Preparation of silybin-phospholipid complex and its bioavailability in rats / 药学学报
Acta Pharmaceutica Sinica
; (12): 611-617, 2005.
Article
em Zh
| WPRIM
| ID: wpr-353464
Biblioteca responsável:
WPRO
ABSTRACT
<p><b>AIM</b>To prepare silybin-phospholipid complex and study its physicochemical properties. To compare the pharmacokinetic characteristics and bioavailability after oral administration of silybinphospholipid complex and silybin material in rats.</p><p><b>METHODS</b>Using acetone as a reaction medium, silybin and phospholipid were resolved into the medium, when the organic solvent was clear, then removed under vacuum evaporation, silybin-phospholipid complex was obtained. The new complex' s physicochemical properties including DSC, UV, IR were determined. The concentrations of non-conjugated and total silybin after oral administration of silybin-phospholipid complex and silybin material at different time in rats were determined by RP-HPLC. The pharmacokinetic parameters were computed by software program 3P97.</p><p><b>RESULTS</b>Experiment results showed that silybin and phospholipid in the silybin-phospholipid complex were combined by non-covalent-bond, not forming a new compound and the solubility of silybin-phospholipid complex in water and n-octanol was effectively enhanced. It was found that mean plasma concentration-time curve of silybin after oral administration of silybin-phospholipid complex in rats was in accordance with one-compartment model with first-order absorption. Pharmacokinetic parameters of non-conjugated and total silybin in rats were respectively T(max) 10 min and 2 h; C(max) 0.11 and 1.08 microg x mL(-1); T1/2 2.18 and 3.84 h; AUC(0-infinity) 1.71 and 12.94 microg x mL(-1) x h. However, after oral administration of silybin material, plasma levels of both non-conjugated and total silybin were within the analytical detection limit.</p><p><b>CONCLUSION</b>It was concluded that after oral administration of silybin-phospholipid complex in rats the bioavailability of silybin increased greatly. This was mainly due to an obvious improvement of the lipophilic property of silybin-phospholipid complex compared with silybin material and an increase in gastrointestinal absorption.</p>
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1
Índice:
WPRIM
Assunto principal:
Fosfolipídeos
/
Silimarina
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Solubilidade
/
Sangue
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Farmacocinética
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Disponibilidade Biológica
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Administração Oral
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Ratos Sprague-Dawley
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Área Sob a Curva
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Composição de Medicamentos
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2005
Tipo de documento:
Article