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Sustained-release composition of sitagliptin and simvastatin

A slow-release composition, simvastatin technology, applied in drug combination, drug delivery, pill delivery, etc., can solve the problems of patients prone to adverse reactions to drugs, low bioavailability, frequent medication times, etc., to improve biological Utilization, stable blood drug concentration, and the effect of avoiding peak and valley phenomena

Inactive Publication Date: 2015-04-01
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is divided into two layers, one layer is sitagliptin, the other layer is simvastatin, and the outer layer is wrapped with a film coating. It is an ordinary tablet. After taking the tablet, the peak and valley phenomenon of blood drug concentration is prone to occur. The effect of the drug on the human body High toxicity and side effects, low bioavailability, frequent medication times, patients are prone to adverse reactions to drugs

Method used

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  • Sustained-release composition of sitagliptin and simvastatin
  • Sustained-release composition of sitagliptin and simvastatin
  • Sustained-release composition of sitagliptin and simvastatin

Examples

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preparation example Construction

[0075] In some embodiments, the preparation method of the sitagliptin coated pellets specifically includes the following steps:

[0076] a. The sitagliptin and the filler are pulverized and sieved separately, mixed evenly and then mixed with the binder, and the sitagliptin-containing pellet core is prepared by the extrusion spheronization method.

[0077] B, the Surelease aqueous dispersion is mixed with water to prepare the Surelease aqueous dispersion coating solution;

[0078] c, get the ball core containing sitagliptin and place it in the fluidized bed, and coat the ball core containing sitagliptin with Surelease aqueous dispersion coating solution;

[0079] Wherein, step a and step b are in no particular order.

[0080] Wherein, in some preferred embodiments, in the preparation method of the sitagliptin-coated pellets, the sieving in step a is 100-mesh sieve.

[0081] In some preferred embodiments, in the preparation method of the sitagliptin coated pellets, the specifi...

Embodiment 1

[0097] Embodiment 1, sitagliptin simvastatin sustained-release capsules

[0098] (1) Pill core containing sitagliptin:

[0099] sitagliptin

50 copies

lactose

80 copies

microcrystalline cellulose

200 copies

[0100] Coating solution:

[0101]

[0102] Grind sitagliptin, sucrose or lactose, and microcrystalline cellulose separately, pass through a 100-mesh sieve, mix evenly, use distilled water as a binder, and prepare by extrusion spheronization. The extrusion rate is 25rpm, and the spheronization speed is 2100rpm. The time is 5 minutes, the finished product is dried at 35°C, and the pellets between 700-900 μm are sieved to obtain the drug-containing pellets;

[0103] prescription amount Aqueous dispersion coating liquid, get above-mentioned drug-containing micropill and place in fluidized bed and carry out coating: fluidization temperature is 35 ℃, and fluidization pressure is 0.4MPa, and spray pressure is 0.15MPa, peristaltic p...

Embodiment 2

[0109] Embodiment 2, sitagliptin simvastatin sustained-release capsules

[0110] (1) Pill core containing sitagliptin:

[0111] sitagliptin

75 copies

lactose

100 copies

microcrystalline cellulose

175 copies

[0112] Coating solution:

[0113]

[0114]Grind sitagliptin, sucrose or lactose, and microcrystalline cellulose separately, pass through a 100-mesh sieve, mix evenly, use distilled water as a binder, and prepare by extrusion spheronization. The extrusion rate is 25rpm, and the spheronization speed is 2300rpm. The time is 6 minutes, the finished product is dried at 40°C, and the pellets between 700-900 μm are screened to obtain the drug-containing pellets;

[0115] prescription amount Aqueous dispersion coating solution, get above-mentioned drug-containing micropill and place in fluidized bed and carry out coating: fluidization temperature is 37 ℃, and fluidization pressure is 0.35MPa, and spray pressure is 0.20MPa, peristal...

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Abstract

The invention belongs to the field of medicine preparation science, and particularly relates to a sustained-release composition of sitagliptin and simvastatin, a preparation method of the sustained-release composition, and a sustained-release preparation of sitagliptin and simvastatin. The sustained-release composition of the sitagliptin and the simvastatin disclosed by the invention is composed of a sitagliptin coated pellet and a simvastatin sustained-release pellet at the mass ratio of (10:1) to (1:1). The sustained-release composition of the sitagliptin and the simvastatin is simple in prescription and process; the sitagliptin and the simvastatin can be slowly released within 24 hours; the sitagliptin and the simvastatin always work together, so that the plasma drug concentration can be well stabilized; the peak valley phenomenon of the plasma drug concentration is avoided; the toxic and side effects on a human body caused by the medicine are reduced; the bioavailability of the medicine is improved; the medication frequency is reduced; and the compliance of a patient is improved. The preparation method of the sustained-release composition of the sitagliptin and the simvastatin disclosed by the invention is simple to operate, and is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a sitagliptin-simvastatin sustained-release composition, a preparation method and a sitagliptin-simvastatin sustained-release preparation. Background technique [0002] Sitagliptin is a triazolylpiperazine compound with a β-amino acid structure, and its chemical name is (2R)-4-oxo-4-[3-(trifluoromethyl)5,6-dihydro- [1,2,4]triazolo[4,3-α]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine. Sitagliptin is a dipeptidyl peptidase (DPP-4) inhibitor, which exerts its active effect by slowing down the inactivation of incretin hormone in patients with type II diabetes, and its specific structural formula is as follows: [0003] [0004] Simvastatin, the chemical name is 2,2-dimethylbutanoic acid-, 1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro- 4-Hydroxy-6-oxo-2H-2-pyranyl)-ethyl]-1-naphthyl ester. Simvastatin is a prodrug, and after administration,...

Claims

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Application Information

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IPC IPC(8): A61K31/4985A61K9/26A61K9/62A61P3/10A61P3/06A61K31/366
CPCA61K9/0002A61K9/1652A61K9/2009A61K9/2081A61K31/366A61K31/4985A61K2300/00
Inventor 颜携国陶安进马亚平袁建成
Owner HYBIO PHARMA
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