CN101199489A - Double hydrogen arteannuic plain guagui slice and preparing method thereof - Google Patents
Double hydrogen arteannuic plain guagui slice and preparing method thereof Download PDFInfo
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- CN101199489A CN101199489A CNA2006101242535A CN200610124253A CN101199489A CN 101199489 A CN101199489 A CN 101199489A CN A2006101242535 A CNA2006101242535 A CN A2006101242535A CN 200610124253 A CN200610124253 A CN 200610124253A CN 101199489 A CN101199489 A CN 101199489A
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- dihydroarteannuin
- quinoline
- guagui
- arteannuic
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Abstract
The invention discloses a piperaquine dihydroartemisinin tablet and the related preparation method, aiming at providing a piperaquine dihydroartemisinin tablet which is convenient to take and is prepared with dihydroartemisinin and piperaquine phosphate. The invention is made of 40 portions of dihydroartemisinin, 320 portions of piperaquine phosphate, 70 to 90 portions of starch, 20 to 30 portions of dextrin, 30 to 35 portions of sodium carboxymethyl starch, 6 to 10 portions of lhydroxypropyl cellulose and 3 to 5 portions of magnesium stearate (based on weight). The invention has the advantages of high finished product rate and low cost.
Description
Technical field
The present invention relates to a kind of double hydrogen arteannuic plain guagui slice and preparation method thereof.
Background technology
Dihydroarteannuin (Dihydroartemisinin), chemical name is: (3R, 5aS, 6R, 8aS, 9R, 12S, 12aR)-and octahydro-3,6,9 trimethyls-3,12-bridging oxygen-12H-pyrans is [4,3-j]-1 also, 2-benzo two Sai Ping-10 (3H) alcohol.Molecular formula: C
15H
24O
5
Its chemical structural formula is as follows:
Dihydroarteannuin is the derivant of arteannuin, is the activity in vivo material of arteannuin, has powerful and killing action fast to the plasmodium erythrocytic stage, can control clinical episodes and symptom rapidly.The mechanism of action of arteannuin mainly is to disturb plasmodial pellicle one mitochondrial function.Arteannuin changes its film structure by influencing the ultrastructure of plasmodium erythrocytic stage.Owing to, blocked plasmodial nutrition intake to the effect of food vacuolar membrane, when plasmodium loses a large amount of endochylemas and nutrient substance, and can not get replenishing, thereby very fast death.Its model of action is by its endoperoxide (dioxygen) bridge, the free iron that the menses red eggs decompose the back generation in vain mediates, produce unsettled organic free radical and/or other electrophilic mediator, form the covalency adduct with plasmodial protein then, and make plasmodium death.The antimalarial active of dihydroarteannuin is big 6 times than arteannuin.
Phosphoric acid croak quinoline (Piperaquine Phosphate) is a 4-quinolin-2-ylamine class antimalarial, malaria effect and chloroquine are similar, influence the ultrastructure of plasmodium erythrocytic stage schizont, mainly can make trophozoite food vacuolar membrane and mitochondrial swelling, cause the destruction of its physiological function, thereby kill plasmodium.
External pharmacodynamic study prompting, the two share dihydroarteannuin and phosphoric acid croak quinoline, has potentiation, does not increase toxic effect and have.
But these two kinds of crude drug are not made a kind of preparation altogether in the prior art, patient needs to buy separately when taking, and takes also inconvenient.
Summary of the invention
Technical problem to be solved by this invention is to overcome the deficiencies in the prior art, provides a kind of dihydroarteannuin and phosphoric acid croak quinoline are lumped together double hydrogen arteannuic plain guagui slice preparation, taking convenience.
Another technical problem to be solved by this invention is that the preparation method of the double hydrogen arteannuic plain guagui slice that a kind of technology is simple, cost is low is provided.
The technical solution adopted in the present invention is: double hydrogen arteannuic plain guagui slice of the present invention is to be made by the dihydroarteannuin of (in weight portion) 40 parts, 320 parts phosphoric acid croak quinoline, 70～90 parts starch, 20～30 parts dextrin, 30～35 parts carboxymethyl starch sodium, 6～10 parts hyprolose, 3～5 parts magnesium stearate.
