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Mutamycine C multivesicular liposome and its preparing method

A technology of mitomycin and liposomes, which is applied in the field of mitomycin C multivesicular liposomes and its preparation, can solve the problems of drug release in the preparation of encapsulation rate and the stability of preparations, and achieve the best anti-cell Proliferation and anti-tumor effect, good sustained-release effect, effect of reducing the number of medications and total dosage

Inactive Publication Date: 2007-10-03
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the current problem is: due to the different physical and chemical properties and mechanism of action of different drug active ingredients, the preparation encapsulation efficiency, drug release and formulation stability are quite different. Therefore, for specific drugs and their release requirements, Specific formulations and processes need to be studied

Method used

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  • Mutamycine C multivesicular liposome and its preparing method
  • Mutamycine C multivesicular liposome and its preparing method
  • Mutamycine C multivesicular liposome and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Step 1: Accurately weigh 200 mg of lecithin, 50 mg of cholesterol, 40 mg of stearylamine and 17.4 mg of glyceryl trioleate, and dissolve them in 5 ml of dichloromethane as the lipid phase;

[0036] Step 2: Accurately weigh 5mg of mitomycin C and 100mg of sucrose, dissolve with appropriate amount of distilled water, adjust the pH to 8.0 with sodium dihydrogen phosphate and sodium hydroxide, and set the volume to 5ml, as the inner water phase, slowly add the lipid phase upper layer;

[0037] Step 3: Use a high-speed shear homogenizer (Fluko, ATS Industrial Systems Co., Ltd.) to act on the mixture obtained in step 2 at a speed of 10,000 rpm for 9 minutes to obtain W / O type colostrum;

[0038] Step 4: In order to prepare the dichloromethane microsphere suspension, add 20mL of the external water phase containing 3.2% (w / v) glucose to the upper layer of the W / O colostrum, and act for 15 seconds at a speed of 4500rpm, forming a suspension of dichloromethane microspheres;

[...

Embodiment 2

[0042] Step 1: Accurately weigh 200 mg of lecithin, 50 mg of cholesterol, 10 mg of collagen and 15.6 mg of triolein, dissolve them in 5 ml of dichloromethane as the lipid phase;

[0043] Step 2: Accurately weigh 5mg of mitomycin C and 200mg of sucrose, dissolve with appropriate amount of distilled water, adjust the pH to 8.7 with potassium dihydrogen phosphate and potassium hydroxide, and set the volume to 5ml, as the inner water phase, slowly add the lipid phase upper layer;

[0044] Step 3: with embodiment 1;

[0045] Step 4: In order to prepare the dichloromethane microsphere suspension, add 20mL of the external aqueous phase containing 6.0% (w / v) glucose to the upper layer of the W / O colostrum, and act for 15 seconds at a speed of 4500rpm, forming a suspension of dichloromethane microspheres;

[0046] Step 5: Same as Example 1.

[0047] The particle size of the mitomycin C multivesicular liposome was measured to be 5-50 μm; the encapsulation efficiency was 75.1%.

Embodiment 3

[0049] Step 1: Accurately weigh 100 mg of dioleoylphosphatidylcholine, 50 mg of cholesterol, 20 mg of stearylamine and 3.4 mg of glyceryl trioleate, and dissolve them with 5 ml of chloroform-ether mixture (1:1 by volume) as lipid Mutually;

[0050] Step 2: Accurately weigh 2.5mg of mitomycin C, dissolve it with an appropriate amount of distilled water, adjust the pH to 8.4 with disodium hydrogen phosphate and sodium hydroxide, and set the volume to 5ml, as the inner water phase, slowly add to the upper layer of the lipid phase;

[0051] Step 3: with embodiment 1;

[0052] Step 4: In order to prepare the chloroform-ether microsphere suspension, add 60mL of the external aqueous phase containing 3.2% (w / v) glucose to the upper layer of the W / O colostrum, and act for 15 seconds at a speed of 4500rpm, Form a suspension of chloroform-ether microspheres;

[0053] Step 5: Same as Example 1.

[0054] The particle size of the mitomycin C multivesicular liposome was measured to be 5-5...

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Abstract

A multilocular liposome of mitomycin for preventing and treating tumor is prepared through dissolving the lipoid component (neutral phosphatide, cholesterol and neutral lipid) in organic solvent, dissolving mitomycin in buffering salt solution, mixing, emulsifying to obtain water-in-oil primary emulsion, adding external water phase containing isotonic regulator, stirring to become water-in-oil-in-water emulsion, and removing organic solvent.

Description

technical field [0001] The invention relates to a slow-release preparation of mitomycin C, in particular to a mitomycin C multivesicular liposome and a preparation method thereof. Background technique [0002] Mitomycin C (MMC) is an antibiotic broad-spectrum anticancer drug discovered by Hata et al. in 1955, and it is a cell cycle non-specific drug. Mitomycin C is most sensitive to the G1 phase of tumor cells, especially the late G1 phase and early S phase. After being activated by enzymes in tissues, it acts like a bifunctional or trifunctional alkylating agent and can cross DNA Link, inhibit DNA synthesis, and also have certain inhibitory effects on RNA and protein synthesis. So far, this product has been used clinically for more than 20 years, and it is an effective drug for treating various solid tumors. It is mainly used clinically for digestive tract cancers, and also has significant curative effects on lung cancer, breast cancer, cervical cancer, etc., and can also...

Claims

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Application Information

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IPC IPC(8): A61K31/40A61K9/127A61P35/00
Inventor 陆伟根陈亭亭
Owner SHANGHAI INST OF PHARMA IND
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