CN101485646B - Andrographolide catablasm and preparation method thereof - Google Patents
Andrographolide catablasm and preparation method thereof Download PDFInfo
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- CN101485646B CN101485646B CN2009100665150A CN200910066515A CN101485646B CN 101485646 B CN101485646 B CN 101485646B CN 2009100665150 A CN2009100665150 A CN 2009100665150A CN 200910066515 A CN200910066515 A CN 200910066515A CN 101485646 B CN101485646 B CN 101485646B
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Abstract
The invention relates to an andrographolidume cataplasm for transdermal administration and a method for preparing the same. The andrographolidume cataplasm consists of a backing layer, a medicine storehouse layer and a protective layer, wherein the medicine storehouse layer consists of hydrophilic substrate and a medicine; the hydrophilic substrate comprises the following components in proportion: 0.1 to 0.5g of polyvinyl alcohol, 1 to 3ml of glycerin, 1 to 5ml of propylene glycol, 1 to 5ml of water solution of 40 percent PVP[k30], 2 to 6ml of 50 percent water solution of gelatin, 1 to 3.0g of sodium cellulose glycolate, 0.4 to 0.6g of sodium polyacrylate, 1 to 3ml of azone, 0.1 to 0.4g of Ca(OH)2, and 0.1 to 0.4g of Al(OH)3; and the medicine is 0.5 to 3g of andrographolidume, clathrate or solid dispersion containing 0.5 to 3g of andrographolidume. The preparation method comprises the steps of preparing the clathrate and solid dispersion of the andrographolidume, preparing the cataplasm substrate and preparing the cataplasm. The andrographolidume cataplasm and the method have the advantages of overcoming the defects of oral administration and injection administration, avoiding toxic and side effects, ensuring safer administration, improving the bioavailability and making patients administrate medicines more conveniently; moreover, the cataplasm is particularly suitable for the administration of the aged and children.
Description
Technical field
The present invention relates to the field of Chinese medicines, be specifically related to andrographolide catablasm of percutaneous dosing and preparation method thereof.
Background technology
Chinese medicine Herba Andrographis, another name: the aerial parts of Herba Andrographitis, ZHANSHEJIAN, Herba vallisneriae Spiralis, heart lotus Andrographis paniculata (Burm.f.) Nees.Herba Andrographis is " olive nuclear lotus etc.Be that acanthaceous plant is worn Chinese pharmacopoeia and recorded, generally acknowledge clinically, commonly used and indispensable, the effective antiinflammatory Chinese medicine of treatment cold, fever, laryngopharynx swelling and pain etc., medicinal history is long, enjoys the good reputation of " Chinese medicine antibiotic ", is accepted by extensive patients.Main effective ingredient is an andrographolide in the Herba Andrographis, studies have shown that it also has antitumor, anti-cardiovascular disease, anti-diabetic, anti-HIV, protects the liver and effect such as function of gallbladder promoting.2005 editions " Chinese pharmacopoeia has been recorded Herba Andrographis medical material and andrographis tablet and preparation method thereof.Herba Andrographis medicine of Ying Yonging and preparation thereof mainly contain tablet (Chinese patent 200510004853.3), capsule (Chinese patent 200310105805.4), drop pill (Chinese patent 03130434.6) and injection (Chinese patent 200510004895.7) etc. clinically, and they are oral formulations and injecting and administering preparations.
There are following shortcoming in above-mentioned Herba Andrographis and interior ester formulation thereof: main effective ingredient andrographolide, be insoluble in water, and when gastrointestinal absorption, the medicine dissolution rate is little, and stripping becomes the speed limit process of absorption, and oral absorption is relatively poor; The andrographolide taste is extremely bitter again, and oral medication, compliance are also relatively poor; In addition, the andrographolide oral administration exists gastrointestinal tract metabolism and liver first-pass effect, and bioavailability is lower.Andrographolide is oral heavy dose of, can cause gastrointestinal upset, loss of appetite; Drug administration by injection needs certain medical condition again, and dangerous, has pain and damage again.Report is arranged, and andrographis tablet, CHUANXINLIAN ZHUSHEYE can cause drug eruption, upper abdominal pain, anaphylactic shock, and severe patient can cause death and die.
