CN1286083A - Micropowdered tanshinone preparation and its microwave aided co-grinding process for preparing it - Google Patents

Abstract

A micropowdered tanshinone is prepared from tanshinone which is difficult to dissolve through microwave radiation and mixing it with hydrophilic auxiliary material while ball grinding. It features higher solubility and short grinding time.

Description

TANSHINONES micropowder preparation and microwave aided co-grinding process for preparing thereof

The present invention relates to a kind of TANSHINONES micropowder preparation, relate in particular to a kind of TANSHINONES and hydrophilicity condiment and grind the TANSHINONES micropowder preparation that forms altogether, and the method for preparing said preparation by microwave aided co-grinding.

TANSHINONES is the fat-soluble effective ingredient in the salviamiltiorrhizabung, not only has natural anti-oxidation, cardiovascular pharmacological effect and antibacterial and anti-inflammation functions, also has obvious antineoplastic.Yet TANSHINONES is an insoluble drug, and zoopery shows that this medicine assimilation effect in vivo is poor.As everyone knows, medicine has only dissolving to be absorbed.The dissolubility of most medicines and rate of dissolution and medicine be absorbed with tangible statistics dependency.Medicine stripping from solid preparation that insoluble drug and rate of dissolution are little is slow, and dissolving becomes the controlled step of drug absorption, and at this moment rate of dissolution directly influences speed, the power of drug effect appearance and holds time.Therefore, the dissolution of raising TANSHINONES is very necessary.

For improving the bioavailability of TANSHINONES, the people was once arranged with the TANSHINONES II _ASulfonation makes it become water-soluble products-TANSHINONES II _ASodium sulfonate, through the experiment of animal anoxia enduring, the result shows effectively.Find the TANSHINONES II by 108 routine coronary heart disease observation of curative effect _ASodium sulfonate has certain curative effect to angina pectoris and symptom uncomfortable in chest, and can improve the ischemic electrocardiogram, and toxicity is little, becomes a kind of medicine of novel treatment coronary heart disease.Yet this technology is the TANSHINONES II _AIn the presence of acetic anhydride, with concentrated acid sulfonation, saltout, get with methanol crystallization.Concentrated sulphuric acid and methanol are all harmful to human body, and wherein methanol is poisonous medicine.TANSHINONES is to heat-labile chemical compound, in removing the process of methanol, if temperature is too high or heat time heating time is long, then causes the degraded of TANSHINONES inevitably.

The dissolution of solid drugs and preparation add that the micronized degree in the process has substantial connection.The quantitative change of granular size can bring the qualitative change of powder characteristics and then produce many new performances.The principle of powder application body technique and method change the existence of medicine in preparation with improve its dissolution be in the present biopharmacy important content this.And insoluble drug and hydrophilicity condiment are ground altogether with the preparation method of the preparation that obtains high-dissolution existing more bibliographical information both at home and abroad, as Shan Netal.J Pharm Sci.1974,63: 117; Nakai Yetal.Chem Pharm Bull.1986,34:315; Toshio O.; Kaznhiro M.; Etsuo Y.Int JPharm 1995,113 (1): 97; Masaaki H; Manabu Y.; Kenji O.Byoin Yakugaku.1996,22 (5): 521; Hideaki S.; Hironori N.; Miwako O.Byoin Yakugaku.1997,23 (2): 107; Deng.It improves the mechanism of dissolution, is because the crystalline size of medicine reduces even becomes amorphously on the one hand, is because hydrophilicity condiment has increased the wettability of medicine to water on the other hand.Yet insoluble drug belongs to nonpolar crystalline solid mostly, lacks fragility, when applying certain mechanical force, easily produces distortion, and this class medicine has stronger cohesiveness to come balance to add mechanical force simultaneously.

