Drug delivery system and preparation method thereof

A drug delivery system and protein technology, which can be used in pharmaceutical formulations, medical formulations without active ingredients, and medical formulations containing active ingredients, etc. Can not identify caveolin and other problems

Inactive Publication Date: 2009-07-22
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Although liposome has its outstanding advantages, there are also some unresolved problems: as (1) the stability of liposome drug is not high; (2) liposome encapsulation efficiency and drug loading are low, for A kind of specific medicine will prepare a kind of comparatively desirable liposome, usually all will do a large amount of screening work; (3) the medicine that is suitable for liposome is also limited; (4) generally will use a large amount of liposomes in the preparation process Toxic solvent; (5) Ordinary liposomes are mainly concentrated in organs rich in reticuloendothelial cells, and cannot recognize caveolin on vascular endothelium
[0011] In addition, the side effects that exist during the administration process mainly include venous irritation, phlebitis, pain, bone marrow suppression, neurotoxicity, allergies, inflammation, skin irritation, etc., which are important issues that must be considered when researching and developing new drug delivery systems. question

Method used

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  • Drug delivery system and preparation method thereof
  • Drug delivery system and preparation method thereof
  • Drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] Example 1 Problems in the preparation of cucurbitacin HSA nanoparticles by probe ultrasonic method

[0093] Cucurbitacin B 0.01g

[0094] HSA 4g

[0095] Appropriate amount of water

[0096] Dissolve cucurbitacin B (purity greater than 98%) in 1 ml of ethanol for later use; the prescribed amount of HSA is dissolved in water to prepare a 4% solution. The HSA solution was added to the cucurbitacin B ethanol solution, and after dispersion, it was placed in an ultrasonic instrument. After 200W ultrasonic treatment, and then 600W ultrasonic dispersion for 5min, the emulsion was obtained. The organic solvent was removed by rotary evaporation. The average particle diameter of the obtained nanoparticles is 282.2nm, the distribution is very wide, and it cannot pass through the microporous membrane of 0.45 μm, and precipitation will occur after standing for 20 minutes, and the system is unstable. After freeze-drying, the dispersibility is poor, and it is difficult to return ...

Embodiment 2

[0097] Example 2 Adding Phospholipids to Solve the Problems Existing in the Preparation of Cucurbitacin HSA Nanoparticles by Probe Ultrasonic Method

[0098] Cucurbitacin B 0.01g

[0099] HSA 4g

[0100] S100 1.5g

[0101] Appropriate amount of water

[0102] Cucurbitacin B (purity greater than 98%) and S100 (soybean lecithin, SPC Germany LIPOID) were dissolved in 1 ml of ethanol for later use; the prescribed amount of HSA was dissolved in water to prepare a 4% solution. Add the HSA solution to the cucurbitacin B / phospholipid ethanol solution, and place it in an ultrasonic apparatus after dispersion. After 200W ultrasonic treatment, and then 600W ultrasonic dispersion for 5min, the emulsion was obtained. The organic solvent was removed by rotary evaporation. The obtained nanoparticles have an average particle size of 156nm and a narrow distribution, and can pass through microporous membranes of 0.45 μm and 0.3 μm without precipitation after being placed for 60 minutes, an...

Embodiment 3

[0103] Example 3 Preparation of cucurbitacin HSA nanoparticles by dissolving phospholipids with tert-butanol

[0104]Cucurbitacin B 0.01g

[0105] HSA 4g

[0106] S100 1.5g

[0107] Appropriate amount of water

[0108] Cucurbitacin B (purity greater than 98%) and S100 (soybean lecithin, SPC Germany LIPOID) were dissolved in 5ml tert-butanol for later use; the prescribed amount of HSA was dissolved in water to prepare a 4% solution. Add the HSA solution into the cucurbitacin B / phospholipid tert-butanol solution, and place it in an ultrasonic apparatus after dispersion. After 200W ultrasonic treatment, and then 600W ultrasonic dispersion for 5min, the emulsion was obtained. The obtained nanoparticles have an average particle size of 139nm and a narrow distribution, and can pass through microporous membranes of 0.45 μm and 0.3 μm without precipitation after being placed for 60 minutes, and the system stability is greatly improved. After freeze-drying, the dispersibility is g...

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PUM

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Abstract

The invention belongs to the technical field of medicines, and discloses a delivery system based on protein-phospholipid. The system comprises a protein-phospholipid dispersion with the weight ratio of between 1:100 and 100:1, wherein the grain size of the protein-phospholipid is between 5 and 1,000nm, and the surface of the phospholipid or the surface and the inside of the phospholipid are coated / covered by a protein layer. The preparation method comprises: preparing a phospholipid containing phase, preparing a protein containing water phase, performing the homogenization treatment on the phospholipid containing phase and the protein containing water phase at a temperature of between 0 and 40 DEG C and under a pressure of between 400 and 40,000psi, and obtaining a dispersion system with the average grain size of less than 1,000nm. The delivery system has the advantages of realizing the delivery in various ways such as injection, oral taking, cavities and canals, skin and the like, and lowering side effects of medicines. The delivery system solves the problems of drug-loading rate and stability of protein nano-grain and liposome, and adopts low-toxicity organic solvent, even no organic solvent; and the preparation method is easy for industrialized application, and can prepare a liquid type protein-phospholipid containing delivery system.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, more specifically to a drug delivery system and a preparation method thereof. Background technique [0002] In recent years, with the rapid development of drug therapy, the concept of "optimization of drug use" has gradually become a matter of great concern to people. This is mainly to reflect the value of drug therapy reasonably and ensure the safety of drug therapy. [0003] By using new technologies and methods to regulate the dynamic changes of drugs in the body to obtain the best therapeutic effect, this is the drug delivery system (DDS). Utilizing the function of the drug delivery system can improve the absorption of drugs, reduce the toxic and side effects of drugs, increase the distribution of drugs in diseased tissues, and achieve the purpose of increasing efficiency and reducing toxicity. [0004] In the field of pharmacy, the size of nanoparticles is generally defined as 1-1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/42A61K47/24A61K45/00
CPCA61K47/44A61K47/42A61K9/1075A61K9/19
Inventor 邓意辉董晓辉石莉卢懿王瑞琪吴悫邹佳张玲洪维为宋阳徐缓王龙
Owner SHENYANG PHARMA UNIVERSITY
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