The dosage form of Chinese medicine external is conventional dosage forms such as unguentum and powder mostly, Chinese medicine percutaneous dosing novel form famine.External Chinese medicine mostly is the medicine that Xin Xianghe walks to scurry, and as Radix Salviae Miltiorrhizae, Rhizoma Chuanxiong, Flos Carthami, Borneolum Syntheticum etc., the disease that relates to comprises and is affixed on acupoint therapy cough with asthma and pneumonia etc.
Summary of the invention
The object of the present invention is to provide andrographolide percutaneous dosing cataplasma and preparation method thereof.
Cataplasma (cataplasma) means medicine dissolution or is mixed in the water-soluble high-molecular material substrate, coats on the back lining materials exterior-applied formulation that supplies skin to stick.
The present invention will not possess Xin Xianghe and walk to scurry effect, and main effective ingredient andrographolide is made cataplasma in the antiinflammatory Chinese medicine Herba Andrographis, realizes percutaneous dosing, reaches the purpose of whole body therapeutic.Specifically take two measures, solve the key technology difficult problem in the andrographolide catablasm preparation.The one, andrographolide is insoluble in the problem of water.Adopt the pharmaceutical preparation new technique, development increases the novel form of andrographolide dissolubility, comprises clathrate and solid dispersion.Clathrate claims the branch ascus again, and the andrographolide molecule enters in the cavity structure of water soluble Beta-cyclodextrin, and the andrographolide water solublity is increased; Solid dispersion is that the andrographolide numberator height is dispersed in the water-solubility carrier material, and the andrographolide dissolubility is increased.Clathrate and solid dispersion have obviously increased the water solublity of slightly solubility andrographolide, and it is absorbed by the skin appendages approach rapidly, reach the purpose of rapid onset.The 2nd, the selection of catablasm base material.The development cataplasma, key is a substrate, the present invention has found the optimum substrate proportioning that is suitable for carrying andrographolide, add the transdermal absorption accelerator azone simultaneously, promote the andrographolide that mainly absorbs to enter in the body, make medicine keep the ideal treatment long lasting, that blood concentration fluctuation is less in vivo with the horny layer approach.
Andrographolide catablasm of the present invention; form by backing layer, drug depot and protective layer; wherein backing layer is a non-woven fabrics; protective layer is polyethylene film or polypropylene screen; the drug-reservoir layer is made up of hydrophilic matrix and medicine, and its component and proportioning are polyvinyl alcohol 0.1～0.5g, glycerol 1～3ml, propylene glycol 1～5ml, 40%PVP
K30 Aqueous solution 1～5ml, 50% aqueous gelatin solution, 2～6ml, sodium carboxymethyl cellulose 1～3.0g, sodium polyacrylate 0.4～-0.6g, azone 1～3ml, Ca (OH)
20.1～0.4g or Al (OH)
30.1～0.4g, medicine are 0.5～3g andrographolide.
The present invention prepares the method for andrographolide catablasm and carries out according to the following steps:
A. provide andrographolide 0.5～3g
B. prepare catablasm base material
A. get 0.1～0.5g PVA and add water, make dissolving at 80～100 ℃;
B. get 0.4～0.6g PANA and pour in 1～3ml glycerol, stir;
C. with a and b gained solution mixing, be cooled to 50 ℃ and add 50% aqueous gelatin solution, 2～6ml, propylene glycol 1～5ml, sodium carboxymethyl cellulose 1～3.0g and 40%PVP successively
K30 Aqueous solution 1～5ml, azone 1～3ml fully stir, and mix homogeneously gets substrate.
