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Stable glucokinase activator compositions

A technology of composition and alkalizing agent, which is applied in the direction of drug combination, organic active ingredients, medical preparations containing active ingredients, etc., can solve the problems of particle aggregation, increasing particle size or inducing stabilizers, etc.

Inactive Publication Date: 2015-11-11
VTV THERAPEUTICS LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Conditions created during the conversion of particle suspensions into solid form can lead to particle aggregation, increase particle size or induce crystallization of stabilizers, which present great challenges in maintaining the size and stability of nanoparticles

Method used

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  • Stable glucokinase activator compositions
  • Stable glucokinase activator compositions
  • Stable glucokinase activator compositions

Examples

Experimental program
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preparation example Construction

[0025] Preparation of solid stabilized particles

[0026] The stabilized pharmaceutical compositions of the invention comprise solid stabilized particles. Stable solid particles can be prepared as follows: starting from the or a pharmaceutically acceptable salt thereof and a solvent, from which the solvent is then removed to form solid stabilized particles. Particle suspensions include microsuspensions, i.e., suspensions comprising particles in the micron size range from about 1 μm to about 100 μm, or nanosuspensions, i.e., suspensions comprising particles in the nanometer size range from about 0.5 nm to about 1000 nm , or a mixture of them. In an exemplary embodiment, the particle suspension includes nanoparticles.

[0027] Suitable methods for removing solvent from particle suspensions include, for example, granulation, lyophilization, vacuum drying, oven drying, desiccant drying and spray drying. Suitable solvents for particle suspensions include any solvent generally r...

Embodiment 1

[0094] A nanosuspension of {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid was prepared using the method described above, wherein The polymer stabilizer is hydroxypropyl methylcellulose (HPMC) and the surfactant stabilizer is sodium lauryl sulfate (SLS). The resulting nanosuspension has a solids content of 10%, an average particle size of 225.6 nm, and a particle size of 0.145. Polydispersity index and zeta potential of -57.6 mV.

[0095] The physical stability of the nanosuspensions is shown in Table 1 below, no aggregation was observed after storage at room temperature for 6-48 hours and at 5°C for 1.5 months.

[0096] Table 1: Physical Stability of Nanoparticle Suspensions

[0097] time / temperature

Average particle size (nm)

0

225.6

6h, RT

223.1

24h, RT

230.9

48h, RT

229.4

1.5 months, 5℃

226.0

[0098] figure 1 Shown is {2-[3-cyclohexyl-3-(trans-4- X-ray ...

Embodiment 2

[0106] Nanosuspensions of {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid were prepared using the method described above, wherein The polymer stabilizer was hydroxypropyl cellulose (HPC) and the surfactant stabilizer was sodium lauryl sulfate (SLS). The resulting nanosuspension had a solids content of 10%, an average particle size of 252.2 nm, a polydispersity index of 0.171 and a zeta potential of -55.6 mV.

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Abstract

The invention relates to stable pharmaceutical compositions comprising a glucokinase (GK) activator suitable for oral administration. The invention also relates to methods of making and using such pharmaceutical compositions.

Description

field of invention [0001] The present invention relates to stable pharmaceutical compositions suitable for oral administration comprising glucokinase (GK) activators. The invention also relates to methods of making and using such pharmaceutical compositions. Background of the invention [0002] {2-[3-Cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid (disclosed in, e.g., U.S. Patent No. 7851636 Middle) is a GK activator that sensitizes the glucokinase (GK) sensor system. GK is an enzyme belonging to the hexokinase family that catalyzes the first step in glucose metabolism, the conversion of glucose to glucose-6-phosphate. GK can regulate carbohydrate metabolism by acting as a glucose sensor and causing changes in metabolism or cellular function in response to fluctuations in blood glucose levels. GK is used as a glucose sensor in the pancreas, liver, intestine and brain. {2-[3-Cyclohexyl 3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-yl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/425
CPCA61K9/146A61K31/425A61K31/426A61P43/00A61P3/10A61K9/145
Inventor Y·莫M·G·戴德希亚A·切特里
Owner VTV THERAPEUTICS LLC
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