Sitagliptin phosphate tablet and preparation method thereof

A technology of sitagliptin phosphate and tablets, which is applied in the field of drug preparation, can solve problems such as uneven tablet quality, and achieve the effects of low production cost, good stability, and high dissolution rate

Inactive Publication Date: 2017-06-13
CISEN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the dissolution rate of the tablet prepared by the invention has been improved, there is a powder layering phenomenon in the mixed material in the direct tableting method and the rolling method, and the quality of the prepared tablet is not uniform.

Method used

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  • Sitagliptin phosphate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Composition: 100g of sitagliptin phosphate, 140g of anhydrous calcium hydrogen phosphate, 140g of microcrystalline cellulose, 10g of croscarmellose sodium, 5g of magnesium stearate, 5g of sodium stearyl fumarate, made into 1000 tablets .

[0020] Preparation method: (1) pass the micronized sitagliptin phosphate raw material through a 90-110 mesh sieve, and respectively pass the filler, binder and disintegrant through a 70-95 mesh sieve; (2) weigh an appropriate amount of Mix the sitagliptin phosphate raw material with filler, binder and disintegrant evenly; (3) granulate the above-mentioned premixed material with a dry granulator, and carry out granulation; (4) add weighing A well-measured lubricant is mixed evenly; (5) directly compressed into tablets through a tablet press; (6) film-coating the tablet core to obtain a finished tablet.

Embodiment 2

[0022] Composition: Sitagliptin phosphate 100g, mannitol 100g, microcrystalline cellulose 180g, croscarmellose sodium 10g, magnesium stearate 10g, made into 1000 tablets.

[0023] Preparation method: same as in Example 1, 1000 sitagliptin phosphate tablets can be prepared.

Embodiment 3

[0025] Composition: 100 g of sitagliptin phosphate, 120 g of calcium carbonate, 160 g of lactose, 10 g of croscarmellose sodium, 5 g of talcum powder, and 5 g of silicon dioxide, made into 1000 tablets.

[0026] Preparation method: same as in Example 1, 1000 sitagliptin phosphate tablets can be prepared.

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PUM

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Abstract

The invention belongs to the technical field of drug preparation and specifically relates to a sitagliptin phosphate tablet and a preparation method thereof. The sitagliptin phosphate tablet comprises the following raw materials in parts by weight: 30 parts of sitagliptin phosphate, 55-70 parts of filler, 0-5 parts of adhesive, 1.5-3.0 parts of disintegrating agent and 1.5-5.0 parts of lubricating agent; the filler is selected from one or more of microcrystalline cellulose, sugar and inorganic salt; the adhesive is selected from one or more of hydroxypropyl methylcellulose, hydroxypropylcellulose, povidone K30 and starch; the disintegrating agent is selected from one or more of crosslinking sodium carboxymethylcellulose, sodium carboxymethyl starch and polyvinylpolypyrrolidone. Compared with the prior art, the sitagliptin phosphate tablet provided by the invention has the technical effects of easily acquired compound raw materials, high disintegration speed, high dissolution rate, high stability, simple steps of preparation method, easily controlled technological process, short production period, low production cost and suitability for industrialized application.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a sitagliptin phosphate tablet and a preparation method thereof. Background technique [0002] Sitagliptin phosphate is a potent and highly selective inhibitor of dipeptidyl peptidase IV (DPP-IV) in patients with type 2 diabetes by increasing the active incretin hormone glucagon-like polypeptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) levels to improve glycemic control. The activity of GLP-1 and GIP is limited by the enzyme DPP-4, which rapidly hydrolyzes incretin hormones to produce inactive products. Sitagliptin prevents DPP-4 from hydrolyzing incretin hormones, thereby increasing plasma concentrations of the active forms of GLP-1 and GIP. By increasing active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in a glucose-dependent manner, thereby lowering blood glucose. [0003] Sitagliptin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K47/38A61K31/4985A61P3/10
CPCA61K9/2054A61K9/28A61K31/4985
Inventor 李翠华邱娟卢秀莲
Owner CISEN PHARMA
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