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Tablet containing trelagliptin or trelagliptin succinate and preparation method of tablet

A technology of trelagliptin succinate and tableting, which is applied to the preparation field of tablets containing trelagliptin or its succinate, and can solve the problem of poor compressibility and enlargement of tablets. It can solve the problems of dosage size, inconvenience of granulation, etc., to achieve the effect of good dissolution, simple process operation and good stability.

Inactive Publication Date: 2017-05-17
BEIJING SHENLANHAI BIO PHARM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The need to deliver higher doses of trexagliptin or its succinate salt compared to once-daily dosing increases tablet size and reduces compliance in some patients, such as infants and elderly patients. This product has a large specification and poor compressibility
At the same time, due to the good solubility of this product, it will cause agglomeration during the granulation process, causing inconvenience in granulation, and then affecting the dissolution of the sample.

Method used

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  • Tablet containing trelagliptin or trelagliptin succinate and preparation method of tablet
  • Tablet containing trelagliptin or trelagliptin succinate and preparation method of tablet
  • Tablet containing trelagliptin or trelagliptin succinate and preparation method of tablet

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Experimental program
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Effect test

Embodiment 1

[0019] Embodiment 1: preparation embodiment

[0020]

[0021]

[0022] Preparation Process:

[0023] (1) prepare hydroxypropyl methylcellulose aqueous solution to make binder, for subsequent use;

[0024] (2) Trexagliptin succinate crude drug is pulverized through an 80 mesh sieve;

[0025] (3) The bulk drug is mixed with mannitol, microcrystalline cellulose and croscarmellose sodium in equal amounts;

[0026] (4) Add adhesive to make soft material by wet method, stir quickly, shear quickly, granulate with 20 mesh, dry, and granulate with 30 mesh;

[0027] (5) Add sodium stearyl fumarate and microcrystalline cellulose to the above mixture, mix well and press into tablets with a tablet weight of 180mg and a hardness of 7-9kg. Opadry coating, weight gain of about 3.0%

Embodiment 2

[0028] Embodiment 2: preparation embodiment

[0029]

[0030] Preparation Process:

[0031] (1) prepare the aqueous solution of hydroxypropyl cellulose to make binder, for subsequent use;

[0032] (2) Trexagliptin succinate crude drug is pulverized through an 80 mesh sieve:

[0033] (3) The bulk drug is mixed with mannitol, microcrystalline cellulose-internal addition and croscarmellose sodium-internal addition in equal amounts;

[0034] (4) Add adhesive to make soft material by wet process, stir quickly, shear quickly, granulate with 20 mesh, dry, and granulate with 24 mesh;

[0035] (5) Add microcrystalline cellulose-extra, croscarmellose sodium-extra and lubricant to the above mixture, mix well and press into tablets with a tablet weight of 90 mg and a hardness of 5-7 kg. Opadry coated, approximately 3.0% weight gain.

Embodiment 3

[0036] Embodiment 3: preparation embodiment

[0037]

[0038] Preparation Process:

[0039] (1) prepare the aqueous solution of hydroxypropyl cellulose to make binder, for subsequent use;

[0040] (2) Trexagliptin succinate crude drug is pulverized through an 80 mesh sieve;

[0041] (3) The bulk drug is mixed with mannitol, microcrystalline cellulose-internal addition and croscarmellose sodium in equal amounts;

[0042] (4) Add adhesive to make soft material by wet process, stir quickly, shear quickly, granulate with 20 mesh, dry, and granulate with 24 mesh;

[0043] (5) Add microcrystalline cellulose-additive and lubricant to the above mixture, mix well and press into tablets with a tablet weight of 180 mg and a hardness of 7-9 kg. Opadry coated, approximately 3.0% weight gain.

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Abstract

The invention relates to a tablet containing trelagliptin or trelagliptin succinate and a preparation method of the tablet, and belongs to the technical field of medicine preparations. The tablet can be singly used or jointly used together with other oral hypoglycemic agents, and is suitable for a patient with Type II diabetics. The tablet contains the trelagliptin or the trelagliptin succinate, a thinner, an adhesive, a disintegrant and a lubricant. The preparation method of the tablet containing the trelagliptin or the trelagliptin succinate comprises the following steps of (1) obtaining of medicine particles: uniformly mixing the trelagliptin or the trelagliptin succinate, the disintegrant and / or the thinner, adding a proper amount of adhesive, and granulating, so as to obtain the medicine particles; (2) obtaining of tabletting particles: uniformly mixing the medicine particles, the lubricant, the disintegrant and / or the thinner, so as to obtain the tabletting particles; (3) compression and forming: compressing and forming the tabletting particles by proper equipment. The tablet containing the trelagliptin or the trelagliptin succinate has the advantages that the dissolvability is good, the stability is good, the technology operation is simple and convenient, and the like; the technology is simple, the repeatability is good, and the tablet is especially suitable for industrial production.

Description

technical field [0001] The invention relates to a troxagliptin succinate tablet, specifically, a tablet containing troxagliptin or a succinate thereof. The present invention also relates to a preparation method of Trexagliptin Succinate Tablets. The preparation process of Trexagliptin Succinate Tablets by the method of the present invention is simple and stable, and is particularly suitable for industrial production. The prepared Trexagliptin Succinate Tablets It has the advantages of good reproducibility, good dissolution, good drug stability, and simple process operation. Background technique [0002] Trelagliptin is a once-weekly dipeptidyl peptidase IV (DPP-4) inhibitor, which controls blood sugar levels through selective and sustained inhibition of DPP-4. Trelagliptin is given weekly One dose of medicine, unique mechanism of action, has unique advantages such as no hypoglycemia, no weight gain, and less side effects, and the incidence of gastrointestinal adverse reacti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/513A61P3/10
Inventor 黄慧玲卫聪聪李桐
Owner BEIJING SHENLANHAI BIO PHARM TECH
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