CN100441194C - Erigeron breviscapus extraction dry suspensoid agent - Google Patents
Erigeron breviscapus extraction dry suspensoid agent Download PDFInfo
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- CN100441194C CN100441194C CNB2004100166840A CN200410016684A CN100441194C CN 100441194 C CN100441194 C CN 100441194C CN B2004100166840 A CNB2004100166840 A CN B2004100166840A CN 200410016684 A CN200410016684 A CN 200410016684A CN 100441194 C CN100441194 C CN 100441194C
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- breviscapine
- suspension agent
- mixed suspension
- dry mixed
- solid powder
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Abstract
The present invention relates to a breviscapine containing dry mixed suspension agent medicinal preparation for treating cardiovascular diseases and cerebrovascular diseases, which belongs to the field of a medicinal preparation. The present invention uses the breviscapine as an active component to add suitable auxiliary materials, such as filling agents, suspending agents, a flow aid, a lubricating agent and a taste modifying agent; the active component and the auxiliary materials are evenly mixed in an equivalently and progressively increasing method to prepare the dry mixed suspension agent after the active component and the auxiliary materials are dried and pulverized. The solid powder of the dry mixed suspension agent of the present invention has the advantages of good flowability, low settling rate and favorable redispersibility. The solid powder of the dry mixed suspension agent can be rapidly changed into the uniform and stable mixed suspension agent after water is added and the solid powder of the dry mixed suspension agent is stirred. The solid powder of the dry mixed suspension agent is convenient for a patient to take. The preparation is verified by animal experiments to have the advantages of quick effect, high biologic utilization rate, simple preparing method and convenient use. The biologic utilization rate of the preparation is more than 10 times higher than that of the ordinary tablet.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relate to a kind of pharmaceutical preparation that is used for the treatment of cardiovascular and cerebrovascular disease.Be specifically related to a kind of dry suspension that contains breviscapine.
Background technology
Breviscapine (Brevescapine) is from feverfew Erigeron breviscapus (Vant.) Hand.-Mazz. (original name Herba Erigerontis, have another name called Herba Erigerontis, Erigeron Breviscapus (Vant.) Hand.-Mazz.) separates the flavonoid material that obtains in, mainly contain scutellarin (Scutellarin, chemistry by name 4 ', 5,6-trihydroxyflavone-7-glucuronide), also contain a small amount of breviscapine and other flavones ingredients.
Existing pharmacodynamic study shows, breviscapine has expansion of cerebral vascular, reduce cerebral vascular resistance, the cerebral blood flow increasing amount, microcirculation improvement improves blood-brain barrier permeability, the immunization of enhancing body macrophage phagocytic, cerebral ischemia due to the antagonism pituitrin, anoxia, and can resist by adenosine diphosphate (ADP) (the platelet gel effect that ADP causes.Breviscapine is widely used in disease such as paralyse after the uncertain apoplexy of treatment cerebral thrombosis, cerebral infarction and type clinically, and is harmless to the heart, liver, spleen, lung, kidney stomach function regulating function, also do not see obvious toxic and side effects.
The listing preparation variety that with the breviscapine is raw material at present has Breviscapini injection, Herba Erigerontis injection, Herba Erigerontis tablet, erigeron breviscapus granule and YIMAIKANG PIAN, all existing national standard of described listing kind.In addition, be in new drug at present and declare the stage, or apply for a patent the preparation in stage and also have breviscapine dispersible tablet, drop pill, slow releasing tablet, controlled release tablet, soft capsule and transfusion etc.
Because breviscapine is a flavones ingredient, its water solublity and fat-soluble all very poor, therefore oral plain particles agent and tablet are often because of the dissolution problem causes drug effect slow, and bioavailability is poor; Though at present oral preparation of quick releasing such as dispersible tablet, drop pill are arranged, all do not report characteristics of pharmacokinetics and bioavailability in its body.Though the absorption of breviscapine drug administration by injection is soon, the bioavailability height uses inconvenience, patient's poor compliance, and prepare, pack, transport, store equal inconvenience.Therefore develop quick-acting, high bioavailability, and Breviscapine easy to use is very necessary.
Summary of the invention
The purpose of this invention is to provide a kind of rapid-action, bioavailability is high, preparation is simple, the breviscapine novel pharmaceutical formulation of taking convenience---breviscapine dry suspension.
Breviscapine dry suspension of the present invention is an active component with breviscapine (commercially available), and adds proper auxiliary materials and make dry suspension.
The content of breviscapine is to contain breviscapine 5～500mg in the unit dose package in the breviscapine dry suspension of the present invention.
Adjuvant in the breviscapine dry suspension of the present invention includes but not limited to filler, suspending agent, fluidizer, lubricant, surfactant and correctives.
Filler of the present invention includes but not limited to starch, pregelatinized Starch, dextrin, lactose, sucrose, mannitol, microcrystalline Cellulose, glucose, xylitol, sorbitol, calcium sulfate, calcium gluconate, calcium phosphate, calcium hydrogen phosphate, calcium carbonate and calcium bicarbonate.
