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Chiral drug intercalation hydrotalcite and its preparing method

A technology of chiral drugs and hydrotalcites, which is applied in the direction of pharmaceutical formulations, drug combinations, organic active ingredients, etc., to achieve effective storage effects

Inactive Publication Date: 2006-10-25
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although hydrotalcite has been widely used in the field of medicine (such as antacids, anti-inflammatory drugs, anti-osteoporosis drugs, etc.), there is no related hydrotalcite-like layered materials used in the treatment of chiral anti-Parkinson's disease at home and abroad. Literature and patent reports in the field of pharmaceuticals

Method used

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  • Chiral drug intercalation hydrotalcite and its preparing method
  • Chiral drug intercalation hydrotalcite and its preparing method
  • Chiral drug intercalation hydrotalcite and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Step A: take by weighing 15.36g Mg(NO 3 ) 2 .6H 2 O and 11.25g Al(NO 3 ) 3 .9H 2 O dissolved in 150ml to remove CO 2 , deionized water to prepare a mixed salt solution, and another 7.2g NaOH was dissolved in 200ml to remove CO 2 , deionized water and placed in a 500mL four-necked flask; using the single-drop co-precipitation method, in a 70°C water bath, N 2 Slowly add the salt solution of the former to the alkali solution of the latter under protection and strong stirring conditions, adjust the pH value to 10.0, and react for 40 hours; wash and filter the product until pH3 -Mg 2 Al-LDHs, its Mg 2+ / Al 3+ =2.

[0025] Step B: According to the molar ratio of chiral drug levodopa / hydrotalcite precursor = 3, first weigh 0.6g (about 3mmol) Levodopa and dissolve it in 400mL to remove CO 2 , deionized water and placed in a 500mL four-necked flask; then weigh 3.6g (about 1 mmol) of the filter cake made by step A and add it, shielded from light, N 2 Protect, vigorous...

Embodiment 2

[0029] Step A: Take a method similar to step A in Example 1 to prepare NO 3 -Mg 2 Al-LDHs precursor.

[0030] Step B: According to the molar ratio of chiral drug levodopa / hydrotalcite precursor = 2, first weigh 0.8g (about 4mmol) Levodopa and dissolve it in 400mL to remove CO 2 , deionized water and placed in a 500mL four-neck flask; then weigh 7.0g (about 2mmol) of the filter cake made by step A and add it, shielded from light, N 2 Protect, vigorously stir, adjust the pH to 7.8, ion exchange at room temperature for 2 days; the product is used to remove CO 2 1. Washing and centrifuging with deionized water for 5 times, drying the precipitate at room temperature in vacuum, and then obtaining a layered composite material containing levodopa anion between layers.

[0031] Step C: Carry out in vitro simulated release test by adopting a method similar to Step C in Example 1, so as to obtain the release curve.

[0032] Elemental analysis can give the chemical formula Mg 4.64 al...

Embodiment 3

[0034] Step A: Take a method similar to step A in Example 1 to prepare NO 3 -Mg 2 Al-LDHs precursor.

[0035] Step B: According to the method similar to Step B in Example 2, after the first ion exchange reaction 2d, the product uses CO 2 , washed with deionized water, and centrifuged for 5 times to obtain a precipitated product.

[0036] Step C: Weigh 0.5g (about 2.5mmol) Levodopa dissolved in 400mL to remove CO 2 , deionized water and placed in a 500mL four-necked flask; 2 Under the conditions of protection and strong stirring, add the precipitate obtained from the above step B to the system, adjust the pH to 7.8, and perform the second ion exchange at room temperature for 2 days; the product is used to remove CO 2 1. Washing and centrifuging with deionized water for 5 times, drying the precipitate at room temperature in vacuum, and then obtaining a layered composite material containing levodopa anion between layers.

[0037] Step D: Take the method similar to Step C in ...

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Abstract

The present invention provides a chiral medicine intercalated hydrotalcite and its preparation method. The described chiral medicine is levodopa, said chiral medicine levodopa can be inlaid into the interlamination of hydrotalcite so as to obtain the invented product chiral medicine intercalated hydrotalcite with the effect of resisting Parkinson's disease. Said invention also provides its chemical structure formula.

Description

technical field [0001] The invention belongs to the technical field of anti-Parkinson's disease drugs, and in particular provides a chiral drug-intercalated hydrotalcite and a preparation method thereof. technical background [0002] Parkinson's disease, commonly known as parkinsonism, is a common neurological disorder that mainly affects middle-aged and elderly people, and mostly occurs after the age of 60. Symptoms include involuntary tremors of the hands, head or mouth at rest, muscle stiffness, slow movement, and postural balance disturbances, leading to inability to take care of oneself. According to research, a group of nerve cells called substantia nigra neurons located in the midbrain of the human brain regulate the motor function of the brain by synthesizing a neurotransmitter called "dopamine". When these substantia nigra neurons degenerate and die When it reaches more than 80%, the symptoms of Parkinson's disease will appear. [0003] Levodopa is the precursor o...

Claims

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Application Information

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IPC IPC(8): A61K31/198A61K47/02A61K47/52A61P25/16
Inventor 段雪卫敏郭剑何静
Owner BEIJING UNIV OF CHEM TECH
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