Oral double-pellet pharmaceutical composition of dabigatran or its salt

A technology of dabigatran etexilate and double pellets, applied in the directions of drug combination, pill delivery, pharmaceutical formulation, etc., can solve the problems affecting the roundness of the tartaric acid pill core, the surface non-roundness of the tartaric acid core and the stability of the active substance. issues of sex

Active Publication Date: 2015-01-14
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The tartaric acid core core prepared by the above method has satellite particles (satellites) on the surface, and these satellite particles affect the roundness of the tartaric acid pellet core, which will cause the integrity of the outer isolation layer wrapped in the tartaric acid pellet core, and cannot make tartaric acid Effective separation from the active ingredient may affect the stability of the active substance in the preparation during storage
Due to the existence of the defect of the tartaric acid core core surface non-roundness prepared by the above method, and this defect is random and unavoidable, the finished preparation pellets prepared by the above tartaric acid core core also have defects during storage. The risk of instability of the active substance

Method used

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  • Oral double-pellet pharmaceutical composition of dabigatran or its salt
  • Oral double-pellet pharmaceutical composition of dabigatran or its salt
  • Oral double-pellet pharmaceutical composition of dabigatran or its salt

Examples

Experimental program
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Effect test

Embodiment

[0058] Prescription and process:

[0059] 1. Preparation of pills containing:

[0060] 1) List of prescriptions containing pills:

[0061]

[0062]

[0063] 2) Preparation method of pills:

[0064] a) Pill core with pills: Add the HPC-EF in the proportion of the prescribed amount into the isopropanol solution, stir to dissolve, add the other components in the prescribed amount and stir to form a uniform suspension, and set aside. Take the sucrose core in the proportion of the prescription and put it into the miniGlatt fluidized bed coating machine, and gradually spray the coating solution on the outside of the sucrose core under the following parameter conditions until a suitable pellet is formed.

[0065] Coating parameters: fluidization pressure 0.15-0.30 bar, atomization pressure 1.20-1.50 bar, liquid feeding speed 3.0-5.0, pellet temperature 20-25 °C.

[0066] b) Isolation gown containing pills: Disperse the prescribed amount of Opadry in purified water to make th...

experiment example

[0080] The inventors conducted in vitro dissolution behavior investigations and in vivo biological studies on capsules of different combinations of the pellets of the examples in the present invention.

[0081] In vitro study: 900ml of 0.01M HCl, purified water, and pH 4.5 acetate buffer salt were used as dissolution media respectively, and the basket method was performed at 100 rpm to investigate the in vitro dissolution rate of the pellets prepared in the examples. Among them, 0.01M HCl and purified water are the main investigation media, and it is stipulated that the cumulative dissolution rate of the drug in the pellets in 0.01M HCl should not be less than 85% in 30 minutes, the cumulative dissolution rate in purified water should not be lower than 70% in 30 minutes, and the cumulative dissolution rate in 60 minutes should not be less than 85%. less than 85%. Dissolution curve see attached Figure 3-7 .

[0082] The results of in vitro study showed that different formula...

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Abstract

This invention relates to an oral double-pellet pharmaceutical composition of dabigatran or its salt. Specifically, the double-pellet pharmaceutical composition comprises: a) a spherical or sphere-like medicated pellet composed of an active substance, a pharmaceutically common pore-foaming agent, and a disintegrating agent and / or an adhesive, with the medicated pellet wrapped by an isolation layer formed by a water soluble polymer; and b) an organic acid pellet containing the adhesive and / or the pore-forming agent and / or the disintegrating agent, with the water solubility of the organic acid at 20DEG C being greater than 1g / 250ml. The two pellets are mixed evenly according to proportion and then loaded into a capsule shell, or a pharmaceutically common diluent and / or a pore-forming agent and / or a disintegrating agent and / or a lubricant are / is added to be pressed into tablets. The pharmaceutical composition has the advantages of simple preparation process, good reproducibility, good in vitro dissolution and higher in vivo bioavailability.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing dabigatran etexilate or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique [0002] The chemical structure of the active substance dabigatran etexilate involved in the present invention is 3-[(2-{[hexyloxycarbonylamino-imino-methyl]phenylamino]-methyl}-methyl-1H- Benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-hexyl propionate. Having the following chemical structure, this active substance is known from WO98 / 37075. [0003] [0004] Dabigatran etexilate [0005] The above-mentioned compound has the function of inhibiting thrombin and prolonging the thrombin time. The Chinese name is dabigatran etexilate, which can be used to prevent deep vein thrombosis and stroke after surgery. Dabigatran etexilate is a kind of prodrug, which is converted into dabigatran with direct anticoagulant...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K9/20A61K9/48A61P9/10A61P7/02
Inventor 王蕊瑞陈玮琦孙长安王小雷
Owner JIANGSU HANSOH PHARMA CO LTD
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