CN1365694A

CN1365694A - Nano medicine 'Huitian Zaizao' and its preparing process

Info

Publication number: CN1365694A
Application number: CN 01100637
Authority: CN
Inventors: 杨孟君
Original assignee: Individual
Current assignee: Individual
Priority date: 2001-01-15
Filing date: 2001-01-15
Publication date: 2002-08-28

Abstract

A nanometre medicine "Huitian Zaizao" is prepared from the nanometre powders of 25 Chinese medicinal materials including frankincense, cinnabar, coptis root, katsumadai seed, etc. through proportioning, microwave extracting, pressure reduction concentrating and supersonic-jet spray drying. Its grain fineness reaches 1200-1500 meshes and grain diameters are 0.1-200 nm. Its advantages include high biological utilization rate and high curative effect.

Description

Nano medicine ' Huitian Zaizao ' and preparation method thereof

Wood invention relates to a kind of expelling wind and cold, the eliminating phlegm of regulating the flow of vital energy, dredge the meridian passage, cures mainly apoplexy, syndrome similar to wind disease, and hemiplegia, facial hemiparalysis, the nano medicine ' Huitian Zaizao ' of slurred speech and invasion by pathogenic cold, middle gas, middle expectorant the invention still further relates to the method for this medication preparation.

Restorative bolus with tremendous power is a kind of classical Chinese patent medicine, mainly contains expelling wind and cold, effect such as the eliminating phlegm of regulating the flow of vital energy, dredge the meridian passage, is used for apoplexy, syndrome similar to wind disease, hemiplegia, facial hemiparalysis, diseases such as slurred speech and invasion by pathogenic cold, middle gas, middle expectorant.But traditional restorative bolus with tremendous power disintegrate is slower, absorbs not exclusively, and bioavailability is not high, slow curative effect.

The object of the present invention is to provide a kind of bioavailability height, solid dispersion is good, absorbs fully the nano medicine ' Huitian Zaizao ' of increase evident in efficacy.

Another object of the present invention provides the preparation method of this nano medicine ' Huitian Zaizao '.

To achieve these goals, the present invention takes following technical scheme:

Medicine of the present invention is to make (consumption is a weight portion) by following component:

Nanometer Agkistrodon 168-432 part nanometer Olibanum (system) 80-200 part nanometer Cinnabaris 80-200 part

Nanometer coptis 157-403 part nanometer Semen Alpiniae Katsumadai 157-403 part nanometer sheet Rhizoma Curcumae Longae 157-403 part

Nanometer Radix Polygoni Multiflori 157-403 part nanometer Radix Aucklandiae 32-80 part nanometer Fructus Amomi Rotundus 157-403 part

Nanometer Radix Puerariae 20-50 part nanometric Herbra Asarum 78-202 part nanometer Rhizoma Et Radix Notopterygii 157-403 part

Nano angelica root 157-403 part nanometer Herba Pogostemonis 157-403 part nanometer Herba Ephedrae 157-403 part

Nanometer Colophonium 39-101 part nanometer SHANSHEN 157-403 part nano tiger bone (short) 224-576 part

Nanometer earthworm 39-101 part nanometer Herba Taxilli 196-504 part nanometer Fructus Caryophylli 78-202 part

Nanometer Myrrha (processed) 78-202 part nanometer Radix Rehmanniae Preparata 157-403 part nano bezoar 20-50 part

Nanometer Cortex Magnoliae Officinalis 39-101 part nanometer Bombyx Batryticatus (stir-fry) 78-202 part nano musk 4-10 part

Nanometer Radde Anemone Rhizome 157-402 part nano Chinese angelica 157-403 part nanometer Radix Paeoniae Rubra 157-403 part

Nano Poria 157-403 part nanometer Scorpio 20-50 part nanometer Rhizoma Atractylodis Macrocephalae (parched with bran) 78-202 part

Nanometer Radix Linderae 78-202 part nanometer Pericarpium Citri Reticulatae Viride 78-202 part nanometer Cortex Cinnamomi 157-403 part

Nanometer Borneolum Syntheticum 20-50 part nanometer Cornu rhinocerotis 62-158 part nanometer Lignum Aquilariae Resinatum 78-202 part

