Nano-structural lipid carrier pharmaceutical composition and preparation method thereof

A technology of nanostructured lipids and compositions, applied in drug combinations, liposome delivery, pharmaceutical formulations, etc.

Inactive Publication Date: 2016-06-29
金银秀 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it is a conventional technical means to make a drug into a nanostructured lipid carrier, due to the nature of the drug itself and the characteristics of the pharmaceutical composition, it does not mean that the corresponding preparation can be obtained by directly replacing the active drug, but it needs to be paid. creative work

Method used

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  • Nano-structural lipid carrier pharmaceutical composition and preparation method thereof
  • Nano-structural lipid carrier pharmaceutical composition and preparation method thereof
  • Nano-structural lipid carrier pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0131] Embodiment 1 Preparation of bezafibrate nanostructured lipid carrier

[0132] Composition formula

[0133] Bezafibrate: 0.05g; solid lipid material glyceryl monostearate: 0.5g; liquid lipid material soybean oil: 10g; fat-soluble emulsifier lecithin: 10g; water-soluble emulsifier Poloxamer 188: 15g; distilled water: 65g.

[0134] The specific preparation method of the above-mentioned bezafibrate nanostructured lipid carrier is as follows:

[0135] Weigh the raw materials according to the weight ratio of the above components, add 10g of fat-soluble emulsifier lecithin and 15g of water-soluble emulsifier Poloxamer-188 into distilled water, heat in a water bath at 65°C and stir evenly to obtain a water phase.

[0136] Heat 0.5g of solid lipid material glyceryl monostearate and 10g of liquid lipid material soybean oil in a 65°C water bath and stir to obtain a liquid oil phase, then add 0.05g of bezafibrate into the liquid oil phase and heat to completely dissolved;

[01...

Embodiment 2

[0138] Preparation of Example 2 Bezafibrate Nanostructured Lipid Carrier

[0139] Composition formula

[0140] Bezafibrate: 0.05g; solid lipid material glyceryl monostearate: 0.3g; liquid lipid material soybean oil: 1g; fat-soluble emulsifier lecithin: 1g; water-soluble emulsifier Poloxamer 188: 1.5g; Phosphate buffer solution with a pH of 7.4 and a concentration of 50mmol / L: 46g.

[0141] The specific preparation method of the above-mentioned bezafibrate nanostructured lipid carrier is as follows:

[0142] Weigh the raw materials according to the weight ratio of the above components, add 1g of fat-soluble emulsifier lecithin and 1.5g of water-soluble emulsifier Poloxamer-188 into phosphate buffer, heat in a water bath at 65°C and stir evenly to obtain a water phase .

[0143] Heat 0.3g of solid lipid material glyceryl monostearate and 1g of liquid lipid material soybean oil in a 65°C water bath and stir evenly to obtain a liquid oil phase, then add 0.05g of bezafibrate int...

Embodiment 3

[0145] Example 3 Preparation of Bezafibrate Nanostructured Lipid Carrier

[0146] Composition formula

[0147] Bezafibrate: 0.1g; solid lipid material glyceryl monostearate: 1g; liquid lipid material soybean oil: 1g; fat-soluble emulsifier lecithin: 1g; water-soluble emulsifier Poloxamer 188: 3g ; Water for injection: 44g.

[0148] The specific preparation method of the above-mentioned bezafibrate nanostructured lipid carrier is as follows:

[0149] Weigh the raw materials according to the weight ratio of the above components, add 1g of fat-soluble emulsifier lecithin and 3g of water-soluble emulsifier poloxamer-188 into water for injection, heat in a water bath at 65°C and stir evenly to obtain a water phase.

[0150] Heat 1g of the solid lipid material glyceryl monostearate and 1g of the liquid lipid material soybean oil in a 65°C water bath and stir evenly to obtain a liquid oil phase, then add 0.1g of bezafibrate into the liquid oil phase, and heat until completely diss...

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Abstract

The invention discloses a nano-structural lipid carrier pharmaceutical composition and a preparation method thereof. The pharmaceutical composition consists of the following components in percentage by weight: 0.02-1% of an insoluble drug, 0.3-15% of a solid-state lipid material, 0.5-20% of a liquid-state liquid material, 0.8-10% of a fat-soluble emulsifier, 1-15% of a water-soluble emulsifier and 39-97.38% of an aqueous solvent. The nano-structural lipid carrier pharmaceutical composition prepared by the invention can greatly overcome the shortcomings of the insoluble drug which is not easy to dissolve in water, low in oral bioavailability and the like. The preparation method is simple and controllable, good in repeatability, and an available drug delivery system is provided for the insoluble drug.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a nanostructured lipid carrier pharmaceutical composition and a preparation method and application thereof. Background technique [0002] Because of poor water solubility and extremely low dissolution rate of poorly soluble drugs, when administered orally, the active ingredients of ordinary preparations containing poorly soluble drugs are not easy to wet and diffuse in water. The oral dosage form prepared by the dispersion system is easy to crystallize or precipitate out in the gastrointestinal fluid and cannot be dissolved, which greatly affects the dissolution and absorption of the drug. Due to the defects of poor water solubility, important medicines often cannot fully exert their curative effect. It is estimated that there are about 65 billion US dollars of drugs in the world each year due to poor bioavailability, which causes a serious imbala...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/19A61K47/44A61K31/192A61K31/55A61P3/06A61P9/10
CPCA61K9/1277A61K9/19A61K31/192A61K31/55A61K47/44
Inventor 金银秀王玉新陶雪芬石雷沈佩佩夏念友
Owner 金银秀
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