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A sustained release agent improving anoxia endurance

A slow-release and tolerance technology, applied in the field of pharmaceutical preparations, can solve the problems of electrolyte imbalance, slow onset of action, and side effects such as oral liquid diarrhea.

Inactive Publication Date: 2014-11-12
CHANGZHOU HI TECH DISTRICT MULTIPLE DIMENSION IND TECH INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The most commonly used drugs to improve hypoxia tolerance are diuretics such as acetazolamide, and there are also adrenal cortex hormones such as dexamethasone and aminophylline. However, these drugs cannot be used for a long time due to their toxic side effects. Use, such as long-term use of acetazolamide can easily cause adverse reactions such as electrolyte disturbance in the body
In addition, traditional Chinese medicine preparations containing Rhodiola are commonly used for the prevention and treatment of hypoxia. This kind of traditional Chinese medicine preparation can help improve the body's adaptability to hypoxia, reduce the stress response and improve the effect of hypoxia tolerance. Traditional Chinese Medicine works slowly and has limited effect
Chinese patent application number 200310104871.X discloses that levocarnitine has the effect of preventing and treating altitude sickness, but because of its low bioavailability, the oral liquid has side effects such as diarrhea and cannot be used in large quantities, and the effect is limited. clinical reports
[0005] Obviously, there is still a lack of a drug that can be used for a long time, has no obvious adverse reactions, can be used for prevention and treatment, and can effectively improve hypoxia tolerance in the market.

Method used

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  • A sustained release agent improving anoxia endurance
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  • A sustained release agent improving anoxia endurance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment one: Observe the effect of levocarnitine + trimetazidine hydrochloride orally in different dosage ratios on normal pressure hypoxia in mice, and verify the effect of the patented composition on improving hypoxia tolerance

[0023] Trimetazidine hydrochloride: 0.15, 1.2, 9.6mg / kg equivalent to human daily dose of 1, 8, 64mg;

[0024] Levocarnitine: 15, 120, 960 mg / kg, approximately equivalent to 0.1, 0.8, 6.4 g of human daily dose;

[0025] Select 100 male mice, weighing 20±2g, and randomly divide them into 10 groups according to body weight, 10 mice in each group, orally administer 20ml / kg, and the blank control group is given equal volume of normal saline, 1 time / day, for 7 consecutive days 1 hour after the last administration, the mice in each group were put into 160ml jars with 5g of soda lime in advance, one for each bottle, and then the bottle caps were sealed tightly with vaseline, and the death of the mice was recorded as an indicator. Survival time,...

Embodiment 2

[0030] Embodiment two: Comparison of Levocarnitine 960mg / kg + Trimet Hydrochloride 9.6mg / kg and Single Oral Administration on Normal Pressure Hypoxia in Mice

[0031] 40 male mice, weighing 20±2g, were randomly divided into 4 groups according to body weight, 10 mice in each group, administered by intragastric administration at 20ml / kg, and the blank control group was given equal volume of normal saline, once a day, for 7 consecutive days 1 hour after the last administration, the mice in each group were put into 160ml jars with 5g of soda lime in advance, one for each bottle, and then the bottle caps were sealed tightly with vaseline, and the death of the mice was recorded as an indicator. survival time. The results are shown in Table 2.

[0032] Table 2 Comparison of survival time against hypoxia under normal pressure (n=10, ±S)

[0033] Group / Dose (mg / kg) Survival time (min) Prolonged survival time (%) normal control group 21.5±5.6 - Trimetazid...

Embodiment 3

[0036] Embodiment three: To observe the effects of different ratios of levocarnitine + trimetazidine hydrochloride on hypobaric hypoxia in rats, and to study the pharmacological mechanism of improving hypoxia tolerance

[0037] Trimetazidine hydrochloride: 2, 4, 6mg / kg, approximately equivalent to the daily dose of 20, 40, 60mg for humans;

[0038] Levocarnitine: 200, 400, 600mg / kg, approximately equivalent to 2, 4, 6g of human daily dose;

[0039] Select 70 Wister rats, weighing 150g to 190g, and randomly divide them into 7 groups: normoxia control group: raise and collect materials in plain areas; acute hypoxia group: place animals in a hypobaric oxygen chamber, and the oxygen partial pressure in the chamber is 11.01 Kpa (approximately equivalent to the partial pressure of oxygen at an altitude of 5000m) after continuous decompression and hypoxia for 3 days, and then placed in a hypobaric oxygen chamber with an oxygen partial pressure of 13.25Kpa (approximately equivalent ...

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Abstract

The present invention discloses a slow-release agent for increasing hypoxia tolerance; the slow-release agent is a composition formed by combining trimetazidine or pharmaceutically acceptable salt thereof and L-carnitine or derivative thereof or pharmaceutically acceptable salt thereof, according to the ratio 1:1.6-6400.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a slow-release agent for improving hypoxia tolerance. Background technique [0002] Hypoxia refers to the pathological process of abnormal changes in tissue metabolism, function, and morphological structure due to insufficient oxygen supply or oxygen use disorder in tissues. Hypoxia can be divided into four types: hypotonic hypoxia, anemic hypoxia, circulatory hypoxia, and tissue hypoxia. Among them, anemic hypoxia and tissue hypoxia belong to oxygen use disorders, and hypotonic hypoxia and Cyclic hypoxia is a deficiency of oxygen supply. [0003] A large number of free radicals produced by hypoxia damage the stability of mitochondrial membranes, resulting in damage to the function and structure of body tissues and energy metabolism disorders. general hypoxic manifestations such as hypoxia, nausea, vomiting, palpitation, shortness of breath, shortness of breath, rapi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61K47/38A61K47/32A61P39/00A61K31/205
CPCA61K31/205A61K31/495A61P9/10A61P39/00A61K2300/00
Inventor 谢和兵李庆宜顾书华吕伟红
Owner CHANGZHOU HI TECH DISTRICT MULTIPLE DIMENSION IND TECH INST
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