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Azilsartan osmotic pump type controlled release tablets and preparation method thereof

A controlled-release tablet and osmotic pump technology, which is applied in the direction of pharmaceutical formulations, non-active ingredient medical preparations, and active ingredient-containing medical preparations, can solve the problem of preparation of azilsartan osmotic pump controlled-release tablets that have not been reported process, cannot be made into a primary osmotic pump, and the preparation process is complex, etc., to achieve stable and effective blood drug concentration, reduce drug side effects and medication times, and release drug residues.

Inactive Publication Date: 2018-08-24
ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But for poorly soluble drugs, because of their solubility (C s ) is low, it is difficult to form a higher concentration and osmotic pressure in the microenvironment of the tablet core to maintain an effective drug release rate, or to maintain a sustained and constant osmotic pressure requires a large amount of osmotic pressure enhancer (beyond the normal tablet weight range), therefore, insoluble drugs generally cannot be made into primary osmotic pumps like water-soluble drugs, and each insoluble drug has its own characteristics. It is a research topic and also a difficult point in this technical field. Many medical researchers are doing research, trying to find meaningful major discoveries; of course, insoluble drugs can be formulated with double-layer osmotic pumps The technology enables the drug and the drug-containing layer polymer to be pushed out of the release hole by the booster layer polymer in the form of a suspension to achieve the purpose of constant drug release, but its complicated preparation process limits its wide application
At present, there is no report of this kind of azilsartan osmotic pump type controlled release tablet and related preparation process.

Method used

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  • Azilsartan osmotic pump type controlled release tablets and preparation method thereof
  • Azilsartan osmotic pump type controlled release tablets and preparation method thereof
  • Azilsartan osmotic pump type controlled release tablets and preparation method thereof

Examples

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preparation example Construction

[0050] 1 Preparation of Azilsartan Osmotic Pump

[0051] Preparation process and influencing factors of azilsartan osmotic pump controlled-release tablets

[0052] 1.1 Preparation process

[0053] Tablet core: Pass azilsartan, sodium chloride, PEO-N10, sodium lauryl sulfate SDS, and lactose through an 80-mesh sieve, weigh according to the prescription amount, mix them by equal addition method, add 95% ethanol solution to prepare Soft material, granulate with 20 mesh sieve, dry at 40°C for 6h, add appropriate amount of magnesium stearate and mix well.

[0054] Preparation of coating solution: Weigh the prescribed amount of cellulose acetate and dissolve it in acetone to prepare a certain concentration of cellulose acetate acetone solution, add a certain amount of PEG4000, and stir on a magnetic stirrer without heating until until the solution is completely dissolved.

[0055] Tablet compression and coating: install the upper and lower punches, adjust the tablet weight and pr...

Embodiment 1

[0147] The azilsartan osmotic pump type controlled-release preparation of this embodiment: the azilsartan osmotic pump type controlled release tablet is a single-chamber single-layer osmotic pump type controlled-release tablet, and the single-chamber single-layer osmotic pump type controlled-release tablet includes a tablet core And the controlled-release semi-permeable coating film with drug release holes wrapped around the tablet core:

[0148] The tablet core includes the following components by weight percentage:

[0149]

[0150]

[0151] The controlled-release semi-permeable coating film is prepared by using a semi-permeable film coating liquid, and the semi-permeable film coating liquid includes the following components by mass-volume ratio:

[0152] Coating material 5% (mass volume ratio, mg·mL -1 );

[0153] Porogen 0.5% (weight to volume ratio, mg·mL -1 ).

[0154] In terms of weight percentage, the weight of the controlled-release semipermeable coating fil...

Embodiment 2

[0172] The azilsartan osmotic pump type controlled-release preparation of this embodiment: the azilsartan osmotic pump type controlled release tablet is a single-chamber single-layer osmotic pump type controlled-release tablet, and the single-chamber single-layer osmotic pump type controlled-release tablet includes a tablet core And the controlled-release semi-permeable coating film with drug release holes wrapped around the tablet core:

[0173] The tablet core includes the following components by weight percentage:

[0174]

[0175] The controlled-release semi-permeable coating film is prepared by using a semi-permeable film coating liquid, and the semi-permeable film coating liquid includes the following components by mass-volume ratio:

[0176] Coating material 10% (mass volume ratio, mg·mL -1 );

[0177] Porogen 20% (weight to volume ratio, mg·mL -1 ).

[0178] In terms of weight percentage, the weight of the controlled-release semipermeable coating film is 10% of ...

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Abstract

The invention discloses azilsartan osmotic pump type controlled release tablets. The azilsartan osmotic pump type controlled release tablets are monolithic osmotic pump type controlled release tabletsand comprise table cores and controlled release semi-transparent coating films which coat the peripheries of the table cores and have drug release holes. The tablet cores comprise components in percentage by weight as follows: 2%-10% of azilsartan, 35%-40% of an osmotic pressure active substance, 5%-15% of a surfactant, 15%-25% of a suspending agent and the balance of a filling agent and / or lubricating agent. The controlled release semi-transparent coating films are prepared from a semi-transparent film coating liquor comprising the components in mass-volume ratio as follows: 5%-10% of a coating material (in mass-volume ratio mg.mL<-1>) and 0.5%-20% of a pore-forming agent (in weight-volume ratio mg.mL<-1>). The controlled released tablets are monolithic osmotic pump type controlled release tablets and have the characteristics of zero-level drug release, and the long-acting stable pressure reducing effect of azilsartan can be realized due to constant plasma concentration of drug.

Description

technical field [0001] The invention relates to an azilsartan osmotic pump type controlled-release tablet and a preparation method thereof. Background technique [0002] Azilsartan is a new generation selective AT 1 Subtype angiotensin Ⅱ receptor antagonist (ARBs) antihypertensive drugs, developed by Takeda Pharmaceutical Company of Japan, was approved for marketing in Japan in January 2012. Compared with angiotensin-converting enzyme inhibitor (ACEI) antihypertensive drugs, azilsartan has the advantages of less side effects and no dry cough. Compared with other angiotensin receptor antagonist antihypertensive drugs, it has Better antihypertensive ability and greater receptor binding ability. Azilsartan has poor water solubility, which is not conducive to release, which limits its clinical application. And through preliminary experiments, it is found that although azilsartan has a long half-life, it is not yet known whether it can maintain a constant effective concentrati...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/36A61K9/32A61K31/4245A61K47/38A61K47/32A61K47/36A61K47/10A61P9/12
CPCA61K9/2027A61K9/205A61K9/2054A61K9/284A61K9/2846A61K9/2853A61K9/2866A61K9/2893A61K31/4245A61P9/12
Inventor 汪电雷樊玲黄鹏杨晔
Owner ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE