Monolauryl phosphate-containing lithontriptic for litholysis of cholesterol gallstone

A technology of laurel phosphate and stone dissolving agent, which is applied in the direction of ether/acetal active ingredients, medical preparations of non-active ingredients, pharmaceutical formulas, etc., can solve problems such as high pressure, uncomfortable and irritating odor, and achieve Obvious curative effect, reduce irritating odor and other side effects, weaken the effect of irritating odor

Inactive Publication Date: 2012-08-08
PEKING UNIV +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since methyl tert-butyl ether was used as a stone-dissolving agent, many scholars at home and abroad have carried out relevant research on the toxic and side effects of methyl tert-butyl ether. The experimental results show that methyl tert-butyl ether is basically safe for the human body, but It has certain defects as a stone-dissolving agent alone. For example, although the boiling point of methyl tert-butyl ether is 55.7°C, which is higher than human body temperature, methyl tert-butyl ether is relatively volatile. the problem of high pressure
At the same time, methyl tert-butyl ether produces a very unpleasant pungent odor

Method used

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  • Monolauryl phosphate-containing lithontriptic for litholysis of cholesterol gallstone
  • Monolauryl phosphate-containing lithontriptic for litholysis of cholesterol gallstone
  • Monolauryl phosphate-containing lithontriptic for litholysis of cholesterol gallstone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation of stone dissolving agent:

[0032] In order to determine the dissolving ability of stone-dissolving agents with different contents of monolauryl phosphate to cholesterol within the specified time, add 3mL of methyl tert-butyl ether to six 10mL stoppered colorimetric tubes, and then add 0.00g , 0.30g, 0.60g, 0.90g, 1.20g, 1.50g of monolauryl phosphate to make a solution.

[0033] Dissolved Cholesterol:

[0034] Cholesterol was gradually added to these 6 test tubes, and after vortexing for 3 minutes, the amount of dissolved cholesterol was calculated respectively.

[0035] Experimental results:

[0036] Listed in table 1 along with the increase of monolauryl phosphate amount, the dissolving situation of cholesterol in this stone-dissolving agent.

[0037]Table 1:

[0038] The amount of methyl tert-butyl ether (mL)

[0039] As can be seen from the experimental results in Table 1, when 0.30g monolauryl phosphate was added to 3mL of methyl te...

Embodiment 2

[0041] Preparation of stone dissolving agent:

[0042] Prepare the stone-dissolving agent according to the ratio of 3 mL of methyl tert-butyl ether to 0.60 g of monolauryl phosphate.

[0043] Dissolving human gallstones:

[0044] Take a gallstone sample taken from a human body, its infrared spectrum is as follows figure 1 As shown in the upper figure, the lower figure is the standard infrared spectrum of cholesterol. Depend on figure 1 The sample was determined to be a cholesterol gallstone. The shape photo of the gallstone before being dissolved by the stone-dissolving agent is as follows image 3 mentioned.

[0045] The gallstone sample is gradually added into the prepared stone-dissolving agent, and the gallstone is basically dissolved after 18 to 20 minutes under ultrasonication, leaving only a small amount of insoluble residue.

[0046] figure 2 It is a comparison between the infrared spectrum of the gallstone sample and the infrared spectrum of the residue le...

Embodiment 3

[0049] Preparation of stone dissolving agent:

[0050] Prepare the stone-dissolving agent according to the ratio of 3 mL of methyl tert-butyl ether to 1.20 g of monolauryl phosphate.

[0051] Dissolving human gallstones:

[0052] Get a cholesterol gallstone sample from human body as in Example 2. Gradually add the gallstone sample into the prepared stone-dissolving agent. Under the ultrasonic wave, the gallstone will be basically dissolved after 13 to 15 minutes, leaving only a small amount of insoluble residue. The photo of its shape is similar to Figure 4 In that way, and the diameter of these residues is basically less than 1mm.

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Abstract

The invention relates to a monolauryl phosphate-containing lithontriptic for litholysis of cholesterol gallstone. The monolauryl phosphate-containing lithontriptic comprises methyl tertiary butyl ether and monolauryl phosphate, wherein based on 1mL of methyl tertiary butyl ether, the mass of used monolauryl phosphate is in a range of 0.05 to 0.60g. The monolauryl phosphate-containing lithontriptic can correspondingly reduce saturated vapor pressure and smell irritation of methyl tertiary butyl ether and thus the novel monolauryl phosphate-containing lithontriptic can be used in non-operative clinical therapies for patients suffering from cholesterol gallstone.

Description

technical field [0001] The present invention relates to a novel calculus-dissolving agent for dissolving cholesterol type calculus, especially the dissolving agent contains monolauryl phosphate. Background technique [0002] With the improvement of living standards, the incidence of gallstones is increasing year by year. According to statistics, at present, about 10% of the population at home and abroad are enduring the pain caused by gallstones. Therefore, it is necessary to explore an effective method for treating gallstones. urgent. [0003] At present, surgical removal of the gallbladder is the main method for the treatment of gallbladder stones, but cholecystectomy not only has high treatment costs, but also has a high risk of operation. At the same time, removing the gallbladder will bring some inconvenience to people's future life. In addition, some patients, such as the elderly, infirm, obese, and other vital organ diseases, are not suitable for cholecystectomy at a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/08A61K47/24A61P1/16
Inventor 刘微李晓佩凌晓锋李昕徐怡庄周孝思吴瑾光
Owner PEKING UNIV
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