QL; Key Laboratory of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Traditional Chinese Medicine Nanchang 330004,China.
Liao ZG; Key Laboratory of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Traditional Chinese Medicine Nanchang 330004,China.
Źródło:
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica [Zhongguo Zhong Yao Za Zhi] 2021 Mar; Vol. 46 (5), pp. 1120-1127.
Typ publikacji:
Journal Article
Język:
Chinese
Imprint Name(s):
Publication: Beijing : Zhongguo yao xue hui : Zhongguo Zhong yi yan jiu yuan Zhong yao yan jiu suo
Original Publication: [Beijing] : Zhongguo yao xue hui : [Zhongguo Zhong yi yan jiu yuan Zhong yao yan jiu suo, 1989-
MeSH Terms:
Drug Delivery Systems*
Nanoparticles*
Administration, Oral ; Biological Availability ; Caco-2 Cells ; Emulsions ; Humans ; Methylcellulose/analogs & derivatives ; Particle Size ; Silybin ; Solubility
Contributed Indexing:
Keywords: Caco-2 cell transport; absorption; pharmacokinetics; silybin; supersaturable self-nanoemulsifying drug delivery system
Substance Nomenclature:
0 (Emulsions)
4RKY41TBTF (Silybin)
71138-97-1 (hydroxypropylmethylcellulose acetate succinate)
9004-67-5 (Methylcellulose)
Entry Date(s):
Date Created: 20210331 Date Completed: 20210402 Latest Revision: 20210402
Update Code:
20240104
DOI:
10.19540/j.cnki.cjcmm.20201210.302
PMID:
33787105
Czasopismo naukowe
To evaluate the effects of Hydroxypropyl methylcellulose acetate succinate(HPMCAS MF) on absorption of silybin(SLB) from supersaturable self-nanoemulsifying drug delivery system which was pre-prepared at the early stage experiment. The cell toxicity of self-emulsifying preparation was evaluated by the MTT method, and the in vitro membrane permeability and absorption promoting effect of the self-emulsifying preparation were evaluated by establishing a Caco-2 cell monolayer model. The in vivo and in vitro supersaturation correlation was evaluated via the blood concentration of SLB. The results of MTT showed that the concentration of the preparation below 2 mg·mL~(-1)(C_(SLB) 100 μg·mL~(-1)) was not toxic to Caco-2 cells, and the addition of polymer had no significant effect on Caco-2 cells viability. As compared with the solution group, the transport results showed that the P_(app)(AP→BL) of the self-emulsifying preparation had a very significant increase; the transport rate of silybin can be reduced by polymer in 0-30 min; however, there was no difference in supersaturated transport between supersaturated SLB self-nanoemulsion drug delivery system(SLB-SSNEDDS) and SLB self-nanoemulsion drug delivery system(SLB-SNEDDS) within 2 hours. As compared with SLB suspension, pharmacokinetic parameters showed that the blood concentration of both SLB-SNEDDS and SLB-SSNEDDS groups were significantly increased, and C_(max) was 5.25 times and 9.69 times respectively of that in SLB suspension group, with a relative bioavailability of 578.45% and 1 139.44% respectively. C_(max) and relative bioavailability of SLB-SSNEDDS were 1.85 times and 197% of those of SLB-SNEDDS, respectively. Therefore, on the one hand, SSNEDDS can increase the solubility of SLB in gastrointestinal tract by maintaining stability of SLB supersaturation state; on the other hand, the osmotic transport process of SLB was regulated through the composition of its preparations, and both of them could jointly promote the transport and absorption of SLB to improve the oral bioavailability of SLB.

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