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Application of tetrodotoxin as analgesic tolerance inhibitor in preparation of compound pain relieving preparation

A technology of tetrodotoxin and inhibitors, applied in the field of biomedicine, to achieve the effects of low production cost, improved therapeutic index, and easy implementation

Active Publication Date: 2008-12-03
江苏华豚药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the inhibitors of existing analgesic drugs mainly include: NOS (nitric oxide synthase) inhibitor L-methylarginine (L-NMMA), N(G)-nitro-L-arginine (L- -NNA), N(G)-nitro-L-arginine methyl ester (L-NAME), 7-N1, etc.; In addition, CaM (calmodulin) inhibitors - trifluoperazine, CaMK II (dependent ( In) calcium-calmodulin protein kinase II) inhibitors KN-62 and KN-93, NMDA (N-methyl-D-aspartate) receptor antagonist MK801, DAMGO (enkephalin) and ketamine etc. can block the generation of morphine tolerance to varying degrees, but some inhibitors have side effects such as increased blood pressure and cross tolerance with morphine in animal experiments (Zhu Xingzu. Pharmacology Progress in Science, Beijing: People's Medical Publishing House, 1997.14; Fan GH, Wang LE, Qiu HC, et al.Mol Pharmacol, 1999, 56(1): 39; Menendez L, Hidalgo A, BaamondeA.Eur J Pharmacol, 1997, 335(1):9; CN1309562A)

Method used

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  • Application of tetrodotoxin as analgesic tolerance inhibitor in preparation of compound pain relieving preparation
  • Application of tetrodotoxin as analgesic tolerance inhibitor in preparation of compound pain relieving preparation
  • Application of tetrodotoxin as analgesic tolerance inhibitor in preparation of compound pain relieving preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Take 10g of morphine hydrochloride and dissolve it in about 900ml of water for injection, and another 5mg of TTX and dissolve it in 10m of benzoic acid with a pH of 4.5. After mixing and stirring evenly, performing fine filtration, potting, and sterilization procedures, the compound morphine hydrochloride injection (1) can be obtained.

Embodiment 2

[0038]Take 10g of morphine hydrochloride and dissolve it in about 900ml of reclaimed water for injection, and take another 10mg of TTX and dissolve it in 0.1% 1ml of dilute hydrochloric acid. After the two medicines are mixed, filter and add water for injection on the self-filter to make the mixed medicine solution reach the dose of 1000ml. , and then mixed and stirred evenly, finely filtered, potted, and sterilized to obtain the compound morphine hydrochloride injection (2).

Embodiment 3

[0040] Get TTX 1mg and morphine hydrochloride 5g, put in the container, add citrate buffer solution again in the container, the two medicines are dissolved, and after mixing and stirring evenly, carry out fine filtration, pack (each bottle of compound morphine hydrochloride The powder contains morphine hydrochloride 5 mg, TTX 1 μg), after low-temperature vacuum drying, and the bottle mouth is melt-sealed, the compound morphine hydrochloride powder can be obtained.

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Abstract

The present invention relates to the application of tetrodotoxin as analgesic tolerance inhibitor in preparing compound analgesic preparation, which may be injection, powder for injection, oral preparation, buccal tablet, spray, capsule, suppository or oil phase preparation. Tetrodotoxin can inhibit the tolerance on analgesic, produce no toxicity affecting the analgesic and raise the curative effect of analgesic. The compound analgesic preparation has the advantages of simple preparation process and low cost.

Description

technical field [0001] The invention relates to the application of tetrodotoxin as an analgesic tolerance inhibitor in the preparation of compound analgesic preparations, belonging to the field of biomedicine. Background technique [0002] Tetrodotoxin (TTX) is a marine biological neurotoxin with unique chemical structure and strong biological activity. Its molecular formula is C 11 h 17 N 3 o 8 , the molecular weight is 319.27. TTX is extremely toxic, and its toxicity is 1250 times stronger than that of sodium cyanide. Only 0.35mg-0.5mg of this dreadful toxin can kill people. Since TTX has the ability to block nerve cell membrane Na + Therefore, TTX has become a very important tool drug in the field of neurobiology and physiology research. [0003] Since the 1930s, Japan has used TTX for human analgesia, local anesthesia, antispasmodic, antipruritic and other clinical trials (Pan Xinfu, Huang Zhiqiang. Pharmacy Bulletin, 1984, 4:40), but because of the strong toxicity...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/529A61K31/485A61K31/135A61K31/4468A61K9/00A61P29/00
Inventor 黄致强黄海燕黄海枫
Owner 江苏华豚药业有限公司