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Trelagliptin succinate solid preparation and preparation method thereof

A technology of troxagliptin succinate and solid preparations, which is applied in the field of solid preparations of troxagliptin succinate and its preparation, can solve the problems of product content uniformity and content not meeting quality standards, unstable dry granulation process, and Problems such as poor rolling formability of auxiliary materials have achieved the effects of good production process reproducibility, stable and controllable process parameters, and improved sticking and astringent punching problems

Pending Publication Date: 2019-07-30
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The preparation method of existing troxagliptin solid preparation adopts dry method direct compression, dry method granulation and wet method granulation technology, because bulk drug is needle-shaped crystallization, density is comparatively loose (bulk density 50%), and the raw material drug is in the form of needle-like crystals, and its self-adhesiveness is poor. If the dry granulation method is used, the rolling formability of the raw and auxiliary materials is poor, resulting in instability of the dry granulation process. Large batch-to-batch differences, cumbersome production process
If wet granulation is used, it can solve the problems of uneven mixing of materials, poor fluidity and poor material formability in the dry granulation process, but because trexagliptin succinate is unstable under hot and humid conditions, it is easy to be used in wet granulation. Reacts with excipients to produce impurities, and the stability of solid preparations is poor

Method used

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  • Trelagliptin succinate solid preparation and preparation method thereof
  • Trelagliptin succinate solid preparation and preparation method thereof
  • Trelagliptin succinate solid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Inspection of the particle size of the raw material drug: the raw material drug is processed in different ways, and the particle size of the raw material drug (D 90 ) are 294 μm, 178 μm, 154 μm, 146 μm, 97 μm, and 49 μm, respectively. Raw materials with different particle sizes were taken to investigate the effect of particle size on the tablet preparation process and tablet quality.

[0035] D. 90 (Also known as D(0.9)) indicates the particle size corresponding to when the cumulative particle size distribution number of a sample reaches 90%. Its physical meaning is that the particles with a particle size smaller than it account for 90%.

[0036] Table 1: Embodiment 1 prescription composition

[0037]

[0038] Preparation Process:

[0039] ① API pretreatment: Take an appropriate amount of trexagliptin succinate API (API) and perform the following pretreatments: untreated, passed through a 40-mesh sieve, passed through a 60-mesh sieve, passed through a 80-mesh siev...

Embodiment 2

[0080] Table 4: Embodiment 2a and 2b prescription composition

[0081]

[0082] Preparation Process:

[0083] ① Weigh API, microcrystalline cellulose, and hydroxypropyl cellulose according to the prescription amount, and mix them evenly to obtain premixed powder.

[0084] ② Take an appropriate amount of purified water, add it to the premixed powder, prepare soft materials with a high-efficiency wet granulator, and perform wet granulation with a granulator to obtain drug-containing granules.

[0085] ③ Place the drug-containing granules in a fluidized bed for drying, and use a granulator to perform dry sizing to obtain the dried drug-containing granules.

[0086] ④ Take the prescription amount of croscarmellose sodium and magnesium stearate or stearic acid, add it to the dried drug-containing granules and mix evenly to obtain the total blend granules.

[0087] ⑤Using tablet pressing equipment and molds to prepare trexagliptin tablet cores, and coating the tablet cores with...

Embodiment 3

[0089] Table 5: Embodiment 3a and 3b prescription composition

[0090]

[0091] Preparation Process:

[0092] ① Weigh the API, lactose or pregelatinized starch, and hydroxypropyl cellulose according to the prescription amount, and mix them evenly to obtain the premixed powder.

[0093] ② Take an appropriate amount of purified water, add it to the premixed powder, prepare soft materials with a high-efficiency wet granulator, and perform wet granulation with a granulator to obtain drug-containing granules.

[0094] ③ Place the drug-containing granules in a fluidized bed for drying, and use a granulator to perform dry sizing to obtain the dried drug-containing granules.

[0095] ④ Take the prescription amount of croscarmellose sodium and sodium stearyl fumarate, add them to the dried drug-containing granules and mix evenly to obtain the total mixed granules.

[0096] ⑤Using tablet pressing equipment and molds to prepare trexagliptin tablet cores, and coating the tablet cores...

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Abstract

The invention discloses a trelagliptin succinate solid preparation and a preparation method thereof. The method comprises the following steps that by mass, 50-80 parts of trelagliptin succinate, 5-20parts of a filling agent, 1-10 parts of an adhesive, 3-15 parts of a disintegrating agent and 0-5 parts of a lubricant are prepared; trelagliptin succinate, the filling agent and the adhesive are mixed proportionally, and pre-mixed powder is obtained; then, water is added into the pre-mixed powder for granulation to obtain medicated granules; the medicated granules are dried by a fluidized bed fordrying, and dried medicated granules are obtained; the disintegrating agent and the lubricant are added into the dried medicated granules, and uniform mixing is performed to obtain total mixed granules; then, pressing and tableting are performed to obtain trelagliptin tablet cores. The method is simple and feasible in technology, the dissolution of the obtained solid preparation meets the requirement of a quick release agent, the tablet wright difference is small, and stability is good.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a solid preparation of trexagliptin succinate and a preparation method thereof. Background technique [0002] Trexagliptin is a long-acting dipeptidyl peptidase IV (DPP-IV) inhibitor developed by Japan's Takeda Pharmaceutical Company Limited. It is currently the only two drugs for type 2 diabetes. One of the long-acting hypoglycemic drugs. Trexagliptin increases blood levels of GLP-1 and GIP by selectively and persistently inhibiting the inactivation effect of DPP-IV on glucagon-like peptide-1 (GLP-1) and diabetes-dependent insulinotropic polypeptide (GIP). The concentration of GIP increases blood sugar level-dependent insulin secretion, thereby controlling blood sugar levels in diabetic patients. [0003] Japan's Takeda Pharmaceutical Co., Ltd. submitted a new drug application for Trexagliptin tablets to the Japanese Ministry of Health, Labor and Welfare (MHLW) on...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/38A61K47/36A61K31/513A61P3/10
CPCA61K9/2054A61K9/2059A61K9/2095A61K31/513
Inventor 陈龙江余义义况其方姚婷婷马宜雪郭创龙王利春王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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