Microwave grinding aid (Microwave-Assisted Grinding) is the new technique of the mineral manufacture field that just risen in recent years.It is that this new and high technology of microwave is combined with Mineral Processing Engineering, thereby improves grinding efficiency.Studies show that microwave radiation can obviously improve the grindability of mineral.The microwave grinding aid can be extracted polycyclic aromatic hydrocarbon and alkane composition effectively from sedimentary rock.Yet the micronization field that microwave technology is applied to medicine yet there are no bibliographical information.

The TANSHINONES micropowder preparation that one of purpose of the present invention is to provide a kind of TANSHINONES and hydrophilicity condiment to grind altogether and forms is to improve the dissolution of TANSHINONES.

Two of purpose of the present invention is to disclose a kind of preparation power method, especially the microwave grinding aid method of above-mentioned TANSHINONES micropowder preparation.

Design of the present invention is such:

The present invention carries out common grinding with hydrophilicity condiment and the TANSHINONES through microwave radiation, thereby obtains a kind of TANSHINONES micropowder preparation than high-dissolution.Because microwave is a kind of frequency electromagnetic waves, has extremely strong penetrating power, porous makes each molecule that the possibility of contact microwave all be arranged to the inside of material.Microwave action is when material, around it, form an electromagnetic field, make the material molecule (dipole) of original disorderly and unsystematic motion in this electromagnetic field, produce orientation polarization and distortion polarization, because the warm-up movement of molecule itself and the interaction between adjacent molecule, molecule turns to polar motion with respect to the variation of external electric field a temporal hysteresis to be arranged, and this hysteresis is called relaxation.The macro-effect of relaxation makes the molecular motion aggravation with regard to making a part of electromagnetic energy change the kinetic energy of molecular thermalmotion into, finally cause dielectric temperature to raise.Compare with traditional heating mode, microwave heating does not need heat transfer process, heats up simultaneously inside and outside the material, and firing rate is fast and evenly, and one of the percentage that only needs the traditional heating method just can be finished whole heating process to several millesimal times.The heat (P) that in the unit interval, is produced in the electrolyte of unit volume and electric field (E), frequency (f), substance dielectric constant (ε _γ) and dielectric dielectric loss coefficient (tg δ) between following relationship arranged: $P=\mathrm{<figure-callout\; id="2"\; label="f\; E"\; filenames="0011957900121.png,0011957900122.png"\; state="\{\{state\}\}">f</figure-callout>}{E}^{}{}^2{\mathrm{\&epsiv;}}_{r}t{g}^{\mathrm{\&delta;}}$ By formula (1) as seen, the heat that material produces in microwave field remove with microwave properties (f, E) have outside the Pass, mainly put to death kind and dielectric property (ε thereof in material _γ, tg δ).

TANSHINONES belongs to the nonpolar crystalline solid of slightly solubility, and its dielectric constant is lower.But, when it contains Free water or bound water, just can absorb microwave energy effectively.The dielectric constant of water is 78.54, and microwave just can make the water of 50mL be heated to 81 ℃ from room temperature in the 1min.In practical operation, moisture content in the medicine is difficult to absolutely remove, when medicine finishes the back also during residual small amount of moisture in drying, under the effect of microwave field, medicine itself and residual moisture content will produce sizable heat, heat simultaneously inside and outside making drug particles, in the extremely short time, just can reach very high temperature.And medicine is heated in the so short time and generally is unlikely to be destroyed.After medicine crystal was heated, its chemical key length and direction will change, and the thermal expansion phenomenon occurs, after being cooled off, will produce stress in the crystal grain, crackle and lattice defect occurred, and compared before the microwave radiation, showed bigger fragility.Therefore, can make it be crushed to small crystal in the short period of time, pulverize the also corresponding raising of the limit, and itself and hydrophilicity condiment are ground altogether, thereby can improve the dissolution of TANSHINONES.

The technical scheme that realizes the object of the invention is as follows:

The said TANSHINONES micropowder of the present invention preparation is a compositions, and its component and content are:

TANSHINONES 4.0～50%

Hydrophilicity condiment 50～96%

More than be mass percent.

