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Temperature-sensitive liposome preparation of vinblastine medicament and preparation method thereof

A technology of liposome preparation and vinblastine, which is applied in the direction of liposome delivery, pharmaceutical formulation, drug combination, etc., can solve the problems of not obviously improving the curative effect, achieve good targeting, overcome easy leakage, and encapsulation efficiency high effect

Inactive Publication Date: 2012-09-26
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, compared with the previous formulations, the liposomes prepared by it did not significantly improve the curative effect.

Method used

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  • Temperature-sensitive liposome preparation of vinblastine medicament and preparation method thereof
  • Temperature-sensitive liposome preparation of vinblastine medicament and preparation method thereof
  • Temperature-sensitive liposome preparation of vinblastine medicament and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1 Preparation of vinorelbine long-circulation thermosensitive liposome preparation

[0043] (1) Preparation of blank liposomes

[0044] Medicines and reagents needed: dipalmitoylphosphatidylcholine (DPPC), DSPE-mPEG2000, monostearylphosphatidylcholine (MSPC), citric acid, trisodium citrate, sodium carbonate, double distilled water.

[0045] Table 1

[0046] Phospholipids

DPPC

DSPE-mPEG2000

MSPC

mass (g)

8.9

0.8

0.3

[0047] Weigh various phospholipids (the amount used to prepare 100ml blank liposomes) according to Table 1, dissolve in 80ml chloroform, and remove the organic solvent by rotary evaporation at 50-60°C to obtain a film that is dry and evenly attached to the bottom of the glass bottle. Hydrate with 100 ml, 0.2M, pH 4 citrate buffer to obtain a multilamellar liposome solution. The polycarbonate membrane is extruded, first through a polycarbonate membrane with a pore diameter of 200nm, and then ...

Embodiment 2

[0049] Embodiment 2 Preparation of vinorelbine long-circulation thermosensitive liposome preparation

[0050] (1) Preparation of blank liposomes

[0051] Same as Example 1.

[0052] (2) Preparation of drug-loaded liposomes by pH gradient method: 0.3 g of vinorelbine was weighed and dissolved in 100 ml of 0.2 M pH4 citrate buffer solution to prepare a 3 mg / ml drug solution. Take 20ml of drug solution and add it to 20ml of blank liposome solution (it can be considered that the amount of drug is about 0.06g), add sodium carbonate solution at 25°C to adjust the pH value of the external phase to 7.45, and load the drug for 60 minutes. The cryoprotectant sucrose (10%) was added and stored in a refrigerator at -20°C.

Embodiment 3

[0053] Embodiment 3 Preparation of vinorelbine long-circulation thermosensitive liposome preparation

[0054] (1) Preparation of blank liposomes

[0055] Required medicines and reagents: dipalmitoylphosphatidylcholine (DPPC), DSPE-mPEG2000, distearoylphosphatidylglycerol (DSPG), tartaric acid, sodium tartrate, sodium carbonate, double distilled water, see Table 2 for specific dosage.

[0056] Table 2

[0057] Phospholipids

DPPC

DSPE-mPEG2000

DSPG

mass (g)

7.7

2

0.3

[0058] Weigh various phospholipids according to Table 2 (the amount used to prepare 100ml blank liposomes), dissolve in 80ml chloroform and methanol solution (1:1) to form a clear and transparent solution, and remove the organic solvent by rotary evaporation at 60°C to obtain a dry, uniform liposome Membrane attached to the bottom of a glass vial. Hydrate with (100ml, 0.2M, pH 4) tartrate buffer to obtain a multilamellar liposome solution. Squeeze through th...

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Abstract

The invention relates to a temperature-sensitive liposome preparation of vinblastine medicaments and a preparation method thereof. The temperature-sensitive liposome preparation includes vinblastine medicament, temperature-sensitive phosphatide and optional long circulating material. A molar ratio of temperature-sensitive phosphatide to optional long circulating material is 70:30-92:8; and a weight ratio of vinblastine medicament to blank liposome is 1:10-1:50. The invention employs a pH gradient active drug loading method to reach an entrapment rate of 90.0-99%. The liposome preparation with heat sensitivity of the present invention can make the liposome to passively target a tumour position and release a lot of medicament simultaneously, so as to improve curative effect and reduce toxic and side effects on the whole body.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to a thermosensitive liposome preparation containing vinblastine drugs, and a preparation method thereof. Background technique [0002] Vinblastine antineoplastic drugs are a class of alkaloids isolated from the vinca flower of the Apocynaceae plant with anticancer activity. It is a cell cycle-specific antineoplastic drug. Its mechanism of action is to block the formation of microtubules in the process of cell mitosis and stop cell division in the middle stage of mitosis. It is mainly used in the treatment of malignant lymphoma, choriocarcinoma, and advanced esophageal cancer. carcinoma, advanced non-small cell lung cancer, and breast cancer. At present, there are intravenous injections and freeze-dried powder injections on the market in my country. However, after intravenous injection of the drug, the side effects are relatively large, and symptoms such as neurotoxicity and blood toxicity...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/475A61P35/00
Inventor 梅兴国张慧
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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