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Oral effervesce tablets for treating cardiovascular and cerebrovascular diseases, and prepn. method therefor

A cerebrovascular disease and effervescent tablet technology is applied to the oral effervescent tablet of breviscapine and its preparation field, and achieves the effects of fast absorption, less intestinal residue and obvious therapeutic effect

Inactive Publication Date: 2005-01-05
上海天晟医药化工研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Breviscapine is a flavonoid glycoside structure, which is a poorly soluble drug. After measuring the release rate of commercially available tablets, the result is that its dissolution rate is 80% within 1.5 hours, and about 70% within 45 minutes. Therefore, Breviscapine Tablets There is not only a disintegration problem, but also a dissolution process, and because breviscapine is insoluble in acidic gastric juice, after oral administration of its tablet, even if it effervescent rapidly in the stomach, breviscapine is rarely released in the gastric juice, so Its solid formulation has problems with absorption rate and bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Components:

[0038] Raw materials - breviscapine 20g;

[0039] Diluent - mannitol 100g, cross-linked polyvinylpyrrolidone 20g, lactose 100g;

[0040] Disintegrant—partially pregelatinized starch (Starch) 8.5g;

[0041] Effervescent agent—sodium bicarbonate 20g, tartaric acid 16g;

[0042] Glidant - micropowder silica gel 10g;

[0043] Flavoring agent——lemon essence 5g; aspartame 1.5g;

[0044] Lubricant - Magnesium Stearate 4g.

[0045] Prepared by powder direct compression method,

[0046] The first step is to accurately weigh each raw material and auxiliary material according to the dosage of the above components, and the total weight is 305g;

[0047] Step 2: Grind breviscapine and pass through a 100-mesh sieve; mannitol, partially pregelatinized starch (Starch), and lactose are dried at 45°C respectively, and ground into powder and passed through a 100-mesh sieve for later use;

[0048] The third step is to dry the sodium bicarbonate and tartaric acid respec...

Embodiment 2

[0052] Components:

[0053] Raw materials - breviscapine 20g;

[0054] Diluent - mannitol 100g, cross-linked polyvinylpyrrolidone 20g, lactose 100g;

[0055] Effervescent agent—partially pregelatinized starch (Starda) 8.5g;

[0056] Effervescent agent—sodium bicarbonate 20g, citric acid 16g;

[0057] Glidant - micropowder silica gel 10g;

[0058] Flavoring agent——lemon essence 5g; aspartame 1.5g;

[0059] Lubricant - Magnesium Stearate 4g.

[0060] Prepared by powder direct compression method,

[0061] The first step is to accurately weigh each raw material and auxiliary material according to the component dosage required by the prescription, and the total weight is 305g;

[0062] Step 2: Grind breviscapine and pass through a 100-mesh sieve; mannitol, partially pregelatinized starch (Starch), and lactose are dried at 45°C respectively, and ground into powder and passed through a 100-mesh sieve for later use;

[0063] The third step is to dry the sodium bicarbonate and cit...

Embodiment 3

[0067] Components:

[0068] Raw materials - breviscapine 20g;

[0069] Diluent - mannitol 100g, cross-linked polyvinylpyrrolidone 10g, lactose 100g;

[0070] Disintegrant—partially pregelatinized starch (Starch) 8.5g;

[0071] Effervescent agent—sodium bicarbonate 20g, fumaric acid 16g;

[0072] Glidant - micropowder silica gel 10g;

[0073] Flavoring agent——lemon essence 5g; aspartame 1.5g;

[0074] Lubricant - Magnesium Stearate 4g.

[0075] Prepared by powder direct compression method,

[0076] The first step is to accurately weigh each raw material and auxiliary material according to the component dosage required by the prescription, and the total weight is 305g;

[0077] Step 2: Grind breviscapine and pass through a 100-mesh sieve; mannitol, partially pregelatinized starch (Starch), and lactose are dried at 45°C respectively, and ground into powder and passed through a 100-mesh sieve for later use;

[0078] The third step is to dry the sodium bicarbonate and fumari...

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PUM

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Abstract

A oral-cavity effervescent talbet for treating cardiovascular and cerebrovascular diseases, such as coronary heart disease, angina pectoris, cerebral thrombosis, cerebral infarction, etc. is prepared from breviscapine, diluent, disintegrant, effervescent agent, flavouring, flowing aid,and lubricant.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to an oral effervescent tablet for treating cardiovascular and cerebrovascular diseases, in particular to an oral effervescent tablet whose main component is breviscapine and a preparation method thereof. Background technique [0002] Breviscapus is a total flavonoid extracted from Erigron breviscapus (Vaniot) Hand Mazz breviscapus of Compositae. Symptoms caused by ischemia are often used in the treatment of cardiovascular diseases such as coronary heart disease, angina pectoris, cerebral thrombosis, and paralysis caused by cerebral infarction. Common breviscapine tablets, which are commonly used in clinical practice at present, have relatively definite curative effects, but have defects such as slow dissolution rate, small dissolution amount, and inconvenient swallowing. Commonly used preparations based on scutellarin, as well as oral preparations such as sustained-release tablets...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/46A61K31/7048A61P9/10
Inventor 蒋雪涛康永贞徐喆
Owner 上海天晟医药化工研究所
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