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Artificial chylomicron containing medicine carrying compound as well as preparation method and application thereof

A composition, artificial technology, applied in the direction of drug combination, pharmaceutical formula, medical preparations of inactive ingredients, etc., can solve the problems of lack of stability and targeting, poor stability, short retention time, etc., to increase passive The effect of targeting function and ensuring stability

Active Publication Date: 2015-04-22
XIAN LIBANG ZHAOXIN BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, from the comparison of the main chemical components of chyle and fat emulsion, it can be seen that the fat emulsion does not use the cholesterol that maintains the rigidity of the milk droplet and the membrane protein that protects the chyle from being cleared prematurely in the blood, making the stability of the fat emulsion and The transport mechanism in the blood is very different from that of real chyle, for example, chyle generally contains 0.8% by weight of cholesterol and 2.0% by weight of membrane protein
Therefore, this fat emulsion only plays the role of dissolving oil-soluble drugs, and does not have the same stability and targeting as chyle, so it cannot be regarded as an advanced targeting agent in the true sense.
[0007] In addition, other fat emulsion preparations are generally less stable, and are easily cleared from the circulation in the body by liver and spleen macrophages, so their retention time in the blood is shorter

Method used

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  • Artificial chylomicron containing medicine carrying compound as well as preparation method and application thereof
  • Artificial chylomicron containing medicine carrying compound as well as preparation method and application thereof
  • Artificial chylomicron containing medicine carrying compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Prescription of artificial chylodrug-loaded composition:

[0066]

[0067] The preparation method is as follows: take 10.0g soybean oil, add 9.5g lecithin, 1.0g cholesterol, 0.5g sodium oleate, 2.5g polyethylene glycol-phospholipid (PEG2000-DSPE), and heat to 75 ℃, stir for about 20 minutes to fully dissolve the various compounds added, then add 5ml vitamin E, dissolve and mix well. Another 800ml of water for injection was taken, and 22g of glycerol was added. Under the protection of nitrogen, the oil solution was added into the aqueous glycerin solution under the condition of shearing and stirring to prepare colostrum, and the total amount was adjusted to 1000ml. The high-pressure homogenizer is used for homogenization 5-15 times, the homogenization pressure is about 100MPa, the pH is adjusted to 6.0-8.0, filtered, sub-packaged, nitrogen gas is introduced, and sealed. Sterilize at 115°C for 30 minutes (or at 121°C for 15 minutes). After passing the light inspectio...

Embodiment 2

[0069] Prescription of artificial chylodrug-loaded composition:

[0070]

[0071] Its preparation method is: take olive oil 100.0g, add 9.5g lecithin, 1.0g cholesterol, 0.5g sodium oleate, 2.5g polyethylene glycol-phospholipid (PEG2000-DSPE), under the condition of nitrogen protection, heat to At 75°C, stir for about 20 minutes to fully dissolve the various compounds added, then add 5ml vitamin E, dissolve and mix well. Another 800ml of water for injection was taken, and 22g of glycerol was added. Under the condition of nitrogen protection, the oil solution was added into the glycerin aqueous solution under the condition of shearing and stirring to prepare colostrum, and the total amount was adjusted to 1000ml. The high-pressure homogenizer homogenizes for 5-8 times, the homogenization pressure is about 100MPa, adjusts the pH to 7.0-8.0, filters, subpackages, injects nitrogen, and seals. Rotate sterilization at 115°C for 30 minutes. After passing the light inspection, det...

Embodiment 3

[0073] Prescription of artificial chylodrug-loaded composition:

[0074]

[0075] Its preparation method is: take fish oil 100.0g, add 9.5g lecithin, 1.0g cholesterol, 0.5g sodium oleate, 2.5g polyethylene glycol-phospholipid (PEG2000-DSPE), under the condition of nitrogen protection, heat to 75 ℃, stir for about 20 minutes to fully dissolve the various compounds added, then add 5ml vitamin E, dissolve and mix well. Another 800ml of water for injection was taken, and 22g of glycerol was added. Under the condition of nitrogen protection, the oil solution was added into the glycerin aqueous solution under the condition of shearing and stirring to prepare colostrum, and the total amount was adjusted to 1000ml. The high-pressure homogenizer homogenizes for 5-8 times, the homogenization pressure is about 100MPa, adjusts the pH to 7.2-8.5, filters, packs, injects nitrogen, and seals. Sterilize at 115°C for 30 minutes. After passing the light inspection, test the fish oil conten...

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Abstract

The invention relates to a novel drug carrying and delivering system and particularly relate to a formula and a preparation method of an artificial chylomicron containing medicine carrying compound. The artificial chylomicron is prepared from the following main components: an animal oil, a vegetable oil, an oily medicine or an oil-soluble medicine, phospholipid which serves as an emulsifier, cholesterol or steroid which serves as a stabilizer, a shape control agent or a biological modifier, oleic acid or an oleate which serves a stabilizer or a co-emulsifier, fatty monoglyceride and fatty diglyceride which serve as co-emulsifiers, polyethylene glycol phospholipid derivatives (artificial chylomicron membrane protein substitutes) which serve as stabilizers and emulsifiers and are used for prolonging the half-life period of artificial chylomicron in blood, vitamin E which serves as an anti-oxidant; (8) a complex which serves as a controlling metal ion and glycerol or a carbohydrate for regulating the isotonicity of a medicinal preparation.

Description

technical field [0001] The present invention relates to an artificial chyle drug-loaded composition, and also relates to the formula, preparation process and application of the artificial chyle drug-loaded composition. Through pharmacokinetics, pharmacodynamics research and safety evaluation, the artificial chyle drug-loaded composition The drug is suitable for intravenous injection or intramuscular injection, and belongs to the technical field of medicine. Background technique [0002] Chyle, also known as chylomicrons (Chylomicron, English abbreviated as CM), mainly contains exogenous triglycerides, which is the main way for the body to absorb and transport exogenous triglycerides and cholesterol. Chyle is a huge lipoprotein rich in exogenous triglycerides synthesized by intestinal wall cells after eating high-fat food, and its particle size is 80-500nm. After 12 hours after eating, there is almost no chyle in the blood of normal people. Chyle is the main channel and tra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K47/24A61K47/28A61P3/02
Inventor 陈涛马玉樊王汝涛王惟娇
Owner XIAN LIBANG ZHAOXIN BIOTECH CO LTD
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