Drug compound containing sodium-glucose synergic transport protein 2 inhibitor

A composition and drug technology, applied in the field of pharmaceutical preparations, to achieve the effect of excellent protein inhibition effect

Active Publication Date: 2017-07-18
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many types of diabetes drugs on the market, but so far, no single drug can maintain the blood sugar level of patients with type 2 diabetes within the target range for a long time

Method used

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  • Drug compound containing sodium-glucose synergic transport protein 2 inhibitor
  • Drug compound containing sodium-glucose synergic transport protein 2 inhibitor
  • Drug compound containing sodium-glucose synergic transport protein 2 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 6

[0040] Mix compound A, mannitol, lactose, pregelatinized starch, microcrystalline cellulose, and croscarmellose sodium according to the ratio in Table 1, and moisten with 10% cross-linked polyvinylpyrrolidone aqueous solution The aerosol is subjected to wet granulation and tablet compression to prepare tablets.

[0041] Table 1

[0042] Element Example 1 Example 2 Example 3 Example 4 Example 5 Example 6 Complex A 1.25 15 60 18 50 50 Mannitol — — — 95.52 72.64 — lactose — — — — — 77.55 pregelatinized starch 53.39 97.48 65.6 — — — microcrystalline cellulose 26 48.8 32.0 47.76 35.0 30.0 CCNa 3.6 7.2 10.8 7.2 10.8 10.8 PVP K30 4.86 9.72 9.8 9.72 9.76 9.85 purified water 43.74 87.48 88.2 87.48 87.84 88.65 Magnesium stearate 0.9 1.8 1.8 1.8 1.8 1.8 total 90 180 180 180 180 180

[0043] Unit: mg

Embodiment 7～9

[0045] With the prescription ratio of Table 2, compound A, pregelatinized starch, microcrystalline cellulose, sodium starch glycolate are mixed evenly, respectively with 10% polyvinylpyrrolidone, 10% hydroxypropyl cellulose and 4% The aqueous solution of hydroxypropyl methylcellulose was used as a wetting agent, and wet granulation was carried out, and tableted to prepare the tablets of Examples 7-9.

[0046] Table 2

[0047] Element Example 7 Example 8 Example 9 Complex A 20 20 20 pregelatinized starch 91.86 92.19 95.9 microcrystalline cellulose 46.0 46.0 48.0 Sodium carboxymethyl starch 10.8 10.8 10.8 PVP K30 9.54 — — HPC — 9.21 — HPMC E5 — — 3.5 purified water 85.86 82.89 84.0 Magnesium stearate 1.8 1.8 1.8 total 180 180 180

[0048] Unit: mg

Embodiment 10～12

[0050] Mix compound A, pregelatinized starch, microcrystalline cellulose, and crospovidone evenly with the prescription ratio in Table 3, and use 10% crospovidone and 10% hydroxypropyl cellulose as moisteners respectively. Wet agent, carry out wet granulation, tabletting, prepare the tablet of embodiment 10~12.

[0051] table 3

[0052] Element Example 10 Example 11 Example 12 Complex A 2.5 20 70 pregelatinized starch 51.5 91.96 63.08 microcrystalline cellulose 25.7 45.9 25 Crospovidone 5.4 10.8 10.8 PVP K30 4.86 — — HPC — 9.54 9.32 purified water 43.74 85.86 83.88 talcum powder 0.9 1.8 1.8 total 90 180 180

[0053] Unit: mg

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PUM

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Abstract

The invention discloses a drug compound containing a sodium-glucose synergic transport protein 2 inhibitor. Specifically, the drug compound contains 1,6-dehydrated-1-C-{4-chlorine-3-[(3-fluorine-4-phenetyl) methyl] phenyl}-5-C-(hydroxymethyl)-beta-L-idose or a compound formed by the same with amino acid, pre-gelled starch and at least one pharmaceutically acceptable excipient. The drug compound disclosed by the invention has the characteristics of strong technical operability and quick and complete dissolution.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a compound containing 1,6-anhydro-1-C-{4-chloro-3-[(3-fluoro-4-ethoxyphenyl)methyl]phenyl}-5 -C-(hydroxymethyl)-β-L-idopyranose and at least one pharmaceutically acceptable carrier, excipient or diluent, the pharmaceutical composition has the characteristics of rapid dissolution and good stability. Background technique [0002] With the development of social economy and the improvement of material living standards, the number of diabetic patients has increased rapidly worldwide. Diabetes is usually divided into two types: type I diabetes and type II diabetes, and more than 90% of them are type II diabetes. There are many types of diabetes drugs on the market, but so far, there is no single drug that can maintain the blood sugar level of type 2 diabetes patients within the target range for a long time. In recent years, in-depth research on the pathogenesis of diabetes h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K47/36A61P3/10A61K31/357
CPCA61K9/2059A61K9/4866A61K31/357
Inventor 卢韵潘晓晨陈昊
Owner JIANGSU HENGRUI MEDICINE CO LTD
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