CN1957935A - Drop pills of seabuckthorn fruit flavone, and preparation method - Google Patents
Drop pills of seabuckthorn fruit flavone, and preparation method Download PDFInfo
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- CN1957935A CN1957935A CNA2006100936110A CN200610093611A CN1957935A CN 1957935 A CN1957935 A CN 1957935A CN A2006100936110 A CNA2006100936110 A CN A2006100936110A CN 200610093611 A CN200610093611 A CN 200610093611A CN 1957935 A CN1957935 A CN 1957935A
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- flavone
- seabuckthorn fruit
- fructus hippophae
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Abstract
A dripping pill of seabucklthorn flavone for treating cardiovascular and cerebrovascular diseases is prepared from seabucklthorn flavone, tween-80 and span. Its preparing process is also disclosed.
Description
Technical field
The present invention relates to a kind of is the medical product of feature with the drops, and especially relating to a kind of extract with plant tissue is the drops of Main Ingredients and Appearance.
Background technology
Fructus Hippophae is traditional medication of Mongolian medicine and Tibetan medicine, and it is warm in nature and sour-puckery flavor has the effect of YIN nourishing and the production of body fluid promoting, reinforce functional activities of the heart, strengthening by means of tonics, and the merit of stronger blood circulation promoting and blood stasis dispelling is arranged.Modern pharmacology and clinically confirm all that Fructus Hippophae flavone contained in the Fructus Hippophae has and increase myocardial flow, improve myocardium microcirculation, reduce effects such as myocardial oxygen consumption, arrhythmia and blood vessel dilating.Therefore, Fructus Hippophae flavone be used for the treatment of angina pectoris, nervous, cardiopalmus, uncomfortable in chest, the disease such as blood vessels are not smooth of breathing hard.General Fructus Hippophae flavone is the alcohol extract of Fructus Hippophae, and the Fructus Hippophae flavone structure is special, composition is complicated, has isolated nearly ten kinds of compositions such as isorhamnetin, Quercetin, kaempferol, glucoside after deliberation.
With Fructus Hippophae flavone is that the tablet that main composition is made claims " Fructus Hippophae flavone sheet ", is the medicine that the national drug standards " the chemical drugs terrestrial reference rises GB " (the 14) go up promulgation; Its capsule preparations then is called " Fructus Hippophae flavone capsule ".These two kinds of preparations have been widely used in the clinical treatment cardiovascular and cerebrovascular disease.But the common drawback of these two kinds of preparations is that the dispersion of Fructus Hippophae flavone wherein is not too high, thereby has delayed the onset time of Fructus Hippophae flavone drug effect; Its administering mode of two has determined that Fructus Hippophae flavone must be through digestive tract then just bring into play drug effect after entering liver in addition, therefore causes this two kinds of dosage forms onset time prolongation.For these two kinds of treatment of diseases of acute and chronic cardiovascular and cerebrovascular vessel, administration time more early effect just better, thereby a kind of onset the new formulation dosage form is more with practical value faster.This is the present invention's purpose that will reach just.
Summary of the invention
The purpose of invention provides a kind of drop pills of seabuckthorn fruit flavone and preparation method thereof, it is to adopt a kind of appropriate drug dosage form--drops, onset time when drops can shorten Fructus Hippophae flavone to the treatment cardiovascular and cerebrovascular disease, improve the bioavailability of Fructus Hippophae flavone simultaneously, give full play to the drug effect of Fructus Hippophae flavone.Purpose of the present invention is implemented by following technical scheme.
Chinese medicine " drop pill " preparation is the dosage form that employing Western medicine advanced person's preparation means are made, this Chinese medicine dripping pills of utilizing solid dispersion technology to make can make the Chinese herbal medicine active ingredient fully contact with mucomembranous surface, after making active ingredient pass through the absorption of mucosa upper surface cell, directly enter the blood of human body blood circulation, thereby reasonably shortened the onset time of active ingredient.Fructus Hippophae flavone is dissolubility and little in water, thereby direct simply oral Fructus Hippophae flavone just is difficult to absorb soon, and promptly bioavailability of medicament is not high.Adopt water miscible polyethylene glycol 6000 so the substrate of Chinese medicine dripping pills preparation is general, but water-soluble slightly Fructus Hippophae flavone is well-dispersed in the water miscible polyethylene glycol 6000, must use surfactant simultaneously.Here traditional surfactant is a tween 80.But our practice finds that because the structure of Fructus Hippophae flavone is special, composition is complicated (see before and state), so use single kind of surfactant tween 80, Fructus Hippophae flavone is being in the drop pill of substrate with the polyethylene glycol 6000, and it is the highest that its dispersion fails to reach.The HLB value (hydrophile-lipophile balance value) of considering tween 80 is bigger, so add the less span of small amount of H LB value, the dispersion of Fructus Hippophae flavone in polyethylene glycol 6000 improved, Fructus Hippophae flavone almost is scattered in the polyethylene glycol 6000 of hot melt attitude with " microemulsified state ", makes Fructus Hippophae flavone keep the high degree of dispersion state subsequently behind the cooling curing.The onset time shortening, the bioavailability that have so just guaranteed drop pills of seabuckthorn fruit flavone dosage form provided by the invention improve.
