CN101703529A - Cordyceps mycelia polysaccharide pellet and preparation method thereof - Google Patents

Abstract

The invention provides a cordyceps mycelia polysaccharide pellet preparation which is prepared by cordyceps mycelia polysaccharide and a pharmaceutic adjuvant. The cordyceps mycelia polysaccharide pellet preparation is characterized in that the pharmaceutic adjuvant comprises an excipient and a bonding agent, wherein the weight percent of the cordyceps mycelia polysaccharide in the pellet preparation is 20-90 percent, the weight percent of the excipient is 5-79 percent, and the weight percent of the bonding agent is 1-5 percent. The pellet preparation can be prepared into slow release or enteric-coated preparation. The cordyceps mycelia polysaccharide pellet preparation has high dissolution rate and high bioavailability; and the method is simple, convenient and easy to operate.

Description

A kind of cordyceps mycelia polysaccharide pellet and preparation method thereof

Technical field:

The present invention relates to micropill of a kind of wholefood extract and preparation method thereof, particularly micropill made from Polysaccharid in Cordyceps Mycelia and preparation method thereof.

Background technology:

Cordyceps claims Cordyceps, Cordyceps again, is a kind of traditional famous and precious tonic Chinese medicine material.Its property of medicine gentleness, equal edible throughout the year, the old or young, sick, weak, virtual person is all suitable, than the tonic of other kinds medical value is widely arranged.

The effective ingredient of Cordyceps mainly is a Cordyceps polysaccharide, the polysaccharide that this polysaccharide is made up of mannose, cordycepin, adenosine, galactose, arabinose, xylose essence, glucose.Experiment showed, that Cordyceps polysaccharide can improve immune function of human body; Strengthen blood flow, vision enhancing; Resisting fatigue; Defying age; Promote memory and nourishing the brain and improving intelligence etc.The clinical malignant tumor that has been used for the treatment of.

At present, be subjected to consumers in general's approval deeply about the product of Polysaccharid in Cordyceps Mycelia, these products are common tablet and capsule substantially, but above-mentioned dosage form exists disintegration time long; A certain position point disintegrate in vivo has certain zest to gastric mucosa; 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 discharge micro-pill type product controlled and that bioavailability is high in vivo, to satisfy consumers in general's demand better.

Generally to add pharmaceutic adjuvants such as excipient, binding agent, porogen, disintegrating agent, plasticizer [" design and development of sustained-release and controlled release preparation " Yan Yaodong etc. in the preparation process of pellet preparations, Chinese Medicine science and technology publishing house, 2006,257-258], in the research process of micropill, need carry out deep research to formulation preparation, just can prepare qualified micropill product.

Summary of the invention:

For these reasons, we carry out deep analysis by physics and chemical property to Polysaccharid in Cordyceps Mycelia, with the dissolution is index, test by science, determine that pharmaceutic adjuvant is excipient and binding agent, and excipient and binding agent are carried out determining of weight percentage: " pharmaceutic adjuvant is excipient and binding agent; wherein the weight percentage of Polysaccharid in Cordyceps Mycelia is 20%～90%; the weight percentage 5%～79% of excipient, the weight percentage of binding agent are 1%～5%."; By this complete technical scheme, those skilled in the art just can prepare satisfactory pellet preparations according to the preparation method of the micropill of prior art; Above-mentioned pellet preparations can be prepared into satisfactory slow releasing preparation or enteric coated preparation, help user's compliance.We have carried out sufficient pulverizing with Polysaccharid in Cordyceps Mycelia and excipient, be that micronization is pulverized, make Polysaccharid in Cordyceps Mycelia be distributed in the excipient well, make particle diameter reach micro powder grade, make micropill with such material, in vivo in the process of Shi Fanging, main constituent can discharge rapidly along with the dissolving of excipient, and this product is made up of the little micropill unit of hundreds of grain, disperse area big in vivo, the organ contacted specific surface area is also big with absorbing, so onset is rapid after making this product take, and the bioavailability height.

The objective of the invention is provides a kind of novel formulation of Polysaccharid in Cordyceps Mycelia---pellet preparations in order to overcome the problems of the prior art.

