CN105497153A - Compound fallopia multiflora (thunb.) harald extract micro-pills and preparation method thereof - Google Patents

Abstract

The present invention provides compound fallopia multiflora (thunb.) harald extract micro-pills, which are prepared from a fallopia multiflora (thunb.) harald extract, puerarin and pharmaceutical auxiliary materials, and are characterized in that the pharmaceutical auxiliary materials comprise an excipient and a binder, and the compound fallopia multiflora (thunb.) harald extract micro-pills comprise, by weight, 5-20% of a fallopia multiflora (thunb.) harald extract, 1-5% of puerarin, 70-85% of an excipient, and 1-5% of a binder. According to the present invention, the micro-pill preparation has characteristics of high dissolution rate and high bioavailability, and the preparation method is simple, convenient and easy to operate.

Description

A kind of Radix Polygoni Multiflori extract micropill and preparation method thereof

technical field:

The present invention relates to medicine food technical field, be specifically related to micropill that a kind of Radix Polygoni Multiflori extract makes and preparation method thereof.

background technology:

The various folk prescription health product of Radix Polygoni Multiflori extract and puerarin are more, but the compound preparation about the two has no report, at present, about the product of Radix Polygoni Multiflori extract and puerarin deeply by the accreditation of consumers in general, these products are except for except single preparations of ephedrine, substantially be common Tablet and Capsula agent, but above-mentioned dosage form to there is disintegration time long; A certain position point disintegrate in vivo, has certain zest to gastric mucosa; The shortcomings such as bioavailability is low.Based on the problems referred to above, we will develop micropill technology transfer rapidly to field of food at field of medicaments, this product made and discharge the controlled and compound recipe micro-pill type product that bioavailability is high in vivo, to meet the demand of consumers in general better.

The pharmaceutic adjuvants such as excipient, binding agent, porogen, disintegrating agent, plasticizer [" design and development of sustained-release and controlled release preparation " Yan Yaodong etc. generally will be added in the preparation process of pellet preparations, China Medical Science Press, 2006,257-258], in the research process of micropill, need to carry out deep research to preparation preparation, just can prepare qualified micropill product.

summary of the invention:

The object of the invention is to overcome the problems of the prior art, a kind of novel formulation---pellet preparations of Radix Polygoni Multiflori extract is provided.

Another object of the present invention is to the preparation method that a kind of Radix Polygoni Multiflori extract micropill preparation is provided, the method is simple, convenient, be easy to operation.

Radix Polygoni Multiflori extract of the present invention can be extract, also can be effective ingredient, prepare according to existing literature method or patented method.

The object of the invention is to be achieved through the following technical solutions:

A kind of Radix Polygoni Multiflori extract micropill preparation, be prepared from by Radix Polygoni Multiflori extract, puerarin, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, in its pellet preparations, Radix Polygoni Multiflori extract weight percentage is 5 ~ 20%, the weight percentage of puerarin is 1 ~ 5%, the weight percentage of excipient is 70 ~ 85%, and the weight percentage of binding agent is 1 ~ 5%.

Slow release formulation prepared by above-mentioned Radix Polygoni Multiflori extract micropill preparation.

Or enteric dosage form prepared by above-mentioned Radix Polygoni Multiflori extract micropill preparation.

Wherein said excipient is the mixture of one or more be selected from sucrose, dextrin, starch, microcrystalline Cellulose, lactose, methylcellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and gelatin.

Wherein said binding agent is the mixture of one or more in polyvinylpyrrolidone, cellulose family, resinae, saccharide, animal acid.

Pellet preparations of the present invention according to technique scheme, can be prepared with the preparation method of prior art pellet preparations, also can be prepared by the following method:

(1) get Radix Polygoni Multiflori extract, puerarin, add excipient, be crushed to micronized rank, mixing;

(2) in the solution in binding agent is water-soluble, dehydrated alcohol or aquiferous ethanol;

(3) micropill forming technique is adopted to make micropill.

Wherein said micropill forming technique comprises and is selected from agitation procedure, method of extruding and kneading to pellets or centrifugal fluidized granulation method.

In conventional art, the degree of grinding of medical material or extract is coarse powder (inside take, particle diameter 850um ± 70um, cross 24 mesh sieves), middle powder (inside take, particle diameter 250um ± 9.9um, cross 65 mesh sieves), fine powder (wound use, particle diameter 150um ± 6.6um, cross 100 mesh sieves), most fine powder (eye dripping use, particle diameter 125um ± 5.8um, 120 mesh sieves) and impalpable powder (particle diameter 75um ± 4.1um, 200 mesh sieves), the present invention then adopts micronization technology that Radix Polygoni Multiflori extract is ground into micropowder, its mean diameter is generally less than 10um, is mainly distributed in 1 ~ 20um.Method of micronization can adopt method of the prior art: physical pulverization method, such as mechanical impact crusher, jet mill, ball mill, vibromill, Ball-stirring mill, Raymond mill, high-pressure pulverizer etc.; Physical chemistry synthetic method, comprises spraying dry, original position micronization and supercritical fluid technology etc.Compared with conventional size reduction technology, this technique main advantage is: increase effective ingredient absorbance, improves bioavailability.The dissolution rate of effective ingredient is directly proportional to its specific grain surface is long-pending, and specific surface area and particle diameter are inversely proportional to.Therefore, the particle diameter of effective ingredient is thinner, then its specific surface area is larger, more contributes to the stripping of effective ingredient.According to the study, the optimal absorption granularity of the intestines and stomach to material grains is about 15um, and the granule of micron composition just reaches this optimal absorption fineness level; Because micron order effective ingredient obviously increases at gastrointestinal dissolubility, thus increase its bioavailability, accelerate its onset time.

