Sitagliptin phosphate composition, sitagliptin phosphate tablet, and preparation method and application of sitagliptin phosphate composition and sitagliptin phosphate tablet

A technology of sitagliptin phosphate and its composition, which is applied in the direction of drug combination, pharmaceutical formula, medical preparations with non-active ingredients, etc., can solve the problem that the safety and effectiveness of generic drugs are not guaranteed, and it is difficult for the original drug to be developed in vitro. consistency and other issues

Active Publication Date: 2021-11-23
北京鑫开元医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In the prior art, when the in vitro dissolution behavior of the generic drug of sitagliptin phosphate was investigated, it was found that the release behavior of the generic drug was significantly different from that of the original drug, and it was difficult to be consistent with the in vitro dissolution of the original drug, resulting in the release of the generic drug. safety and effectiveness are not guaranteed

Method used

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  • Sitagliptin phosphate composition, sitagliptin phosphate tablet, and preparation method and application of sitagliptin phosphate composition and sitagliptin phosphate tablet
  • Sitagliptin phosphate composition, sitagliptin phosphate tablet, and preparation method and application of sitagliptin phosphate composition and sitagliptin phosphate tablet
  • Sitagliptin phosphate composition, sitagliptin phosphate tablet, and preparation method and application of sitagliptin phosphate composition and sitagliptin phosphate tablet

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preparation example Construction

[0066] In the third aspect, the embodiments of the present invention provide a method for preparing the sitagliptin phosphate tablet according to the second aspect, the preparation method comprising the following steps: combining the sitagliptin phosphate tablet described in the first aspect It can be directly compressed into tablets.

[0067] The preparation method of sitagliptin phosphate tablet provided in the embodiment of the present invention adopts powder direct compression technology to reduce granulation, drying and other processes, the preparation process is simple, high in safety, low in cost, saves manpower and material resources, and is more suitable for scale chemical production.

[0068] Further, the preparation method includes the following steps:

[0069] S1. Weigh sitagliptin phosphate monohydrate, calcium hydrogen phosphate anhydrous, microcrystalline cellulose, croscarmellose sodium, magnesium stearate and sodium stearyl fumarate according to the formula q...

Embodiment 1

[0091] The contents of the components of the sitagliptin phosphate tablets provided in this example are shown in Table 1.

[0092] Preparation:

[0093] S1. Pass anhydrous calcium hydrogen phosphate, croscarmellose sodium, magnesium stearate and sodium stearyl fumarate through a 40-mesh sieve for later use. Weigh sitagliptin phosphate monohydrate (D90 particle size is 30 μm), anhydrous calcium hydrogen phosphate, microcrystalline cellulose (D90 particle size is 260 μm), croscarmellose sodium, hard Magnesium stearate and sodium stearyl fumarate;

[0094] S2. Mix the sitagliptin phosphate monohydrate, anhydrous calcium hydrogen phosphate, microcrystalline cellulose and croscarmellose sodium in a three-dimensional mixer, and the mixing time is 20 minutes to obtain the first mixture;

[0095] S3. Add magnesium stearate and sodium stearyl fumarate to the first mixture, and continue mixing in a three-dimensional mixer for 5 minutes to obtain a second mixture;

[0096] S4. Using a...

Embodiment 2

[0098] The contents of the components of the sitagliptin phosphate tablets provided in this example are shown in Table 1.

[0099] Preparation:

[0100] S1. Pass anhydrous calcium hydrogen phosphate, croscarmellose sodium, magnesium stearate and sodium stearyl fumarate through a 40-mesh sieve for later use. Sequentially weigh sitagliptin phosphate monohydrate (D90 particle size is 40 μm), anhydrous calcium hydrogen phosphate, microcrystalline cellulose (D90 particle size is 260 μm), croscarmellose sodium, hard Magnesium stearate and sodium stearyl fumarate;

[0101] S2~S4 are completely the same as S2~S4 in embodiment 1.

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Abstract

The invention belongs to the field of medicines, and particularly relates to a sitagliptin phosphate composition, sitagliptin phosphate tablets and a preparation method and application of the sitagliptin phosphate composition and the sitagliptin phosphate tablets, and the sitagliptin phosphate composition comprises the following components in percentage by mass: 25-35% of sitagliptin phosphate monohydrate; 20%-40% of anhydrous calcium hydrogen phosphate; 20%-40% of microcrystalline cellulose; 1%-4% of croscarmellose sodium; 0.5%-2% of magnesium stearate; and 1%-4% of sodium stearyl fumarate, wherein the D90 particle size of the sitagliptin phosphate monohydrate is 30-90 [mu]m, and the D90 particle size of the microcrystalline cellulose is greater than or equal to 260 [mu]m. The in-vitro dissolution curve of the sitagliptin phosphate tablet provided by the invention is similar to that of an imported original development agent produced by Merk Company, so that the possibility of bioequivalence with the original development agent is improved, and the requirement of consistency evaluation is met.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a sitagliptin phosphate composition, sitagliptin phosphate tablets, a preparation method and application thereof. Background technique [0002] Diabetes is a metabolic disease characterized by high blood sugar. Hyperglycemia is caused by defective insulin secretion or impaired biological action, or both. Long-term high blood sugar leads to chronic damage and dysfunction of various tissues, especially the eyes, kidneys, heart, blood vessels, and nerves. Studies have shown that in 2015, the number of adult diabetic patients in my country has reached 109.6 million, ranking first in the world. The prevalence and incidence of diabetes are gradually increasing worldwide. [0003] Sitagliptin phosphate is a potent and highly selective inhibitor of dipeptidyl peptidase IV (DPP-IV) in patients with type 2 diabetes by increasing the active incretin hormone glucagon-like polypeptide-1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/28A61K47/38A61K47/02A61K47/12A61K31/4985A61P3/10
CPCA61K9/2009A61K9/2054A61K9/2013A61K9/2095A61K9/28A61K31/4985A61P3/10Y02A50/30
Inventor 王志超伏开强庞建梅郎福双戴信敏
Owner 北京鑫开元医药科技有限公司
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