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

A technology for cerebrovascular diseases and effervescent tablets, which is applied in the oral effervescent tablet of breviscapine and its preparation field, to achieve fast absorption, obvious therapeutic effect, and improve clinical curative effect

Inactive Publication Date: 2007-06-20
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 material-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-micronized silica gel 10g;

[0043] Flavoring agent-lemon flavor 5g; aspartame 1.5g;

[0044] Lubricant-Magnesium stearate 4g.

[0045] Prepared by powder direct compression method,

[0046] The first step is to correctly weigh the raw materials and auxiliary materials 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, and then ground through a 100-mesh sieve for use;

[0048] The third step is to dry the sodium bicarbonate and tartaric acid at 45°C, grind them, and pass through a 100-mesh sieve for use;

...

Embodiment 2

[0052] Components:

[0053] Raw material-breviscapine 20g;

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

[0055] Effervescent agent-partially pregelatinized starch (Starch) 8.5g;

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

[0057] Glidant-micronized silica gel 10g;

[0058] Flavoring agent-lemon flavor 5g; aspartame 1.5g;

[0059] Lubricant-Magnesium stearate 4g.

[0060] Prepared by powder direct compression method,

[0061] The first step is to accurately weigh the ingredients and excipients 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, and then ground through a 100-mesh sieve for use;

[0063] The third step is to dry the sodium bicarbonate and citric acid at 45°C, grind them, and pass through a 100-mesh sieve for u...

Embodiment 3

[0067] Components:

[0068] Raw material-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-micronized silica gel 10g;

[0073] Flavoring agent-lemon flavor 5g; aspartame 1.5g;

[0074] Lubricant-Magnesium stearate 4g.

[0075] Prepared by powder direct compression method,

[0076] The first step is to accurately weigh the ingredients and excipients 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, and then ground through a 100-mesh sieve for use;

[0078] The third step is to dry the sodium bicarbonate and fumaric acid at 45°C, grind them, and pass through a 100-mesh sieve for use;...

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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 medicine, and relates to an oral effervescent tablet for treating heart and cerebrovascular diseases, and in particular to an oral effervescent tablet whose main component is breviscapine and a preparation method thereof. Background technique [0002] Breviscapus (Vaniot) Hand Mazz is a total flavonoids extracted from Erigron breviscapus (Vaniot) Hand Mazz. It has the functions of promoting blood circulation, removing blood stasis, dilating coronary and cerebral blood vessels, and can improve the heart and brain. Symptoms caused by ischemia are often used to treat cardiovascular diseases such as coronary heart disease, angina pectoris, cerebral thrombosis, and paralysis caused by cerebral infarction. Although the common breviscapine tablets that are commonly used in clinical practice are more effective, they have the disadvantages of slow dissolution rate, small dissolution rate, and inconvenient swallowing. C...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K9/20A61K9/46A61P9/10
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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