The preparation method of double hydrogen arteannuic plain guagui slice of the present invention is carried out according to the following steps:
(1) get the described dihydroarteannuin of described weight proportion, described phosphoric acid croak quinoline, described carboxymethyl starch sodium and pulverized the back separately and cross 100 mesh sieves, standby;
(2) get the described starch of described weight proportion, described hyprolose, described dextrin, described magnesium stearate and cross 100 mesh sieves, standby;
(3) with described phosphoric acid croak quinoline, described starch, described dextrin mix homogeneously, be that binding agent is made soft material with the medicated powder of mix homogeneously with described hyprolose solution, cross 14 mesh sieves and make wet granular;
(4) 16 mesh sieves are crossed in wet granular oven dry back and make dried granule;
(5) described dihydroarteannuin, described carboxymethyl starch sodium, described magnesium stearate are fully mixed the back compacting in flakes with described dried granule;
(6) packed products after the assay was approved.
The invention has the beneficial effects as follows: the present invention lumps together dihydroarteannuin and phosphoric acid croak quinoline and is prepared into double hydrogen arteannuic plain guagui slice, taking convenience; Double hydrogen arteannuic plain guagui slice of the present invention is to be made by active component dihydroarteannuin, active component phosphoric acid croak quinoline, diluent starch (Starch), diluent dextrin (Dextrine), disintegrating agent carboxymethyl base Starch Sodium (Carboxymethyl Starch Sodium), binding agent hyprolose (Hypromellose) and magnesium stearate lubricant (Stearate Magnesium), select for use above-mentioned raw materials principal agent dihydroarteannuin and phosphoric acid croak quinoline can be processed into the tablet that meets drug standard easily, its yield rate height; Preparation method of the present invention is earlier with phosphoric acid croak quinoline, starch, dextrin mix homogeneously, with hyprolose solution is that binding agent is made soft material with the medicated powder of mix homogeneously, cross 14 mesh sieves and make wet granular, the oven dry back is crossed 16 mesh sieves and is made dried granule, again dihydroarteannuin, carboxymethyl starch sodium, magnesium stearate are fully mixed the back compacting in flakes with dried granule, packed products after the assay was approved, technology is simple, and cost is low.
The specific embodiment
Described double hydrogen arteannuic plain guagui slice is to be made by active component dihydroarteannuin, active component phosphoric acid croak quinoline, diluent starch, diluent dextrin, disintegrating agent carboxymethyl base Starch Sodium, binding agent hyprolose and magnesium stearate lubricant, select for use above-mentioned raw materials principal agent dihydroarteannuin and phosphoric acid croak quinoline can be processed into the tablet that meets drug standard easily, its yield rate height.
The preparation method of double hydrogen arteannuic plain guagui slice of the present invention is carried out according to the following steps:
(1) get the described dihydroarteannuin of described weight proportion, described phosphoric acid croak quinoline, described carboxymethyl starch sodium and pulverized the back separately and cross 100 mesh sieves, standby;
(2) get the described starch of described weight proportion, described hyprolose, described dextrin, described magnesium stearate and cross 100 mesh sieves, standby;
(3) with described phosphoric acid croak quinoline, described starch, described dextrin mix homogeneously, be that binding agent is made soft material (it is agglomerating that soft material should be held, and that touches promptly looses) with the medicated powder of mix homogeneously with described hyprolose solution, cross 14 mesh sieves and make wet granular;
(4) 16 mesh sieves are crossed in wet granular oven dry back and make dried granule;
(5) described dihydroarteannuin, described carboxymethyl starch sodium, described magnesium stearate are fully mixed the back compacting in flakes with described dried granule;
(6) packed products after the assay was approved.
Embodiment one:
In the present embodiment, the weight of each raw material is respectively:
Dihydroarteannuin 40g, phosphoric acid croak quinoline 320g, starch 70g, dextrin 20g, carboxymethyl starch sodium 30g, hyprolose 6g, magnesium stearate 3g, can prepare 1000 of double hydrogen arteannuic plain guagui slices, every contains active component dihydroarteannuin 40mg+ phosphoric acid croak quinoline 320mg.
Instructions of taking: oral.8 of adult's accumulated doses, sooner or later respectively once, each 2.The child is cut down according to the circumstance by doctor's advice.