Another object of the present invention is to provide a kind of preparation method of cordyceps mycelia polysaccharide pellet preparation, this method is simple, convenient, easy operating.

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

A kind of cordyceps mycelia polysaccharide pellet preparation, form by Polysaccharid in Cordyceps Mycelia, pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, wherein the weight percentage of Polysaccharid in Cordyceps Mycelia is 20%～90%, the weight percentage 5%～79% of excipient, the weight percentage of binding agent are 1%～5%.

The slow release formulation of above-mentioned cordyceps mycelia polysaccharide pellet formulation preparation.

Or the enteric dosage form of above-mentioned cordyceps mycelia polysaccharide pellet formulation preparation.

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

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

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

(1) gets Polysaccharid in Cordyceps Mycelia, add excipient, be crushed to micronized rank, mixing;

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

(3) adopt the micropill forming technique to make micropill.

In the conventional art, the degree of grinding of medical material or extract is coarse powder (in take, particle diameter 850um ± 70um, cross 24 mesh sieves), middle powder (in take, particle diameter 250um ± 9.9um, cross 65 mesh sieves), fine powder (wound usefulness, particle diameter 150um ± 6.6um, cross 100 mesh sieves), fine powder (eye dripping usefulness, 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 Polysaccharid in Cordyceps Mycelia is ground into micropowder, its mean diameter is generally less than 10um, mainly is distributed in 1～20um.Method of micronization can adopt method of the prior art: physical pulverization method, for example mechanical impact crusher, jet mill, ball mill, vibromill, stirring mill, Raymond mill, high-pressure micronizer machine etc.; The physical chemistry synthetic method comprises spray drying, original position micronization and supercritical fluid technology etc.Compare with traditional crushing technology, the main advantage of this technology is: increase the effective ingredient absorbance, improve bioavailability.The dissolution rate of effective ingredient is directly proportional with 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 thin more, and then its specific surface area is big more, helps the stripping of effective ingredient more.According to the study, the intestines and stomach is about 15um to the optimal absorption granularity of material grains, and the granule of micron composition has just reached this optimal absorption fineness level; Because the micron order effective ingredient obviously increases at the gastrointestinal dissolubility, thereby increases its bioavailability, has accelerated its onset time.

Micropill forming technique among 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:

(1) we have carried out sufficient pulverizing with Polysaccharid in Cordyceps Mycelia and excipient, make Polysaccharid in Cordyceps Mycelia be distributed in the excipient well, and particle diameter has reached micro powder grade, make micropill with such material, in vivo in the process of Shi Fanging, main constituent can discharge rapidly along with the dissolving of excipient, and the every capsules of this product is made up of the little micropill unit of hundreds of grain, disperse area big in vivo, also big with the gastric juice contacted specific surface area, admittedly onset is rapid after making this product take, the bioavailability height.

(2) the micropill of the present invention micropill that can be as required make rapid release or discharge at a slow speed by different prescriptions, belong to multiple agent type, can form by the micropill of different drug release rates. also can pass through packaging technique, micropill is made positioned releasing micropills such as stomach dissolution type, enteric solubility. this micropill can encapsulatedly be made capsule, or tabletting is made tablet, or make other various packaged forms. micropill of the present invention is compared with single dose dosage form (as tablet), supplementary product consumption is few, steady quality, have curative effect repeatability preferably, adverse reaction rate is low; This product micropill increases at the area of gastrointestinal tract surface distributed, bioavailability is improved and local excitation is less or eliminate, and selects for consumers in general provide more consumption.

One, dissolution contrast experiment:

We have carried out release in vitro contrast test (experimental technique is according to Pharmacopoeia of People's Republic of China version dissolution in 2005 check and analysis method) with this product and commercially available tablet and conventional capsule agent, and the result is as follows:

The conventional capsule agent (the Zhengzhou manufacturer production, lot number: 090112) the 30min dissolution rate is 47% in gastric juice;

Tablet (the Shanghai manufacturer production, lot number: 081203) the 30min dissolution rate is 54% in gastric juice;

And this product 30min dissolution rate in gastric juice promptly reaches 92%.

