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Stable capsule preparation containing dabigatran etexilate mesylate and preparation method of stable capsule preparation

A technology of dabigatran etexilate mesylate and tartaric acid is applied in the field of pharmaceutical preparations, which can solve the problems of rupture of the isolation membrane and reduce the stability of drugs, and achieve the effects of good dissolution, ensuring stability and product stability.

Inactive Publication Date: 2018-01-12
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method isolates the drug from the organic acid by coating the core of the drug pellet, but during the tableting process, the isolation film on the core of the drug pellet may be broken, allowing the drug to come into contact with the organic acid, reducing the stability of the drug

Method used

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  • Stable capsule preparation containing dabigatran etexilate mesylate and preparation method of stable capsule preparation
  • Stable capsule preparation containing dabigatran etexilate mesylate and preparation method of stable capsule preparation
  • Stable capsule preparation containing dabigatran etexilate mesylate and preparation method of stable capsule preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Preparation of tartrate pellets

[0061]

[0062] *Water and 95% ethanol are solvents that are removed during the process.

[0063] Preparation Process:

[0064] (1) Ball core process: Put the prescribed amount of tartaric acid granules (30-40 mesh) into the centrifugal granulation coating machine, mix the tartaric acid powder (100 mesh) and silicon dioxide, put them into the powder supply machine, and turn on The main engine and the blower can be adjusted until the particle flow in the cavity is smooth. Set the material temperature to 40°C, and when the temperature of the granules reaches the required temperature, turn on the spray gun to spray the slurry, wet the masterbatch with 3% hypromellose aqueous solution, observe the wetting status of the granules, and turn on the powder supply machine to start powder supply when appropriate . During the granulation process, the main machine speed, spraying speed and powder supply speed can be adjusted in time according ...

Embodiment 2

[0069] Preparation of dabigatran etexilate mesylate capsules

[0070] Dabigatran etexilate mesylate 173g

[0071] Mannitol 45 g

[0072] Silica 8 g

[0073] Crospovidone 25 g

[0074] Sodium stearyl fumarate (additional) 5 g

[0075] Sodium stearyl fumarate (additional) 2 g

[0076] Tartrate pellets 208 g

[0077] Made into 1000 capsules, wherein the capsule shell is selected from hypromellose capsule shell,

[0078] Specific steps:

[0079] 1. Preprocessing

[0080] Put the silicon dioxide and crospovidone into a blast drying oven at 80°C and dry until the water content is less than 2.5%.

[0081] 2. weighing

[0082] Double-checked and weighed dabigatran etexilate mesylate, mannitol, crospovidone, silicon dioxide and sodium stearyl fumarate, each passed through a 60-mesh sieve for later use.

[0083] 3. Primary mix:

[0084] According to the batch prescription, after checking the dosage by two people, put dabigatran etexilate mesylate, mannitol, crospovidone, silic...

Embodiment 3

[0096] Specification 110mg

[0097] Dabigatran etexilate mesylate 127g

[0098] Mannitol 33 g

[0099] Silica 6 g

[0100] Crospovidone 18 g

[0101] Sodium stearyl fumarate (internal addition) 3.6 g

[0102] Sodium stearyl fumarate (additional) 1.5 g

[0103] Tartrate pellets 152 g

[0104] Make 1000, wherein capsule shell is selected hypromellose capsule shell, and concrete preparation method is with embodiment 1.

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Abstract

The invention relates to the field of medicinal preparations, and in particular relates to a stable capsule preparation containing dabigatran etexilate mesylate and a preparation method of the stablecapsule preparation. Under the state of water solution, especially in acidic and alkaline media, dabigatran etexilate mesylate is prone to oxidation and hydrolysis. Due to the adoption of a specific process and selection for specific auxiliary materials, the preparation is good in stability, the loading differences conform to the limitation requirement, in addition, a preparation process has repeatability, and large-scale production can be realized.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a solid pharmaceutical preparation containing dabigatran etexilate mesylate and a preparation method thereof. Background technique [0002] Dabigatran etexilate mesylate is a new type of non-peptide direct thrombin inhibitor, which was approved by the US FDA on October 19, 2010 for the prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation treat. Dabigatran etexilate mesylate has the characteristics of oral administration, strong potency, no need for special drug monitoring, and few drug interactions. It has good clinical application prospects. Its structural formula is: [0003] [0004] Molecular formula: C34H41N7O5・CH4O3S [0005] Molecular weight: 723.86 [0006] Appearance: light yellow to yellow crystalline powder [0007] Solubility: pH dependent drug, greater solubility at low pH. Soluble in methanol, soluble in N,N-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K47/12A61K31/4439A61P7/02A61P9/10
Inventor 严洁
Owner TIANJIN HANRUI PHARMA
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