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 da

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0035] Example 1: Preparation of dabigatran etexilate solid dispersion

[0036] Set the control temperature of the Hake micromixing rheometer as 130 °C, the screw speed as 40 r / min, and the torque as 20 N.cm. Diol graft copolymer) is mixed at a ratio of 1:3 and placed in the feeding hopper. After the material is extruded, it is extruded in strips through the film hole of the die head, cooled at room temperature, pulverized, and passed through an 80-mesh sieve to obtain dabigatran Ester solid dispersion.

Example Embodiment

[0037] Example 2: Preparation of dabigatran etexilate enteric-coated tablets:

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

Example Embodiment

[0039] Example 3: Preparation of dabigatran etexilate enteric-coated tablets:

[0040] 350g of the solid dispersion of dabigatran etexilate 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. After the soft material is passed through a 30-mesh sieve, it is made into granules, pressed into tablets, and used for later use; the gelatin is added into pure water, heated until the gelatin is completely swollen, cooled to room temperature, and a plasticizer is added and stirred to dissolve, and a gelatin solution is obtained. The tablets were coated, and the coating weight gain was 15%, and 1000 tablets were made to obtain enteric-coated tablets.

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PUM

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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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