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A kind of Empagliflozin medicinal composition and preparation method thereof

A technology of empagliflozin and its composition, which is applied in the field of empagliflozin pharmaceutical composition and its preparation, can solve the problems of increased risk of hypoglycemia, β cell toxicity, weight gain, etc., and achieve improved blood sugar control, The effect of prolonging the action time and reducing the fluctuation of blood sugar

Active Publication Date: 2022-05-03
浙江诺得药业有限公司 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Combining saxagliptin with sulfonylureas, sulfonylureas bind to sulfonylurea receptor 1 of β cells, and finally stimulate insulin secretion, can significantly improve blood sugar, but the disadvantages are its potential β cell toxicity, weight gain and increased risk of hypoglycemia
[0008] However, there is no relevant literature report on the combination of empagliflozin and saxagliptin in the treatment of type 2 diabetes.

Method used

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  • A kind of Empagliflozin medicinal composition and preparation method thereof
  • A kind of Empagliflozin medicinal composition and preparation method thereof
  • A kind of Empagliflozin medicinal composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0031] The preparation method of the pharmaceutical composition containing empagliflozin and saxagliptin, the steps are as follows:

[0032] ① Weigh all saxagliptin, half of empagliflozin, filler, 1 / 2-2 / 3 disintegrant, skeleton material, sieve, and mix well;

[0033] ② Prepare binder solution, wet granulate, dry at 60°C, and granulate with 40 mesh sieve;

[0034] ③ Add the remaining empagliflozin, the remaining disintegrant croscarmellose sodium, glidant, and lubricant, mix well and press into tablets, compound tablets.

[0035] The specifications of the obtained tablet are respectively: saxagliptin 1-15mg; empagliflozin 0.5-30mg.

Embodiment 4

[0037] Experimental group: the compound tablet prepared in Preparation Example 1 of the present invention. Batch number: 20191113.

[0038] Control group: 1. Saxagliptin tablets; specification: 5 mg; manufacturer: AstraZeneca Pharmaceutical Co., Ltd.; 2. Empagliflozin tablets; specification: 10 mg; manufacturer: Shanghai Boehringer Ingelheim Pharmaceutical Co., Ltd.

[0039] Instrument: Waters ARC high performance liquid chromatography, including: pump system, diode array detector and workstation.

[0040] Test plan: select 6 Beagle dogs, half male and half male, average body weight 10.0 ± 1.0Kg, be divided into 3 groups at random, be respectively control group (saxagliptin), control group (empagliflozin), treatment group (implementation). Example 1 sample). Fasting 8h before the administration experiment, blank blood was drawn before the administration, the experimental group took 1 compound tablet prepared in Example 1, and the control group took the reference preparation Sa...

Embodiment 5

[0044] The administration method and group setting are the same as in Example 4, and the hypoglycemic effect of the sample in Example 1 of the present invention in the human body is investigated.

[0045] Dosing regimen: 12 patients with type Ⅱ diabetes mellitus were randomly divided into treatment group, control group 1, and control group 2, each with 4 cases. Among them, the treatment group was given the test preparation, and the control group was given the reference preparation, once a day. The drug was administered for 8 consecutive weeks, and fasting blood glucose (FPG), two-hour postprandial blood glucose (2hPG) and glycosylated hemoglobin (HbA1c) were detected before and after treatment at 0, 4, and 8 weeks. The experimental results are shown in the table below:

[0046]

[0047] The experimental results show that compared with the reference preparation, using the compound saxagliptin / empagliflozin tablet provided by the preparation embodiment 1 of the present invent...

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Abstract

The invention discloses an empagliflozin pharmaceutical composition and a preparation method thereof. The composition comprises empagliflozin, saxagliptin and pharmaceutically acceptable excipients; wherein, empagliflozin and its combination with saxagliptin The parts by weight of liptin are as follows: the mass ratio of saxagliptin to empagliflozin is (1-2): (2-1); the pharmaceutically acceptable auxiliary materials include: filler, disintegrant, adhesive , Glidants, lubricants, skeleton materials. The preparation method is as follows: wet granulation of the whole saxagliptin, half of the empagliflozin, part of the disintegrant, and skeleton material, and then adding the remaining empagliflozin and the disintegrant for tablet compression to obtain compound tablets. It has the characteristics of fast drug release, lasting drug effect, stable glucose control, and small side effects.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to an empagliflozin medicinal composition and a preparation method thereof. Background technique [0002] Empagliflozin belongs to the class of sodium-glucose cotransporter-2 (SGLT-2) inhibitors. The chemical name is (1S)-1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furyl]oxy]phenyl]methyl ]phenyl]-D-glucitol, its structural formula is as follows: [0003] [0004] Empagliflozin, as an emerging SGLT-2 inhibitor drug, has been proven to block the reabsorption of glucose in the kidney and excrete excess glucose out of the body, thereby achieving the effect of lowering blood sugar levels, and the hypoglycemic Effects were independent of beta-cell function and insulin resistance. The sodium-glucose co-transporter 2 (SGLT-2) inhibitor empagliflozin, in addition to being effective in lowering blood sugar, also contributed to weight loss and lower blood pressure compared wi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K9/16A61P3/10A61P5/50A61K31/403
CPCA61K31/7048A61K31/403A61K9/167A61K9/0053A61K9/1652A61P3/10A61P5/50A61K2300/00
Inventor 詹怡飞潘新殷学治李晓庆
Owner 浙江诺得药业有限公司
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