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Ipragliflozin oral solid preparation and preparation method thereof

A solid preparation, ipagliflozin technology, applied in the field of pharmaceutical preparations, can solve the problems of low drug bioavailability, poor disintegration, poor solubility and the like

Inactive Publication Date: 2017-07-07
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] It can be seen that the class of SLGT2 inhibitors generally has poor solubility or poor disintegration, which leads to the problem of low bioavailability of such drugs

Method used

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  • Ipragliflozin oral solid preparation and preparation method thereof
  • Ipragliflozin oral solid preparation and preparation method thereof
  • Ipragliflozin oral solid preparation and preparation method thereof

Examples

Experimental program
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preparation example Construction

[0028] In the case that the oral solid preparation of Epagliflozin of the present invention is a tablet, the preparation method comprises the following steps:

[0029] (1) L-proline epagliflozin eutectic and anti-tacking agent are mixed evenly to form a premix of bulk drug;

[0030] (2) adding the filler, binder, and disintegrant to the premix of the crude drug, and mixing uniformly to form a drug-containing mixture;

[0031] (3) Mix the drug-containing mixture in step (2) with a lubricant, and compress into tablets to obtain plain tablets;

[0032] (4) Make a film coat with a stomach-soluble coating material.

[0033] In the case that the oral solid preparation of Epagliflozin of the present invention is a capsule, the preparation method comprises:

[0034] (1) L-proline epagliflozin eutectic and anti-tacking agent are mixed evenly to form a premix of bulk drug;

[0035] (2) adding the filler to the premix of the crude drug, and mixing uniformly to form a drug-containing m...

Embodiment 1

[0044] Embodiment 1: Preparation of L-proline Epagliflozin

[0045] In this example, the raw materials and reagents used are all commercially available.

[0046]

[0047] The preparation of formula 3 compound:

[0048]Compound 1 (160.6 g, 0.5 mol) was added into a 3 L round-bottomed three-neck flask, dissolved by adding 400 ml THF and 800 ml toluene, and protected by argon. After cooling to -78°C, 2.5M n-butyl lithium in hexane (184ml, 0.5mol) was added dropwise, keeping the temperature not higher than -70°C. Stir at -78 °C for 30 min. Then the reaction solution was slowly transferred to toluene ( 1.1L) solution, keep the temperature not higher than -70°C. After stirring at -78°C for 30 min, methanesulfonic acid (1 L, 0.6N MeOH) was added, and the reaction was allowed to warm up to room temperature and stirred for 16 h. Adjust the pH to 7.5 with saturated sodium bicarbonate solution (about 200ml), separate the organic phase, extract the aqueous phase with ethyl acetate...

Embodiment 2

[0053] Embodiment 2: the preparation of Epagliflozin coated tablet

[0054] Table 1: Composition of Epagliflozin Coated Tablets

[0055]

[0056] Preparation method: Mix L-proline epagliflozin eutectic and fumed silica in a mixer for about 5 minutes, pass through a 60-mesh sieve, and set aside; then add microcrystalline cellulose 102, PVPP, and PVP K30, and mix After about 15 minutes, set aside; finally add magnesium stearate and mix for 3 minutes, compress into tablets, and coat with Opadry.

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Abstract

The invention provides an ipragliflozin oral solid preparation. The ipragliflozin oral solid preparation can be in the form of tablets, powder or capsules and contains an anti-sticking agent, filler, a disintegrating agent, a bonding agent, a lubricating agent and a coating material, wherein the disintegrating agent, the bonding agent, the lubricating agent and the coating material are optional. Correspondingly, the invention provides a preparation method of the ipragliflozin oral solid preparation. The preparation method includes the steps of premix forming, medicine-containing mixture forming, tabletting and coating and is characterized in that a capsule shell is filled with a medicine-containing mixture if the ipragliflozin oral solid preparation is prepared into the capsules, and a packaging container is filled with the medicine-containing mixture if the ipragliflozin oral solid preparation is prepared into the powder.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations. Specifically, the present invention provides an oral solid preparation of epagliflozin and a preparation method thereof. Background technique [0002] Glucose cotransporters (SLGTs) are a class of membrane proteins that transport glucose into cells. SLGT has two subtypes, SLGT1 and SLGT2, which are distributed in the small intestinal mucosa and renal tubules, respectively. SLGT2 plays a key role in proximal tubular glucose reabsorption. [0003] Epagliflozin is a class of SLGT2 inhibitors, which selectively known SLGT2, so that the glucose in the renal tubules cannot be reabsorbed into the blood, but excreted with the urine, thereby reducing the blood sugar concentration. The chemical name of Egretide is (1S)-1,5-anhydro-1-{3-[(1-benzothiophen-2-yl)methyl]-4-fluorophenyl}-D-glucitol, The structure of the co-crystal formed by epagliflozin and L-proline is shown in formula (I). [00...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K9/48A61K47/02A61K31/381A61K31/401A61P3/10
CPCA61K9/2009A61K9/2866A61K9/485A61K31/381A61K31/401A61K2300/00A61K9/28A61K9/48A61K47/02
Inventor 左灵静颜携国陶安进袁建成
Owner HYBIO PHARMA