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Oral preparation of quick releasing Breviscapini and producing method

A technology of breviscapine and quick-release preparations, which is applied in the direction of pill delivery, pharmaceutical formulations, and medical preparations containing active ingredients, etc. It can solve problems such as poor solubility, danger of occurrence, and stuck in the esophagus, and achieve oral immediate release Strong, stable and reliable product, good stability effect

Inactive Publication Date: 2005-11-16
云南一尧科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because breviscapine has poor solubility and is a glycoside compound, the bioavailability of breviscapine after oral administration is very poor (<5%). Therefore, improving the bioavailability of breviscapine after oral administration is an important problem for its oral preparations
In addition, patients with cardiovascular and cerebrovascular diseases often have some critical illnesses. For example, in special environments where drinking water cannot be found on the road or in the field, if ordinary oral preparations are used, it is difficult for the patient to swallow the medicine, and even if swallowed, it may be stuck in the esophagus. , in danger

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Prepare breviscapine orally disintegrating tablets, formula (1000 tablets):

[0022] Breviscapine (particle size<35μm) 5g

[0023] Microcrystalline fiber (100 mesh) 125g

[0024] Soluble starch (120 mesh) 50g

[0025] Carmellose sodium (80 mesh) 10g

[0026] Magnesium stearate (60 mesh) 12g

[0027] Mannitol (100 mesh) 60g

[0028] Preparation process: crush breviscapine and the above-mentioned various raw materials to the required particle size by air-flow freezing crushing method or ball milling method, and mix thoroughly according to the formula, and then directly compress into tablets to obtain 5 mg of breviscapine (specification) per tablet orally disintegrating tablets.

Embodiment 2

[0030] Prepare breviscapine orally disintegrating tablets, formula (1000 tablets):

[0031] Breviscapine (particle size<35μm) 20g

[0032] Microcrystalline fiber (100 mesh) 120g

[0033] Lactose (120 mesh) 54g

[0034] Carmellose sodium (80 mesh) 10g

[0035] Polyethylene glycol-10000 (60 mesh) 8g

[0036] L-arginine hydrochloride (80 mesh) 2.1g

[0037] Sorbitol (120 mesh) 40g

[0038] Strawberry essence 0.1g

[0039] Preparation process: subdivide scutellarin and the above-mentioned various raw materials by the method of Example 1, mix thoroughly according to the formula, and then directly compress into tablets to obtain orally rapidly disintegrating tablets containing 20 mg of scutellarin (specification).

Embodiment 3

[0041] Breviscapine orally disintegrating tablets, formula (1000 tablets):

[0042] Breviscapine (particle size<35μm) 35g

[0043] Microcrystalline fiber (100 mesh) 120g

[0044] Soluble starch 50g

[0045] Lactose (120 mesh) 24g

[0046] Low-substituted hydroxypropyl cellulose (80 mesh) 40g

[0047] Polyethylene glycol-10000 (60 mesh) 8g

[0048] L-malic acid 2.5g

[0049] Preparation process: refine and mix according to the method of Example 1, wet granulate with tablets, dry, granulate, and sieve, and press with granules to obtain 35 mg of scutellarin (specification) per tablet orally disintegrating tablets.

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PUM

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Abstract

A quickly-releasing tablet of breviscapine for treating the acute cardiovascular and cerebrovascular diseases is prepared from breviscapine and the medicinal auxiliary able to promote the secretion of saliva.

Description

technical field [0001] The invention relates to an oral drug for treating cardiovascular and cerebrovascular diseases, more precisely, relates to a breviscapine oral quick-release preparation which is taken without water or only uses a small amount of water and a production method thereof. Background technique [0002] Erigeron breviseapus (Vant.) Hand.-Mazz is the dry whole plant of Erigeron breviseapus (Vant.) Hand.-Mazz. Yunnan folks call it Erigeron breviscapus, Erigeron elegans, and Asarum esophagus. Has been included in the national standard. The so-called scutellarin is a flavonoid compound isolated and extracted from Erigeron breviscapine, the main component is scutellarin, and it still contains a small amount of scutellarin. Breviscapine and its injections, tablets, powder injections and other varieties have all met national standards. The implementation standard is WS 3 -B-3822-98,WS 3 -B-3879-98, etc., are a kind of botanical medicine unearthed during the vig...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048
Inventor 任秀云
Owner 云南一尧科技开发有限公司
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