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Disodium sulfodehydroabietate (DSDA) and composition and application thereof

A technology of disodium abietic acid and dehydroabietic acid, which is applied in drug combination, digestive system, drug delivery, etc.

Active Publication Date: 2009-12-02
ZHEJIANG ASEN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] It can be seen that the scope of protection of the above application is very wide. When treating inflammatory bowel diseases, all salts with sulfonated dehydroabietic acid belong to the scope of protection, but in such a broad scope of protection, it can be supported by instructions It is only the monosodium salt of sulfodehydroabietic acid, and other salts of sulfodehydroabietic acid are not supported by the instructions. Their pharmacological effects and clinical application are worthy of further study

Method used

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  • Disodium sulfodehydroabietate (DSDA) and composition and application thereof
  • Disodium sulfodehydroabietate (DSDA) and composition and application thereof
  • Disodium sulfodehydroabietate (DSDA) and composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0203] Preparation of disodium sulfonated dehydroabietic acid:

[0204] (1) Preparation of abietic acid

[0205] Take 5 kg (about 15.5 mol) of golden yellow 310 resin, that is, rosin calcium grease, crush it, place it in a three-necked flask equipped with a stirrer and a reflux condenser, add 3 L of industrial ethyl acetate (about 30.6 mol) and 600 ml of hydrochloric acid, Adjust the pH value to 3-4, heat and reflux under stirring, react for 1 hour, stop stirring and let stand for a while, so that the insoluble matter settles completely, pour out the supernatant while it is hot, and place the supernatant for crystallization (about 2 days). Filtrate, wash the filter cake with an appropriate amount of ethyl acetate, combine the lotion and filtrate, concentrate and recover about 1L of ethyl acetate, continue to place it for crystallization, crystallize and filter out, then wash with industrial ethyl acetate, dry the crystallization, and obtain crude abietic acid A total of 2225g...

Embodiment 2

[0215] Preparation of disodium sulfonated dehydroabietic acid granules, capsules and solutions:

[0216] (1) The weight proportion of combination and the binder selected in each prescription are listed in Table 8

[0217] The weight proportion of combination and the adhesive selected for use in each prescription of table 8 Unit: gram

[0218] Raw materials

Prescription 1

Prescription 2

Prescription 3

Prescription 4

Prescription 5

Prescription 6

Prescription 7

Sulfonated dehydroabietic acid II

Sodium (calculated as anhydrous)

500

500

500

500

500

500

500

lactose

300

400

500

400

300

400

500

aspartame

70

40

70

70

40

70

90

Adhesive

10% pvp

water

30% B

Alcohol

70% B

Alcohol

95%

ethanol

10% pvp B

alcohol solution

5%...

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Abstract

The invention discloses disodium sulfodehydroabietate (DSDA) and a composition, a preparation method and application thereof in medicaments for preventing hyperacid peptic ulcer and gastrointestinal inflammation. A patent application disclosed by CN00818150.0 is of the opinion that monosodium sulfodehydroabietate is superior to disodium salt, but does not further disclose test conditions and data conclusion; moreover, the pharmacological action and clinical application of the disodium salt deserve further research. The invention compares the in-vitro acid making effects of monosodium salt and the disodium salt, the dissolution of the monosodium salt and the disodium salt in artificial gastric juice and intestinal juice as well as the clinical efficacies in treating gastric ulcer, acute gastritis and acute attack of chronic gastritis. Results show that DSDA has the advantages that DSDA has stronger acid-making capability during treating the gastric ulcer, acute gastritis and acute attack of chronic gastritis and faster dissolution speed in stomach and intestine; and medicaments prepared from the DSDA have better curative effect and quick response.

Description

technical field [0001] The present invention relates to sulfonated dehydroabietic acid disodium, in particular to sulfonated dehydroabietic acid disodium, its composition, preparation method and its use in medicines for preventing and treating hyperacidity peptic ulcer and gastrointestinal inflammatory disease application. Background technique [0002] The compound sulfonated dehydroabietic acid was reported as early as the 1930s as an intermediate for the preparation of pure dehydroabietic acid; its derivatives were reported in the 1970s as detergents, but as drugs, especially for gastric Drug research for the prevention or treatment of intestinal diseases is very rare. [0003] Gastrointestinal diseases are one of the common and frequently-occurring diseases, among which ulcer disease is the most common, and the total incidence rate accounts for about 10-20% of the world's population. Gastrointestinal diseases include: peptic ulcer, gastritis, intestinal disease (here re...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61P1/04A61K9/16A61K9/48A61K9/08
CPCA61K31/192A61P1/04
Inventor 邓金明吴海英张平一
Owner ZHEJIANG ASEN PHARMA
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