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Self asembled precusor liposome containing camptothecin kind medicine and its preparation method

A proliposome and self-assembly technology, which is applied in drug combination, liposome delivery, medical preparations containing active ingredients, etc., can solve the problem of reduced drug encapsulation rate, poor stability of preparation quality, complicated preparation process, etc. problem, to achieve the effect of stable and controllable quality, stable product quality and simple process

Inactive Publication Date: 2006-08-30
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 1. The preparation process is complicated, prone to bacterial contamination, poor reproducibility, difficult to industrialized large-scale production, and high manufacturing cost
[0007] 2. Poor preparation quality stability
[0009] (2) During storage of drug-containing liposome liquid preparations, there are objectively: the phenomenon of drug diffusion (or leakage) from liposomes to the liquid medium, resulting in reduced or unstable drug encapsulation efficiency; (or aggregation) tendency, also causes the important factor that liposome particle size becomes larger or unstable
[0010] (3) During the dissolution and dispersion process of drug-containing liposome solid (lyophilized) preparations before use, liposome aggregation or particle size increase due to incomplete local dissolution and uneven dispersion of liposome nanoparticles; Or liposome rupture, drug leakage, resulting in decreased encapsulation efficiency of drug-containing liposomes
In view of the fact that in the process of preparing solid proliposomes, the process of removing organic solvents is the main technical bottleneck to realize industrialization, and the hydration process of solid proliposomes will also objectively have a slow hydration rate and incomplete local dissolution , uneven dispersion and other problems, resulting in the main quality indicators such as drug encapsulation rate and average particle size are difficult to effectively control, and it is difficult to meet the requirements of clinical use
In the existing published patents, research literature and reports on the preparation of liposomes and proliposomes, no preparation technology directly using liquid self-assembled proliposomes has been found.

Method used

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  • Self asembled precusor liposome containing camptothecin kind medicine and its preparation method
  • Self asembled precusor liposome containing camptothecin kind medicine and its preparation method
  • Self asembled precusor liposome containing camptothecin kind medicine and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Prescription: 10-Hydroxycamptothecin 1g

[0053] Soy Lecithin 180g

[0054] Poloxamer 188 (trade name F-68) 5g

[0055] Benzyl alcohol 250g

[0056] Add absolute ethanol to 1000ml

[0057] Preparation process: according to figure 1 Dissolve the prescribed amount of soybean lecithin in an appropriate amount of ethanol, then add the prescribed amount of drug, poloxamer 188, benzyl alcohol and the remaining amount of ethanol. After the drug and other components are completely dispersed or dissolved, After filtering and sterilizing with a 0.22 μm microporous membrane, the filtrate is filled and sealed in a nitrogen-filled ampoule or a vial under aseptic conditions to obtain the 10-hydroxycamptothecin self-assembled proliposome.

[0058] Take the 10-hydroxycamptothecin self-assembled proliposome according to the clinical dose before use and add it to 150 times the amount (v / v) of 5% glucose solution to dilute and disperse, and quickly form 10-hyd...

Embodiment 2

[0060] Prescription: Camptothecin 1g

[0061] Egg phospholipids 200g

[0062] Tween 80 5g

[0063] n-Butanol 150g

[0064] Vitamin E 2g

[0065] Macrogol 400 up to 1000ml

[0066] Preparation process: dissolve the prescribed amount of egg phospholipids in an appropriate amount of polyethylene glycol 400, then add the prescribed amount of medicine, Tween 80, n-butanol, vitamin E and the remaining amount of polyethylene glycol 400, and wait for the medicine and After all the other components are dispersed or dissolved, the 0.22μm microporous membrane is filtered to sterilize, and the filtrate is filled and sealed in nitrogen-filled ampoules or vials under sterile conditions to obtain camptothecin self-assembled proliposomes .

[0067] Take the camptothecin self-assembled proliposome according to the clinical dosage before use and add it to 200 times the amount (v / v) of 5% glucose solution to dilute and disperse, and then quickly form a camptoth...

Embodiment 3

[0069] Prescription: 10-Hydroxycamptothecin 0.8g

[0070] Hydrogenated Phospholipids 200g

[0071] Polyoxyethylene hydrogenated castor oil (Cremophor RH40) 2g

[0072] Benzyl alcohol 120g

[0073] Deoxycholic acid 0.8g

[0074] Propylene glycol 200g

[0075] Add absolute ethanol to 1000ml

[0076] Preparation process: dissolve the prescribed amount of hydrogenated phospholipids in an appropriate amount of ethanol, then add the prescribed amount of drugs, polyoxyethylene hydrogenated castor oil Cremophor RH40, benzyl alcohol, propylene glycol, deoxycholic acid and the remaining amount of ethanol, and wait for the drug and After all other components are dispersed or dissolved, 0.22μm microporous membrane is filtered to sterilize, and the filtrate is filled and sealed in nitrogen-filled ampoules or vials under sterile conditions to obtain the self-assembled precursor of 10-hydroxycamptothecin Liposomes.

[0077] Take the 10-hydroxycamptot...

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Abstract

A self-assembled precursor liposome of camptothecine contained medicine is proportionally prepared from camptothecine contained medicine, phosphatide, polyethylene glycol and dispersing medium through mixing, dispersing, press filtering by millipore film, and pouring it in a container full of N2.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a self-assembled proliposome containing camptothecin drugs, and also relates to a preparation method of the self-assembled proliposome. Background technique [0002] In view of the unique anti-cancer mechanism of camptothecin and its derivatives (specifically blocking the synthesis of Top I enzymes), since 1985, especially after entering the 1990s, countries such as the United States, Japan, Canada and the United Kingdom have actively invested a lot of The research and development of camptothecin has made camptothecin the second most important woody anti-cancer medicinal plant after paclitaxel, and has become a worldwide hot research topic. [0003] Since camptothecin and its derivatives are mostly difficult to dissolve in water, the currently existing domestic marketed varieties utilize alkaline solution to open their lactone rings to form carboxylate salts to prepare in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/34A61K31/4745A61P35/00A61K47/10A61K47/26A61K47/44
Inventor 周建平谢俊杨静杨俊仝新勇徐向阳曹春陵陈振飞
Owner CHINA PHARM UNIV
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