CN101579396A - Euphorbia humifusa dispersing tablet and preparation process thereof - Google Patents

Abstract

The invention discloses a euphorbia humifusa extract dispersing tablet and a preparation process thereof. A euphorbia humifusa dispersing tablet prescription comprises euphorbia humifusa general flavone extract, lactose, microcrystalline cellulose, crosslinked polyethylene ketopyrrolidine, polyvidone and magnesium stearate. Disintegrant adopts a combined form of primary addition and following addition during preparation, the obtained dispersing tablet has rapid disintegration, and the solubility in five minutes can reach more than 85 percent.

Description

Euphorbia humifusa dispersing tablet and preparation method thereof

Technical field

The invention belongs to field of traditional Chinese, be specifically related to a kind of Herba Euphorbiae Humifusae extract dispersible tablet and preparation method thereof.

Background technology

Herba Euphorbiae Humifusae is the ground herb of Euphorbiaceae euphorbia Herba Euphorbiae Humifusae (Euphorbia himifusa Willd.), has another name called Herba Chenopodii Hybridi, red shank grass, Herba euphorbiae prostratae, milk grass etc., is born in wasteland, open country, roadside, field, and aboundresources is distributed more widely.Herba Euphorbiae Humifusae belongs to antipyretic and antidotal type Chinese medicine, effect with heat-clearing and toxic substances removing, promoting blood circulation and hemostasis, dampness removing lactogenesis, be usually used in treatment and let out dysentery, too fat to move furuncle, hemorrhage, jaundice due to damp-heat and galactostasis etc., be widely used in clinically, its water decoction, tincture have better curative effect to bacillary dysentery, enteritis etc.Its composition mainly contains flavonoid and tannin class, and the tannin composition is more in its middle period.Existing Herba Euphorbiae Humifusae preparation is conventional capsule and tablet, but used extract is a Herba Euphorbiae Humifusae ethanol crude extract in the existing dosage form, and drug release rate is slow in vivo for the big and ordinary preparation of the assorted dosage of composition, and easy disintegrating absorbs.

Summary of the invention

The object of the invention is to provide a kind of taking convenience, absorbs fast, that bioavailability is high Herba Euphorbiae Humifusae extract oral dispersion tablet preparation and preparation technology thereof.

Herba Euphorbiae Humifusae extract of the present invention prepares through degree of depth purification, general flavone content height in the extract, and effective ingredient is comparatively clear and definite, and dose is few.

The present invention improves absorption and the bioavailability of human body to the Herba Euphorbiae Humifusae total flavones to shorten in vivo disintegration time of tablet, to improve its dissolution and start with.Solution of the present invention is that high-load Herba Euphorbiae Humifusae extract is configured to a kind of dispersible tablet of disintegrate rapidly.

Herba Euphorbiae Humifusae extract of the present invention can prepare in the following way:

Herba Euphorbiae Humifusae medical material 1000g, the alcohol reflux with 60% three times filters, merge each time extracting solution, be evaporated to into the extractum shape, the NaOH aqueous solution dissolving extractum with 5% filters, get the NaOH clear liquid, transfer pH to about 3 with 10% hydrochloric acid, leave standstill, filter, precipitation is washed till water lotion with distilled water and becomes neutral, the dissolve with ethanol of insoluble matter reuse 10% disperses, and with polyamide adsorption resin column on the dispersion liquid, resin is earlier with 10% ethanol elution, thin out to the eluent color, use 65% ethanol elution instead, thin out to the eluent color, essentially no flavone reaction, the ethanol elution part of collection 65%, merge concentrating under reduced pressure, drying, get extract 14.6g, general flavone content is 53.47% in the extract.

In the dispersible tablet of the present invention, contain the Herba Euphorbiae Humifusae extract for preparing as upper type, filler, disintegrating agent, binding agent and lubricant, particularly, in the dispersible tablet prescription of the present invention, each ingredient is counted by weight: 10%～30% Herba Euphorbiae Humifusae extract, 40%～70% lactose, 5%～10% crospolyvinylpyrrolidone, 10%～20% microcrystalline Cellulose, 1%～3% polyvidone and 0.5%～1% magnesium stearate.

Preferably, in the present invention's prescription, each ingredient by weight percentage, 15%～25% Herba Euphorbiae Humifusae extract, 45%～65% lactose, 6%～8% crospolyvinylpyrrolidone, 13%～16% microcrystalline Cellulose, 1%～3% polyvidone and 0.5%～1% magnesium stearate.

The technology of preparation dispersible tablet of the present invention can realize in the following way:

(1) Herba Euphorbiae Humifusae extract is pulverized, crossed 200 mesh sieves, respectively lactose, microcrystalline Cellulose, crospolyvinylpyrrolidone, polyvidone, magnesium stearate are pulverized, cross 100 mesh sieves, standby;

(2) with the crospolyvinylpyrrolidone mix homogeneously of Herba Euphorbiae Humifusae extract and interior dosage, add lactose and microcrystalline Cellulose more successively, mix homogeneously sieves, and is standby;

(3) polyvidone is dissolved in 70% the ethanol, is made into 5% polyvidone ethanol liquid;

(4) polyvidone ethanol liquid is joined in the mixed-powder in the step (2), makes soft material, with 30 eye mesh screens granulate, oven dry; With 30 mesh sieve granulate, make the disintegrate granule of particle diameter again less than 0.5mm;

(5) with the crospolyvinylpyrrolidone and the exsiccant disintegrate granule mix homogeneously of magnesium stearate and outer dosage, pressing cost invention dispersible tablet.

Add in the present invention adopts the adding of disintegrating agent and add the mode that combines, and the different proportion of specifically having investigated interior dosage and outer dosage is to the dispersible tablet EFFECT OF CORK STOPPER, thereby add ratio in definite the best.The result is as shown in table 1.