Nanometer Arisaema Cum Bile 8-20 part nanometer Concretio Silicea Bambusae 78-202 part nanometer Rhizoma Drynariae (boiling hot, unhairing) 78-202 part

Nano amber 157-403 part nanometric Radix Aconiti Lateralis Preparata (system) 78-202 part nanometer Radix Saposhnikoviae 157-403 part

Nanometer Carapax et Plastrum Testudinis (quench in vinegar) 78-202 part nanometer Radix Glycyrrhizae 157-403 part nanometer Rhizoma Chuanxiong 157-403 part

Nanometer Sanguis Draxonis 63-193 part nanometer Radix Scrophulariae 157-403 part nano gastrodia 157-403 part

Nano cyperus tuber (vinegar system) 112-168 part nanometer Benzoinum 208-312 part nanometer Sanguis Naemorhedi 78-202 part

Nanometric Hypoglaucous Collett Yam Rhizome 157-403 part nanometer Squama Manis (vinegar system) 157-403 part nano safflower 63-193 part

Nanometer Radix Clematidis 20-50 part nano astragalus (processed with honey) 157-403 part nano rhubarb (processed with wine) 157-403 part

The formula optimization weight proportion scope of medicine of the present invention is:

Nanometer Agkistrodon 240-360 part nanometer Olibanum (system) 112-168 part nanometer Cinnabaris 112-168 part

Nanometer coptis 224-336 part nanometer Semen Alpiniae Katsumadai 224-336 part nanometer sheet Rhizoma Curcumae Longae 224-336 part

Nanometer Radix Polygoni Multiflori 224-336 part nanometer Radix Aucklandiae 45-67 part nanometer Fructus Amomi Rotundus 224-336 part

Nanometer Radix Puerariae 28-42 part nanometric Herbra Asarum 112-168 part nanometer Rhizoma Et Radix Notopterygii 224-336 part

Nano angelica root 224-336 part nanometer Herba Pogostemonis 224-336 part nanometer Herba Ephedrae 224-336 part

Nanometer Colophonium 56-84 part nanometer SHANSHEN 224-336 part nano tiger bone (short) 320-480 part

Nanometer earthworm 56-84 part nanometer Herba Taxilli 280-420 part nanometer Fructus Caryophylli 112-168 part

Nanometer Myrrha (processed) 112-168 part nanometer Radix Rehmanniae Preparata 224-336 part nano bezoar 28-42 part

Nanometer Cortex Magnoliae Officinalis 56-84 part nanometer Bombyx Batryticatus (stir-fry) 112-168 part nano musk 6-8 part

Nanometer Radde Anemone Rhizome 224-336 part nano Chinese angelica 224-336 part nanometer Radix Paeoniae Rubra 224-336 part

Nano Poria 224-336 part nanometer Scorpio 28-42 part nanometer Rhizoma Atractylodis Macrocephalae (parched with bran) 112-168 part

Nanometer Radix Linderae 112-168 part nanometer Pericarpium Citri Reticulatae Viride 112-168 part nanometer Cortex Cinnamomi 224-336 part

Nanometer Borneolum Syntheticum 28-42 part nanometer Cornu rhinocerotis 88-132 part nanometer Lignum Aquilariae Resinatum 112-168 part

Nanometer Arisaema Cum Bile 11-17 part nanometer Concretio Silicea Bambusae 112-168 part nanometer Rhizoma Drynariae (boiling hot, unhairing) 112-168 part

Nano amber 224-336 part nanometric Radix Aconiti Lateralis Preparata (system) 112-168 part nanometer Radix Saposhnikoviae 224-336 part

Nanometer Carapax et Plastrum Testudinis (quench in vinegar) 112-168 part nanometer Radix Glycyrrhizae 224-336 part nanometer Rhizoma Chuanxiong 224-336 part

Nanometer Sanguis Draxonis 90-134 part nanometer Radix Scrophulariae 224-336 part nano gastrodia 224-336 part

Nano cyperus tuber (vinegar system) 112-168 part nanometer Benzoinum 208-312 part nanometer Sanguis Naemorhedi 112-168 part

Nanometric Hypoglaucous Collett Yam Rhizome 224-336 part nanometer Squama Manis (vinegar system) 224-336 part nano safflower 90-134 part