Said TANSHINONES is a Radix Salviae Miltiorrhizae extract, the visible document of the extracting method of this extract " institute of Materia Medica,Chinese Academy of Medical Sciences, the prosperous pharmaceutical factory in Hebei, Chinese herbal medicine communication.1977,12:12 " and " Lei Qiyun, Zhu new people, Zhu Suqin, etc.The Shaanxi new medicine.1984，13(3)：61”。

Said hydrophilicity condiment is chitosan, chitin (Shanghai big health health product company limited), microcrystalline Cellulose (Changshu food adjuvant factory), pregelatinized Starch (food chemical plant, Pedicellus et Pericarpium Trapae lake), lactose, a kind of in Macrogol 4000, the polyethylene glycol 6000 etc., they are pharmaceutic adjuvant.

Hydrophilicity condiment improves the dispersion of TANSHINONES on the one hand, improves the wettability of TANSHINONES to water on the other hand.Therefore, the hydrophilicity condiment proportion is big more, and the dispersion of TANSHINONES is just big more, and is also just strong more to the wettability ability of water.Yet, consider that from economic angle the hydrophilicity condiment proportion is big more, cost is also just high more.Therefore, the ratio of above-mentioned composition is preferably:

TANSHINONES 15～50%

Hydrophilicity condiment 50～85%

More than be mass percent.

Above-mentioned TANSHINONES co-milled mixtures also is preparation like this:

At first TANSHINONES powder art is placed microwave oven, carry out microwave radiation, again itself and hydrophilicity condiment are pressed the rearmounted grinding in ball grinder of above-mentioned mixed, can obtain said TANSHINONES micropowder preparation.

Microwave irradiation time, radiation number of times and will directly influence the quality of product in the time of grinding in ball grinder and the ratio of TANSHINONES and hydrophilicity condiment.Among the present invention, microwave irradiation time is 1-10 minute, radiation 1-3 time, and milling time is 15 minutes-24 hours altogether.

Experimental technique involved in the present invention is such: TANSHINONES Determination on content in (1) sample:

By uv scan, find that red sage root ethanol extraction part maximum absorption wavelength is near 268nm.Silver is new again once with the highest TANSHINONES II of content in the tanshinol extract _ABe primary standard substance, ethanol is solvent, they are mixed with the solution of a series of concentration, adopt ultraviolet spectrophotometry to measure its absorbance at the 268nm place, obtained the standard curve of a TANSHINONES concentration, it obeys following linear equation: C=11.8509A-0.1121 (γ=0.9998), in the formula, C is a TANSHINONES concentration, and unit is μ g/mL, and A is the absorbance of TANSHINONES.

It is an amount of accurately to take by weighing sample, places the 100mL volumetric flask, it is all dissolved and is diluted to scale with dehydrated alcohol, detects the absorbance of TANSHINONES then at the 268nm place, again by the content of TANSHINONES in the standard curve calculation sample.(2) mensuration of dissolution in vitro:

Adopt the slurry method algoscopy in the Chinese Pharmacopoeia nineteen ninety-five version.Dissolution medium is the distilled water of 900mL, pH=5.8, and temperature is 37 ± 0.5 ℃, and rotating speed is 100r/min.When rigidly connecting, medicine powder art picks up counting when touching solution, respectively at 5,10,15,20,30,40,50,60,90, and 120min location draw solution 5mL, with 0.45 μ m filtering with microporous membrane, the while is added equality of temperature medium 5mL immediately in dissolution medium.After filtrate is diluted with dehydrated alcohol, be that absorbance is detected at the 268nm place, calculate the dissolution of TANSHINONES according to measured value by standard curve in wavelength.(3) X-ray diffraction analysis:

TANSHINONES crystal in the sample is analyzed.Working condition is: Cuk α target, voltage 40kV, electric current 60mA, slit DS1 °, RS0.3mm, SS1 °, 4 °/min of scanning speed, 0.02 °/RP of step-length.(4) preparation of common co-milled mixtures of contrast and physical mixture:

Place ball mill under identical condition, to grind altogether with hydrophilicity condiment with ratio identical in the microwave grinding aid mixture TANSHINONES, promptly get common co-milled mixtures; With TANSHINONES and the ratio uniform mixing of hydrophilicity condiment, promptly get physical mixture to take charge of mutually in the microwave grinding aid mixture.(5) test used instrument:

WP800SL23 type household microwave oven (Galanz); WL-1 type ball mill (Chongqing Chemical Machinery Plant); RC-1A type stripping experiment instrument (Shanghai Huanghai Sea medicine inspection instrument plant); Rlga Ku3030E3 type x-ray diffractometer (Japan is of science); 760CRT type dual-beam ultraviolet-uisible spectrophotometer (Shanghai the 3rd analytical tool factory).

Below will be that hydrophilicity condiment is an example with the chitosan, result's (experimental result is shown in accompanying drawing) be to microwave irradiation time, radiation number of times, describe the stability of TANSHINONES and the influence of dissolution in the time of grinding in ball grinder and the ratio of TANSHINONES and hydrophilicity condiment by experiment.

Fig. 1 be under the above-mentioned microwave oven peak power microwave irradiation time to the experimental result of the influence of TANSHINONES stability.

Fig. 2 is the experimental result of the influence of microwave radiation frequency series TANSHINONES co-milled mixtures dissolution.Wherein, TANSHINONES and chitosan ratio are 1: 2 (w/w) in the laboratory sample, and every time through microwave radiation 1 time of TANSHINONES is 1min, and milling time is 30min altogether.

Fig. 3 is for being total to the experimental result of milling time to the influence of TANSHINONES co-milled mixtures dissolution.Wherein, TANSHINONES and chitosan ratio are 1: 2 (w/w) in the laboratory sample, and during the microwave grinding aid, TANSHINONES is earlier through microwave radiation 2 times, each 1min.

Fig. 4 is the experimental result of the consumption of chitosan to the influence of TANSHINONES co-milled mixtures dissolution.Wherein, laboratory sample is for grinding the co-milled mixtures of 1h altogether, and during the microwave grinding aid, TANSHINONES is earlier through microwave radiation 2 times, each 1min.

Fig. 5, Fig. 6 be microwave grinding aid and common altogether Ginding process to TANSHINONES from the comparative result of crystal to amorphous conversion rates.In the laboratory sample, the ratio of TANSHINONES and chitosan is 1: 2 (w/w), and during the microwave grinding aid, TANSHINONES is earlier through microwave radiation 2 times, each 1min.

Each curve meaning is as follows in Fig. 2-5:

The TANSHINONES that the 1---microwave radiation is 0 time-chitosan co-milled mixtures dissolution line; The TANSHINONES that the 2---microwave radiation is 1 time-chitosan co-milled mixtures dissolution line; The TANSHINONES that the 3---microwave radiation is 2 times-chitosan co-milled mixtures dissolution line; The TANSHINONES that the 4---microwave radiation is 3 times-chitosan co-milled mixtures dissolution line; The former medicine dissolution of 5---TANSHINONES line; 6---TANSHINONES-chitosan physical mixture dissolution line; 7---grinds the common co-milled mixtures dissolution of the TANSHINONES-chitosan line of 15min altogether; 8---grinds the common co-milled mixtures dissolution of the TANSHINONES-chitosan line of 30min altogether; 9---grinds the common co-milled mixtures dissolution of the TANSHINONES-chitosan line of 60min altogether; 10---grinds the common co-milled mixtures dissolution of the TANSHINONES-chitosan line of 120min altogether; 11---grinds TANSHINONES-chitosan microwave grinding aid mixture dissolution line of 15min altogether; 12---grinds TANSHINONES-chitosan microwave grinding aid mixture dissolution line of 30min altogether; 13---grinds TANSHINONES-chitosan microwave grinding aid mixture dissolution line of 60min altogether; 14---grinds TANSHINONES-chitosan microwave grinding aid mixture dissolution line of 120min altogether; 15---1: the common co-milled mixtures dissolution of 2 (w/w) TANSHINONES-chitosan line; 16---1: the common co-milled mixtures dissolution of 4 (w/w) TANSHINONES-chitosan line; 17---1: the common co-milled mixtures dissolution of 6 (w/w) TANSHINONES-chitosan line; 18---1: 2 (w/w) TANSHINONES-chitosan microwave grinding aid mixture dissolution line; 19---1: 4 (w/w) TANSHINONES-chitosan microwave grinding aid mixture dissolution line; 20---1: 6 (w/w) TANSHINONES-chitosan microwave grinding aid mixture dissolution line; The X-ray diffracting spectrum of the former medicine of TANSHINONES that the 21---laboratory extracts; The X-ray diffracting spectrum of 22---chitosan; The X-ray diffracting spectrum of 23---TANSHINONES-chitosan physical mixture; The X-ray diffracting spectrum of the common co-milled mixtures of 24---TANSHINONES-chitosan (grinding 30min); The X-ray diffracting spectrum of 25---TANSHINONES-chitosan microwave grinding aid mixture (grinding 30min); The X-ray diffracting spectrum of the common co-milled mixtures of 26---TANSHINONES-chitosan (grinding 120min); The X-ray diffracting spectrum of 27---TANSHINONES-chitosan microwave grinding aid mixture (grinding 120min); In the common co-milled mixtures of 28---, TANSHINONES product body diffraction peak intensity ° is located with the change curve of milling time altogether in 2 θ=7.12;