C. prepare cataplasma
Andrographolide 0.5～the 3.0g of steps A is joined in the substrate that 2 steps obtain, add Ca (OH)
20.1～0.4g or Al (OH)
30.1～0.4g crosslinking curing stirs, and is placed to room temperature, coats on the back lining materials, covers protective layer, and is dry below 50 ℃, cut out, pack.
The present invention makes clathrate or solid dispersion for increasing the andrographolide dissolubility with andrographolide.Therefore, cataplasma of the present invention, the medicine in the drug-reservoir can also be clathrate or the solid dispersion that contains 0.5～3g andrographolide.
The preparation method of above-mentioned cataplasma is carried out according to the following steps:
A. be equipped with andrographolide clathrate or solid dispersion by following either party's legal system
A. saturated water solution method-freeze-drying prepares the andrographolide clathrate
By medicine: beta-schardinger dextrin-is 1: 1～3 mol ratio, will contain the alcoholic solution of andrographolide 0.5～3g, slowly joins in 50～70 ℃ the beta-schardinger dextrin-saturated aqueous solution, stirs 3～5h, and rotating speed is 300～800r.min
-1, stopping to heat the back and continue to stir 5～8h, stored refrigerated is spent the night, and lyophilization again gets white clathrate powder, weighs, and preserves standby;
B. solvent method prepares andrographolide solid dispersion
Select polyvinylpyrrolidone (PVP for use
K30) be carrier material, by medicine: the mass ratio of carrier material is 1: 1～6 preparations.At first, add PVP again with medicine 0.5～3g dissolve with ethanol
K30Make dissolving, reclaim ethanol, lyophilization is preserved standby;
C. fusion method prepares andrographolide solid dispersion
Press medicine: the mass ratio of carrier material 1: 1～6 is heating and melting in 40～70 ℃ water-bath with Polyethylene Glycol (PEG6000, PEG4000) or poloxamer (Poloxamer188), the andrographolide fine powder 0.5～3g that added 120 mesh sieves while stirring, wave diffusing ethanol, lyophilization is preserved standby.
B. prepare catablasm base material
A. get 0.1～0.5g PVA and add water, make dissolving at 80～100 ℃;
B. get 0.4～0.6g PANA and pour in 1～3ml glycerol, stir;
C. with a and b gained solution mixing, be cooled to 50 ℃ and add 50% aqueous gelatin solution, 2～6ml, propylene glycol 1～5ml, sodium carboxymethyl cellulose 1～3.0g and 40%PVP successively
K30 Aqueous solution 1～5ml, azone 1～3ml fully stir, and mix homogeneously gets substrate.
C. prepare cataplasma
Clathrate that contains andrographolide 0.5～3.0g that steps A is obtained or solid dispersion join in the substrate that the B step obtains, and add Ca (OH)
20.1～0.4g or Al (OH)
30.1～0.4g crosslinking curing stirs, and is placed to room temperature, coats on the back lining materials, covers protective layer, and is dry below 50 ℃, cuts out packing.
The inside and outside percutaneous experimentation of animal body:
Externally select improved Franz diffusion cell for use, with the rat skin is model, remove fat deposit, horny layer upwards is clipped in the diffusion cell, medicine is attached to horny layer, the skin opposite side is close to reception liquid, and receiving liquid is 5% ethanol, 37 ℃ ± 0.5 ℃ of constant temperature, the electromagnetism constant speed stirs, mixing speed 100～200r.min.15min, 30min, 45min, 1h, 2h, 4h extract respectively and receive liquid 5ml at interval respectively, replenish 5% ethanol with 37 ℃ of the pre-temperature of volume simultaneously immediately.The acceptable solution that each time point takes out is measured andrographolide concentration with the HPLC method, calculates the accumulation transdermal penetration amount of each time point, curve when drawing medicine.
Selecting rabbit for use in the experiment of body percutaneous is object, remove the hair of rabbit back, cataplasma is attached to Wu Maochu, fixing, 15min, 30min, 45min, 1h, 2h, 4h extract ear vein blood at interval respectively, and blood sample is measured andrographolide concentration with the HPLC method after centrifugal, quantitative, dissolve with methanol etc. handled, calculate the blood drug level of each time point, curve when drawing medicine.
