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Atorvastatin calcium submicroemulsion and preparation method thereof

A technology of atorvastatin calcium and submicron emulsion, which is applied in the field of pharmacy, can solve the problems of slow dissolution rate and poor solubility, etc., and achieve the effects of stable method, good property quality and good process reproducibility

Inactive Publication Date: 2017-09-15
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because atorvastatin calcium belongs to BCS II drugs, its poor solubility makes the dissolution rate of the drug in the gastrointestinal tract slow, resulting in its absolute bioavailability of only 12%, the biological activity of HMG-CoA reductase inhibitors Utilization is only 30%

Method used

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  • Atorvastatin calcium submicroemulsion and preparation method thereof
  • Atorvastatin calcium submicroemulsion and preparation method thereof
  • Atorvastatin calcium submicroemulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The atorvastatin calcium submicron emulsion of the present embodiment includes the following components in every 100mL submicron emulsion: 0.5g atorvastatin calcium phospholipid complex, 5.0g soybean oil, 0.40g lecithin, 0.40g poloxa Mu 188, 0.20g Tween 80, 0.024g sodium oleate, 1.0g glycerol and distilled water added to 100mL, wherein the atorvastatin calcium phospholipid complex is used as a prodrug to increase the concentration of atorvastatin calcium in Solubility in soybean oil, the molar ratio of atorvastatin calcium to phospholipids is 1:1.

[0042]The steps for preparing the above atorvastatin calcium submicron emulsion are as follows: Weigh 0.5 g of atorvastatin calcium phospholipid complex and add it to 5.0 g of soybean oil as the oil phase, and heat in a water bath at 60°C. Weigh 0.40 g of lecithin, 0.40 g of poloxamer 188, 0.20 g of Tween 80, 0.024 g of sodium oleate, and 1.0 g of glycerin in an appropriate amount of distilled water at 60° C. as the water ph...

example 2

[0044] The atorvastatin calcium submicron emulsion of the present embodiment includes the following components in every 100mL submicron emulsion: 0.5g atorvastatin calcium phospholipid complex, 10.0g soybean oil, 0.67g lecithin, 0.67g poloxa Mu 188, 0.20g Tween 80, 0.024g sodium oleate, 2.0g glycerol and distilled water added to 100mL, wherein the atorvastatin calcium phospholipid complex is used as a prodrug to increase the concentration of atorvastatin calcium in Solubility in soybean oil, the molar ratio of atorvastatin calcium to phospholipids is 1:1.

[0045] The steps for preparing the above atorvastatin calcium submicron emulsion are as follows: Weigh 0.5 g of atorvastatin calcium phospholipid complex and add it to 10.0 g of soybean oil as the oil phase, and heat in a water bath at 60°C. Weigh 0.67g of lecithin, 0.67g of poloxamer 188, 0.20g of Tween 80, 0.024g of sodium oleate, and 2.0g of glycerol in an appropriate amount of distilled water at 60°C as the water phase....

example 3

[0047] The atorvastatin calcium submicron emulsion of the present embodiment includes the following components in every 100mL submicron emulsion: 0.5g atorvastatin calcium phospholipid complex, 5.0g soybean oil, 0.80g lecithin, 0.40g poloxa Mu 188, 0.20g Tween 80, 0.024g sodium oleate, 1.0g glycerol and distilled water added to 100mL, wherein the atorvastatin calcium phospholipid complex is used as a prodrug to increase the concentration of atorvastatin calcium in Solubility in soybean oil, the molar ratio of atorvastatin calcium to phospholipids is 1:1.

[0048] The steps for preparing the above atorvastatin calcium submicron emulsion are as follows: Weigh 0.5 g of atorvastatin calcium phospholipid complex and add it to 5.0 g of soybean oil as the oil phase, and heat in a water bath at 60°C. Weigh 0.80 g of lecithin, 0.40 g of poloxamer 188, 0.20 g of Tween 80, 0.024 g of sodium oleate, and 1.0 g of glycerin in an appropriate amount of distilled water at 70° C. as the water p...

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Abstract

The present invention provides an atorvastatin calcium submicroemulsion and a preparation method thereof. The atorvastatin calcium submicroemulsion comprises atorvastatin calcium (phospholipid complex form), an oil phase solvent, an emulsifier, a stabilizer, a potential modifier, glycerol and water, wherein the atorvastatin calcium phospholipid complex is used as a precursor drug so as to increase the solubility of atorvastatin calcium in the oil phase, and a molar ratio of atorvastatin calcium to the phospholipid is 1:1. According to the present invention, the drug-containing phospholipid complex is adopted as the precursor drug of atorvastatin calcium, such that the solubility and the stability of the drug in the oil phase are improved, the drug loading is increased, and the use of the high-concentration organic solvent can be avoided; and compared to the commercially available lipitor (atorvastatin calcium tablet), the atorvastatin calcium submicroemulsion of the present invention has the following characteristics that the absorption of the drug in the small intestine is improved, and the high blood drug level is provided and is maintained for a long time after the atorvastatin calcium submicroemulsion is orally taken so as to effectively improve the bioavailability of the drug.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to an atorvastatin calcium submicron emulsion and a preparation method thereof. Background technique [0002] Atorvastatin calcium (Atorvastatin calcium, ATC) is a classic third-generation statin lipid-lowering drug. Atorvastatin calcium can inhibit the biosynthesis of cholesterol and HMG-CoA reductase in the liver, thereby reducing the serum lipoprotein concentration and plasma cholesterol concentration, and can also increase the hepatic low-density lipoprotein (LDL) receptor on the cell surface The body increases the uptake and catabolism of LDL to reduce the production of LDL. Atorvastatin calcium can reduce plasma total cholesterol, apolipoprotein, triglyceride and LDL cholesterol levels in patients with lipid metabolism defects, and it can significantly alleviate familial hypercholesterolemia caused by homozygotes and heterozygotes syndrome and non-familial cholesterolemia. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/24A61K31/40A61P3/06
CPCA61K9/1075A61K9/0053A61K31/40A61K47/24
Inventor 秦凌浩牛亚伟董晓婷赵嘉兰王悦敏
Owner GUANGDONG PHARMA UNIV
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