In the 29---microwave grinding aid mixture, TANSHINONES crystal diffraction peak intensity ° is located with the change curve of milling time altogether in 2 θ=7.12;

In the common co-milled mixtures of 30---, TANSHINONES crystal diffraction peak intensity ° is located with the change curve of milling time altogether in 2 θ=17.74;

In the 31---microwave grinding aid mixture, TANSHINONES crystal diffraction peak intensity ° is located with the change curve of milling time altogether in 2 θ=17.74;

Go out Fig. 1 as seen, through microwave radiation 2min, the basic free of losses of TANSHINONES content.Radiation 3min, content reduces by 0.579%.And after this with the prolongation of radiated time, TANSHINONES content sharply descends.5min descends 20.33%, and 8min descends 26.32%, and 10min descends 30.96%.

TANSHINONES is formed by the chemical compound that is contained o-quinone or para-quinoid structure by kind more than 30, and is very unstable to high temperature.Microwave radiation 3min, the TANSHINONES particle temperature may be quite high, and TANSHINONES begins oxidation.Behind the radiation 5min, TANSHINONES tends to carbonization owing to temperature is too high.Therefore, microwave irradiation time should be above 3 minutes.

As can be seen from Figure 2, the dissolution of the TANSHINONES co-milled mixtures of microwave grinding aid is apparently higher than the dissolution of common co-milled mixtures.This shows that TANSHINONES is behind microwave radiation, and change has taken place its mechanical characteristic.The TANSHINONES crystal is owing to crackle and defective appear in the thermal stress effect, and fragility increases.When grinding altogether with chitosan, it grinds limit increase, has bigger dispersion in co-milled mixtures.In addition, as can be seen from Figure 2, the dissolution of the co-milled mixtures of the TANSHINONES that microwave radiation is 2 times is bigger than microwave radiation 1 time, but not remarkable, and with the almost indifference of comparing of microwave radiation 3 times.This shows TANSHINONES through microwave radiation 2 times (each 1min), and its thermal expansion is near the limit, and the crystal grain internal stress substantially no longer increases.

