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Compound preparation of Fasudil and Beraprost as well as preparation method and application thereof

A technology of beraprost and fasudil, applied in the field of pharmacy, can solve problems such as unsatisfactory effects and complicated treatment

Inactive Publication Date: 2011-09-21
TIANJIN CHASE SUN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Pulmonary hypertension, common in adolescent patients, is an extremely nasty disease that is now complicated and less effective in treatment

Method used

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  • Compound preparation of Fasudil and Beraprost as well as preparation method and application thereof
  • Compound preparation of Fasudil and Beraprost as well as preparation method and application thereof
  • Compound preparation of Fasudil and Beraprost as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074]

[0075]

[0076] Preparation:

[0077] After crushing the prescribed amount of Fasudil through a 120 mesh sieve, mix it with low-substituted hydroxypropyl cellulose, lactose, microcrystalline cellulose, starch, and calcium hydrogen phosphate that have passed through an 80 mesh sieve to obtain a mixed powder. Dissolve with appropriate amount of water, add mixed powder and mix evenly, then add 10% starch slurry to make soft material, granulate through 24 mesh sieve, ventilate and dry at 55°C, granulate with 20 mesh sieve, mix evenly with magnesium stearate, press tablet, get compound tablet core.

Embodiment 2

[0079]

[0080] Preparation:

[0081] Grind the prescribed amount of Fasudil through a 100-mesh sieve, mix evenly with low-substituted hydroxypropyl cellulose, lactose, and microcrystalline cellulose that have passed through an 80-mesh sieve, and add 2% hydroxypropyl methylcellulose as a soft material , granulated through a 24-mesh sieve, ventilated and dried at 55°C, granulated through a 20-mesh sieve and mixed evenly with magnesium stearate to obtain Granule 1 for later use.

[0082] After dissolving the prescribed amount of beraprost with an appropriate amount of water, mix it evenly with low-substituted hydroxypropyl cellulose, lactose starch, and microcrystalline cellulose that have passed through an 80-mesh sieve, and add 2% hydroxypropyl methylcellulose as a soft material , granulated through a 24-mesh sieve, ventilated and dried at 55°C, granulated through a 20-mesh sieve and mixed evenly with magnesium stearate to obtain granule 2 for later use.

[0083] The granu...

Embodiment 4

[0090]

[0091]

[0092] Dissolve the prescribed amount of fasudil and beraprost in 300ml of water to obtain solution 1; pass the prescribed amount of microcrystalline cellulose, lactose, and starch through a 100-mesh sieve and mix them evenly, place them in a vulcanized bed, and heat them with 60°C hot air Boil the mixed powder, then spray the atomized liquid of Solution 1 into the boiling mixed powder to make granules of suitable size, pass through a 40-mesh sieve for granulation, mix with magnesium stearate, fill 3# capsules, Get compound capsules.

[0093] Examples 3 and 4 prepared capsule samples, 300 capsules were filled by hand, 20 capsules were randomly weighed, and the RSD was calculated, which showed that the difference in weight between capsules was small. Dissolution is ideal. See Table 2 for the data.

[0094] Table 2

[0095]

[0096] Preparation:

[0097] Grind the prescribed amount of fasudil and beraprost through a 100-mesh sieve, low-substituted ...

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PUM

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Abstract

The invention belongs to the pharmaceutical field and relates to a compound preparation of Fasudil and Beraprost as well as a preparation method and application thereof to treating pulmonary hypertension. The compound preparation in the invention comprises Fasudil, Beraprost and auxiliary materials chosen from auxiliary materials acceptable in pharmacy, such as a disintegrating agent, an adhesive, an excipient, diluents, a lubricant, framework materials used for controlling the release of active ingredients in slow and controlled release agents, and the like. Proper carriers are chosen according to different types of drugs.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a compound preparation of fasudil and beraprost and its preparation method and application, which are used for the treatment of pulmonary hypertension. Background technique [0002] Fasudil [hexahydro-1-(5-isoquinolinesulfonyl)-homopiperazine, Fasudil] is a Rho kinase inhibitor. Its molecular weight is 327.83 and its molecular formula is C 14 h 17 N 30 2S·HCl, structural formula: [0003] [0004] Studies have confirmed that the Rho kinase pathway is one of the important pathogenic pathways leading to pulmonary artery constriction and pulmonary vascular remodeling in patients with pulmonary arterial hypertension. For pulmonary hypertension, fasudil can reduce the activity of Rho kinase, inhibit the contraction of pulmonary artery vascular smooth muscle, dilate pulmonary arteries, reduce pulmonary artery resistance, and reduce pulmonary arterial pressure. [0005] Beraprost is a deriv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/551A61K31/343A61P9/12
Inventor 姚小青孙长海董凯韩志东
Owner TIANJIN CHASE SUN PHARM CO LTD
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