The present invention, i.e. drop pills of seabuckthorn fruit flavone, technical process as follows: the polyethylene glycol 6000 after the metering, after 80 ℃ of fusings, be metered into tween 80 and span, add quantitative, as to cross 100 mesh sieves Fructus Hippophae flavones under the stirring gradually.Utilize " drop pill machine " the polyethylene glycol 6000 mixing system of molten state then, dropwise splash in the liquid paraffin below 10 ℃, be frozen into drop pill gradually, remove the liquid paraffin of most surface attachment after, promptly get product " drop pills of seabuckthorn fruit flavone ".
Advantage of the present invention: Fructus Hippophae flavone is in the high degree of dispersion state in " drop pills of seabuckthorn fruit flavone ", contact the rapid disintegrate in back with mucosa and enter blood circulation, avoided " first pass effect " of liver effectively, therefore shown the rapid and high characteristics of bioavailability of onset.In addition, compare with capsule formulation, do not have dust in the production process of drop pill with tablet, operation is few, and equipment is simple, and promptly production cost is lower, have the quality of drop pill product to control easily again, thus dosage accurately, the ball method of double differences different little, medicine stability is high, not facile hydrolysis and oxidation.
The present invention is used for the production of Fructus Hippophae flavone medicament to solid dispersion technology, and it is the first making " drop pills of seabuckthorn fruit flavone ".
Embodiment:
Get an amount of (about about 7.8 grams) Fructus Hippophae flavone, detect that the active ingredient " flavone " that shows wherein is equivalent to isorhamnetin and the Quercetin total content is 1000mg, grind the back and cross 100 mesh sieves, standby.Take by weighing the 40.0g polyethylene glycol 6000, add 0.08-0.12g (this example is 0.1g) tween 80, add 0.001-0.012g span (this example is 0.005g) again, heat melts to 78-83 ℃ (this example is 80 ℃) altogether, add quantitative, as to cross 100 mesh sieves Fructus Hippophae flavone under the stirring gradually, stir the back and dropwise splash in 5-10 ℃ of (this example is 9 ℃) liquid paraffin with the drop pill machine, control drop pill particle diameter, make it 1000 drop pill of output.Separate drop pill, remove drop pill adhering on surface liquid paraffin, airing, screening promptly gets " drop pills of seabuckthorn fruit flavone " finished product.
Claims (6)
1, a kind of preparation method of drop pills of seabuckthorn fruit flavone, it is characterized in that the quantitative Fructus Hippophae flavone of pulverizing is with quantitatively polyethylene glycol 6000, tween 80, span dropwise splash in the liquid paraffin with the drop pill machine behind the molten state mixing, control drop pill particle diameter makes it to make drops.
2, the preparation method of a kind of drop pills of seabuckthorn fruit flavone according to claim 1 is characterized in that, the effective ingredient in the described quantitative Fructus Hippophae flavone, and must keep isorhamnetin and Quercetin total content after check is 1000mg.
3, the preparation method of a kind of drop pills of seabuckthorn fruit flavone according to claim 1, it is characterized in that the mass ratio when described quantitative Fructus Hippophae flavone and quantitative polyethylene glycol 6000, tween 80, span mixing is: Fructus Hippophae flavone 1.0-10 gram, polyethylene glycol 6000 39.5-40.5 gram, tween 80 0.08-0.12 gram, span 0.001-0.012 restrain.
4, the preparation method of a kind of drop pills of seabuckthorn fruit flavone according to claim 1, it is characterized in that, quantitative Fructus Hippophae flavone of pulverizing and quantitative polyethylene glycol 6000, tween 80, span are behind the molten state mixing, dropwise splash in the liquid paraffin with the drop pill machine, control the drop pill particle diameter, make it to make drops, its drop pill quantity is 1000.
5, a kind of drop pills of seabuckthorn fruit flavone is characterized in that, according to the drop pills of seabuckthorn fruit flavone of the method for claim 1 preparation.
6, a kind of drop pills of seabuckthorn fruit flavone according to claim 5 is characterized in that, this drop pills of seabuckthorn fruit flavone is used for the treatment of acute and chronic cardiovascular and cerebrovascular disease.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100936110A CN100571697C (en) | 2006-06-21 | 2006-06-21 | A kind of drop pills of seabuckthorn fruit flavone |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100936110A CN100571697C (en) | 2006-06-21 | 2006-06-21 | A kind of drop pills of seabuckthorn fruit flavone |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1957935A true CN1957935A (en) | 2007-05-09 |
| CN100571697C CN100571697C (en) | 2009-12-23 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006100936110A Expired - Fee Related CN100571697C (en) | 2006-06-21 | 2006-06-21 | A kind of drop pills of seabuckthorn fruit flavone |
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| CN (1) | CN100571697C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102552491A (en) * | 2012-01-11 | 2012-07-11 | 福建中医药大学 | Dai-dai fruit total flavonoid self-microemulsion micro pill and preparation method thereof |
-
2006
- 2006-06-21 CN CNB2006100936110A patent/CN100571697C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102552491A (en) * | 2012-01-11 | 2012-07-11 | 福建中医药大学 | Dai-dai fruit total flavonoid self-microemulsion micro pill and preparation method thereof |
| CN102552491B (en) * | 2012-01-11 | 2013-12-18 | 福建中医药大学 | Dai-dai fruit total flavonoid self-microemulsion micro pill and preparation method thereof |
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| Publication number | Publication date |
|---|---|
| CN100571697C (en) | 2009-12-23 |
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Granted publication date: 20091223 Termination date: 20150621 |
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