Nanometer Radix Clematidis 28-42 part nano astragalus (processed with honey) 224-336 part nano rhubarb (processed with wine) 224-336 part

The optimum weight proportioning of medicine of the present invention is:

280 parts of 140 parts of nanometer coptis of 140 parts of nanometer Cinnabaris of 300 parts of nanometer Olibanums of nanometer Agkistrodon (system)

56 parts of 280 parts of nanometer Radix Aucklandiae of 280 parts of nanometer Radix Polygoni Multiflori of 280 parts of nanometer sheet Rhizoma Curcumae Longaes of nanometer Semen Alpiniae Katsumadai

280 parts of 140 parts of nanometer Rhizoma Et Radix Notopterygiis of 35 parts of nanometric Herbra Asarums of 280 parts of nanometer Radix Puerariaes of nanometer Fructus Amomi Rotundus

70 parts of 280 parts of nanometer Colophonium of 280 parts of nanometer Herba Ephedraes of 280 parts of nanometer Herba Pogostemoniss of nano angelica root

350 parts of 70 parts of nanometer Herba Taxillis of 400 parts of nanometer earthworms of 280 parts of nano tiger bones of nanometer SHANSHEN (short)

35 parts of 280 parts of nano bezoars of 140 parts of nanometer Radix Rehmanniae Preparata of 140 parts of nanometer Myrrha (processed) of nanometer Fructus Caryophylli

280 parts of 7 parts of nanometer Radde Anemone Rhizomes of 140 parts of nano musks of 70 parts of nanometer Bombyx Batryticatus of nanometer Cortex Magnoliae Officinalis (stir-fry)

35 parts of 280 parts of nanometer Scorpios of 280 parts of nano Porias of 280 parts of nanometer Radix Paeoniae Rubra of nano Chinese angelica

280 parts of 140 parts of nanometer Cortex Cinnamomis of 140 parts of nanometer Pericarpium Citri Reticulatae Virides of 140 parts of nanometer Radixs Linderae of the nanometer Rhizoma Atractylodis Macrocephalae (parched with bran)

14 parts of 140 parts of nanometer Arisaema Cum Bile of 110 parts of nanometer Lignum Aquilariae Resinatum of 35 parts of nanometer Cornu rhinocerotiss of nanometer Borneolum Syntheticum

280 parts of 140 parts of nano ambers of 140 parts of nanometer Rhizoma Drynariae of nanometer Concretio Silicea Bambusae (boiling hot, unhairing)

280 parts in 140 parts of nanometer Radix Glycyrrhizaes of nanometric Radix Aconiti Lateralis Preparata (system) 280 parts of nanometer Carapax et Plastrum Testudiniss of 140 parts of nanometer Radix Saposhnikoviaes (quench in vinegar)

280 parts of 280 parts of nano gastrodias of 112 portions of nanometer Radix Scrophulariaes of 280 parts of nanometer Sanguis Draxonis of nanometer Rhizoma Chuanxiong

280 parts of 140 parts of nanometric Hypoglaucous Collett Yam Rhizomes of 260 parts of nanometer Sanguis Naemorhedi of 140 parts of nanometer Benzoinumes of nano cyperus tuber (vinegar system)

35 parts of 112 parts of nanometer Radix Clematidis of 280 parts of nano safflowers of nanometer Squama Manis (vinegar system)

280 parts of 280 parts of nano rhubarbs of nano astragalus (processed with honey) (processed with wine)

Technical scheme of the present invention is based on the modern material technology.One of modern material Developing Trend in Technology is to develop to the more and more littler direction of yardstick.The granule of the past composition material, its size all are at micron or more than the millimeter magnitude, and have occurred the material to the nanoscale development now.Because extremely refinement of granule, the shared percentage by volume of crystal boundary increases, and makes some performance of material that outstanding variation take place.

The property of nano material be since special construction----the material grains size of nano material less than the ultra-micro powder of 100nm, its body surface area is very big, the atom number ratio at crystal boundary place makes it to produce four big effects up to 15--50%: i.e. small-size effect, quantum effect (containing macro quanta tunnel effect), skin effect and interfacial effect.Thereby has the not available physical and chemical performance of traditional material.Nanotechnology will bring a technological revolution of the field of Chinese medicines.

