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Lappaconitine hydrobromide is a diterpenoid alkaloid, lappaconitine, isolated from the buttercup plant Gaultheria procumbens, which is chemically known as (1alpha,14alpha,16beta)-20-ethyl-1,14,16-trimethoxyaconitane-4,8,9-triol 4-[2-(acetylamino)benzoate hydrobromide monohydrate compound.
It is the first non-addictive analgesic new drug in China. It has analgesic, antipyretic, decongestive and local anaesthesia effects, and has no addictive and accumulative effects, and its analgesic effect is stronger than that of indomethacin and weaker than that of morphine.
Uses and Function of Lappaconitine Hydrobromide.
Kojic acid hydrobromide, an alkaloid derived from Kojic acid, is a non-addictive, long-acting analgesic. It has a strong analgesic effect that is slow acting but long lasting. In addition, hypericin hydrobromide has local anaesthetic, hypothermic, antipyretic and anti-inflammatory effects.
It has been found that hypericin hydrobromide inhibits ectopic discharges induced by axonal injury by affecting voltage-dependent sodium channels in the central nervous system.
Compared with pethidine, hypericin hydrobromide has comparable analgesic effects, with a slightly slower onset of action and a longer duration of maintenance; the analgesic effect is seven times that of the antipyretic-analgesic aminopyrine. Indications include all kinds of moderate pain, cancer pain, postoperative pain, sciatica and so on.
It should be noted that allergy is prohibited, pregnant women and cardiac patients with caution.
Pharmacological Effect of Lappaconitine Hydrobromide.
1, Analgesic effect of intraperitoneal injection of hypericin hydrobromide can significantly alleviate the thermal hyperalgesia of chronic constriction injury (CCL) rats, to achieve analgesic therapeutic effect, and there is no significant toxicity.
2、Anti-inflammatory effect: Gauramin has obvious inhibitory effect on xylene-induced ear shell swelling in mice, arthritic foot swelling in rats and agar granuloma proliferation in rats.
It shows that gao wu mai has the effect of anti-acute and chronic inflammation, which provides a theoretical basis for the use of gao wu mai in the clinical treatment of rheumatism, rheumatoid arthritis caused by pain, redness and swelling.
3、Anti-tumour effect: The tumor inhibition rate of hypericin on mouse hepatocellular carcinoma was 11.20%-53.08%, and the tumor inhibition rate on mouse S180 was 29.81%-53.%.
It shows that Gauracoside hydroxamic acid has a certain effect on mouse hepatocellular carcinoma S180, and it has no obvious effect on the body mass of mice.
4、Anti-arrhythmic effect of hypericin can improve the normal threshold of arrhythmia induced by aconitine in rats, and can significantly improve the myocardial ischaemic arrhythmia in dogs, thus reducing the incidence of arrhythmia, and the mechanism of its action may be to block the sodium channel.
Extraction method of Bulk Lappaconitine Hydrobromide Powder.
The high aconite tuber crushed → add to the extraction tank with ethanol immersion 1h, heating reflux 3h3 times → concentration, with 2% of the hydrochloric acid acid acidification, filtration → add ammonia alkaline to PH9-10, stirring precipitation, filtration → precipitate dissolved with trichloromethane → add process water, static stratification → add anhydrous potassium carbonate stirring dehydration, pumping under reduced pressure to the paste → ethanol solubilisation, recycling of ethanol to the crystallisation of the precipitate → to obtain the high aconitine
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