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

Therefore after we make slow-release micro-pill with this product, have the slow-release function of 12h, can effectively control the burst size of Polysaccharid in Cordyceps Mycelia, safety, effectiveness are better; Slow-release micro-pill can make blood drug level reach curative effect concentration rapidly, and keeps steady, long valid density, and blood concentration fluctuation is little; This product has reduced the accumulated dose of taking than common dosage form simultaneously, has reduced the number of times of taking of consumer.We find that by the release in vitro simulation test its release profiles is obvious with this product, and when 2h, release is more than 30%; During 5h, release is more than 50%; During 8h, release is more than 70%; During 12h, release is more than 90%.

Have the consumer of stomach illness for some, for fear of the influence of product to stomach, this product is absorbed by the body better, we can also make enteric coated preparation with this product, promptly by micropill is carried out enteric coated technology, make product reach the purpose of enteric.We find when this enteric coated micropill is carried out the release in vitro simulation test, enteric coated micropill in simulated gastric fluid in 2 hours without any stripping, outward appearance is also without any variation, and when we put it to when carrying out dissolution test in the simulated intestinal fluid, it has just reached more than 85% 30 minutes releases.

Two, pellet preparations research process:

Get Polysaccharid in Cordyceps Mycelia, method [" design and development of sustained-release and controlled release preparation " Yan Yaodong etc. according to existing document micropill preparation, Chinese Medicine science and technology publishing house, 2006,257-258] be prepared, can not prepare qualified pellet preparations, therefore, we further study, and experimentize by following experimental technique:

1, the Polysaccharid in Cordyceps Mycelia weight percentage is 25% in the pellet preparations, and the excipient weight percentage is 73%, and the percentage composition of binding agent is 2%.

2, the Polysaccharid in Cordyceps Mycelia weight percentage is 35% in the pellet preparations, and the excipient weight percentage is 90%, and the percentage composition of binding agent is 5%.

3, the Polysaccharid in Cordyceps Mycelia weight percentage is 50% in the pellet preparations, and the excipient weight percentage is 45%, and the percentage composition of binding agent is 4%.

4, the Polysaccharid in Cordyceps Mycelia weight percentage is 70% in the pellet preparations, and the excipient weight percentage is 26%, and the percentage composition of binding agent is 4%.

5, the Polysaccharid in Cordyceps Mycelia weight percentage is 80% in the pellet preparations, and the excipient weight percentage is 15%, and the percentage composition of binding agent is 5%.

Get the micropill of above-mentioned different experiments scheme,, detect according to the Pharmacopoeia of the People's Republic of China (version in 2005) appendix dissolution detection method.

Experimental result: the micropill of above-mentioned different schemes reaches more than 90% at 30 minutes dissolution, proves absolutely that the pellet preparations that the present invention prepares has scientific meaning.

Claims (7)

1. cordyceps mycelia polysaccharide pellet preparation, it is to be prepared from by Polysaccharid in Cordyceps Mycelia and pharmaceutic adjuvant, it is characterized in that pharmaceutic adjuvant is excipient and binding agent, wherein the weight percentage of Polysaccharid in Cordyceps Mycelia is 20%～90%, the weight percentage 5%～79% of excipient, the weight percentage of binding agent are 1%～5%.

2. the slow release formulation of a kind of cordyceps mycelia polysaccharide pellet formulation preparation according to claim 1.

3. the enteric dosage form of a kind of cordyceps mycelia polysaccharide pellet formulation preparation according to claim 1.

4. according to described a kind of cordyceps mycelia polysaccharide pellet preparation of claim 1, wherein said excipient is one or more the mixture that is selected from sucrose, dextrin, starch, Celluloasun Microcrystallisatum, lactose, methylcellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone, ethyl cellulose, acrylic resin, hydroxypropyl emthylcellulose and the gelatin.

5. a kind of cordyceps mycelia polysaccharide pellet preparation according to claim 1, wherein said binding agent are one or more the mixture in polyvinylpyrrolidone, cellulose family, resinae, saccharide, the animal acid.

6. according to the preparation method of each described a kind of cordyceps mycelia polysaccharide pellet preparation of claim 1-5, the steps include:

(1) gets Polysaccharid in Cordyceps Mycelia, add excipient, be crushed to micronized rank, mixing;

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

(3) adopt the micropill forming technique to make micropill.

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