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Bulleyaconitine A lipidosome freeze-dried powder injection and preparation method thereof

A technology of freeze-dried powder injection and clathrate, which is applied in the field of liposome freeze-dried powder injection containing clathrin and its preparation, which can solve the problem of unmentioned skin irritation and the stability of liposomes. It can reduce skin irritation, prolong drug action time, and improve stability.

Inactive Publication Date: 2009-11-18
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

"Aconitin Powder Injection and Its Production Method" with application number 03031018.4 and "Aconitin New Powder Injection and Its Production Method" with application number 200410079538.2 disclose two freeze-dried powder injections of Aconitin and preparation method, although the two preparation methods of freeze-dried powder injection avoid the fatal process defect that aconitin A injection will be rapidly degraded after autoclave sterilization, and have a negative impact on the quality of aconitin A injection However, the problem of narrow therapeutic window, high toxicity and strong skin irritation during injection is still unavoidable.
The patent application number is 200610024926.X discloses a kind of aconitin multivesicular liposome and preparation method thereof, and this liposome has obvious slow-release effect compared with common aconitin preparation, but this product does not have Overcoming the problem of liposome stability, it cannot be applied to large-scale industrial production
This patent specification also does not mention the skin irritation problem of the liposome clinical use of preparation

Method used

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  • Bulleyaconitine A lipidosome freeze-dried powder injection and preparation method thereof
  • Bulleyaconitine A lipidosome freeze-dried powder injection and preparation method thereof
  • Bulleyaconitine A lipidosome freeze-dried powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Prescription (100 formulation units):

[0056] Phospholipid S100 2g

[0057] Cholesterol 0.3g

[0058] Aconitine 40mg

[0059] Ethanol 90ml

[0060] 0.15mol / L citrate buffer solution of pH4.0 100ml

[0061] 0.10mol / L sodium carbonate aqueous solution several ml

[0062] Mannitol 10g

[0063] Preparation method: Take the prescribed amount of phospholipid S100 and cholesterol, dissolve in an appropriate amount of ethanol, remove the solvent by rotary evaporation under reduced pressure at 48°C, and after forming a dry film, add citrate buffer solution with pH 4.0, shake to wash the film completely Take off, obtain the blank liposome of large particle size. High-speed shearing with a high-shear divergent emulsifier for 5 minutes, and high-pressure emulsification at 800 bar for 10 times to obtain blank liposomes with small particle sizes. Use a carbonate solution to adjust the pH of the external phase to 7-8 to obtain sample 1; weigh the prescribed amount of aconitin,...

Embodiment 2

[0066] Prescription (100 formulation units):

[0067] Phospholipid S100 4.8g

[0068] Cholesterol 0.6g

[0069] Aconitine 80mg

[0070] Methanol 50ml

[0071] 0.15mol / L citrate buffer solution of pH4.0 100ml

[0072] 0.10mol / L sodium carbonate aqueous solution several ml

[0073] Sucrose 4.8g

[0074] Preparation method: Take the prescribed amount of phospholipid S100 and cholesterol, dissolve in an appropriate amount of methanol, and remove the solvent by rotary evaporation at 40°C under reduced pressure. After forming a dry film, add citrate buffer solution with pH 4.0, and shake to wash the film completely. Take off, obtain the blank liposome of large particle size. High-speed shearing with a high-shear divergent emulsifier for 10 minutes, and high-pressure emulsification at 700 bar for 20 times to obtain blank liposomes with small particle sizes. Use a carbonate solution to adjust the pH of the external phase to 7-8 to obtain sample 1; weigh the prescribed amount of...

Embodiment 3

[0077] Prescription (100 formulation units):

[0078] Phospholipid S100 20mg

[0079] Cholesterol 20mg

[0080] Aconitine 20mg

[0081] Chloroform 30ml

[0082] 0.15mol / L citrate buffer solution of pH4.0 100ml

[0083] 0.10mol / L sodium carbonate aqueous solution several ml

[0084] Glucose 7g

[0085] Preparation method: Take the prescribed amount of phospholipid S100 and cholesterol, dissolve it in an appropriate amount of chloroform, remove the solvent by rotary evaporation under reduced pressure at 48°C, and after forming a dry film, add citrate buffer solution with pH 4.0, shake to wash the film completely Take off, obtain the blank liposome of large particle size. High-speed shearing with a high-shear divergent emulsifier for 10 minutes, and high-pressure emulsification at 700 bar for 10 times to obtain blank liposomes with a small particle size. Use a carbonate solution to adjust the pH of the external phase to 7-8 to obtain sample 1; weigh the prescribed amount o...

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Abstract

The invention provides a bulleyaconitine A lipidosome freeze-dried powder injection and a preparation method thereof. The injection mainly comprises the following compositions by weight ratio: bulleyaconitine A:phospholipid:cholesterol:freeze-dry protecting agent=1:1-60:1-10:1-360. The prepared freeze-dried powder injection with encapsulation rate of between 75 and 90 percent not only can obviously improve storage stability, but also can lead the bulleyaconitine A lipidosome freeze-dried powder to be re-dissolved after injection water is added. The prepared bulleyaconitine A lipidosome freeze-dried powder injection has light or non irritation in clinic application compared with the prior bulleyaconitine A injection, and has slow release property compared with common preparation.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a liposome freeze-dried powder injection containing aconitin and a preparation method thereof. Background technique [0002] Bulleyaconitione A was also known as Dianxi Dianxi aconitine A or thick stem aconitine A, molecular formula C 35 h 49 o 10 N, molecular weight 643.77, is a colorless prismatic crystal. Soluble in ether, alcohol, acid water, insoluble in water, has strong analgesic and obvious anti-inflammatory effects. Experiments have proved that the analgesic effect of this product is central and closely related to the level of serotonin in the brain. Non-addictive. Its anti-inflammatory effect does not pass through the adrenal system, but is related to the suppression of PG levels; this product also has antipyretic and local anesthetic effects. After taking the medicine, there were no abnormal changes in the patients' ECG, EEG, liver and kidney function and urine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/127A61K31/439A61P29/00A61P25/04A61P19/02A61P19/04A61P23/02
Inventor 张伟刘国光龚云麒刘一丹杨兆祥
Owner KPC PHARM INC
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