The different proportion that adds crospolyvinylpyrrolidone in the table 1 is the influence in time limit to disintegrate

From table the result as can be known, the inside and outside additional proportion of disintegrating agent crospolyvinylpyrrolidone was an optimum efficiency with 3: 4.

For showing progressive of the present invention, we have done the disintegration time and the experiment of dissolution degree of dispersible tablet of the present invention, and contrast with the Herba Euphorbiae Humifusae tablet.Dissolution determination method adopts two appendix xc second methods of Chinese Pharmacopoeia version in 2000, and rotating speed is 75 rev/mins, and experimental result sees Table 2 and table 3

Table 2 euphorbia humifusa dispersing tablet and ordinary tablet disintegration time are relatively

Table 3 euphorbia humifusa dispersing tablet and conventional tablet dissolution are relatively

As can be seen from Table 2, the disintegration time of dispersible tablet has improved 10～20 times than ordinary tablet.

As can be seen from Table 3, the dissolution of dispersible tablet is about 22 times of ordinary tablet in 5 minutes.

Specific embodiment

The invention will be further described with embodiment below, provides implementation detail of the present invention, takes a blame and be intended to limit protection scope of the present invention.

Embodiment 1

Herba Euphorbiae Humifusae extract (obtaining) 60g according to the description method

Lactose 150g

Microcrystalline Cellulose 50g

Crospolyvinylpyrrolidone 21g

Polyvidone 9g

Magnesium stearate 3g

Preparation technology: earlier Herba Euphorbiae Humifusae extract was pulverized 200 mesh sieves, and successively lactose, microcrystalline Cellulose, crospolyvinylpyrrolidone, magnesium stearate were pulverized again, and crossed 100 mesh sieves.

Take by weighing polyvidone 9g, the dissolve with ethanol with 75% is made into 5% polyvidone ethanol liquid;

Get crospolyvinylpyrrolidone 9g, the mode that increases progressively with equivalent is with the Herba Euphorbiae Humifusae extract mix homogeneously, the microcrystalline Cellulose, the lactose that add recipe quantity more successively, mix homogeneously, with polyvidone ethanol liquid is that binding agent prepares soft material, granulate with 30 mesh sieves, after 60 ℃ of dryings, make the granule of particle diameter with 30 sieve granulate again less than 0.5mm, add 3g magnesium stearate and 12g crospolyvinylpyrrolidone then, mix homogeneously is pressed into 1000 euphorbia humifusa dispersing tablets, measuring disintegration time is 1 ' 30 ", dissolution was 87.6% in 5 minutes.

Following examples provide the dispersible tablet prescription to be formed, and preparation technology is with embodiment 1

Embodiment 2

Prescription (1000 recipe quantities)

Herba Euphorbiae Humifusae extract 90g

Lactose 130g

Microcrystalline Cellulose 50g

Crospolyvinylpyrrolidone 15g

Polyvidone 3g

Magnesium stearate 1.5g

The priority additional proportion of crospolyvinylpyrrolidone is 3: 5

Measuring disintegration time is 1 ' 41 ", dissolution was 86.3% in 5 minutes.

Embodiment 3

Prescription (1000 amounts)

Herba Euphorbiae Humifusae extract 30g

Lactose 200g

Microcrystalline Cellulose 45g

Crospolyvinylpyrrolidone 30g

Polyvidone 4.5g

Magnesium stearate 2g

The priority additional proportion of crospolyvinylpyrrolidone is 1: 1

Measuring disintegration time is 1 ' 37 ", dissolution was 88.9% in 5 minutes.

Claims (4)

1, a kind of euphorbia humifusa dispersing tablet, contain Herba Euphorbiae Humifusae extract, disintegrating agent, filler, binding agent and lubricant, it is characterized in that, by weight percentage, contain 10%～30% Herba Euphorbiae Humifusae extract, 40%～70% lactose, 5%～10% crospolyvinylpyrrolidone, 10%～20% microcrystalline Cellulose, 1%～3% polyvidone and 0.5%～1% magnesium stearate.

2, dispersible tablet as claimed in claim 1, it is characterized in that, by weight percentage, contain 15%～25% Herba Euphorbiae Humifusae extract, 45%～65% lactose, 6%～8% crospolyvinylpyrrolidone, 13%～16% microcrystalline Cellulose, 1%～3% polyvidone and 0.5%～1% magnesium stearate.

3, dispersible tablet as claimed in claim 1 or 2 is characterized in that described Herba Euphorbiae Humifusae extract is a Herba Euphorbiae Humifusae flavones ingredient extract.

4, a kind of dispersion as claimed in claim 1 or 2 method just for preparing is characterized in that may further comprise the steps:

(1) Herba Euphorbiae Humifusae extract is pulverized, crossed 200 mesh sieves, respectively lactose, microcrystalline Cellulose, crospolyvinylpyrrolidone, polyvidone, magnesium stearate are pulverized, cross 100 mesh sieves, standby;

(2) with the crospolyvinylpyrrolidone mix homogeneously of Herba Euphorbiae Humifusae extract and interior dosage, add lactose and microcrystalline Cellulose more successively, mix homogeneously sieves, and is standby;

(3) polyvidone is dissolved in 70% the ethanol, is made into 5% polyvidone ethanol liquid;

(4) polyvidone ethanol liquid is joined in the mixed-powder in the step (2), makes soft material, with 30 eye mesh screens granulate, oven dry; With 30 mesh sieve granulate, make the disintegrate granule of particle diameter again less than 0.5mm;

(5) with the crospolyvinylpyrrolidone and the exsiccant disintegrate granule mix homogeneously of magnesium stearate and outer dosage, pressing cost invention dispersible tablet.