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

Medicine composition containing empagliflozin and dimethylbiguanide hydrochloride

A technology of metformin hydrochloride and its composition, which is applied in the field of medicine, can solve problems such as day-to-day blood drug concentration variation, unfavorable coating process, and unqualified friability, and achieve the effects of high hardness, rapid dissolution, and adjustable output

Active Publication Date: 2017-07-07
HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
View PDF6 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In this formulation, due to the small amount of binder, when it is made into tablets, the resulting tablets will have low hardness, resulting in unqualified friability, which is not conducive to the subsequent coating process. ; At the same time, the dissolution RSD between the final tablets is too large, and the 15min dissolution RSD exceeds 10%, which may lead to large variations in blood drug concentration during the day and cause blood sugar fluctuations

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
  • Medicine composition containing empagliflozin and dimethylbiguanide hydrochloride
  • Medicine composition containing empagliflozin and dimethylbiguanide hydrochloride
  • Medicine composition containing empagliflozin and dimethylbiguanide hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The selection of embodiment 1 prescription quantity

[0029] The amount of excipients in the formulation was determined by the method of Design of Experiments (DOE), and the factors affecting the key quality attributes of the tablet were investigated at the same time. use 2 2 -The full factorial design of three central points, to investigate the effect of binder dosage and binder concentration on particle properties (the weight of particles passing through 24 mesh sieve but not 100 mesh sieve), hardness and dissolution rate. The experimental combination and results are shown in Table 1.

[0030] Table 1 Amount and concentration of excipients 2 2 -Three center point full factorial design table and results

[0031]

[0032] The specific amount of raw and auxiliary materials for each combination is shown in Table 2

[0033] Table 2 The amount of raw and auxiliary materials used in each combination

[0034] Dosage (g) std 1 std 2 std 3 std 4 std 5...

Embodiment 2

[0038] The selection of embodiment 2 adhesive types

[0039] When adopting the granulation process, the type of adhesive will have a greater impact on the dissolution of the tablet. The present invention has carried out a screening test on the type of adhesive. The experimental combination and results are shown in Table 3-4

[0040] Table 3 composition of different adhesive formulations

[0041]

[0042] Table 4 The results of the investigation on the impact of the type of binder on the key attributes of the tablet

[0043] Measurement items Example 2-1 Example 2-2 Example 2-3 Particle properties (%) 90 67 65 Hardness (kg) 12.1 7.0 8.9 Dissolution of Empagliflozin (%) 94.8 98.6 76.6 Dissolution rate of metformin (%) 101.1 100.5 89.2 Dissolution RSD of Empagliflozin (%) 3.4 12 14

[0044] According to the above test results, va64 is more suitable for the completion of the present invention than other types of adhes...

Embodiment 3

[0045]Embodiment 3 Concrete prescription

[0046] See Table 5 for the composition of single-layer tablets (cores) of Empagliflozin, Metformin Hydrochloride 5mg / 500mg and 12.5mg / 500mg.

[0047] Table 5 Prescription

[0048] Embodiment 3-1 (10,000 pieces) Feed amount (g) weight% Empagliflozin 50 0.85 Metformin 5000 84.75 microcrystalline cellulose 153.1 2.6 va64 620 10.5 silica 41.4 0.7 Magnesium stearate 35.5 0.6 purified water 2700L (va64 concentration) 23

[0049] Embodiment 3-2 (10,000 pieces) Feed amount (g) weight% Empagliflozin 125 2.12 Metformin Hydrochloride 5000 84.75 Microcrystalline Cellulose PH101 167.1 2.83 va64 531 9.00 Colloidal silica 41.4 0.70 Magnesium stearate 35.5 0.60 purified water 2140L (va64 concentration) 24.8

[0050] Preparation operation:

[0051] Metformin hydrochloride and microcrystalline cellulose, empagliflozi...

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

No PUM Login to View More

Abstract

The invention discloses a medicine composition containing empagliflozin and dimethylbiguanide hydrochloride. The medicine composition contains a filling agent, a binder, a flow aid and a lubricating agent, wherein the content of the binder is 9 to 11 percent .The invention also discloses a method for preparing the empagliflozin and dimethylbiguanide hydrochloride medicine composition. The empagliflozin and dimethylbiguanide hydrochloride medicine composition disclosed by the invention is high in hardness and rapid in dissolution, and an interslice dissolution degree RSD is small.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically relates to a pharmaceutical composition containing empagliflozin and metformin hydrochloride. Background technique [0002] The incidence of type II diabetes is increasing, and its complications (such as diabetic foot, blindness, renal failure, etc.) not only affect the quality of life of patients, but also may lead to shortened life span. [0003] Empagliflozin is an oral sodium-glucose cotransporter-2 (SGLT-2) inhibitor. SGLT-2 is the transporter mainly responsible for the reabsorption of glucose from the glomerular filtrate into the systemic circulation. By inhibiting SGLT-2, empagliflozin reduces the renal reabsorption of filtered glucose and lowers the renal threshold of glucose, Thereby increasing the excretion of urinary sugar. Metformin hydrochloride is a classic hypoglycemic drug that can reduce fasting and postprandial hyperglycemia in patients with type II diab...

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): A61K31/351A61K31/155A61K47/32A61P3/10
CPCA61K31/155A61K31/351A61K47/32A61K2300/00
Inventor 白海波章小永
Owner HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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