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Alogliptin benzoate tablet and preparation method thereof

A technology for alogliptin tablets and benzoic acid, which is applied in the field of alogliptin benzoate tablets and preparation thereof, can solve the problems of cumbersome steps, high cost and high equipment requirements, and achieves simple preparation steps, good dissolution rate, cost reduction effect

Active Publication Date: 2014-06-25
NEW FOUNDER HLDG DEV LLC +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of this method is that the powder direct compression method has high requirements for equipment and workshops, especially for equipment. In addition, it also has high requirements for auxiliary materials. Generally, special auxiliary materials for powder direct compression are required. Comprehensive higher cost
This method not only has the disadvantage of cumbersome steps, but also uses croscarmellose sodium as a disintegrant, and the inventors found in the course of their research that when wet granulation was used, croscarmellose sodium was used Sodium as a tablet disintegrant will cause the active ingredient alogliptin benzoate to interact with the disintegrant, affecting the dissolution rate of the tablet
Although this patent adopts a complete external addition method to the disintegrant croscarmellose sodium, thereby avoiding direct contact between croscarmellose and water, however, if left for too long, the main drug will still occur. Interaction with disintegrants, thereby affecting tablet dissolution

Method used

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  • Alogliptin benzoate tablet and preparation method thereof
  • Alogliptin benzoate tablet and preparation method thereof
  • Alogliptin benzoate tablet and preparation method thereof

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preparation example Construction

[0073] The method for preparing alogliptin benzoate tablet of the present invention can also be such method, and it comprises the following steps:

[0074] i) Mix alogliptin benzoate, filler, disintegrant in 1 / 2 formula amount, add binder solution, and make soft material;

[0075] ii) sieving the soft material to prepare wet granules, and drying;

[0076] iii) Whole granules, add disintegrants, glidants and lubricants in the remaining formulation amount, and mix to form a mixture;

[0077] iv) compressing the mixture obtained in step iii) to form tablets;

[0078] v) Optionally, coating the tablet obtained in step iv) to make a coated tablet.

[0079] The standards and definitions of suitable soft materials can be defined in accordance with the 6th edition of "Pharmacy" published by People's Health Publishing House in April 2008 (editor-in-chief Cui Fude).

[0080] In a specific embodiment of the present invention, the method includes: mixing alogliptin benzoate with mannit...

Embodiment 1

[0094] (1) Prescription (per tablet)

[0095]

[0096] (2) Preparation process

[0097] Mix the raw material with mannitol, then add microcrystalline cellulose and 1 / 2 formula amount of cross-linked polyvinylpyrrolidone, and add an appropriate amount (about 10ml / 100 tablets) of 3(w / v)% hydroxypropylmethylcellulose Aqueous solution, to obtain soft material, pass through 18-mesh sieve to granulate, dry at 60°C for 1 hour, pass through 18-mesh sieve for granulation, add the remaining cross-linked polyvinylpyrrolidone, colloidal silicon dioxide and magnesium stearate, and tablet to obtain Tablets are coated with Opadry.

Embodiment 2

[0099] (1) Prescription (per tablet)

[0100]

[0101] (2) Preparation process

[0102] Mix the raw material drug with mannitol, then add microcrystalline cellulose and 1 / 2 formula amount of low-substituted hydroxypropyl cellulose, and add an appropriate amount of 3 (w / v)% hydroxypropyl methylcellulose aqueous solution to obtain soft material, granulated through a 18-mesh sieve, dried at 60°C for 1 hour, granulated through a 18-mesh sieve, added the remaining low-substituted hydroxypropyl cellulose, colloidal silicon dioxide and magnesium stearate, and compressed to obtain tablets. The resulting tablets were coated with Opadry.

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Abstract

The invention provides an alogliptin benzoate tablet and a preparation method thereof. The alogliptin benzoate tablet of the invention comprises alogliptin benzoate tablet, a disintegrating agent, a filler, an adhesive, a flow aid and a lubricant, wherein the disintegrating agent is selected from crosslinked polyvinylpyrrolidone or low-substituted hydroxy propyl cellulose. The method of the invention adopts wet granulation, is low in requirements for equipment and auxiliary materials, and reduces cost; the preparation steps are simple; the effective component of alogliptin benzoate in the tablet of the invention does not interact with the disintegrating agent; the tablet is good in dissolubility; in the preparation process, the adding mode of the disintegrating agent can be selected randomly; the alogliptin benzoate tablet of the invention has good stability, and can keep stable under conditions of high temperature and high humidity.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to an alogliptin benzoate tablet and a preparation method thereof. Background technique [0002] The chemical name of alogliptin benzoate is (R)-2-[(6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-di Hydropyrimidin-1(2H)-yl)methyl]benzonitrile benzoic acid, the molecular formula is C 18 h 21 N 5 o 2 ·C 7 h 6 o 2 , the molecular weight is 461.5, and the CAS number is 850649-62-6. The chemical structural formula of alogliptin benzoate is as shown in formula I: [0003] [0004] Formula 1. [0005] Alogliptin benzoate is a serine protease dipeptidyl peptidase (DPP-IV) inhibitor developed by Takeda Corporation of Japan. like peptide-1, GLP-1), glucagon-like peptide-1 is a hormone that promotes insulin secretion. Alogliptin benzoate can maintain the levels of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) in the body, promote the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K9/36A61K31/513A61K47/38A61K47/32A61P3/10
Inventor 易崇勤贾增荣杨俊郑少辉郭欲晓
Owner NEW FOUNDER HLDG DEV LLC
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