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Supermolecular intercalation-structure slow-release captopril and its preparing method

A slow-release and slow-release agent technology, which is applied in the field of supramolecular intercalation structure slow-release captopril and its assembly, to achieve the effect of suppressing odor, good slow-release effect, and good taste

Inactive Publication Date: 2005-07-20
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The literature (Abubakr O.Nur, Jun S.Zhang, Int.J.Pharm.194 (2000) 139-146) reviewed the research progress in the controlled release of captopril in recent years, but the porous inorganic material water There is no relevant report on the preparation of captopril sustained-release preparation with talc as carrier

Method used

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  • Supermolecular intercalation-structure slow-release captopril and its preparing method
  • Supermolecular intercalation-structure slow-release captopril and its preparing method
  • Supermolecular intercalation-structure slow-release captopril and its preparing method

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Experimental program
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Effect test

Embodiment 1

[0037] 1. Add Zn(NO 3 ) 2 ·6H 2 O(5.3545g) and Al(NO 3 ) 3 9H 2 O (2.2508g) is made into mixed salt solution A with Zn / Al molar ratio equal to 3 with 80ml water; In addition, NaOH (2.5000g) / captopril original drug (3.9114g) is made into molar ratio equal to 3 with 120ml water The mixed alkali solution B;

[0038] 2. In N 2 Under protection, slowly drop the mixed salt solution A into the vigorously stirred mixed alkali solution B, after the addition is complete, adjust the pH to 8.5 with 0.1M NaOH;

[0039] 3. The obtained slurry was crystallized at 25° C. for 48 hours, suction filtered, washed, and vacuum-dried at room temperature for 72 hours to obtain captopril-intercalated zinc-aluminum LDH. The water used in the process is decarbonized deionized water.

[0040] The obtained Cpl-LDHs were characterized by X-ray powder diffraction, the results are shown in figure 1 ,Depend on figure 1 It can be seen that the Cpl-LDHs has the crystal structure of hydrotalcite-like...

Embodiment 2

[0044] According to the synthesis process of Example 1, change step 2 to drop the mixed salt solution A and the mixed alkali solution B into deionized water at the same time, stir vigorously, control the pH to 9, and crystallize the obtained slurry at 25°C for 48 hours, and filter with suction , washed, and vacuum-dried at room temperature for 72 hours to obtain captopril-intercalated zinc-aluminum LDH. The water used in the process is decarbonized deionized water.

[0045] Adopt the method of embodiment 1 to analyze product, obtain its chemical formula / formation as:

[0046] [Zn 0.732 Al 0.268 (OH) 2 ](C 9 h 14 NO 3 S - ) 0.268 0.9H 2 O, captopril content is 33.2%, water content is 9.3%.

Embodiment 3

[0048] Zn(NO 3 ) 2 ·6H 2 O(35.6815g), Al(NO 3 ) 3 9H 2 O (22.6103g), NaNO 3 (9.0712g) is made into the mixed salt solution A that Zn / Al molar ratio is 3 with 160ml water, and NaOH (12.0282g) is made into alkaline solution B with 100ml water in addition, N 2 Under protection, slowly drop the alkaline solution B into the mixed salt solution A, stir vigorously, and stop the dropwise addition when the pH is 6.5. The slurry was crystallized at 70°C for 24 hours, then suction filtered, washed with water, and dried at 70°C for 18 hours to obtain zinc aluminum nitrate hydrotalcite.

[0049] The original drug of captopril (4.0000g) and the prepared zinc-aluminum nitrate hydrotalcite (3.0000g) were mixed in 100ml of water at a molar ratio of 4, and the pH was adjusted to 6.5 with 0.1M NaOH, and the resulting slurry was heated at 25°C After crystallization for 48 hours, suction filtration, washing, and vacuum drying at room temperature for 72 hours, the captopril-intercalated zinc...

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Abstract

The present invention relates to a supermolecular intercalation structure slow-released captopril and its preparation method. Said invention uses anionic lamellar material LDH as main body, uses captopril as intercalation guest, and utilizes two soluble metal salts to make them into a mixed salt solution, then makes said mixed salt solution and alkali solution of captopril undergo the process of intercalation assembling treatment so as to obtain supermolecular structure CpI-LDHs. Said invention also provides its chemical formula. In said slow-released captopril preparation the mass percentage content of captopril is 20-50% and the mass percentage content of water is 5-20%, and its slow-released efficiency duration can be up to 0.5 hr-12hr.

Description

Technical field: [0001] The invention relates to a drug sustained-release agent and a preparation method thereof, in particular to a supramolecular intercalation structure sustained-release captopril and an assembly method thereof. Background technique: [0002] At present, in response to the requirements of developing safe, efficient, economical and convenient sustained-release drugs, traditional drugs are used to create new dosage forms to realize the research and application of drug-controlled release systems with controllable drug release quantity, release time and release space. increasingly people's attention. The pharmaceutical sustained-release dosage forms developed based on traditional medicines can maintain a specific concentration at a point of action for a long time and have fewer side effects when administered, so they have the following advantages: (1) make the medicine release slowly and prolong the lasting effect; 2) Reduce toxicity; (3) Reduce side effects...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/127A61K9/24A61K31/401A61K47/00A61K47/48A61P9/04A61P9/12A61P19/02
CPCA61K9/1275A61K47/48961B82Y5/00A61K31/401A61K47/6949A61P9/04A61P9/12A61P19/02
Inventor 段雪张慧徐向宇
Owner BEIJING UNIV OF CHEM TECH
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