As can be seen from Figure 3, the dissolution of the co-milled mixtures of TANSHINONES and chitosan obviously increases than physical mixture and the former medicine of TANSHINONES.And the dissolution of the co-milled mixtures of microwave grinding aid is apparently higher than common co-milled mixtures, and the dissolution of common co-milled mixtures that grinds 120min when wherein the dissolution of the co-milled mixtures of microwave aided co-grinding 30min is than no microwave grinding aid altogether is also high.This shows that again microwave radiation has improved the grinding limit of TANSHINONES, when itself and chitosan are ground altogether bigger dispersion is arranged, thereby makes TANSHINONES have bigger specific surface area and the chemical potential of Geng Gao, thereby dissolution has improved.Milling time is long more altogether, and the dissolution of co-milled mixtures is big more, but grinds 1h and 2h, and the difference of dissolution is little, and this shows that when grinding reached 2h altogether, TANSHINONES was near the grinding limit.As for the former medicine of the also a little higher than TANSHINONES of the dissolution of TANSHINONES in the physical mixture, this mainly is because the hydroaropic substance chitosan has increased TANSHINONES to the event of the wettability of water.

As seen from Figure 4, the chitosan ratio is big more in the co-milled mixtures, and the dissolution of TANSHINONES is just big more, this be since the dispersion of TANSHINONES with chitosan dosage increase and increase so.In addition, can find out also from figure that the dissolution of the co-milled mixtures of microwave grinding aid is bigger, wherein TANSHINONES and chitosan are the dissolution that the dissolution of 1: 4 microwave grinding aid mixture is equivalent to 1: 6 common co-milled mixtures substantially.

It is to be noted, when detecting the dissolution of co-milled mixtures, if when adopting the simulated gastric fluid of pH=1.2, the TANSHINONES that is attached to the chitosan surface will all be scattered in the dissolution medium because of the dissolving gradually of chitosan, chitosan after the dissolving has increased the hydrophilic of TANSHINONES on the one hand, to stop dissolved TANSHINONES coalescence again on the other hand, therefore, will be than bigger dissolution (because chitosan is almost insoluble in distilled water and alkaline solution) is arranged in the distilled water of pH=5.8.

As can be seen from Figure 5, TANSHINONES has stronger crystal diffraction peak, in the physical mixture of 1: 2 TANSHINONES and chitosan, the crystal diffraction peak of TANSHINONES still keeps very obviously, and in 1: 2 co-milled mixtures, the intensity at TANSHINONES crystal diffraction peak weakens, and with the prolongation of milling time altogether, crystal begins to turn to amorphous.In the co-milled mixtures of microwave grinding aid, the intensity at TANSHINONES crystal diffraction peak is the most weak.Wherein, ° locate in TANSHINONES crystal diffraction angle 2 θ=7.12 ° and 2 θ=17.74, in the co-milled mixtures of microwave grinding aid and no microwave grinding aid, the intensity at TANSHINONES crystal diffraction peak with the rate of change of milling time as shown in Figure 6.

Fig. 6 shows, in the co-milled mixtures of microwave grinding aid, TANSHINONES crystal diffraction peak in 2 θ=7.12 ° and the 2 θ=17.74 ° intensity of locating all be lower than the intensity at TANSHINONES crystal diffraction peak in the common co-milled mixtures, and it is also low to grind in the common co-milled mixtures of 120min TANSHINONES crystal diffraction peak intensity when TANSHINONES crystal diffraction peak intensity is than no microwave radiation in the co-milled mixtures during microwave grinding aid 30min altogether.

By accompanying drawing as seen, in the co-milled mixtures of microwave grinding aid, the more common co-milled mixtures of the dissolution of TANSHINONES, physical mixture and the former medicine of TANSHINONES are significantly improved.During the microwave grinding aid, TANSHINONES from crystalline state to the amorphous state rate of transition than common fast when grinding altogether.This method efficient height, technology is simple, does not use solvent, and adjuvant is nontoxic, pollution-free, can realize suitability for industrialized production.Method of the present invention is suitable for the preparation of other insoluble medicines equally.

Below will be further described related content of the present invention by embodiment.