Fig. 1 is the x-ray diffraction curve, Fig. 2 infrared spectrogram.By these two kinds of results that method obtains, prove that fully the andrographolide clathrate forms, rather than the mixing of andrographolide and enclose rings of material dextrin machinery.Fig. 3 is the compatible line of writing music of separating, and curve shows that the Benexate Hydrochloride that andrographolide forms is A
LType, cyclodextrin and andrographolide form clathrate with 1: 1 mol ratio.Fig. 4 uses the transdermal tester, is the transdermal test in vitro experimentation that model carries out with the rat skin, and the result shows that the transdermal effect of clathrate is better than the not medicine of enclose, and penetrance improves.Fig. 5 is the clathrate and not enclose drug transdermal experiment that rabbit back carries out of being in, and the result shows the transdermal effect of clathrate significantly better than the andrographolide without cyclodextrin inclusion compound, and medicine transdermal ability obviously improves.Fig. 6 is an andrographolide in rabbit body inner injecting and administering and transdermal administration effect relatively, and the result shows that percutaneous dosing is littler than drug administration by injection blood concentration fluctuation, J curve effectJ when having reached ideal body giving drugs into nose.
Beneficial effect of the present invention: andrographolide catablasm, overcome the shortcoming of the oral and drug administration by injection of andrographolide, avoided toxic and side effects, owing to take the pharmaceutical preparation new technique, andrographolide is processed into cyclodextrin clathrate and solid dispersion, obviously increase the water solublity of andrographolide, it is absorbed by the skin appendages approach rapidly, reached the purpose of rapid onset.Add transdermal absorption accelerator, promote the andrographolide that mainly absorbs to enter in the body, make medicine keep the ideal treatment long lasting, that blood concentration fluctuation is less in vivo with the horny layer approach.After andrographolide catablasm was used, the substrate adjuvant all rests on to be mounted on the backing material, made to enter intravital non-ingredient and significantly reduce with oral comparing with injection, the assurance medication is safer, improve bioavailability, made patient's medication more convenient, be specially adapted to old man and children.The present invention has realized that percutaneous dosing reaches the purpose of whole body therapeutic, have than oral and better effectiveness of drug administration by injection and practicality, be for the Chinese medicine Herba Andrographis that does not have hot perfume (or spice) to walk to scurry, realized the once useful trial of Herba Andrographis inner disease outer treat, obtained satisfied effect.
Description of drawings:
Fig. 1: the x-ray diffraction pattern of cyclodextrin clathrate.4 curves are represented respectively among the figure: a. andrographolide clathrate; B. andrographolide; C. cyclodextrin; D. the physical mixture of andrographolide and cyclodextrin.
Fig. 2: the infared spectrum of cyclodextrin clathrate.4 curve representatives respectively from top to bottom among the figure: andrographolide; Cyclodextrin; The andrographolide clathrate; The physical mixture of andrographolide and cyclodextrin.
Fig. 3: the phase solubility figure of clathrate.Abscissa is the concentration of andrographolide in cyclodextrin, the andrographolide concentration of vertical coordinate for measuring.
Fig. 4: transdermal test in vitro experimental result.Abscissa be the time (minute), the andrographolide peak accumulative total transit dose of vertical coordinate for measuring.Square frame is represented clathrate, and round dot is represented the physical mixture of andrographolide and cyclodextrin, and triangle is represented andrographolide.
Fig. 5: rabbit back of the body transdermal experiment result.Abscissa be the time (minute), the andrographolide peak area of vertical coordinate for measuring.Square frame is represented andrographolide, and round dot is represented clathrate.
Fig. 6: rabbit body inner injecting and administering and transdermal administration effect are relatively.Abscissa is the time, and vertical coordinate is plasma drug level a: drug administration by injection b: the clathrate percutaneous dosing.
