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Preparation of vinorelbine lipoplast, for injection

A technology of vinorelbine tartrate and rebin lipid, which is applied in the field of preparation of vinorelbine tartrate liposomes, can solve the problems of cell membrane damage, pH change, vein damage and the like, and achieves improved action time, stable properties and exact curative effect Effect

Inactive Publication Date: 2007-07-18
XIAN LIBANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The occurrence of phlebitis caused great pain to the patient, and even led to the termination of medication. The reason is that NVB is highly permeable and can enter the subcutaneous space through blood vessels, resulting in high local concentration, which destroys the balance of osmotic pressure inside and outside the cell membrane, and at the same time causes localized pH changes, resulting in damage to veins

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] (1) Preparation of blank liposomes

[0017] prescription:

[0018] Phosphatidylcholine 27.38g (36mmol)

[0019] DSPE-PEG 2000 10.10g (3.61mmol)

[0020] Cholesterol 12.55g (32.5mmol)

[0021]

[0022] Prepare 500mL liposomes

[0023] Preparation method: phosphatidylcholine, DSPE-PEG 2000 and cholesterol in a mixed solvent with a volume ratio of 1:1 ethanol and tert-butanol until the solution is clear and transparent; another appropriate amount of citric acid buffer is taken, according to the ratio of lipid solution to citric acid buffer volume ratio of 1:4, Proliposomes were prepared by mixing with a gradient pump; the gradient pump was connected to an extruder, and 5 polycarbonate films of 100 nm were laid in the extruder; the mixed proliposomes were extruded to a uniform particle size through the extruder , the liposome mixed solution flowing out is ultrafiltered through an ultrafilter immediately, and 2.5 liters...

Embodiment 2

[0030] (1) Preparation of blank liposomes

[0031] prescription:

[0032] Phosphatidylcholine 12.5g (12.7mmol)

[0033] HSPE-S-mPEG 2000 36.80g (10.2mmol)

[0034] Cholesterol 50.7g (101.9mmol)

[0035]

[0036] Prepare 1000mL liposomes

[0037] Preparation method: Phosphatidylcholine, HSPE-S-mPEG 2000 and cholesterol in a mixed solvent with a volume ratio of 1:1 isopropanol and n-butanol until the solution is clear and transparent; take another appropriate amount of citric acid buffer, according to the ratio of lipid solution to citric acid buffer volume 1:4 , mix and prepare proliposome by gradient pump; Gradient pump is connected with extruder, spreads the polycarbonate film of 5 pieces of 100nm in extruder; Mixed proliposome is extruded uniform granule by extruder diameter, the outflowing liposome mixed solution is ultrafiltered through an ultrafilter immediately, and 2.5 liters of citric acid buffer solution is consta...

Embodiment 3

[0044] (1) Preparation of blank liposomes

[0045] prescription:

[0046] Phosphatidylcholine 88.5g (116.4mmol)

[0047] HSPE-S-mPEG 5000 6.47g (1.3mmol)

[0048] Cholesterol 5.0g (12.9mmol)

[0049]

[0050] Prepare 1000mL liposomes

[0051] Preparation method: Phosphatidylcholine, HSPE-S-mPEG 5000 and cholesterol in a mixed solvent of chloroform and methanol at a volume ratio of 1:1 until the solution is clear and transparent; take another appropriate amount of citric acid buffer, and pass through the gradient The pump is mixed to prepare proliposomes; the gradient pump is connected to the extruder, and five polycarbonate membranes of 100 nm are laid in the extruder; the mixed proliposomes are extruded by the extruder to uniform particle size, and flow The liposome mixed solution was ultrafiltered through an ultrafilter immediately, and 2.5 liters of citrate buffer solution was continuously added in the middle, and then the li...

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Abstract

A process for preparing the vinorelbine liposome for injection, especially the vinorelbine liposome tartrate, includes such steps as dissolving multiple kinds of lipoid in organic solvent, mixing it with buffer liquid in HPLC gradient pump while pressing, ultrafiltering to remove organic solvent and obtain simple liposome, regulating pH=7-9 by special alkali solution, mixing with medicine solution, and encapsulating to obtain medicine.

Description

technical field [0001] The invention relates to a preparation method of vinorelbine tartrate liposome, in particular to a preparation method of vinorelbine liposome for injection. Background technique [0002] Vinorelbine (vinorelbine, Navelbine) was developed by Pierre Fabre and first launched in France in 1989. It is a semi-synthetic alkaloid of the genus Vinca, and its 9-ring has been changed to 8-ring. The tartrate of vinorelbine was approved by FDA in December 1994 for the first-line treatment of patients with advanced non-small cell lung cancer. It has been used in the treatment of NSCLC in more than 40 countries abroad, and it has been used in the treatment of advanced breast cancer in 18 countries. At present, the dosage forms on the market in my country include intravenous injection (1ml:10mg), freeze-dried powder injection (10mg, 20mg). [0003] The main side effects of vinorelbine common dosage forms are myelosuppression and local phlebitis. The occurrence of p...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/34A61K31/475A61P35/00A61P11/00A61P15/14A61K47/24
Inventor 黄馨惠傅经国党晓怡佐建锋魏春龙杨洁
Owner XIAN LIBANG PHARMA TECH
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