Tetrodotoxin compound preparation and use thereof

A technology of tetrodotoxin and compound preparations, which is applied in the direction of medical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of high toxicity of tetrodotoxin, limited application range, and undiscovered problems, reaching Enhance analgesic effect, reduce neuropathy, and reduce toxicity

Active Publication Date: 2017-01-04
YOUCARE PHARMA GROUP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tetrodotoxin used alone also has a certain analgesic effect, and can inhibit the inflammatory pain and edema caused by formaldehyde; the combined application of tetrodotoxin and indoxacarb has synergistic analgesic and anti-inflammatory effects, and the combined use of small doses of tetrodotoxin and aspirin can significantly improve the analgesic effect. Pain curative effect, but tetrodotoxin is highly toxic, limiting its scope of application
There is no related report about the compatible use of tetrodotoxin and lidocaine in this field

Method used

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  • Tetrodotoxin compound preparation and use thereof
  • Tetrodotoxin compound preparation and use thereof
  • Tetrodotoxin compound preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1 (formula and preparation of excipient)

[0019] Excipients are prepared from stearic acid, glyceryl monostearate, lanolin, white oil, cetyl alcohol, stearyl alcohol, triethanolamine, glycerin, Tween-80, potassium hydroxide and distilled water. The components by mass fraction are: 5-15% stearic acid, 1-3% glycerol monostearate, 1-5% lanolin, 1-5% white oil, 1-5% cetyl alcohol, 1-10% stearyl alcohol, 1-3% triethanolamine, 5-15% glycerin, 1-3% Tween-80, 1-3% potassium hydroxide and 40-85% distilled water. The excipients were prepared according to the formulations shown in Table 1 and Table 2.

[0020] Formulation of table 1 excipient

[0021]

[0022]

[0023] Formulation of table 2 excipients

[0024]

[0025] Preparation of excipients:

[0026] 1. Add glyceryl monostearate, lanolin, white oil, cetyl alcohol, and stearyl alcohol in the oil phase into a 500ml beaker according to the formula, heat to 90 degrees Celsius, melt and stir evenly.

[00...

Embodiment 2

[0031] Embodiment 2 (preparation of product)

[0032] The components of tetrodotoxin compound preparation are: tetrodotoxin, lidocaine, puerarin and excipients, wherein each unit product contains: tetrodotoxin 1-600pg; lidocaine 10-60mg; puerarin 1-500mg; excipients 10-500g. Prepare product by formula shown in table 3 and table 4.

[0033] Formulation 1 of Table 3 product

[0034]

[0035]

[0036] Formulation 2 of Table 4 product

[0037]

[0038] Product preparation method:

[0039] Tetrodotoxin and lidocaine with a purity of more than 99% are dissolved in a solution with a pH of 3-5 in proportion, and added to a spare excipient ointment, vibrated by an oscillator to make it uniform, and dispensed for use.

Embodiment 3

[0040] Embodiment 3 (clinical experiment)

[0041] Clinical Trial of Tetrodotoxin Compound Preparation (Nantongting) and Its Placebo Observation in Treating 55 Cases of Diabetic Peripheral Neuralgia

[0042] 1. Clinical data

[0043] A randomized, double-blind, placebo observation method was adopted to select 55 patients with diabetic peripheral neuralgia. Wantongding group: 13 males and 34 females, aged 35-77 years, with an average age of 59.87 years, weighing 43-69kg. Placebo group: 4 males and 4 females, aged 45-71 years, average age 58.5 years, body weight 40-62 kg, pain history 3-5 years. Moderate pain (pain score 5-6) 12 people, severe pain (pain score 7--10) 43 people. Before and after the treatment, the hematological analysis of the patients was tested. All the patients were taught to use the pain visual analogue scale (VAS) (0-10cm, 0=no pain, 10=extreme pain) before the medication to record the pain intensity.

[0044] 2. How to use

[0045] The patients were ra...

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PUM

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Abstract

The invention discloses a tetrodotoxin compound preparation which comprises the following components: tetrodotoxin, lidocaine, puerarin and an excipient. The invention also discloses use of the tetrodotoxin compound preparation in the preparation of a medicament for treating neuropathic pain, wherein the neuropathic pain is diabetic peripheral neuropathic pain or neuropathic injury pain. The novel tetrodotoxin compound preparation provided by the invention is used for treating diabetic peripheral neuropathic pain and neuropathic injury pain, and has advantages of small toxic side effect, good analgesic effect and the like.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a compound preparation of tetrodotoxin and its application. Background technique [0002] Pain is a patient's perception of being hurt. Pain is associated with actual or potential injury and tissue damage caused by inflammation, ischemia, mechanical or other stimuli. It can be acute or chronic, and it cannot be accurately described or defined by a third party except the patient himself. [0003] Diabetic peripheral nerve pain is one of the various lesions that occur in the nervous system of diabetes. It is one of the most common, complex and serious complications of diabetes. It is caused by chronic hyperglycemia in diabetes and various pathophysiological changes The resulting nervous system damage can affect any part of the peripheral nervous system, including sensory nerves, motor nerves, and autonomic nerves. Clinically, limb pain, hypoesthesia, numbness, burning, coldness...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/529A61K47/26A61P3/10A61P25/02A61P25/00A61K31/167A61K31/352
CPCA61K31/167A61K31/352A61K31/529A61K47/26A61K2300/00
Inventor 付蕾于伟仕杨磊董庆滨
Owner YOUCARE PHARMA GROUP
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