Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Sitagliptin phosphate tablet and preparation method thereof

A technology of sitagliptin phosphate and disintegrant, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can solve the problems of slow release speed and slow hypoglycemic effect, Achieve the effect of fast dissolution rate, simple preparation process and good reproducibility

Inactive Publication Date: 2021-11-30
SHANDONG RENHE PHARMA
View PDF4 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The release speed of this method is slow, the dissolution rate in aqueous medium is less than 70% in 5 minutes, and the hypoglycemic effect is slow

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Sitagliptin phosphate tablet and preparation method thereof
  • Sitagliptin phosphate tablet and preparation method thereof
  • Sitagliptin phosphate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Sitagliptin Phosphate Tablets Prepared by Direct Compression

[0030] The raw material formula (1000 prescription quantities) of sitagliptin phosphate tablet described in the present embodiment is as follows:

[0031]

[0032] The preparation technology of sitagliptin phosphate tablet described in the present embodiment is as follows:

[0033] 1. Screening: Pass sitagliptin phosphate, disintegrant and filler through 80-mesh sieve respectively;

[0034] 2. Premixing: Mix the sieved sitagliptin phosphate, disintegrant and filler evenly to prepare the premixed drug powder;

[0035] 3. Total mixing: add a lubricant to the premixed powder prepared in step 2, and mix evenly to obtain a mixed powder;

[0036] 4. Tablet compression: use a tablet press to compress the mixed medicinal powder prepared in step 3 into a tablet core with a hardness of 8kg±1kg;

[0037] 5. Coating: film-coat the tablet core obtained in step 4, and increase the weight by 3.2%, to obtai...

Embodiment 2

[0038] Embodiment 2: Preparation of Sitagliptin Phosphate Tablets by Direct Compression

[0039] The raw material formula (1000 prescription quantities) of sitagliptin phosphate tablet described in the present embodiment is as follows:

[0040]

[0041] The preparation technology of sitagliptin phosphate tablet described in the present embodiment is as follows:

[0042] 1. Screening: Pass sitagliptin phosphate, disintegrant and filler through 80-mesh sieve respectively;

[0043] 2. Premixing: Mix the sieved sitagliptin phosphate, disintegrant and filler evenly to prepare the premixed drug powder;

[0044] 3. Total mixing: add a lubricant to the premixed powder prepared in step 2, and mix evenly to obtain a mixed powder;

[0045] 4. Tablet compression: use a tablet press to compress the mixed medicinal powder prepared in step 3 into a tablet core with a hardness of 8kg±1kg;

[0046] 5. Coating: film-coat the tablet core obtained in step 4, and increase the weight by 3.5%,...

Embodiment 3

[0052] Using the raw material formula and preparation method of Example 2, the difference is only: when the tablet core is film-coated, the weight gain: 3%, 4.5%, and then two different sitagliptin phosphate tablet products are tested for dissolution rate. Determination, measurement conditions: 900ml water, paddle method, rotating speed 50rpm. The dissolution results are shown in the table below:

[0053] time point (min) Dissolution at 3% weight gain (%) Dissolution at 4.5% weight gain (%) 0 0.00 0.00 5 77.06 82.81 10 91.75 93.75 15 96.14 98.56 20 98.18 102.17 30 100.40 103.04 45 101.89 103.76

[0054] It can be known from the above table that the weight gain of the coating has a certain influence on the dissolution rate of sitagliptin phosphate tablets, and the weight gain should be controlled at 3% to 4.5%.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
hardnessaaaaaaaaaa
volumeaaaaaaaaaa
Login to View More

Abstract

The invention relates to the technical field of medicine production, in particular to a sitagliptin phosphate tablet and a preparation method thereof. The sitagliptin phosphate tablet is prepared from the following raw materials in parts by mass: 30 parts of sitagliptin phosphate, 40-80 parts of a filling agent, 2-5 parts of a disintegrating agent and 10-20 parts of a lubricating agent. Compared with the prior art, through the measurement of the dissolution rate, the sitagliptin phosphate tablet prepared by adopting the formula and the two methods has the dissolution rate of more than 70% in 900ml of water medium (slurry method, 50rpm) in 5minutes, the dissolution rate is higher, and the blood sugar reducing effect is good; and the preparation process is simple, the reproducibility is good, and the industrial production condition is provided.

Description

technical field [0001] The invention relates to the technical field of medicine production, in particular to a sitagliptin phosphate tablet and a preparation method thereof. Background technique [0002] Sitagliptin phosphate is a potent and highly selective dipeptidyl peptidase IV (DPP-IV) inhibitor that acts in patients with type 2 diabetes through the active incretin hormone glucagon-like polypeptide-1 ( GLP-1) and glucose-dependent insulinotropic polypeptide (GLP) levels to improve glycemic control. Sitagliptin phosphate prevents DPP-4 from hydrolyzing incretin hormones, thereby increasing plasma concentrations of the active forms of GLP-1 and GIP. By increasing levels of active incretins, sitagliptin phosphate increases insulin release and decreases glucagon levels in a glucose-dependent manner, thereby lowering blood glucose. [0003] Sitagliptin Phosphate was first developed by Merck, and it was the first DDP-4 inhibitor launched in the United States in 2006. Sitag...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/4985A61K47/38A61P3/10
CPCA61K9/28A61K9/2054A61K9/2095A61K31/4985A61P3/10
Inventor 王嘉锋王爱明王广金
Owner SHANDONG RENHE PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com