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Sodium rabeprazole enteric-coated sustained-release microsphere preparation method and oral solid preparation containing sodium rabeprazole enteric-coated sustained-release microspheres

A technology of rabeprazole sodium and sustained-release microspheres, which is applied in the preparation of rabeprazole sodium enteric-coated sustained-release microspheres and in the field of oral solid preparations, can solve the problem of poor acid resistance of oral solid preparations of rabeprazole sodium, and Low sealing rate and other problems, to achieve good slow-release characteristics, low production cost, good acid resistance effect

Inactive Publication Date: 2018-12-25
CHANGZHOU SUNLIGHT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Rabeprazole sodium oral solid preparations prepared by conventional methods have the disadvantages of poor acid resistance and low encapsulation efficiency

Method used

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  • Sodium rabeprazole enteric-coated sustained-release microsphere preparation method and oral solid preparation containing sodium rabeprazole enteric-coated sustained-release microspheres

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0028] The preparation method of the rabeprazole sodium enteric-coated sustained-release microspheres of this example is as follows:

[0029] ①Dissolve 300g rabeprazole sodium and 300g Eudragit L 100 (weight ratio 1:1) in 2400g medicinal ethanol to obtain a mixed solution.

[0030] ②Set the inlet temperature of the spray dryer (Yamato DL410) to 100°C, the atomization pressure to 0.1MPa, and the air volume to 0.8m 3 / min, the above-mentioned mixed solution is spray-dried, and the spray-dried powder is then vacuum-dried to obtain rabeprazole sodium enteric-coated sustained-release microspheres.

Embodiment 1）

[0032] The rabeprazole sodium enteric-coated sustained-release microspheres prepared in Example 1 were used to make capsules, and the formula is shown in Table 1.

[0033] Table 1

[0034] Element

[0035] The preparation method is as follows: Weigh the rabeprazole sodium enteric-coated sustained-release microspheres, magnesium oxide, lactose, polyvinylpyrrolidone, hydroxypropyl cellulose and crospovidone prepared in Example 1 according to the prescription amount, and mix them uniformly Add an appropriate amount of ethanol as a wetting agent to make soft materials, granulate with a 24-mesh sieve, dry in an oven at 50±5°C, pass through a 24-mesh sieve for granulation, then add magnesium stearate, mix evenly to obtain granules, and fill 2 #Capsule, the content of each capsule weighs about 120mg.

（ example 2）

[0037] The preparation method of the rabeprazole sodium enteric-coated sustained-release microspheres of this example is as follows:

[0038] ①Dissolve 300g rabeprazole sodium and 600g Eudragit S 100 (weight ratio 1:2) in 2400g purified water to obtain a mixed solution.

[0039] ②Set the inlet temperature of the spray dryer (Yamato DL410) to 100°C, the atomization pressure to 0.1MPa, and the air volume to 0.8m 3 / min, the above-mentioned mixed solution is spray-dried, and the spray-dried powder is then vacuum-dried to obtain rabeprazole sodium enteric-coated sustained-release microspheres.

[0040] The rabeprazole sodium enteric-coated slow-release microspheres that this example makes carries out scanning electron microscope observation, and the results are shown in figure 1 .

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Abstract

The invention discloses a sodium rabeprazole enteric-coated sustained-release microsphere preparation method and an oral solid preparation containing sodium rabeprazole enteric-coated sustained-release microspheres. The method includes: dissolving sodium rabeprazole and eudragit to obtain mixed solution, subjecting the mixed solution to spray drying, and then performing vacuum drying to obtain thesodium rabeprazole enteric-coated sustained-release microspheres. The oral solid preparation is prepared from the sodium rabeprazole enteric-coated sustained-release microspheres and pharmaceuticallyacceptable auxiliary materials. The enteric-coated sustained-release microspheres prepared from sodium rabeprazole according to a special process are high in acid resistance and encapsulation efficiency and have great sustained-release chacteristics, and the method is simple in operation, low in production cost and suitable for industrial production. Pharmaceutical preparations prepared from thesodium rabeprazole enteric-coated sustained-release microspheres are effective in reduction of the in-vitro dissolution rate and dissolubility of sodium rabeprazole, and accordingly bioavailability isimproved, and commercial feasibility is realized.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a preparation method of rabeprazole sodium enteric-coated sustained-release microspheres and an oral solid preparation containing rabeprazole sodium enteric-coated sustained-release microspheres. Background technique [0002] Digestive system disease is one of the common frequently-occurring diseases, among which peptic ulcer is the main one, often accompanied by serious complications, such as gastric ulcer and duodenal ulcer can be complicated by upper gastrointestinal bleeding, perforation, etc. A lot of pain and a serious threat to people's health. [0003] Rabeprazole sodium is a new generation of benzimidazole substitute after omeprazole and lansoprazole, and it is a strong inhibitor of the proton pump in the parietal cell tip secretion membrane. Rabeprazole sodium specifically inhibits H + -K + - The activity of ATPase, which has an inhibit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/4439A61K47/32A61P1/04A61P31/04A61P7/04
CPCA61K9/5026A61K31/4439A61P1/04A61P7/04A61P31/04
Inventor 胡国宜胡锦平黄健丁盛何继文陈佳琪
Owner CHANGZHOU SUNLIGHT PHARMA
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