Micropill forming technique in the present invention can adopt any micropill forming technique of the prior art, and these technology include but not limited to: agitation procedure, method of extruding and kneading to pellets or centrifugal fluidized granulation method etc.

Beneficial effect of the present invention is:

First, Radix Polygoni Multiflori extract, puerarin and excipient have been carried out sufficient pulverizing by us, Radix Polygoni Multiflori extract and puerarin is made to be distributed in excipient well, and particle diameter reaches micro powder grade, micropill is made with such material, in the process discharged in vivo, main constituent can discharge rapidly along with the dissolving of excipient, and the every capsules of this product is made up of the micropill unit that hundreds of grain is little, diffusional area is large in vivo, the specific surface area contacted with gastric juice is also large, admittedly make this product take rear onset rapidly, bioavailability is high.

Micropill of the present invention as required by the micropill that different prescription is made release fast or discharged at a slow speed, can belong to multiple agent type, can be made up of the micropill of different drug release rate.Also by packaging technique, micropill is made the positioned releasing micropills such as stomach dissolution type, enteric solubility.This micropill encapsulatedly can make capsule, or tablet made by tabletting, or makes other various packaged forms.Micropill of the present invention is compared with Single unit dosage forms (as tablet), and supplementary product consumption is few, steady quality, and have good curative effect repeatability, adverse reaction rate is low; This product micropill increases at the area of gastrointestinal tract surface distributed, makes bioavailability raising and local excitation is less or eliminate, for consumers in general provide more consumption choice.

Meanwhile, we can also, by carrying out the technology of coating to micropill, by different coating materials, make product become the product of the different sizes such as slow release, controlled release, enteric.

Some are existed to the consumer of gastric lesions, in order to avoid product is on the impact of stomach, make this product be absorbed by the body better, this product can also be made enteric coated preparation by us simultaneously, namely by carrying out enteric coated technology to micropill, makes product reach the object of enteric.This enteric coated micropill is carried out the discovery of release in vitro simulation test by us, micropill in simulated gastric fluid 2 hours without any stripping, outward appearance also without any change, when we taken out be put into dissolution test in simulated intestinal fluid time, its 30 minutes releases just reach more than 90%.

Detailed description of the invention

embodiment 1

Get the raw material for standby of following formula

Radix Polygoni Multiflori extract 15g(is in sterling)

Puerarin 1g

Celluloasun Microcrystallisatum 80g

Hydroxypropyl emthylcellulose 4g

Prepare pellet preparations in accordance with the following methods:

(1) Radix Polygoni Multiflori extract, the puerarin of getting above-mentioned formula ratio add Celluloasun Microcrystallisatum, are crushed to micronization rank with ball mill, mixing;

(2) hydroxypropyl emthylcellulose is dissolved in 75% alcoholic solution;

(3) method of extruding and kneading to pellets is adopted to make micropill.

embodiment 2

Get the raw material for standby of following formula

Radix Polygoni Multiflori extract 10g(is in sterling)

Puerarin 3g

Celluloasun Microcrystallisatum 82g

Hydroxypropyl emthylcellulose 5g

Prepare pellet preparations in accordance with the following methods:

(1) Radix Polygoni Multiflori extract, the puerarin of getting above-mentioned formula ratio add starch, are crushed to micronization rank with ball mill, mixing;

(2) polyvinyl pyrrolidone is soluble in water;

(3) agitation procedure is adopted to make micropill.

embodiment 3

Get the raw material for standby of following formula

Radix Polygoni Multiflori extract 8g(is in sterling)

Puerarin 5g

Sucrose 49g

Starch 34g

Polyvinylpyrrolidone 4g

Prepare pellet preparations in accordance with the following methods:

(1) Radix Polygoni Multiflori extract, the puerarin of getting above-mentioned formula ratio add sugarcane sugar and starch, are crushed to micronization rank with ball mill, mixing;

(2) polyvinylpyrrolidone is dissolved in suitable quantity of water;

(3) centrifugal fluidized granulation method is adopted to make micropill.

Claims (7)

1. a Radix Polygoni Multiflori extract micropill preparation, be prepared from by Radix Polygoni Multiflori extract, puerarin, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, in its pellet preparations, Radix Polygoni Multiflori extract weight percentage is 5 ~ 20%, the weight percentage of puerarin is 1 ~ 5%, the weight percentage of excipient is 70 ~ 85%, and the weight percentage of binding agent is 5 ~ 10%.

2. the slow release formulation prepared of a kind of Radix Polygoni Multiflori extract micropill preparation according to claim 1.

3. the enteric dosage form prepared of a kind of Radix Polygoni Multiflori extract micropill preparation according to claim 1.

4. a kind of Radix Polygoni Multiflori extract micropill preparation according to claim 1, wherein said excipient is the mixture of one or more be selected from sucrose, dextrin, starch, microcrystalline Cellulose, lactose, methylcellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and gelatin.

5. a kind of Radix Polygoni Multiflori extract micropill preparation according to claim 1, wherein said binding agent is the mixture of one or more in polyvinylpyrrolidone, cellulose family, resinae, saccharide, animal acid.

6. the preparation method of a kind of Radix Polygoni Multiflori extract micropill preparation according to any one of Claims 1 to 5, the steps include:

(1) get Radix Polygoni Multiflori extract, puerarin, add excipient, be crushed to micronized rank, mixing;

(2) in the solution of binding agent is water-soluble, dehydrated alcohol or aquiferous ethanol;

(3) micropill forming technique is adopted to make micropill.

7. preparation method according to claim 6, wherein said micropill forming technique comprises and is selected from agitation procedure, method of extruding and kneading to pellets or centrifugal fluidized granulation method.