One of method of above-mentioned each component being made medicine of the present invention is:

1. divide and get the Chinese crude drug of respectively distinguishing the flavor of, be processed into the common Chinese decoction pieces according to process of preparing Chinese medicine of Chinese Pharmacopoeia version in 2000.

2. divide and get the common Chinese decoction pieces of respectively distinguishing the flavor of, be processed into the nanometer prepared slices of Chinese crude drugs, its method comprises the following steps:

1. the common Chinese decoction pieces is placed extraction pot, solubilizer also imports microwave extracting, makes its speed with 20--30 hundred million times/second do the change in polarity motion, and the temperature of its microwave extracting is 30 ℃--and 60 ℃, time 1-10 hour;

2. above-mentioned extract is carried out concentrating under reduced pressure, temperature is 30 ℃--60 ℃, the time is 3-72 hour, collects volatile material in the Chinese medicine simultaneously in addition;

3. decompressed concentrate and volatile material merging are placed spray drying tower, use the supersonic jet technology, 330 meters of effluxvelocities--990 meter per seconds, at 30 ℃--60 ℃ of temperature, under 0 to the 0.05MPa pressure,, promptly make the nanometer prepared slices of Chinese crude drugs with the instantaneous drying of hypersonic velocity.

3. the nanometer prepared slices of Chinese crude drugs (powder) are prepared mixing in described ratio, according to Chinese Pharmacopoeia version two-shift system in 2000 agent standard, make pill, powder, tablet, suppository, granule, membrane, capsule, microcapsule, drop pill, aerosol, injection, unguentum, medicated wine, syrup, oral solution.

Two of medicine method for making of the present invention is:

1. be equipped with whole common Chinese decoction pieces in the proportioning ratio, place extraction pot, solubilizer also imports microwave extracting, makes its speed with 20--30 hundred million times/second do the change in polarity motion, and the temperature of its microwave extracting is 30 ℃-60 ℃, time 1-10 hour;

3. decompressed concentrate and volatile material merging are placed spray drying tower, use the supersonic jet technology, 330 meters of effluxvelocities--990 meter per seconds, at 30 ℃--60 ℃ of temperature, under 0 to the 0.05MPa pressure,, get the 'Huitian Zaizao ' nano powder with the instantaneous drying of hypersonic velocity jet;

4. its nano powder is made aforementioned various preparation according to Chinese Pharmacopoeia version standard preparation in 2000.

The pharmacological effect that above-mentioned two kinds of methods are made nano medicine ' Huitian Zaizao ' is identical.

A kind of important feature of the present invention is: the made drug material of the present invention has reached nanoscale, common restorative bolus with tremendous power preparation material is micron or the above particle diameter of millimeter, can only cross the 80-120 mesh sieve, the drug material that the present invention is made, particle diameter is at 0.1--200nm, the overwhelming majority can be crossed the 1200--1500 mesh sieve less than 100nm.

Another important feature of the present invention is: solid preparation of the present invention disintegrate rapidly, and solid dispersion is good in water, absorb fully, the bioavailability height, the pharmacological action effect that mainly contains effective constituent is significantly higher than conventional formulation.

The pharmaceutical preparation that the present invention is made does not need to add any adjuvant, and is more favourable to human body.

The present invention has also created the new drug formulation that powder, tablet, suppository, granule, membrane, capsule, microcapsule, drop pill, aerosol, injection, unguentum, medicated wine, syrup, oral solution of nano medicine ' Huitian Zaizao ' etc. is had no precedent in the past.

Pharmaceutical preparation of the present invention can be used for apoplexy, syndrome similar to wind disease, and hemiplegia, facial hemiparalysis, treatment of conditions such as slurred speech and invasion by pathogenic cold, middle gas, middle expectorant, clinical efficacy significantly is better than traditional restorative bolus with tremendous power.

The present invention's added solvent in microwave extracting is water or ethanol.

The present invention carries out in the concentrating under reduced pressure step at extract, and its concentrating under reduced pressure is conventional scheme.

