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Alkaloid liposome in vinca and production technique

A technology of alkaloid lipid and production process, applied in the directions of liposome delivery, drug combination, organic active ingredients, etc., can solve the problems of drug stability and circulation time in vivo, etc., and achieve prolongation of circulation time in vivo and leakage rate. Low, good stability

Active Publication Date: 2007-12-26
BEIJING WENZHUO PHARMA BIOPROD TECH DEV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This liposome reduces the toxicity of vincristine, but drug stability and circulation time in the body need to be improved

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 1. Preparation of multilamellar liposomes

[0035] Combine SM, cholesterol and DSPE-PEG for injection 2000 The three were dissolved in chloroform / methanol (v / v, 2:1), and the antioxidants α-tocopherol and desferal were added. The above liquid was put into a rotary evaporating flask to rotary evaporate to form a film, and then the film was soaked in 300mM pH4.0 citric acid solution.

[0036] 2. Preparation of Small Unilamellar Liposomes

[0037] After five freezing-thawing cycles, the liquid was put into an extruder and extruded several times to obtain small unilamellar liposomes with a particle diameter of 100 nanometers. The carbon fiber membranes used for extrusion are 0.14 and 0.08 nm, respectively.

[0038] 3. Preparation of Vincristine Liposomes

[0039] Under the condition of 60 DEG C, add vincristine sulfate solution for injection into the small unilamellar liposomes in the amount of 0.2:1 according to the drug / lipid ratio, and apply 0.5M disodium hydrogen ph...

Embodiment 2

[0043] 1. Dissolve SM and cholesterol for injection in chloroform / methanol solution (v / v, 2:1), and add antioxidants α-tocopherol and desferal. The above liquid was put into a rotary evaporating flask to rotary evaporate to form a film, and then the film was soaked in 300mM pH4.0 citric acid solution.

[0044] 2. Preparation of Small Unilamellar Liposomes

[0045] After five freezing-thawing cycles, the liquid was put into an extruder and extruded several times to obtain small unilamellar liposomes with a particle diameter of 100 nanometers. The carbon fiber membranes used for extrusion are 0.14 and 0.08 nm, respectively.

[0046] 3. Preparation of Vincristine Liposomes

[0047] Under the condition of 60 DEG C, add vincristine sulfate solution for injection into the small unilamellar liposomes in the amount of 0.2:1 according to the drug / lipid ratio, and apply 0.5M disodium hydrogen phosphate (Na 2 HPO 4 ) solution to adjust the pH value to 7.2, and place it in a water bat...

Embodiment 3

[0050] 1. Preparation of multilamellar liposomes

[0051] DSPC, Cholesterol and DSPE-PEG for Injection 2000 The three were dissolved in chloroform / methanol (v / v, 2:1), and the antioxidants α-tocopherol and desferal were added. The above liquid was put into a rotary evaporating flask to rotary evaporate to form a film, and then the film was soaked in 300mM pH4.0 citric acid solution.

[0052] 2. Preparation of Small Unilamellar Liposomes

[0053] After five freezing-thawing cycles, the liquid was put into an extruder and extruded several times to obtain small unilamellar liposomes with a particle diameter of 100 nanometers. The carbon fiber membranes used for extrusion are 0.14 and 0.08 nm, respectively.

[0054] 3. Preparation of Vincristine Liposomes

[0055] Under the condition of 60 DEG C, add vincristine sulfate solution for injection into small unilamellar liposomes in the amount of 0.1:1 according to the ratio of drug / fat, and mix with 0.5M disodium hydrogen phosphat...

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Abstract

A myrtle alkaloid lipid is proportionally prepared from myrtle alkaloid, the lipid material chosen from phosphatide and cholesterol and the antioxidizing material chosen from alpha-tocopherol and desferal through preparing multi-layer lipid, preparing small single-layer lipid and preparing myrtle alkaloid lipid.

Description

technical field [0001] The invention relates to a vinca alkaloid liposome and a production process thereof, specifically liposomes of vincristine, vinblastine and vinorelbine and their pH gradient production process, belonging to the field of chemical pharmacy. Background technique [0002] Vinca alkaloids such as vincristine, vinorelbine and vinblastine are broad-spectrum antineoplastic drugs commonly used in clinic. At present, it is mainly used in acute and chronic leukemia, lymphoma, multiple myeloma, and some solid tumors, such as neuroblastoma, Wilms tumor, Ewing sarcoma, breast cancer and small cell lung cancer. However, like other anti-tumor chemotherapeutic drugs, vincristine produces relatively large toxic and side effects on patients during use, mainly due to dose-limited toxic and side effects, including neurotoxicity, which mostly occurs 6 to 8 weeks after administration, manifested as sensation Neurological and autonomic damage, severe ataxia, foot drop, or cr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/475A61K9/127A61P35/00
Inventor 曹利人马洁
Owner BEIJING WENZHUO PHARMA BIOPROD TECH DEV