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Slow-release prepn. contg. alpha-lipoic acid or its derivatives, and preparing method therefor

A sustained-release preparation, lipoic acid technology, applied in the field of biomedicine, can solve problems affecting biological activity and achieve the effect of prolonged and sustained release

Inactive Publication Date: 2006-11-29
ZHUJIANG HOSPITAL SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] α-lipoic acid or its derivatives are thermally unstable compounds. Since the current conventional tablets are melt-extruded by hot cutting method, the temperature is generally 50-200°C, which may thermally decompose α-lipoic acid and affect its biological activity. At present, there is no report on the development of sustained-release preparations of α-lipoic acid or its derivatives that are practical and can maintain the drug effect for a long time

Method used

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  • Slow-release prepn. contg. alpha-lipoic acid or its derivatives, and preparing method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045]The prescription of the double-layer sustained-release tablet whose main ingredient is R-(+)-α-lipoic acid is:

[0046] Sustained-release drug raw material components and content are:

[0047] R-(+)-alpha-lipoic acid 200 mg

[0048] Lactose 10mg

[0049] Hydroxypropyl Methyl Cellulose 125 mg

[0050] Ethylcellulose 20 mg

[0051] 1.5% hydroxypropyl methylcellulose solution 40 mg

[0052] Talc 5 mg

[0053] Magnesium stearate 2mg

[0054] The components and content of the raw material of the long-release drug are:

[0055] R-(+)-alpha-lipoic acid 100 mg

[0056] Starch 10 mg

[0057] 6% polyvinylpyrrolidone solution 10 mg

[0058] Talc 2 mg

[0059] Magnesium stearate 2mg

[0060] The film coat composition and content of this double-layer sustained-release tablet are:

[0061] Hydroxypropyl Methyl Cellulose 4 mg

[0062] Macrogol 400 6 mg

[0063] Titanium dioxide 0.5 mg

[0064] Talc 1mg

[0065] 80ml food grade ethanol

[0066] water 20ml

[0067] The ...

Embodiment 2

[0079] The main ingredient is S-(-)-α-lipoic acid The prescription of the double-layer sustained-release tablet is:

[0080] Sustained-release drug raw material components and content are:

[0081] S-(-)-alpha-lipoic acid 250 mg

[0082] Lactose 10mg

[0083] Hydroxypropyl Methyl Cellulose 125 mg

[0084] Ethylcellulose 20 mg

[0085] 1.5% hydroxypropyl methylcellulose solution 40 mg

[0086] Talc 5mg

[0087] Magnesium stearate 2mg

[0088] The components and content of the raw material of the long-release drug are:

[0089] S-(-)-alpha-lipoic acid 50 mg

[0090] Starch 10 mg

[0091] 6% polyvinylpyrrolidone solution 10 mg

[0092] Talc 2 mg

[0093] Magnesium stearate 2mg

[0094] The film coat composition and content of this double-layer sustained-release tablet are:

[0095] Hydroxypropyl Methyl Cellulose 4mg

[0096] Macrogol 400 6 mg

[0097] Titanium dioxide 0.5 mg

[0098] Talc 1mg

[0099] 80ml food grade ethanol

[0100] water 20ml

[0101] The prep...

Embodiment 3

[0113] The prescription of sustained-release tablets whose main drug is a mixture of R-(+)-α-lipoic acid and S-(-)-α-lipoic acid is:

[0114] Blend of R-(+)-alpha-lipoic acid and S-(-)-alpha-lipoic acid 300mg

[0115] Lactose 10mg

[0116]Hydroxypropyl Methyl Cellulose 125 mg

[0117] Ethylcellulose 20 mg

[0118] 1.5% hydroxypropyl methylcellulose solution 40 mg

[0119] Talc 5mg

[0120] Magnesium stearate 2mg

[0121] The film coat component and content of this layer sustained-release tablet are:

[0122] Hydroxypropyl Methyl Cellulose 4mg

[0123] Macrogol 400 6 mg

[0124] Titanium dioxide 0.5 mg

[0125] Talc 1mg

[0126] 80ml food grade ethanol

[0127] water 20ml

[0128] The preparation process of this slow-release tablet is as follows:

[0129] Mixture of R-(+)-α-lipoic acid and S-(-)-α-lipoic acid, starch, hydroxypropylmethylcellulose, ethylcellulose, microcrystalline cellulose, sodium starch glycolate According to the composition and content of the pre...

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Abstract

A slow-release tablet of alpha-thioctic acid or its derivative used as medicine, food additive, or cosmetic has a single slow-release layer made of hydroxypropyl methylcellulose or one slow-release layer plus one ordinary-release layer for quickly releasing the alpha-thioctic acid or its derivative. Its preparing process is also disclosed.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a sustained-release preparation of alpha-lipoic acid or a derivative thereof and a preparation method thereof. Background technique [0002] α-lipoic acid (LA) is known as the "universal antioxidant" and is the most effective known natural antioxidant. Its chemical name is 1,2-dithiolane- 3-pentanoic acid. In animal and plant tissues, LA is usually covalently bound to the ε-amino group of lysine residues in protein molecules, and exists in the form of amide bonds. The plant with the highest LA content is spinach, followed by tomato and cabbage; LA content is the highest in liver and kidney tissues in animals. LA is a cofactor for pyruvate dehydrogenase. It is a metabolic antioxidant that can be converted into reduced dihydrolipoic acid (DHLA) in the body, with the molecular formula C 8 h 14 S 2 o 2 , the molecular weight is 206.33. [0003] In recent years, the importan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/385A61K47/38A61K47/26A61K47/02A61P39/06A61P3/10A61P1/16A61P29/00A23L1/30
Inventor 季爱民王秉钧姚育法张守尧杨月莲李晓东张忠义
Owner ZHUJIANG HOSPITAL SOUTHERN MEDICAL UNIV
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