Embodiment 1:

Prepare nano raw material by preceding method:

Production method is as follows:

In the GMP cleaning shop, after the above-mentioned nanometer prepared slices of Chinese crude drugs or powder prepared mixing in described ratio, according to Chinese Pharmacopoeia version two-shift system in 2000 agent capsules agent standard, do not add adjuvant, do not granulate, directly divide encapsulated with the fully-automatic capsule racking machine, make capsule, every capsules content of dispersion is the 0.1--0.6 gram, and the patient takes the 1-5 grain at every turn, and take 1-4 every day.

Embodiment 2:

Prepare nano raw material by preceding method:

Production method is as follows:

In the GMP cleaning shop, with the above-mentioned nanometer prepared slices of Chinese crude drugs or the described mixed of powder good after, according to 2000 editions two-shift system agent of Chinese Pharmacopoeia powder needle injection standard, do not add any adjuvant, make nanometer save the situation reproduce powder needle injection, every injection content is the 5-20 milligram, each consumption is that 1-2 props up, and use 1-3 every day.

Embodiment 3:

Prepare nano raw material by preceding method:

Production method is as follows:

In the GMP cleaning shop, with the above-mentioned nanometer prepared slices of Chinese crude drugs or powder by described mixed good after, according to 2000 editions two-shift system agent of Chinese Pharmacopoeia membrane standard, filmogen adopts polyvinyl alcohol, make nanometer and save the situation and reproduce membrane, every membrane area size is the 2-100 square centimeter, and content of dispersion is the 1-50 gram, every medicine film pasted 1-7 days, pasted the medicine position: abdominal part, back, chest.

Claims

1, a kind of nano medicine ' Huitian Zaizao ' is characterized in that it is the medicament that the nano raw material of following weight proportioning is made:

And adopt following method to make: to select the formula Chinese drug material to concoct and be processed into the prepared slices of Chinese crude drugs; Place extraction pot, solubilizer also imports microwave extracting, makes it do the change in polarity motion with hundred million times/second speed of 20--30, and the temperature of its microwave extracting is 30--60 ℃, time 1-10 hour; Above-mentioned extract is carried out concentrating under reduced pressure, and temperature is 30--60 ℃, and the time is 3-72 hour, collects volatile material in the Chinese medicine simultaneously in addition; Decompressed concentrate and volatile material merging are placed spray drying tower, use the Supersonic fluidics, 30--60 ℃ of temperature, under 0 to the 0.05MPa pressure, with hypersonic velocity instantaneous jet drying, wherein supersonic jet speed is 330 meters-990 meter per seconds, promptly makes the nanometer prepared slices of Chinese crude drugs.

2, nano medicine ' Huitian Zaizao ' according to claim 1, wherein the weight proportion of each nano raw material is:

3, nano medicine ' Huitian Zaizao ' according to claim 1, wherein the weight proportion of each nano raw material is:

4,, it is characterized in that said medicine is pill, powder, tablet, suppository, granule, membrane, capsule, microcapsule, drop pill, aerosol, injection, unguentum, medicated wine, syrup, oral solution according to claim 1 or 2 or 3 described nano medicine ' Huitian Zaizao 's.

5,, it is characterized in that this method comprises the steps: to select the formula Chinese drug material to concoct and is processed into the prepared slices of Chinese crude drugs according to the pharmaceutical methods of claim 1 or 2 or 3 described nano medicine ' Huitian Zaizao 's; Place extraction pot, solubilizer also imports microwave extracting, makes it do the change in polarity motion with hundred million times/second speed of 20--30, and the temperature of its microwave extracting is 30--60 ℃, time 1-10 hour; Above-mentioned extract is carried out concentrating under reduced pressure, and temperature is 30--60 ℃, and the time is 3-72 hour, collects volatile material in the Chinese medicine simultaneously in addition; Decompressed concentrate and volatile material merging are placed spray drying tower, use the Supersonic fluidics, 30--60 ℃ of temperature, under 0 to the 0.05MPa pressure, with hypersonic velocity instantaneous jet drying, wherein supersonic jet speed is 330 meters-990 meter per seconds, promptly makes the nanometer prepared slices of Chinese crude drugs.

6, wherein respectively distinguish the flavor of Chinese medicine in the ratio of prescription or Chinese crude drug concoct be processed into the prepared slices of Chinese crude drugs after mixing, or after making the nanometer prepared slices of Chinese crude drugs mixing.