Embodiment two:
In the present embodiment, the weight of each raw material is respectively:
Dihydroarteannuin 40g, phosphoric acid croak quinoline 320g, starch 90g, dextrin 30g, carboxymethyl starch sodium 35g, hyprolose 10g, magnesium stearate 5g, can prepare 1000 of double hydrogen arteannuic plain guagui slices, every contains active component dihydroarteannuin 40mg+ phosphoric acid croak quinoline 320mg.
All the other are with embodiment one.
Embodiment three:
In the present embodiment, the weight of each raw material is respectively:
Dihydroarteannuin 40g, phosphoric acid croak quinoline 320g, starch 70g, dextrin 25g, carboxymethyl starch sodium 32.5g, hyprolose 8g, magnesium stearate 4g, can prepare 1000 of double hydrogen arteannuic plain guagui slices, every contains active component dihydroarteannuin 40mg+ phosphoric acid croak quinoline 320mg.
All the other are with embodiment one.
Claims (2)
1. double hydrogen arteannuic plain guagui slice, it is characterized in that: it is to be made by the dihydroarteannuin of (in weight portion) 40 parts, 320 parts phosphoric acid croak quinoline, 70～90 parts starch, 20～30 parts dextrin, 30～35 parts carboxymethyl starch sodium, 6～10 parts hyprolose, 3～5 parts magnesium stearate.
2. the preparation method of the described double hydrogen arteannuic plain guagui slice of claim 1 is characterized in that, it carries out according to the following steps:
(1) get the described dihydroarteannuin of described weight proportion, described phosphoric acid croak quinoline, described carboxymethyl starch sodium and pulverized the back separately and cross 100 mesh sieves, standby;
(2) get the described starch of described weight proportion, described hyprolose, described dextrin, described magnesium stearate and cross 100 mesh sieves, standby;
(3) with described phosphoric acid croak quinoline, described starch, described dextrin mix homogeneously, be that binding agent is made soft material with the medicated powder of mix homogeneously with described hyprolose solution, cross 14 mesh sieves and make wet granular;
(4) 16 mesh sieves are crossed in wet granular oven dry back and make dried granule;
(5) described dihydroarteannuin, described carboxymethyl starch sodium, described magnesium stearate are fully mixed the back compacting in flakes with described dried granule;
(6) packed products after the assay was approved.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101242535A CN101199489A (en) | 2006-12-15 | 2006-12-15 | Double hydrogen arteannuic plain guagui slice and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101242535A CN101199489A (en) | 2006-12-15 | 2006-12-15 | Double hydrogen arteannuic plain guagui slice and preparing method thereof |
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| CN101199489A true CN101199489A (en) | 2008-06-18 |
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| CNA2006101242535A Pending CN101199489A (en) | 2006-12-15 | 2006-12-15 | Double hydrogen arteannuic plain guagui slice and preparing method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010004573A1 (en) * | 2008-07-07 | 2010-01-14 | Ipca Laboratories Limited | Synergistic antimalarial pharmaceutical composition |
| CN101984970A (en) * | 2010-11-23 | 2011-03-16 | 浙江华立南湖制药有限公司 | Dihydroartemisinin piperaquine phosphate tablets and preparation process thereof |
| CN103263418A (en) * | 2013-06-06 | 2013-08-28 | 南京正宽医药科技有限公司 | Dihydroartemisinin piperaquine phosphate tablets and preparation method thereof |
-
2006
- 2006-12-15 CN CNA2006101242535A patent/CN101199489A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010004573A1 (en) * | 2008-07-07 | 2010-01-14 | Ipca Laboratories Limited | Synergistic antimalarial pharmaceutical composition |
| CN101984970A (en) * | 2010-11-23 | 2011-03-16 | 浙江华立南湖制药有限公司 | Dihydroartemisinin piperaquine phosphate tablets and preparation process thereof |
| CN103263418A (en) * | 2013-06-06 | 2013-08-28 | 南京正宽医药科技有限公司 | Dihydroartemisinin piperaquine phosphate tablets and preparation method thereof |
| CN103263418B (en) * | 2013-06-06 | 2015-08-19 | 南京正宽医药科技有限公司 | A kind of dihydroarteannuin piperaquine phosphate tablet and preparation method thereof |
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Open date: 20080618 |