The specific embodiment
Embodiment 1: the preparation of andrographolide catablasm
A., andrographolide 2.0g is provided, and the andrographolide that the present invention uses is commercially available andrographolide.
B. prepare catablasm base material
A. get 0.1g PVA and add water, make dissolving at 80 ℃;
B. get 0.6g PANA and pour in the 3ml glycerol, stir;
C. with a and b gained solution mixing, be cooled to 50 ℃ and add 50% aqueous gelatin solution 2ml, propylene glycol 1ml, sodium carboxymethyl cellulose 1g and 40%PVP successively
K30Aqueous solution 5ml, azone 3ml fully stir, and mix homogeneously gets substrate.
C. cataplasma preparation
With the andrographolide 2.0g of A step, add in the catablasm base material, add Ca (OH)
20.1g crosslinking curing, the abundant stirring is placed to room temperature, coating, and epiphragma, dry below 50 ℃, to cut out, packing gets finished product.
Inside and outside percutaneous experimentation:
Selecting improved Franz diffusion cell for use, is model with the rat skin, removes fat deposit, and horny layer upwards, be clipped in the diffusion cell, medicine is attached to horny layer, the skin opposite side is close to reception liquid, and receiving liquid is 5% ethanol, 37 ℃ ± 0.5 ℃ of constant temperature, the electromagnetism constant speed stirs, mixing speed 100r/min.15min, 30min, 45min, 1h, 2h, 4h extract respectively and get reception liquid 5ml respectively at interval respectively, replenish 5% ethanol with 37 ℃ of the pre-temperature of volume simultaneously immediately.The acceptable solution that each time point takes out is measured andrographolide concentration with the HPLC method, calculates the accumulation transdermal penetration amount of each time point.
Selecting rabbit for use in the experiment of body percutaneous is object, remove the hair of rabbit back, cataplasma is attached to Wu Maochu, fixing, 15min, 30min, 45min, 1h, 2h, 4h extract ear vein blood at interval respectively, and blood sample is measured andrographolide concentration with the HPLC method after centrifugal, quantitative, dissolve with methanol etc. handled, calculate the blood drug level of each time point, curve when drawing medicine.
Embodiment 2: the preparation of andrographolide catablasm
A., andrographolide 0.5g is provided.
B. prepare catablasm base material
A. get 0.2g PVA and add water, make dissolving at 80 ℃;
B. get 0.4g PANA and pour in the 2ml glycerol, stir;
C. with a and b gained solution mixing, be cooled to 50 ℃ and add 50% aqueous gelatin solution 2ml, propylene glycol 1ml, sodium carboxymethyl cellulose 1g and 40%PVP successively
K30Aqueous solution 3ml, azone 1ml fully stir, and mix homogeneously gets substrate.
C. cataplasma preparation
With the andrographolide 2.0g of A step, add in the catablasm base material, add Al (OH)
30.1g crosslinking curing, the abundant stirring is placed to room temperature, coating, and epiphragma, dry below 50 ℃, to cut out, packing gets finished product.
Inside and outside percutaneous experimentation is with embodiment 1.
Embodiment 3: the preparation of andrographolide clathrate cataplasma
A. saturated aqueous solution-freeze-drying prepares the andrographolide clathrate
In the distilled water of 80 ℃ of 100ml, add beta-schardinger dextrin-8.0g, stirring make dissolve the beta-schardinger dextrin-saturated aqueous solution, be cooled to 50 ℃, will contain the alcoholic solution of 3.0g andrographolide, slowly join in the saturated aqueous solution of beta-schardinger dextrin-, simultaneously at 500r.min
-1Condition under stirred 300 minutes, stop heating, continue to stir 8h, stored refrigerated is spent the night, lyophilization, white clathrate powder, standby.Through x-ray and infrared analysis, prove that clathrate forms.
