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Effects of high sucrose diet, gemfibrozil, and their combination on plasma paraoxonase 1 activity and lipid levels in rats

100%

Macan M., Vrkić N., Vrdoljak A. L., Radić B., Bradamante V.

2010

vol. 57

issue 3

321-326

We investigated the influence of high sucrose diet (HSD) after 3 or 5 weeks of administration on paraoxonase 1 (PON1) activity in plasma of normolipidemic rats and the relationship between serum PON1 activity, triacylglycerides (TGs), HDL and total cholesterol vs. the control group of rats fed normal, control diet (CD). Because the data about the influence of gemfibrozil (GEM) on PON1 activity are controversial, we also investigated its effects (administration in the 4th and 5th week in rats on HSD and CD) on plasma PON1 activity and lipid levels in normolipidemic rats, and in rats with hypertriglyceridemia caused by HSD. Our results obtained in rats on HSD show a significant increase of plasma TGs levels by 47% (P<0.05) after 5 weeks of treatment, and PON1 activity by 32% and 23% (P<0.05) after 3 and 5 weeks, but without change in lipid levels vs. rats on CD. In the rats on CD and HSD, GEM caused a significant decrease of PON1 activity by 44% and 33%, while a significant decrease of TGs level by 38% (P<0.05) was measured only in rats on CD. The effects of GEM on total cholesterol, HDL and LDL in both groups of rats were typical for its action on lipoprotein metabolism. Because GEM in the rat liver stimulates proliferation of peroxisomes, β oxidation, and production of H2O2, it is possible that the oxidative stress induced by GEM damages hepatocytes and lowers the synthesis of PON1.

Surface-active agents from the group of polyoxyethylated glycerol esters of fatty acids. Part IV. Equilibrium micellar solubilization of selected lipophilic therapeutic agents (BCS class II and III) in aqueous solutions of products of catalytic oxyethylation of triglyceride fractions extracted from pharmacopoeial lard (Adeps suillus PP XI) of nTE≥50

88%

Marczyński Z., Kołodziejczyk M. K., Nachajski M. J., Zgoda M. M.

Acta Poloniae Pharmaceutica - Drug Research

2019

vol. 76

issue 4

707-714

Summary: Preformulation studies were carried out to estimate the solubilization capacity of products of catalytic oxyethylation of triglyceride fractions extracted from the pharmacopoeial lard (Adeps suillus, PP XI). There were determined basic viscosity ([ɳ], Mɳ) and hydrodynamic (Ro, Robs., Ω) values of micellar solutions of oxyethylated derivatives as well as their surface activity - . Critical micellar concentration (cmc) was used to calculate the thermopotential for the formation of micelles (∆ ). Model studies on micellar solubilization of gemfibrozil, loratadine and valsartan from the solid body surface (phase boundary) were performed under equilibrium conditions at the surfactant concentration of cexp>>cmc. The amount of dissolved lipophilic therapeutic agents with qualitative and quantitative involvement of micellar solubilization was determined by spectrophotometric (UV) method - cǀsǀ (mg/100mL) as well as by calculating the solubilization indices - n|s| (mol / mol). The research study has identified structures of oxyethylated derivatives of triglyceride fractions which selectively and effectively solubilize gemfibrozil, loratadine and valsartan from the solid surface in the equilibrium system. The obtained results are a technological inspiration to create a model form of the drug (tablet) with continuous dispersion of lipophilic therapeutic agents (gemfibrozil, loratadine and valsartan), obtained on the basis of the liquefied surfactant structure. Key words: micellar solubilization, products of triglyceride fraction ethoxylation, gemfibrozil, loratadine, valsartan

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1 Acta Biochimica Polonica

1 Acta Poloniae Pharmaceutica - Drug Research

1 2019

1 2010

1 Bradamante V.

1 Kołodziejczyk M. K.

1 Macan M.

1 Marczyński Z.

1 Nachajski M. J.

1 Radić B.

1 Vrdoljak A. L.

1 Vrkić N.

1 Zgoda M. M.

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Effects of high sucrose diet, gemfibrozil, and their combination on plasma paraoxonase 1 activity and lipid levels in rats