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Lipid carrier, indissolvable pharmaceutical composition and preparation method thereof

A technology for insoluble drugs and lipid carriers, which is used in pharmaceutical formulations, medical preparations containing active ingredients, and emulsion delivery, etc., can solve problems such as instability of lipid carriers, avoid drug precipitation, and increase dissolution specific surface area. , promotes the effect of entering the lymphatic system

Inactive Publication Date: 2014-06-25
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is a common problem with lipid carriers during oral administration: lipid carriers are unstable in the small intestine
[0006] At present, there are many reports about lipid carriers improving the oral bioavailability of poorly soluble drugs through solubilization, but there is no report about the method of controlling lipase hydrolysis to improve bioavailability

Method used

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  • Lipid carrier, indissolvable pharmaceutical composition and preparation method thereof
  • Lipid carrier, indissolvable pharmaceutical composition and preparation method thereof
  • Lipid carrier, indissolvable pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Preparation of self-microemulsion insoluble pharmaceutical composition

[0040] Weigh 4g of medium-chain fatty acid glyceride (MCT), 404g of Cermophor CO and 2g of 1,2-propanediol, mix well, stir at room temperature for 3h, and obtain microemulsion. Take 30 mg of hydroxymecoumarin, add it to the above self-microemulsion, and stir it magnetically for 2 hours to obtain the insoluble pharmaceutical composition of self-microemulsion

[0041] The compound has no obvious layering phenomenon after standing for half a year at room temperature. It is diluted 20-1000 times with deionized water, and the particle size is measured by a laser particle size analyzer. The particle size distribution is as follows: figure 1 As shown, the average particle size is 54nm.

Embodiment 2

[0042] Embodiment 2: Preparation of self-microemulsion insoluble pharmaceutical composition

[0043] Weigh 6g of C8-C10 medium-chain fatty acid glycerides (MCT), 2.67g of Cermophor CO40, 1.33g of 1,2-propanediol and 30mg of hymecoumarin, mix well, and stir at room temperature for 3h, which is obtained from microemulsion insoluble pharmaceutical composition. After the complex was diluted 100 times, its particle size was 129nm.

Embodiment 3

[0044] Embodiment 3: Preparation of self-microemulsion insoluble pharmaceutical composition

[0045]Weigh 4g of ethyl oleate, 404g of Cermophor CO and 2g of 1,2-propanediol, mix well, stir at room temperature for 3h, and obtain microemulsion. Take 30 mg of resveratrol, add it into the self-microemulsion, and stir it magnetically for 2 hours to obtain the insoluble pharmaceutical composition from the microemulsion.

[0046] After the complex was diluted 100 times, its particle size was 59nm.

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Abstract

The invention provides a lipid carrier, an indissolvable pharmaceutical composition and a preparation method thereof. The composition includes a self-microemulsion indissolvable pharmaceutical composition and a composition composed of a solid lipid nanoparticle carrier and an indissolvable pharmaceutical. The self-microemulsion indissolvable pharmaceutical composition comprises, by weight, 0.05%-10% of an indissolvable pharmaceutical, 5%-60% of a liquid lipid, 20%-50% of a surfactant and 10%-35% of a cosurfactant; the composition composed of a solid lipid nanoparticle carrier and an indissolvable pharmaceutical comprises, by weight, 0.05%-5% of the indissolvable pharmaceutical, 40%-60% of a solid lipid and 30%-59% of the surfactant. By changing the type and the proportion of the lipid in the composition composed of a solid lipid nanoparticle carrier and an indissolvable pharmaceutical, the degree of hydrolysis can be controlled between 3%-90%, wherein the hydrolysis is carried out with a lipase. Because that the releasing rate of the indissolvable pharmaceutical in the lipid carrier is related to the hydrolysis of the lipid carrier, the purpose of changing the pharmacokinetics of the indissolvable pharmaceutical is achieved by controlling the hydrolysis rate of the lipid carrier.

Description

technical field [0001] The invention relates to a lipid carrier and an insoluble pharmaceutical composition and a preparation method thereof, in particular to the preparation of a lipase hydrolyzed controllable lipid carrier and its application in drug release. Background technique [0002] Drug solubility is an important factor affecting drug bioavailability. Many drugs have low oral bioavailability due to poor solubility and difficulty in absorption, which greatly limits their application. With the application of computer-aided drug design and high-throughput screening, the obtained new active drugs are often insoluble in water, which limits the possibility of their development as new drugs to a certain extent. According to reports, more than 40% of new active drugs have many problems in oral bioavailability due to poor water solubility, so it is of great significance to improve the solubility and dissolution rate of poorly soluble drugs. [0003] The current solubilizat...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/107A61K45/00
Inventor 马小军张建斌吕国军于炜婷赵姗吕岩王冰汪岩
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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