Described suspending agent includes but not limited to arabic gum, tragakanta, Resina persicae, Rhizoma Bletillae gel, pectin, gelatin, guar gum, carrageenin, starch, sodium alginate, chitosan, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl-cellulose, carbomer, microcrystalline Cellulose, polyvidone, glucosan, sodium polyacrylate and kieselguhr.
Described fluidizer includes but not limited to micropowder silica gel and Pulvis Talci.
Described lubricant includes but not limited to stearic acid, magnesium stearate, calcium stearate, zinc stearate, Pulvis Talci, hydrogenated vegetable oil, glyceryl monostearate, Macrogol 4000, polyethylene glycol 6000, Polyethylene Glycol 8000, sodium laurylsulfate and magnesium laurylsulfate.
Described surfactant comprises but is not limited to span, tween, Myrij, Brij, poloxamer, sucrose fatty acid ester, sodium lauryl sulphate and phospholipid.
Described correctives includes but not limited to steviosin, fructose, glucose, high fructose syrup, Mel, aspartame, protein sugar, xylitol, mannitol, lactose, sorbitol, maltose alcohol, glycyrrhizin, stem tea element, sodium cyclamate, Fructus Musae glucide, Fructus Ananadis comosi glucide, Fructus Citri tangerinae glucide, Herba Menthae glucide, Fructus Foeniculi, vanillin, Fructus Citri Limoniae essence, cherry essence and rose essence.
Breviscapine dry suspension of the present invention prepares by following method,
Get and cross 120 mesh sieves after breviscapine is pulverized, other adjuvant except that correctives drying and crushing is respectively crossed 100 mesh sieves.Progressively increase method with active component and filler, suspending agent mix homogeneously with equivalent, add fluidizer, lubricant, correctives again and fully be mixed into pressed powder, packing promptly.
The good fluidity of breviscapine dry suspension pressed powder of the present invention adds and can change even, stable suspensoid rapidly into after water stirs, and the rate of settling is slow, and redispersibility is good, facilitates patients.
Breviscapine dry suspension of the present invention has been carried out the intravital absolute bioavailability research of rabbit.The result shows that behind the oral 120mg of the present invention of rabbit (in breviscapine), drug absorption is rapid, the short (T of peak time
Max≈ 0.25～0.5h), blood drug level height (C
Max≈ 10～30 μ g/ml), compare with intravenous injection, the absolute bioavailability of dry suspension is about 20%～45%, is more than 10 times of ordinary tablet.
The result confirms that preparation of the present invention has the advantage of instant effect, bioavailability height, strong drug action.And preparation method is simple, easy to use.
Description of drawings
Fig. 1 is the blood concentration curve behind the oral dry suspension of rabbit.
The specific embodiment:
Be that the basis describes the present invention in detail below with embodiments of the invention, but the present invention is not limited thereto.
Embodiment 1
Breviscapine 20g
Microcrystalline Cellulose 200g
Polyvidone 20g
Micropowder silica gel 10g
Magnesium stearate 10g
Correctives 10g
Lactose adds to 1000g
By the said components amount, get and cross 120 mesh sieves after breviscapine is pulverized, other adjuvant except that correctives drying and crushing is respectively crossed 100 mesh sieves, progressively increase method with active component breviscapine and microcrystalline Cellulose, polyvidone, lactose mix homogeneously with equivalent, add micropowder silica gel, magnesium stearate and correctives again and fully be mixed into pressed powder, press the single dose packing.Make 1000 bags altogether, every bag heavy 1g wherein contains breviscapine 20mg.
Embodiment 2
Breviscapine 20g
Microcrystalline Cellulose 50g
Hydroxyethyl-cellulose 100g
Micropowder silica gel 10g
Magnesium stearate 10g
Mannitol adds to 1000g
By the said components amount, to get and cross 120 mesh sieves after breviscapine is pulverized, other adjuvant drying and crushing is respectively crossed 100 mesh sieves.Progressively increase method with active component breviscapine and microcrystalline Cellulose, hydroxyethyl-cellulose, mannitol mix homogeneously with equivalent, add micropowder silica gel, the abundant mix homogeneously of magnesium stearate again, press the single dose packing.Make 1000 bags altogether, every bag of 1g contains breviscapine 20mg.
Embodiment 3
Breviscapine 40g
Hydroxypropyl methylcellulose 100g
Sodium carboxymethyl cellulose 40g
Micronization Pulvis Talci 10g
Magnesium stearate 10g
Correctives 10g
Mannitol adds to 1000g
By the said components amount, to get and cross 120 mesh sieves after breviscapine is pulverized, other adjuvant except that correctives drying and crushing is respectively crossed 100 mesh sieves.Progressively increase method with active component breviscapine and hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, mannitol mix homogeneously with equivalent, add the abundant mix homogeneously of micronization Pulvis Talci, magnesium stearate and correctives again, press the single dose packing.Make 1000 bags altogether, every bag of 1g contains breviscapine 40mg.
