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Aconitine injection for intrathecal injection and preparation method thereof

A technology of intrathecal injection and aconitine, which is applied in the field of medicine, can solve the problems of difficulty in producing qualified products, excessive degradation of related substances, and low therapeutic index, and achieve rapid onset, small dose, and good analgesic effect Effect

Pending Publication Date: 2016-06-29
云南扬软生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The existing technology of aconitine (especially aconitine) injection has the problem of poor stability, which leads to the degradation of related substances exceeding the standard (>5.0%) in the product during the sterilization process, making it difficult to produce qualified products. Therefore, there is no injection now listed products
This technical solution solves two long-standing technical problems of aconitine (especially aconitine) injections—poor stability and low therapeutic index

Method used

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  • Aconitine injection for intrathecal injection and preparation method thereof
  • Aconitine injection for intrathecal injection and preparation method thereof
  • Aconitine injection for intrathecal injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1. Aconitin A injection prescription consists of (1000):

[0051] Aconitin 0.04g

[0052] Hydrobromic acid (47%) 0.011g

[0053] Water for injection 500ml

[0054] The preparation process of Aconitin A injection of the present invention is as follows: under 100-level laminar flow conditions, add 400ml of water for injection at 20-49°C in a beaker, carefully add 0.010g of hydrobromic acid (47%) and stir evenly under heat preservation , add 0.04g of aconitin, continue to stir until dissolved, and then add 0.001g of hydrobromic acid (47%) dissolved in 10ml of water for injection at 20 to 49°C under stirring to adjust the pH to 4.5 to 6.0, filter, and add 20 Water for injection at ~49°C to a total volume of 500ml, filtered through a 0.2μm membrane, and aseptically filled into 0.5ml / bottle, to obtain the Aconitin A injection for intrathecal injection with a specification of 0.5ml:0.04mg.

Embodiment 2

[0055] Embodiment 2. The prescription of Aconitin prefilled injection is (1000):

[0056] Aconitin 0.02g

[0057] Hydrobromic acid (47%) 0.006g

[0058] Water for injection 250ml

[0059] The preparation process of aconitin prefilled injection of the present invention is as follows: under 100-level laminar flow conditions, add 200ml of water for injection at 20-49°C in a beaker, carefully add 0.005g of hydrobromic acid (47%) under heat preservation Stir evenly, add 0.02 g of aconitin, continue to stir until dissolved, then add 0.006 g of hydrobromic acid (47%) dissolved in 10 ml of water for injection at 20 to 49 ° C under stirring to adjust the pH to 4.5 to 6.0, filter, and replenish Add water for injection at 20-49°C to a total volume of 250ml, filter with a 0.2μm membrane, and aseptically fill each 0.25ml into a pre-filled syringe to form a pre-filled 0.02mg of aconitin injection. According to the pharmacopoeia aconitin standard, it is tested by HPLC, and the related su...

Embodiment 3

[0060] Embodiment 3. Aconitin freeze-dried powder injection prescription is (1000):

[0061] Aconitine 0.20g

[0062] Hydrobromic acid 0.017ml (47%)

[0063] L-Mannitol 10g

[0064] The preparation process of the Aconitin freeze-dried powder injection of the present invention is as follows: under the condition of grade 100, the hydrobromic acid is first dissolved in 90ml of water for injection at 20-49°C to completely dissolve it; Add 0.2g of the element, dissolve under stirring, add water for injection at 20-49°C to 200ml, mannitol 10g, stir until dissolved, add water for injection at 20-49°C to 1000ml. Filtration, the filtrate is filtered through a 0.4 μm membrane, finely filtered by a 0.2 μm membrane, and the fine filtrate is sent to a packaging machine, divided into 1.0ml (2ml vials) per bottle, covered with a slotted lid, and sent to a freeze vacuum dryer. Quickly cool to -40°C for 2-3 hours, turn on the vacuum pump to reduce pressure, gradually increase the temperatur...

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Abstract

The invention discloses an aconitine injection for intrathecal injection and a preparation method thereof. Aconitine refers to a compound with a structural feature in the formula shown in the description, wherein R1-R18 represent H or OH or X or OX, the X comprises Me, Ac, Bzl, a para methoxyphenyl formyl group and an o-acetamido benzoyl group, but not limited to the groups. The dosage of the aconitine injection ranges from 0.02 mg to 20 mg per bottle, and the aconitine injection is used for treating pain; the preparation forms comprise the injection, a freeze-dried powder injection, a prefilled injection and the like which are delivered through injection; the dosage is decreased to about one-tenth of original dosage, the toxic and side effects are greatly reduced, and the safety window and the therapeutic index are increased, processing of an aconitine preparation is completed through a low-temperature technology at the temperature lower than 50 DEG C, impurities produced through high-temperature hydrolysis of the aconitine are avoided, and therefore qualified products can be produced in a batched mode.

Description

technical field [0001] The invention belongs to the injection in the technical field of medicine, in particular to an aconitine injection for intrathecal injection and a preparation method thereof. Background technique [0002] Pain is caused by stimuli that can damage or destroy body tissues and is a protective adaptation to the surrounding environment. After being received by pain receptors, this pain-inducing stimulus passes through different levels of pain conduction pathways, and finally reaches the brain, causing pain sensation. Pain conduction pathways in the central nervous system are mainly the new spino-thalamic tract, the old spino-thalamic tract, the spinal-cervical tract, the posterior chordal-medial lemniscus, and the proper spinal cord tract. The main pain transmission is the spinal-cervical tract. , whose main neuronal cell bodies are located in the dorsal horn of the spinal cord. [0003] Intrathecal drug infusion therapy refers to the infusion of pain rel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K31/439A61P29/00
CPCA61K9/0019A61K9/0085A61K9/08A61K9/19A61K31/439A61K47/02A61K47/12A61K47/26
Inventor 任杨帆
Owner 云南扬软生物科技有限公司
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