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Tracleer capsule and preparation method thereof

A technology of bosentan and capsules, which is applied in the field of pharmaceutical preparations, can solve the problems of reduced bioavailability, poor fluidity, and inconvenience in taking, and achieve the effects of promoting bioavailability, improving dissolution rate, and small difference in loading capacity

Active Publication Date: 2012-12-12
WUHAN WUYAO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The volume of bosentan capsules produced by this method is too large and inconvenient to take, and the wet granules prepared by adding the binder in the form of powder have poor formability and poor fluidity, which is not conducive to the dissolution of bosentan and reduces its bioavailability
[0006] Disclosed in CN101229373A is a preparation method of bosentan and rosiglitazone complex capsules, in which no solid dispersion is added, the lubricant is added internally, and the particles made by the PVP ethanol used are loose and powdery. Not conducive to the filling of capsules
[0007] At present, bosentan is only available in the form of tablets at home and abroad, and the price is expensive, which limits the choice of medication for both doctors and patients
It has been reported in the literature that the absorption rate of its oral tablet is about 50%. If the release in vitro is improved, there is a possibility to further increase its absorption rate

Method used

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  • Tracleer capsule and preparation method thereof
  • Tracleer capsule and preparation method thereof
  • Tracleer capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111]Example 1 Bosentan capsules (specification: 31.25mg / capsule)

[0112] prescription:

[0113] Bosentan 31.25g

[0114] Polyethylene glycol 6000 9g

[0115] Lactose 50g

[0116] Pregelatinized starch 12g

[0117] Sodium Carboxymethyl Starch 8.5g

[0118] 5% Povidone K30 aqueous solution appropriate amount

[0119] Micro Powder Silica 0.5g

[0120] Makes 1000 capsules

[0121] Preparation process: pass the raw materials and each auxiliary material through a 100-mesh sieve for use, mix polyethylene glycol 6000 and bosentan evenly, and then pour the mixture into a container containing lactose, pregelatinized starch, and sodium carboxymethyl starch Stir well, add an appropriate amount of 5% povidone K30 aqueous solution into the container to make soft materials, granulate with a 14-mesh sieve; dry at 50°C-60°C to a moisture content of 2.0-4.5%, 14-mesh sieve for granulation, and add micropowder The silica gel is mixed evenly and sent to test the content; the capsule fi...

Embodiment 2

[0122] Example 2 Bosentan capsules (specification: 31.25mg / capsule)

[0123] prescription:

[0124] Bosentan 31.25g

[0125] Polyethylene glycol 6000 10g

[0126] Lactose 55g

[0127] Sodium Carboxymethyl Starch 6g

[0128] 5% hypromellose aqueous solution

[0129] Magnesium Stearate 0.5g

[0130] Makes 1000 capsules

[0131] Preparation process: pass the raw materials and each auxiliary material through a 100-mesh sieve for use, mix polyethylene glycol 6000 and bosentan evenly, pour the mixture into a container containing lactose and sodium carboxymethyl starch and stir evenly, 5% aqueous solution of hypromellose is added to the container to make soft material, granulated with 14 mesh sieve; dried at 50 ℃-60 ℃ to moisture 2.0-4.5%, 14 mesh sieve and granulated, add magnesium stearate and mix Evenly, send the test content; determine the capsule filling range according to the test results, carry out 3# capsule filling, and package after passing the test.

Embodiment 3

[0132] Example 3 Bosentan capsules (specification: 31.25mg / capsule)

[0133] prescription:

[0134] Bosentan 31.25g

[0135] Polyethylene glycol 6000 8g

[0136] Lactose 60g

[0137] Sodium Carboxymethyl Starch 8g

[0138] 5% Povidone K30 aqueous solution appropriate amount

[0139] Magnesium Stearate 0.4g

[0140] Makes 1000 capsules

[0141] Preparation process: pass the raw materials and auxiliary materials through a 100-mesh sieve respectively for use, mix polyethylene glycol 6000 and bosentan evenly, then pour the mixture into a container containing lactose and sodium carboxymethyl starch and stir evenly, A 5% aqueous solution of povidone K30 is added to a container to make a soft material, granulated with a 14-mesh sieve; dried at 50°C-60°C to a moisture content of 2.0-4.5%, 14-mesh sieve and granulated, add magnesium stearate and mix well , send the test content; determine the capsule filling range according to the test results, carry out 3# capsule filling, and ...

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Abstract

The invention relates to a tracleer capsule and a preparation method thereof. The main medicaments of the capsule is characterized in that per 1000 capsules comprise the following components in parts by weight: 31.25 to 125 parts of tracleer, 6 to 15 parts of solid dispersion, 55 to 80 parts of filler, 6 to 13 parts of disintegrant, a proper amount of adhesive, and 0.4 to 1.0 part of lubricant, wherein the solid dispersion is polyethylene glycol 6000, polyvinylpyrrolidone, or combination of the polyethylene glycol 6000 and the polyvinylpyrrolidone in an arbitrary proportion; the filler is one or combination of a plurality of lactose, pregelatinized starch and microcrystalline cellulose; the disintegrant is sodium carboxymethyl starch; and the adhesive is hydroxypropyl methylcellulose and povidone; and the lubricant is magnesium stearate. The preparation method is simple, has the advantages of few process links and process parameters, short production cycle, low production cost and suitability for industrial production.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a capsule for treating pulmonary hypertension and a preparation method thereof, in particular to a bosentan capsule and a preparation method thereof. Background technique: [0002] Bosentan is a specific, competitive dual endothelin receptor blocker with affinity for ETA and ETB receptors, with a slightly lower affinity for ETA receptors than for ETB receptors. high. It can reduce vascular pressure, prevent the proliferation of heart and blood vessels, reduce pulmonary fibrosis and inflammation, and is clinically used for the treatment of patients with pulmonary arterial hypertension who have dyspnea symptoms during rest or light exercise (functional status score of III or IV), and for improving Exercise tolerance and related symptoms. [0003] On November 20, 2001, the US FDA approved the marketing of bosentan oral tablets (specifications: 62.5mg and 125mg) of ACTELIO...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/48A61K31/506A61K47/32A61K47/34A61K47/38A61P11/00A61P9/12A61P39/00A61K47/10
Inventor 耿海明冯小路黄璐杨波
Owner WUHAN WUYAO SCI & TECH