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Ticagrelor oral-disintegrating sustained release tablet and preparation method thereof

A technology of ticagrelor and sustained-release tablets, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of patients missing medication, increasing the risk of acute thrombosis, and unfavorable patients problems swallowing

Inactive Publication Date: 2016-08-17
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although ticagrelor has shown superiority over clopidogrel in clinical studies, the half-life of ticagrelor is only 12 hours. In order to maintain the drug effect, it needs to be taken twice a day, resulting in poor patient compliance. Most of the patients are middle-aged and elderly people, which leads to the occurrence of missed and off-time medications
Because the anticoagulant effect of ticagrelor will reverse rapidly after drug withdrawal, direct drug withdrawal is likely to increase the risk of acute thrombosis in patients, leading to myocardial infarction or stroke
In order to solve this problem, the patent CN102657629 discloses a sustained-release preparation of ticagrelor. Patients only need to take one tablet a day to exert the curative effect. Weak ability, ticagrelor needs to take 180mg per day, making sustained-release tablets will inevitably lead to larger tablet weight, which is not conducive to patients swallowing
The ticagrelor immediate-release / sustained-release double-layer tablet disclosed in patent CN201310522017 also does not solve this problem

Method used

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  • Ticagrelor oral-disintegrating sustained release tablet and preparation method thereof
  • Ticagrelor oral-disintegrating sustained release tablet and preparation method thereof
  • Ticagrelor oral-disintegrating sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Preparation of orally disintegrating sustained-release tablets of ticagrelor

[0022] Prescription composition:

[0023]

[0024]

[0025] Preparation Process:

[0026] (1) Co-dissolve ticagrelor and ethyl cellulose in ethyl acetate to form an oil phase, dissolve sodium lauryl sulfate in a saturated aqueous solution of ethyl acetate to form a water phase, slowly drop the oil phase into water Microspheres are formed in the phase, and then add an appropriate amount of water to precipitate the microspheres, wash with pure water three times, and dry at 60°C to constant weight to obtain the microspheres;

[0027] (2) Weigh ticagrelor sustained-release microspheres, microcrystalline cellulose PH101 and low-substituted hydroxypropyl cellulose, mix evenly, granulate with purified water, granulate with 24 mesh, dry the granules at 50°C to 1~ 3%, 24 mesh whole grains, plus magnesium stearate and aspartame, compressed into tablets. The ticagrelor orally disinte...

Embodiment 2

[0028] Example 2: Preparation of orally disintegrating sustained-release tablets of ticagrelor

[0029] Prescription composition:

[0030]

[0031]

[0032] Preparation Process:

[0033] (1) Dissolve ticagrelor and polylactic acid in ethyl acetate to form an oil phase, dissolve poloxamer 188 in a saturated aqueous solution of ethyl acetate to form a water phase, slowly drop the oil phase into the water phase to form Microspheres, then add appropriate amount of water to precipitate the microspheres, wash with pure water three times, and dry in a fluidized bed to constant weight to obtain the microspheres;

[0034] (2) Weigh ticagrelor sustained-release microspheres, maltodextrin, hydroxypropyl methylcellulose and crospovidone, mix evenly, use purified water to granulate, granulate with 24 mesh, and dry the granule moisture at 50°C To 1~3%, 24 mesh whole grains, plus talcum powder, magnesium stearate and sucralose, compressed into tablets. The orally disintegrating sust...

Embodiment 3

[0035] Example 3: Preparation of orally disintegrating sustained-release tablets of ticagrelor

[0036] Prescription composition:

[0037]

[0038]

[0039] Preparation Process:

[0040] (1) Dissolve ticagrelor and PLGA in ethyl acetate to form an oil phase, dissolve Tween 80 in a saturated aqueous solution of ethyl acetate to form a water phase, slowly drop the oil phase into the water phase to form microspheres, Then add an appropriate amount of water to precipitate the microspheres, wash with pure water three times, and dry in a fluidized bed to constant weight to obtain the microspheres;

[0041] (2) Weigh ticagrelor sustained-release microspheres, mannitol, microcrystalline cellulose PH101 and pregelatinized starch, granulate with purified water, granulate with 24 mesh, and dry the granules at 50°C to 1-3% moisture , 24 mesh whole grains, plus magnesium stearate and stevioside, compressed into tablets. The orally disintegrating sustained-release tablet of ticagre...

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Abstract

The invention discloses a ticagrelor oral-disintegrating sustained release tablet, belongs to the field of medicinal preparations, and concretely relates to a sustained release preparation rapidly disintegrating in the oral cavity after being taken. The ticagrelor oral-disintegrating sustained release tablet is prepared through the following steps: preparing microcapsules with a sustained release effect from a main medicine and a suitable capsule material, proportioning the microcapsules and auxiliary materials, and carrying out wet granulation, wherein the auxiliary materials comprise a filler, an adhesive, a disintegrating agent, a lubricant and a flavoring. The ticagrelor oral-disintegrating sustained release tablet can rapidly disintegrate in the oral cavity after being orally taken, can continuously and stably release in vivo after being orally taken, can reduce the acute thrombus formation risk of patients, increases the compliance of the patients, and has important clinic application values.

Description

technical field [0001] The invention relates to a pharmaceutical preparation for treating cardiovascular diseases, in particular to a ticagrelor orally disintegrating sustained-release tablet and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Ticagrelor is an oral anti-platelet aggregation drug developed by AstraZeneca. Ticagrelor was approved by the European Union in December 2010 for reducing the occurrence of thrombotic events in patients with acute coronary syndrome (ACS), and its trade name is Brilique in the European market. The drug was approved by the US FDA on July 20, 2011, and its trade name is Brilinta. [0003] Ticagrelor is a novel, selective anticoagulant and the first reversible binding P2Y12 adenosine diphosphate receptor (ADP) antagonist that can reversibly act on vascular smooth muscle cells (VSMC ) on the purine 2 receptor subtype P2Y12, which has obvious inhibitory effect on ADP-induce...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K47/38A61K47/34A61K31/519A61P7/02
CPCA61K9/0002A61K9/2031A61K9/2054A61K9/2077A61K31/519
Inventor 冯思欣张庭
Owner BEIJING VENTUREPHARM BIOTECH
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