Azilsartan pellet tablet and preparation method thereof

A technology of azilsartan pellets and pellets, which is applied in the fields of pill delivery, microcapsules, cardiovascular system diseases, etc. It can solve the problems of organic solvent residue, high control requirements, difficult process operation, etc., and increase the surface area , Gastric emptying effect is small, and the effect of reducing high cost

Inactive Publication Date: 2017-01-18
JIANGSU ZHONGBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent application CN102895205A discloses a fast-dissolving azilsartan pharmaceutical preparation, which is characterized in that the particle size D of azilsartan is controlled 90 ≤20μm, higher requirements for particle size control; Chinese patent application CN101528262A discloses a stable pharmaceutical composition with excellent dissolution properties, the main feature of which is the use of low-viscosity binders to improve the azilsartan Dissolution, but this method improves the effect of in vitro dissolution is limited; Chinese patent application CN103260605A discloses a kind of azilsartan solid dispersion and its preparation method and pharmaceutical composition, and carrier material is selected from povidone, poloxamer , polyethylene glycol, hydroxypropyl cellulose, and polyethylene oxide, the active ingredient and carrier material need to be dissolved in an organic solvent and then removed, the process operation is difficult, and there is a problem of organic solvent residue

Method used

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  • Azilsartan pellet tablet and preparation method thereof
  • Azilsartan pellet tablet and preparation method thereof
  • Azilsartan pellet tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: the preparation of azilsartan pellets.

[0029] (1) Preparation of Azilsartan pellets:

[0030] Weigh the components according to the following formula:

[0031]

[0032] Dissolve hypromellose E5 in 60% ethanol solution to obtain a 3.5% (w / v) adhesive solution, then add azilsartan to the adhesive solution, and after dispersing evenly, obtain the drug Coating liquid; put the sucrose blank core in the fluidized bed, start the bottom spray program, preheat, and after the temperature of the material reaches equilibrium, spray the coating liquid with the drug to obtain the core containing the drug; dissolve Opadry in In water, an 8% (w / v) coating solution was obtained, which was sprayed into a fluidized bed for film coating to obtain azilsartan pellets.

[0033] (2) Preparation of Azilsartan Micropellets:

[0034] Weigh the components according to the following formula:

[0035]

[0036] Add lactose, pregelatinized starch, hydroxypropyl cellulose, sod...

Embodiment 2

[0037] Embodiment 2: Preparation of azilsartan pellets.

[0038] (1) Preparation of Azilsartan pellets:

[0039] Weigh the components according to the following formula:

[0040]

[0041] Dissolve povidone K30 in 60% ethanol solution to obtain a 3.5% (w / v) adhesive solution, then add azilsartan to the adhesive solution, and disperse evenly to obtain a drug-coated coating solution; put the sucrose blank ball core in the fluidized bed, start the bottom spray program, preheat, and after the temperature of the material reaches equilibrium, spray into the coating solution to obtain the drug-containing ball core; dissolve Opadry in water, An 8% (w / v) coating solution was obtained, which was sprayed into a fluidized bed for film coating to obtain azilsartan pellets.

[0042] (2) Preparation of Azilsartan Micropellets:

[0043] Weigh the components according to the following formula:

[0044]

[0045]

[0046] Add microcrystalline cellulose, hydroxypropyl cellulose, low-s...

Embodiment 3

[0047] Embodiment 3: Preparation of azilsartan pellets.

[0048] (1) Preparation of Azilsartan pellets:

[0049] Weigh the components according to the following formula:

[0050]

[0051] Dissolve hydroxypropyl cellulose in 60% ethanol solution to obtain a 3.5% (w / v) binder solution, then add azilsartan to the binder solution, and after dispersing evenly, obtain a drug pack Coating liquid; put the microcrystalline cellulose blank pellet core in the fluidized bed, start the bottom spray program, preheat, and after the temperature of the material reaches equilibrium, spray the coating solution with the drug to obtain the pellet core containing the drug; put Opadry It is dissolved in water to obtain an 8% (w / v) coating solution, which is sprayed into a fluidized bed for film coating to obtain azilsartan pellets.

[0052] (2) Preparation of Azilsartan Micropellets:

[0053] Weigh the components according to the following formula:

[0054]

[0055] Add lactose, microcrystal...

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Abstract

The invention discloses an Azilsartan pellet tablet and a preparation method thereof. Specifically, the Azilsartan pellet tablet is formed by tabletting an Azilsartan pellet and a pharmaceutic adjuvant, wherein the Azilsartan pellet occupies 75 to 88 percent, and the pharmaceutic adjuvant occupies 12 to 25 percent; the Azilsartan pellet is formed from Azilsartan, a hollow pellet core, an adhesive and a coating material; the pharmaceutic adjuvant comprises a thinner, an adhesive, a disintegrant and a lubricant. The Azilsartan pellet is prepared through a fluidized bed coating technology, the content of main medicine is uniform, and then the Azilsartan pellet tablet is formed by adding the pharmaceutic adjuvant and performing tabletting, the tablet forms regular small units after entering an alimentary tract, the surface area is increased, the dissolving-out speed and the bioavailability of the tablet are improved, moreover, particles are uniformly distributed, and the release stability of the tablet is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to azilsartan pellets and a preparation method thereof. Background technique [0002] Azilsartan (English name Azilsartan, structure shown below) is an angiotensin Ⅱ receptor antagonist (sartan) drug, which is mostly used to treat hypertension, and is currently the only sartan drug in the late clinical stage It has the advantages of stable antihypertensive effect, good curative effect, long action time and less side effects shared by sartan drugs. With the increasing prevalence of hypertension year by year, sartan drugs are increasingly concerned. Azilsartan tablets, developed by Japan's Takeda Pharmaceutical Company, were approved for marketing in Japan in 2012. Compared with valsartan and olmesartan, which are currently commonly used antihypertensive drugs of the same kind, their clinical efficacy is more significant. [0003] [0004] Azilsartan is a po...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/50A61K47/38A61K31/4245A61P9/12
CPCA61K9/2081A61K9/2059A61K9/5047A61K9/5078A61K9/5089A61K31/4245
Inventor 夏彬许林菊杨健王飞唐景玉
Owner JIANGSU ZHONGBANG PHARMA
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