BAPTA and application of derivant thereof in preparing analgesic drugs

A technology of derivatives and uses, applied in the field of BAPTA and its derivatives, can solve the problems of no dependence potential and poor effect, and achieve the effect of rapid action and fast onset.

Inactive Publication Date: 2010-01-27
HENGXING PHARMA INST HEFEI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Analgesics can generally be divided into opioids and non-opioids. Opioid analgesics can be used for severe pain or moderate pain. The representative drug is morphine, but these drugs have varying degrees of dependence. After repeated use, patients will To produce physical and mental dependence on it, the indications must be strictly controlled and its use restricted; the classic non-opioid analgesic is aspirin, which is mainly used for patients with mild pain, and has poor effect on severe pain or intractable pain , they are generally considered to have no dependent potential

Method used

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  • BAPTA and application of derivant thereof in preparing analgesic drugs
  • BAPTA and application of derivant thereof in preparing analgesic drugs
  • BAPTA and application of derivant thereof in preparing analgesic drugs

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Embodiment Construction

[0028] BAPTA reacts with acetoxymethyl group to form acetoxymethoxy tetranitrile (BAPTA-AM). BAPTA-AM has high fat solubility, and plays a role in the cell through the cell membrane, so it is also called "cell permeable" sex". BAPTA-AM is processed into liposomes together with suitable excipients to solve the key problems in pharmacy, so that BAPTA-AM can be administered intravenously with rapid action and rapid onset. HXB-08 is the water-soluble disodium salt of BAPTA, the molecular formula is C 42 H 62 N 2 O 12 Na 2 .

[0029] The present invention utilizes BAPTA derivatives to directly and rapidly reduce the concentration of free calcium in cells and reduce or eliminate the effect of calcium overload. , BAPTA-AM, BAPTA-AM liposome, HXB-08 conducted a more systematic study of analgesic effect, to understand the intensity of its analgesic effect, to evaluate its time-effect and dose-effect relationship.

[0030] Research on the analgesic effect of BAPTA derivatives:

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Abstract

The invention discloses a BAPTA and an application of a derivant thereof, in particular to an application of the derivant in preparing analgesic drugs. Clinical indications include headache, prosopalgia, dysmenorrheal, postoperative pain, cancer pain, viscera pain, postherpetic neuralgia, phantom limb pain, HIV, pathologic pain related to multiple sclerosis, morphine class medicine tolerance or addiction patient pain and serious chronic intractable pain or usual clinical pain diseases.

Description

technical field [0001] The present invention relates to the use of a class of compounds and derivatives thereof, in particular the use of BAPTA and derivatives thereof. Background technique [0002] Pain is a very common clinical symptom, which can make patients have unpleasant emotions such as tension, anxiety, anxiety, fear, etc. Severe pain can lead to shock. Pain relievers reduce pain sensations and alter emotional responses to pain. Analgesics can be generally divided into opioid and non-opioid. Opioid analgesics can be used for severe pain or moderate pain, and the representative drug is morphine, but such drugs have different degrees of dependence, and patients will suffer from repeated use. Physical dependence and mental dependence must be strictly controlled and the use must be restricted; the classic non-opioid analgesic drug is aspirin, which is mainly used for patients with mild pain, and has poor effect on severe pain or intractable pain , they are generally c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/216A61K31/25A61P29/00A61P25/04
Inventor 刘经星魏伟宋必卫储昭兴
Owner HENGXING PHARMA INST HEFEI
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