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Vecuronium bromide liposome injection

A technology of vecuronium bromide fat and injections, which is applied in the field of medicine, can solve the problems of poor stability of physical and chemical properties, long production cycle of freeze-dried powder injections, and impurities in the quality of medicines, so as to improve the quality of preparation products and improve bioavailability Degree, enhance the effect of solubility

Inactive Publication Date: 2012-01-18
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The currently marketed vecuronium bromide dosage forms are mainly injections and freeze-dried powder injections. The vecuronium bromide injections prepared by ordinary techniques have poor physical and chemical properties. Toxic and side effects, leaving hidden dangers for clinical use
The production cycle of freeze-dried powder injection is long, the cost is high, and the price is expensive
[0007] Patent CN101843593A discloses a freeze-dried powder preparation for injection and its preparation process, which is prepared with vecuronium bromide, amino acids or polysaccharides, polyethylene glycol, vitamin E and glycerin, but amino acids are unstable, which will accelerate the instability of drugs sex, but also increase the production cost

Method used

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  • Vecuronium bromide liposome injection
  • Vecuronium bromide liposome injection
  • Vecuronium bromide liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] The preparation of embodiment 1 vecuronium bromide liposome injection

[0062] The ingredients used and their weights are as follows:

[0063]

[0064] Adopt preparation process to prepare vecuronium liposome injection:

[0065] (1) 120g cholesterol, 150g phosphatidylethanolamine, 30g soybean lecithin and 10g Tween 80 are dissolved in the phosphate-buffered saline solution that 1000ml pH is 7.2, make blank liposome;

[0066] (2) The blank liposomes prepared above were sterilized by circulating steam, and then ultrasonically treated twice, each time for 15 minutes;

[0067] (3) under aseptic conditions, add 4g vecuronium bromide to the liposome in molten state at 60 DEG C, add 100g trehalose, 70g mannitol and 80g PVP under constant stirring;

[0068] (4) Filter through a 0.45 μm microporous membrane, fill, and then freeze-dry. The pre-freezing temperature is -30°C, the pre-freezing time is 5 hours, the sublimation time is 48 hours, the drying temperature is 35°C, ...

Embodiment 2

[0069] The preparation of embodiment 2 vecuronium bromide liposome injections

[0070] The ingredients used and their weights are as follows:

[0071]

[0072] Adopt preparation process to prepare vecuronium liposome injection:

[0073] (1) 75g cholesterol, 100g phosphatidylethanolamine, 25g soybean lecithin and 20g Tween 80 are dissolved in the phosphate-buffered saline solution of 7.2 in the pH of 1000ml, make blank liposome;

[0074] (2) The blank liposomes prepared above were sterilized by circulating steam, and then ultrasonically treated twice, each time for 15 minutes;

[0075] (3) under aseptic conditions, add 4g vecuronium bromide to the liposome in molten state at 60 DEG C, add 30g trehalose, 30g mannitol and 40g PVP under constant stirring;

[0076] (4) Filter with 0.45 μm microporous membrane, fill, and then freeze-dry. Hours, the vecuronium liposome injection was obtained.

Embodiment 3

[0077] The preparation of embodiment 3 dimensional curonium liposome injection

[0078] The ingredients used and their weights are as follows:

[0079]

[0080] Adopt preparation process to prepare vecuronium liposome injection:

[0081] (1) 30g cholesterol, 40g phosphatidylethanolamine, 10g soybean lecithin and 10g Tween 80 are dissolved in the phosphate-buffered saline solution of 7.2 in the pH of 1000ml, make blank liposome;

[0082] (2) The blank liposomes prepared above were sterilized by circulating steam, and then ultrasonically treated twice, each time for 15 minutes;

[0083] (3) under sterile conditions, add 2g vecuronium bromide to the liposome in molten state at 60°C, add 10g trehalose, 10g mannitol and 30g PVP under constant stirring;

[0084] (4) 0.45 μm microporous membrane filtration, filling, and then freeze-drying, the pre-freezing temperature is -45 ° C, the pre-freezing time is 3.5 hours, the sublimation time is 25 hours, the drying temperature is 30...

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Abstract

The invention discloses a vecuronium bromide liposome injection and a preparation method thereof. The liposome injection is prepared from vecuronium bromide, cholesterol, phosphatidyl ethanolamine, soyabean lecithin, twain 80, trehalose, mannitol and polyvinylpyrrolidone in a specific weight ratio. The liposome injection has high preparation stability, and the liposome is not cracked due to fusion, ice crystals and the like in the refrigerating process and keeps high entrapment efficiency even after being stored for a long-time. Due to the adoption of the injection, the solubility of the vecuronium bromide is improved, the quality of a preparation product is improved, toxic and side effects are reduced, the retention time of a medicament is increased during systemic circulation, the bioavailability of the medicament is enhanced, the curative effect is improved remarkably; and moreover, the preparation method is simple and is suitable for industrial production.

Description

technical field [0001] The invention relates to a liposome injection and a preparation method thereof, in particular to a vecuronium bromide liposome injection and a preparation method thereof, and belongs to the technical field of medicine. Background technique [0002] Vecuronium bromide, chemical name is 1-[3α,17β-diacetoxy-2-β(1-piperidinyl)-5α-androstane-16β-yl]-1-methylpiperidine bromide , the molecular weight is 637.73, and the structural formula is as follows: [0003] [0004] Vecuronium bromide is a white or off-white loose substance, slightly soluble in water, easily soluble in dichloromethane, almost insoluble in absolute ethanol. [0005] Vecuronium bromide is a new type of non-depolarizing diaminoandrostane muscle relaxant, which is used for endotracheal intubation and maintenance of anesthesia. It is an adjuvant drug for general anesthesia and can promote skeletal muscle relaxation. It acts quickly after intravenous injection, has no effect on the vagus n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/58A61K47/36A61P21/02
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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