Preparation method of compound oral solid preparation containing Ticagrelor

A technology for ticagrelor and solid preparations, which is applied in the field of preparation of ticagrelor compound oral solid preparations, can solve problems such as increased incidence of gastrointestinal side effects, and achieves improved compliance, scientific preparation method, and compound specification setting. reasonable effect

Inactive Publication Date: 2017-10-20
XIAMEN ENCHENG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0022] Oral aspirin is gastric irritating, studies show increased incidence of gastrointestinal side effects with routine use

Method used

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  • Preparation method of compound oral solid preparation containing Ticagrelor
  • Preparation method of compound oral solid preparation containing Ticagrelor
  • Preparation method of compound oral solid preparation containing Ticagrelor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Example 1 (Tablet - Formulation A)

[0065]

[0066] Preparation:

[0067] a. Preparation of aspirin enteric-coated tablets

[0068]Mix aspirin with microcrystalline cellulose, pregelatinized starch, and stearic acid evenly and then directly compress into tablets; prepare the isolation coating layer solution with Opadry film coating powder; mix Eudragit L30D-55 (30% water dispersion Glyceryl monostearate and triethyl citrate were added to the body) and stirred evenly to prepare an enteric-coated layer solution. Use a high-efficiency coating pan to coat the plain tablets with an isolation coating and an enteric coating, and dry them in an oven at 40°C for 24 hours.

[0069] b. Preparation of ticagrelor granules:

[0070] Crush ticagrelor to particle size D 90 <85μm, then mixed with mannitol, calcium hydrogen phosphate, carboxymethyl starch sodium, wet granulation with hydroxypropyl cellulose solution as binder, dried, and then mixed with external magnesium stearat...

Embodiment 2

[0073] Example 2 (Capsules - Formulation B)

[0074]

[0075] Preparation:

[0076] a. Preparation of aspirin enteric-coated pellets

[0077] Mix aspirin and microcrystalline cellulose, use hypromellose and povidone as binders, and use an extrusion spheronization process to prepare active drug pellet cores. Then prepare Opadry film coating powder into film coating solution; dissolve Eudragit L100-55 in 95% ethanol, add triethyl citrate and stir evenly, then pour the suspension of talcum powder into In the L100-55 solution, the enteric-coated layer solution was prepared, and then the film coating layer and the enteric-coated layer were sprayed on the upper drug pellets by fluidized bed spraying technology to make aspirin enteric-coated pellets, and dried in an oven at 40°C Available within 24 hours.

[0078] b. Preparation of ticagrelor pellets:

[0079] Crush ticagrelor to particle size D 90 <85μm, and then mixed with microcrystalline cellulose and sodium carboxymethyl...

Embodiment 3

[0084] Example 3 (Tablet - Formulation C)

[0085]

[0086] Preparation:

[0087] a. Preparation of blank pellet core

[0088] The microcrystalline cellulose blank pellet core was used as the blank pellet core.

[0089] b. Preparation of aspirin enteric-coated pellets

[0090] The aspirin is dissolved in the ethanol solution of povidone to prepare the drug-containing layer solution. Mix Eudragit L30D-55 (30% water dispersion) and Eudragit NE30D (30% water dispersion) in proportion, then add glycerol monostearate and triethyl citrate and stir evenly to prepare Enteric layer solution. Opadry film coating powder is used to prepare film isolation coating solution. The drug-containing layer solution is sprayed onto the core of blank pellets by fluidized bed spraying technology to prepare drug-coated pellets. Then spray the coating solution of the isolation layer on the upper drug pellets, and then spray the enteric coating layer to make aspirin enteric-coated pellets, and ...

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PUM

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Abstract

The invention relates to a preparation method of a compound oral solid preparation containing Ticagrelor. According to the compound oral solid preparation, the content of Ticagrelor per unit of the preparation is 60-180 mg, preferably 60-90 mg; the content of aspirin or pharmaceutically acceptable salt or ester per unit of the preparation is 35-75 mg, preferrably 35-50 mg. The compound oral solid preparation is prepared from Ticagrelor, aspirin, a pellet core material, an adhesive, a film coating material, an enteric coating material, a diluent, a disintegrating agent and a lubricant. Ticagrelor granules, pellets or tablets and aspirin enteric pellets or enteric tablets are prepared separately, then mixed and bagged, capsulated or tableted, so that the purpose that Ticagrelor and aspirin are not directly contacted in a medicine composition preparation and can thereby keep stable is achieved.

Description

technical field [0001] The invention belongs to the field of the pharmaceutical industry, and in particular relates to a preparation method of a compound oral solid preparation of ticagrelor, specifically, preparing ticagrelor granules, pellets or tablets, and aspirin or a pharmaceutically acceptable salt thereof Or enteric-coated granules, enteric-coated pellets or enteric-coated tablets of esters, mixed in proportion to bag, or packed into capsules or compressed tablets to achieve ticagrelor and aspirin or its pharmaceutically acceptable salt or ester in the compound preparation product The purpose of increasing stability without direct contact. Background technique [0002] Acute coronary (coronary) syndrome (acute coronary syndrome, ACS) is one of the clinically common cardiovascular emergencies, with extremely high mortality and morbidity, and anti-platelet aggregation drugs have been listed as routine clinical treatment of ACS medication. [0003] Ticagrelor, also kn...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/20A61K31/519A61K31/616A61P9/10
CPCA61K9/2059A61K9/2072A61K9/2081A61K9/5042A61K9/5084A61K31/519A61K31/616A61K2300/00
Inventor 欧阳旭郭云珍王斌
Owner XIAMEN ENCHENG PHARMA CO LTD
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