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A dabigatran etexilate solid dispersion enteric-coated preparation and a preparing method thereof

A technology of dabigatran etexilate and solid dispersion, which is applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc., can solve problems such as low bioavailability, and achieve inhibition of repolymerization. knot, improve dissolution, and the effect of simple process

Inactive Publication Date: 2017-06-23
GUIZHOU YIBAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to overcome the defects in the above-mentioned prior art, the invention provides a kind of enteric-coated preparation containing dabigatran etexilate, which overcomes the solubility of dabigatran etexilate and its salt and the dependence of the oil-water partition coefficient on the pH value, Solving the technical problem of low oral bioavailability of dabigatran etexilate and its salts

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: preparation of dabigatran etexilate mesylate solid dispersion

[0036] It is 130 ℃ to set the control temperature of the Huck micro mixing rheometer, the screw speed is 40r / min, and the torque is 20N.cm, and the drug dabigatran etexilate and Solupus (polyethylene caprolactam-polyvinyl acetate-polyethylene Glycol graft copolymer) is mixed according to 1:3 and placed in the hopper. After the material is extruded, it is extruded in strips from the film hole of the machine head, cooled at room temperature, crushed, and passed through a 80-mesh sieve to obtain dabigatran ester solid dispersion.

Embodiment 2

[0037] Embodiment 2: the preparation of dabigatran etexilate enteric-coated tablet:

[0038] 300g of dabigatran etexilate solid dispersion prepared in step 1, 20g of low-substituted hydroxypropyl cellulose, 20g of crospovidone, 2g of microcrystalline cellulose, 2g of micropowder silica gel, and an appropriate amount of 5% PVP aqueous solution are prepared After the soft material is passed through a 24-mesh sieve, it is made into granules, pressed into tablets, and used for later use; add gelatin to pure water, heat until the gelatin swells completely, cool down to room temperature, add a plasticizer and stir to dissolve, and obtain a gelatin solution. The tablets are coated, and the coating weight gain is 10%, and 1000 tablets are made to obtain enteric-coated tablets.

Embodiment 3

[0039] Embodiment 3: the preparation of dabigatran etexilate enteric-coated tablet:

[0040] 350g of the dabigatran etexilate solid dispersion prepared in step 1, 50g of low-substituted hydroxypropyl cellulose, 50g of crospovidone, 6g of microcrystalline cellulose, 4g of micropowder silica gel, and an appropriate amount of 5% PVP aqueous solution are prepared After the soft material is passed through a 30-mesh sieve, it is made into granules, pressed into tablets, and used for later use; add gelatin to pure water, heat until the gelatin swells completely, cool down to room temperature, add a plasticizer and stir to dissolve, and obtain a gelatin solution. The tablets are coated, and the coating weight gain is 15%, and 1000 tablets are made to obtain enteric-coated tablets.

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Abstract

A dabigatran etexilate enteric-coated preparation and a preparing method thereof are provided. Dabigatran etexilate that is a medicine active component is prepared into a solid dispersion through a hot melting extrusion technique, and further prepared into the enteric-coated preparation. The preparation overcomes dependence of solubility and oil-water partition coefficients of the dabigatran etexilate and salts thereof on pH values, improves membrane permeability of a medicine in intestinal juice, improves medicine absorption, avoids or reduces hepatic first-pass effects, increases medicine bioavailability, and avoids hydrolysis of water-insoluble dabigatran etexilate and adverse irritation of the medicine on the gastrointestinal tract. A process is simple. Medicine properties are stable. The preparation is convenient to take.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a dabigatran etexilate solid dispersion enteric-coated preparation and a preparation method thereof. Background technique [0002] The active substance dabigatran etexilate was first disclosed in WO98 / 37075, and it is a double prodrug developed by Boehringer Ingelheim (Boehringer Ingelheim), Germany, which can be converted into dabigatran with anticoagulant activity in vivo. group. Dabigatran binds to the fibrin-specific binding site of thrombin, preventing fibrinogen from being cleaved into fibrin, thereby blocking the final step of the coagulation cascade network and thrombus formation. [0003] Both the solubility and the oil-water partition coefficient of dabigatran etexilate have significant pH value dependence. The solubility decreases with the increase of pH value, while the oil-water partition coefficient is just the opposite, which increases with the increase ...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K31/4439A61K9/40A61P7/02
Inventor 窦啟玲黄成武
Owner GUIZHOU YIBAI PHARMA CO LTD
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