5-amino-salicylic acid intercalation medicinal slow-release agent and production thereof

A technology of aminosalicylic acid and sustained-release agent, applied in the field of 5-aminosalicylic acid sustained-release dosage form and its assembly, to achieve the effect of suppressing peculiar smell, good taste and good sustained-release effect

Inactive Publication Date: 2007-01-31
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And take the porous inorganic material hydrotalcite as carrier to prepare 5-aminosalicylic acid slow-release dosage form and there is no report yet

Method used

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  • 5-amino-salicylic acid intercalation medicinal slow-release agent and production thereof
  • 5-amino-salicylic acid intercalation medicinal slow-release agent and production thereof
  • 5-amino-salicylic acid intercalation medicinal slow-release agent and production thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 1. Add Zn(NO 3 ) 2 ·6H 2 O (1.788g, 0.006mol) and Al(NO 3 ) 3 9H 2 O (0.56g, 0.0015mol) is equal to 4 and is made into mixed solution A with 100ml water according to Zn / Al molar ratio, in addition NaOH (0.5g, 0.0125mol) and 5-amino salicylic acid former drug (0.60g, 0.004mol ) Mix solution B with 50ml of water at a molar ratio equal to 3:1.

[0035] 2. Put the mixed solution A in the container, under N 2 Under protection, the mixed solution B was slowly dropped into the vigorously stirred mixed solution A, and after the addition was completed, the pH was adjusted to 8.5 with 0.1M NaOH.

[0036] 3. The resulting slurry was crystallized at 60°C for 48 hours, filtered, washed, and dried in an oven at 60°C for 8 hours to obtain 5-aminosalicylic acid intercalated zinc-aluminum LDH. The water used in the process is decarbonized deionized water.

[0037] The obtained 5-ASA-LDHs is characterized by X-ray powder diffraction, and the results are shown in figure 1 ,Depen...

Embodiment 2

[0041] Step 1 is the same as embodiment 1;

[0042] Step 2: Drop mixed solution A and mixed solution B into a container filled with deionized water at the same time, stir vigorously, and control the pH to 8.5;

[0043] Step 3: crystallize the obtained slurry at 60°C for 48h, filter with suction, wash, and dry in an oven at 60°C for 8h to obtain 5-aminosalicylic acid intercalated zinc-aluminum LDH. The water used in the process is decarbonized deionized water.

[0044] Adopt the method for embodiment 1 to analyze product, obtain its chemical formula / formation as: [Zn 0.79 Al 0.20 (OH) 2 ](C 7 h 6 NO 3 ) 0.20 0.86H 2 O, 5-aminosalicylic acid content of 17.98%, water content of 12.27%;

Embodiment 3

[0046] Mg(NO 3 ) 2 ·6H 2 O (1.14g, 0.0045mol) and Al(NO 3 ) 3 9H 2 O (0.56g, 0.0015mol) is equal to 3 and is made into mixed solution A with 50ml water according to Mg / Al molar ratio, in addition NaOH (0.4g, 0.01mol) / 5-amino salicylic acid former drug (0.60g, 0.004mol )) Mix solution B, N with 150ml of water at a molar ratio equal to 2.5:1 2 Slowly drip the mixed alkali solution into the salt solution under protection, stir vigorously, and adjust the pH to 10 with 0.1M NaOH after the addition is complete. The slurry was crystallized at 60°C for 18 hours, suction filtered, washed, and dried at 60°C for 8 hours to obtain 5-aminosalicylic acid intercalated magnesium aluminum LDH. The water used in the process is decarbonized deionized water.

[0047] Adopt the method for embodiment 1 to analyze product, obtain its chemical formula / form as: Mg 0.74 Al 0.26 (OH) 2 (C 7 h 6 NO 3 -1 ) 0.18 (CO 3 2- ) 0.04 0.7H 2 O, 5-aminosalicylic acid content of 26.6%, water cont...

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Abstract

A slow-releasing intercalated 5-aminosalicilic acid 5-ASA-LDHs is proportionally prepared from two soluble metallic salts (LDHs) and 5-aminosalicilic acid (5-ASA) through preparing the mixed solution of LDHs, preparing the alkaline solution of 5-ASA, and intercalating reaction between them.

Description

Technical field: [0001] The invention relates to a drug sustained-release agent and a preparation method thereof, in particular to a 5-aminosalicylic acid sustained-release dosage form and an assembly method thereof. Background technique: [0002] With the high development of modern medicine, people pay more and more attention to the research and application of drug controlled release system in medicine. Therefore, it has always been the focus of research to seek drugs with advantages such as long-acting, high efficiency, low toxicity, sustained release, good selectivity, and small side effects. Based on the drug sustained-release dosage form, when administered, it can maintain a specific concentration at a point of action for a long time and has fewer side effects, so it has the following advantages: (1) slow drug release and prolonged effect; (2) reduce toxicity (3) reduce side effects; (4) enhance selectivity; improve efficacy; (5) easy to use, etc. [0003] 5-aminosali...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/606A61K9/22A61K9/00A61K47/02A61P1/00A61K31/60
Inventor 段雪张慧邹亢徐向宇
Owner BEIJING UNIV OF CHEM TECH
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