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Lappaconitine hydrochoric acid, its production method and its uses in preparing analgetic

A technology of high urine and its production method, which is applied in antipyretics, drug combinations, non-central analgesics, etc., and can solve problems such as side effects, slow onset time, slow analgesic onset, etc.

Inactive Publication Date: 2007-05-16
韦璧瑜 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the 1980s, it was officially used as a drug in clinical practice. It was clinically verified by 12 hospitals in Lanzhou and two hospitals in Shanghai. The analgesic effect of 385 cases of various pains, regardless of intravenous infusion, intramuscular injection, or oral administration, was all the same. It has a curative effect, with a marked rate of 49.09% and a total effective rate of 87.27%. Its onset time is slightly slower than that of meperidine, but its maintenance time is longer
[0003] Due to the insoluble in water of homogenin hydrobromide, if the patient needs the water injection of higher concentration of homogenin hydrobromide during treatment, there will be certain difficulties; at the same time, due to its insoluble in water, it The absorption in the body is also affected, resulting in a slow onset of pain relief
In addition, free bromide ions have certain side effects in the body, and a small number of patients will have allergic reactions. It is reported that bromide ions also have suspected carcinogenic effects.

Method used

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  • Lappaconitine hydrochoric acid, its production method and its uses in preparing analgetic
  • Lappaconitine hydrochoric acid, its production method and its uses in preparing analgetic

Examples

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Effect test

Embodiment 1

[0017] The preparation of embodiment 1 homogenate hydrochloride

[0018] The production method of quinine hydrochloride of the present invention uses the method of 93100499.3 patent, which is to immerse the aconitum head in ethanol, heat and reflux extraction, filter, and further purify, and prepare the obtained quinine crystals, which are dissolved in ethanol or methanol , the filtrate is concentrated under reduced pressure, ethanol is recovered, and concentrated until crystals appear on the wall of the vessel; stand still, precipitate out; add hydrochloric acid solution dropwise, shake well, make the Congo red test paper just turn blue, place, precipitate crystals, filter, and use for crystallization Rinse with a small amount of ethanol or methanol solvent, and dry to obtain homogenate hydrochloride.

Embodiment 2

[0019] The analgesic test result of embodiment 2 homogenate hydrochloride

[0020] Experiments on mice showed that the analgesic effect of orally administered homogenin hydrobromide was slightly faster than that of homogenin hydrobromide, and the duration of analgesia was comparable.

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Abstract

The invention discloses a manufacturing method of alcaine high-sinomontanine and application in the anodyne, which comprises the following steps: dissolving high-sinomontanine through alcohol or carbinol; dripping alcaine solution; stewing; eluting; crystallizing; filtering; washing crystallization through little solvent; drying.

Description

technical field [0001] The present invention relates to a new compound goujiaine hydrochloride, its production method and its application in the preparation of analgesics. Background technique [0002] Aconitum sinomontanea (Radix aconiti sinomontanea) is the dried taproot of Ranunculaceae plant Aconitum sinomontanum Nakai, which is pungent, bitter, warm and poisonous in nature and flavor. Before the 1980s, it had never been used clinically as a single drug or its active ingredient. In the 1970s, one of the applicants studied the diterpenoid alkaloids in aconitum, and extracted several alkaloids from it. The main component of aconitine was determined to be rabaaconitine ( Lappaconitine) has a good analgesic effect, and it is made into homogenate hydrobromide for clinical use. The results show that it has a strong analgesic effect, and is non-addictive, non-teratogenic, and will not Cumulative poisoning occurs. In the 1980s, it was officially used as a drug in clinical pra...

Claims

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Application Information

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IPC IPC(8): C07D225/04A61K31/55A61P29/00
Inventor 韦璧瑜方圣鼎
Owner 韦璧瑜
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