Embodiment 4:
Breviscapine 40g
Hydroxyethyl-cellulose 200g
Micropowder silica gel 50g
Magnesium stearate 10g
Correctives 10g
Icing Sugar adds to 1000g
By the said components amount, to get and cross 120 mesh sieves after breviscapine is pulverized, other adjuvant except that correctives drying and crushing is respectively crossed 100 mesh sieves.Progressively increase method with active component breviscapine and hydroxyethyl-cellulose, Icing Sugar mix homogeneously with equivalent, add the abundant mix homogeneously of micropowder silica gel, magnesium stearate and correctives again, press the single dose packing.Make 1000 bags altogether, every bag of 1g contains breviscapine 40mg.
Claims (4)
1, a kind of breviscapine dry suspension is grouped into by following one-tenth:
Breviscapine 20g
Microcrystalline Cellulose 200g
Polyvidone 20g
Micropowder silica gel 10g
Magnesium stearate 10g
Correctives 10g
Lactose adds to 1000g.
2, a kind of breviscapine dry suspension is grouped into by following one-tenth:
Breviscapine 20g
Microcrystalline Cellulose 50g
Hydroxyethyl-cellulose 100g
Micropowder silica gel 10g
Magnesium stearate 10g
Mannitol adds to 1000g.
3, a kind of breviscapine dry suspension is grouped into by following one-tenth:
Breviscapine 40g
Hydroxypropyl methylcellulose 100g
Sodium carboxymethyl cellulose 40g
Micronization Pulvis Talci 10g
Magnesium stearate 10g
Correctives 10g
Mannitol adds to 1000g.
4, a kind of breviscapine dry suspension is grouped into by following one-tenth:
Breviscapine 40g
Hydroxyethyl-cellulose 200g
Micropowder silica gel 50g
Magnesium stearate 10g
Correctives 10g
Icing Sugar adds to 1000g.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100166840A CN100441194C (en) | 2004-03-03 | 2004-03-03 | Erigeron breviscapus extraction dry suspensoid agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100166840A CN100441194C (en) | 2004-03-03 | 2004-03-03 | Erigeron breviscapus extraction dry suspensoid agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1559424A CN1559424A (en) | 2005-01-05 |
| CN100441194C true CN100441194C (en) | 2008-12-10 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100166840A Expired - Fee Related CN100441194C (en) | 2004-03-03 | 2004-03-03 | Erigeron breviscapus extraction dry suspensoid agent |
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Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100425242C (en) * | 2005-09-26 | 2008-10-15 | 云南昊邦制药有限公司 | Erigeron breviscapus effervescent dry mixed suspension and its making method |
| CN101185653B (en) * | 2006-10-16 | 2012-09-05 | 复旦大学 | Breviscapine oral administration composition and preparation method thereof |
| CN101637441B (en) * | 2008-07-28 | 2011-11-23 | 广州达信生物技术有限公司 | Moguisteine dried suspension and preparation method thereof |
| CN102232929A (en) * | 2010-05-06 | 2011-11-09 | 杭州赛利药物研究所有限公司 | Voriconazole dried suspension and preparation method thereof |
| CN103006556B (en) * | 2012-10-31 | 2014-11-26 | 澳门科技大学 | Scutellarin nanosuspension and preparation method thereof |
| CN107929243A (en) * | 2017-12-11 | 2018-04-20 | 河南惠通天下生物工程有限公司 | A kind of thiabendazolum dry suspensoid agent and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1341420A (en) * | 2001-09-11 | 2002-03-27 | 上海绿谷伟业生态工程有限公司 | Medicine formed from ganglioside and erigeron breviscapus extract and health-care product and their application |
| CN1437950A (en) * | 2002-12-21 | 2003-08-27 | 李睿宇 | Herba florigen oral drip-ball and production method |
| CN1457782A (en) * | 2003-05-17 | 2003-11-26 | 南昌弘益科技有限公司 | Dry spaxxacin suspension agent for resisting bacterial infection and its preparing method |
-
2004
- 2004-03-03 CN CNB2004100166840A patent/CN100441194C/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1341420A (en) * | 2001-09-11 | 2002-03-27 | 上海绿谷伟业生态工程有限公司 | Medicine formed from ganglioside and erigeron breviscapus extract and health-care product and their application |
| CN1437950A (en) * | 2002-12-21 | 2003-08-27 | 李睿宇 | Herba florigen oral drip-ball and production method |
| CN1457782A (en) * | 2003-05-17 | 2003-11-26 | 南昌弘益科技有限公司 | Dry spaxxacin suspension agent for resisting bacterial infection and its preparing method |
Non-Patent Citations (2)
| Title |
|---|
| 高效液相色谱法测定灯盏花素分散片中灯盏乙素的含量. 邹薇，何国华，魏东峰.中药新药与临床药理，第14卷第3期. 2003 |
| 高效液相色谱法测定灯盏花素分散片中灯盏乙素的含量. 邹薇，何国华，魏东峰.中药新药与临床药理，第14卷第3期. 2003 * |
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| Publication number | Publication date |
|---|---|
| CN1559424A (en) | 2005-01-05 |
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Granted publication date: 20081210 Termination date: 20110303 |