Embodiment 1

The TANSHINONES powder that 1 gram laboratory is extracted places microwave oven, and microwave power places maximum, after 1 minute, is cooled to room temperature through microwave radiation immediately, and then radiation 1 minute, is cooled to room temperature equally immediately.With behind this TANSHINONES and the 2 gram chitosan uniform mixing, place ball mill to grind altogether 30 minutes then, promptly obtain the TANSHINONES micropowder preparation of said microwave grinding aid method preparation.This co-milled mixtures is carried out the dissolution test, and the result is:

Dissolution time/min 5 10 15 20 30 40 50 60 90 120 accumulation stripping percentage rate/% 6.05 6.76 6.97 7.28 8.11 8.63 8.94 9.35 11.01 12.18

Comparative Examples 1

Behind the TANSHINONES powder and 2 gram chitosan uniform mixing with 1 gram laboratory extraction, place ball mill to grind altogether 30 minutes, promptly obtain the TANSHINONES micropowder preparation of said common Ginding process altogether preparation.This co-milled mixtures is carried out the dissolution test, and the result is:

Dissolution time/min 5 10 15 20 30 40 50 60 90 120

Accumulation stripping percentage rate/% 3.34 4.17 4.58 4.79 5.41 6.24 6.55 7.07 7.59 8.21

Comparative Examples 2

Behind the TANSHINONES powder and 2 gram chitosan uniform mixing with 1 gram laboratory extraction, promptly obtain the physical mixture of said TANSHINONES and chitosan.This physical mixture is carried out the dissolution test, and the result is:

Dissolution time/min 5 10 15 20 30 40 50 60 90 120

Accumulation stripping percentage rate/% 1.13 1.77 1.98 2.06 2.32 2.69 2.93 3.25 3.61 3.92

Comparative Examples 3

The former medicine of TANSHINONES powder that laboratory is extracted carries out the dissolution test, and the result is:

Dissolution time/min 5 10 15 20 30 40 50 60 90 120

Accumulation stripping percentage rate/% 0.59 0.70 0.80 1.12 1.44 1.66 2.08 2.51 2.83 2.90

Can find out that from embodiment the co-milled mixtures of TANSHINONES and chitosan and the dissolution of physical mixture are big than the dissolution medicine of the former medicine of TANSHINONES, and the mixture dissolution maximum of microwave grinding aid, common co-milled mixtures takes second place.At 37 ℃ speeds of agitator is in the 900mL distilled water of 100r/min during stripping 120min, the dissolution of TANSHINONES is 4.20 times of the former medicine of TANSHINONES in the mixture of microwave grinding aid, the dissolution of TANSHINONES is 2.83 times of the former medicine of TANSHINONES in the common co-milled mixtures, and the dissolution of TANSHINONES is 1.35 times of the former medicine of TANSHINONES in the physical mixture.It is pointed out that being total to milling time in the present embodiment only is 30min, is dissolution medium simultaneously with the distilled water, and therefore the dissolution value that records is all lower.

Claims (5)

1. TANSHINONES micropowder preparation is characterized in that component and content are:

TANSHINONES 4.0～50%

Hydrophilicity condiment 50～96%

More than be mass percent;

Said TANSHINONES is a Radix Salviae Miltiorrhizae extract;

Said hydrophilicity condiment is a kind of in chitosan, chitin, microcrystalline Cellulose, pregelatinized Starch, lactose, Macrogol 4000, the polyethylene glycol 6000.

2. TANSHINONES micropowder preparation as claimed in claim 1, it is characterized in that component and content are: TANSHINONES 15～50% hydrophilicity condiments are mass percent more than 50～85%.

3. TANSHINONES micropowder preparation as claimed in claim 1 is characterized in that said hydrophilicity condiment is a chitosan.

4. as the microwave aided co-grinding process for preparing of the described TANSHINONES micropowder of the arbitrary right of claim 1-3 preparation, it is characterized in that comprising the steps:

At first the TANSHINONES powder is placed microwave oven, carried out microwave radiation 1-10 minute, radiation 1-3 time is placed on grinding in ball grinder with itself and hydrophilicity condiment by above-mentioned mixed again, can obtain said TANSHINONES micropowder preparation.

5. the microwave aided co-grinding process for preparing of TANSHINONES micropowder preparation as claimed in claim 4 is characterized in that, milling time is 15 minutes-24 hours.

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