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Bulleyaconitine A micro-balloons and bulleyaconitine A long-acting injection and preparation method and application of same

A technology of aconitin and aconitin, which is applied to medical preparations with no active ingredients, medical preparations containing active ingredients, anti-inflammatory agents, etc., which can solve the problems of large fluctuations in blood drug concentration, application restrictions, and adverse reactions and other issues, to achieve the effect of reducing the number of administration, good safety and high patient compliance

Inactive Publication Date: 2009-10-14
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Injections are administered twice a day, and continuous administration has the characteristics of large fluctuations in blood drug concentration, which will bring many adverse reactions, so its application is subject to certain restrictions

Method used

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  • Bulleyaconitine A micro-balloons and bulleyaconitine A long-acting injection and preparation method and application of same
  • Bulleyaconitine A micro-balloons and bulleyaconitine A long-acting injection and preparation method and application of same
  • Bulleyaconitine A micro-balloons and bulleyaconitine A long-acting injection and preparation method and application of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Prescription of Microspheres

[0051] Aconitin 3g

[0052] Glycolide-Lactide Copolymer 12g

[0053] In the glycolide-lactide copolymer, the molar ratio of the monomers is 50:50, the weight average molecular weight is 5000 Daltons, and the average particle diameter of the microspheres is 200 μm;

[0054] Preparation:

[0055] The device used in the preparation method can refer to the device disclosed in the Chinese patent, Patent No. 200420081682.5, and the diameter of the nozzle hole of the nozzle is 1mm;

[0056] Dissolving aconitin and glycolide-lactide copolymer in dichloromethane to prepare a solution with a total solid weight content of 30%, filtered through a filter with a pore size of 0.45 μm and used as a dispersed phase;

[0057]Dissolving polyvinyl alcohol 04-86 in water to make an aqueous solution with a weight content of 0.1%, filtered through a filter with a pore size of 5 μm, and used as the water phase;

[0058] The disperse phase and the water phase ...

Embodiment 2

[0060] Prescription of microspheres:

[0061] Aconitine 10g

[0062] Polylactide 10g

[0063] In the glycolide-lactide copolymer, the molar ratio of the monomers is 25:75, the weight average molecular weight is 100,000 Daltons, and the average particle size of the microspheres is 1 μm;

[0064] Preparation:

[0065] The device used in the preparation method can refer to the device disclosed in the Chinese patent, Patent No. 200420081682.5, and the diameter of the nozzle hole of the nozzle is 0.1mm;

[0066] Dissolving aconitin and polylactide in ethyl acetate to prepare a solution with a total solid weight content of 10%, filtered through a filter with a pore size of 0.45 μm and used as a dispersed phase;

[0067] Dissolving polyvinyl alcohol 05-88 in water to make an aqueous solution with a weight content of 5%, filtered through a filter with a pore size of 5 μm, and used as the water phase;

[0068] The dispersed phase and the aqueous phase enter the nozzle submerged in ...

Embodiment 3

[0070] Prescription for Suspension Injection:

[0071] The aconitin microspheres 50g of embodiment 1

[0072] Suspending agent 10g

[0073] Osmotic pressure regulator 1g

[0074] Wetting agent 0.2g

[0075] Water for injection 38.8g

[0076] The suspending agent is sodium carboxymethyl cellulose, the osmotic pressure regulator is sodium chloride, and the wetting agent is polysorbate.

[0077] Stir the above-mentioned various raw materials evenly, then pack them into ampoules, seal and sterilize by autoclaving at 115°C for 30 minutes, and then it can be made into a suspension injection.

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Abstract

The invention provides a bulleyaconitine A micro-balloons, bulleyaconitine A long acting injection and a preparation method and application of the same. The micro-balloons contain therapeutically effective dosage of bulleyaconitine A and biodegradable polymer. The bulleyaconitine A long-acting injection has good safety, convenient use, long drug action time and high obedience of patient, can achieve the aim of reducing administration time, prolonging the drug action time, reducing blood concentration fluctuation and increasing the administration obedience of the patient, can achieve a week drug action by administration once and has higher clinical application value.

Description

technical field [0001] The present invention relates to a kind of injection of aconitin. technical background [0002] Bulleyaconitine A (BLA) is a diterpene diester alkaloid, which is isolated from the plant Acomitum bullyanum Diels of Ranunculaceae. In 1983, the Shanghai Institute of Materia Medica, Chinese Academy of Sciences confirmed that aconitin has obvious analgesic and anti-inflammatory effects, and is an excellent analgesic and anti-inflammatory drug. Its analgesic effect is central and closely related to the level of 5-hydroxytryptamine in the brain. , the analgesic effect is 1.75-2.27 times that of morphine, and 371.5-1371 times that of aspirin. The onset time is slower than that of morphine, but the maintenance time is long, and it is not addictive; (PG) level, has antipyretic and local anesthetic effects. It is mainly used for the treatment of osteoarthritis, rheumatism and rheumatoid arthritis, advanced cancer pain and other pain diseases. [0003] Currentl...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/10A61K9/19A61K31/439A61K47/34A61P29/00A61P19/02A61P19/04A61P35/00A61P25/04
Inventor 栾瀚森王浩侯惠民
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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