B. prepare catablasm base material
A. get 0.5g PVA and add water, make dissolving at 100 ℃;
B. get 0.6g PANA and pour in the 3ml glycerol, stir;
C. with a and b gained solution mixing, be cooled to 50 ℃ and add 50% aqueous gelatin solution 6ml, propylene glycol 3ml, sodium carboxymethyl cellulose 3.0g and 40%PVP successively
K30Aqueous solution 3ml, azone 1ml fully stir, and mix homogeneously gets substrate.
C. cataplasma preparation
With the clathrate that contains the 3.0g andrographolide of steps A preparation, add in the catablasm base material Al (OH)
30.2g crosslinking curing fully stirs, and is placed to room temperature, coating, and epiphragma, dry below 50 ℃, to cut out, packing gets finished product.
Inside and outside percutaneous experimentation is with embodiment 1.
Embodiment 4: the preparation of andrographolide solid dispersion cataplasma
A. fusion method prepares the solid dispersion body method
Taking polyethylene glycol (PEG6000 or PEG4000) or poloxamer (Poloxamer188) 9.0g, heating and melting in 50 ℃ water-bath adds andrographolide 1.5g while stirring, and makes the medicine dispersing and dissolving, and drying is standby.
B. prepare catablasm base material
A. get 0.5g PVA and add water, make dissolving at 90 ℃;
B. get 0.5g PANA and pour in the 3ml glycerol, stir;
C. with a and b gained solution mixing, be cooled to 50 ℃ and add 50% aqueous gelatin solution 4ml, propylene glycol 1ml, sodium carboxymethyl cellulose 2.0g and 40%PVP successively
K30Aqueous solution 1ml, azone 3ml fully stir, and mix homogeneously gets substrate.
C. cataplasma preparation
The solid dispersion that contains andrographolide 1.5g that steps A is obtained joins in the substrate, adds Ca (OH)
20.3g crosslinking curing stirs, and is placed to room temperature, coats on the back lining materials, covers protective layer, and is dry below 50 ℃, cuts out packing.
Inside and outside percutaneous experimentation is with embodiment 1.
Embodiment 5: the preparation of andrographolide solid dispersion cataplasma
A. solvent method prepares the solid dispersion body method
Select polyvinylpyrrolidone (PVP for use
K30) be carrier material, get andrographolide 1.0g, use dissolve with ethanol, add 9.0gPVP
K30Make dissolving, reclaim ethanol, drying, standby.
B. prepare catablasm base material
A. get 0.3g PVA and add water, about 100 ℃, make dissolving;
B. get 0.4g PANA and pour in the 2ml glycerol, stir;
C. with a and b gained solution mixing, be cooled to 50 ℃ and add 50% aqueous gelatin solution 4ml, 1ml propylene glycol, sodium carboxymethyl cellulose 3.0g and 40%PVP successively
K30Aqueous solution 2ml, azone 2ml fully stir, and mix homogeneously gets substrate.
C. cataplasma preparation: the solid dispersion that contains andrographolide 1.0g that steps A is obtained joins in the substrate, adds Al (OH)
30.4g crosslinking curing stirs, and is placed to room temperature, coats and mounts on the backing material, covers protective layer, and is dry below 50 ℃, cuts out packing.
Inside and outside percutaneous experimentation is with embodiment 1.
Claims (4)
1. andrographolide catablasm; form by backing layer, drug-reservoir and protective layer; it is characterized in that the drug-reservoir layer is made up of hydrophilic matrix and medicine, its component and proportioning are polyvinyl alcohol 0.1～0.5g, glycerol 1～3ml, propylene glycol 1～5ml, 40%PVP
K30Aqueous solution 1～5ml, 50% aqueous gelatin solution, 2～6ml, sodium carboxymethyl cellulose 1～3.0g, sodium polyacrylate 0.4～-0.6g, azone 1～3ml, Ca (OH)
20.1～0.4g or Al (OH)
30.1～0.4g, medicine 0.5～3g andrographolide.
2. andrographolide catablasm according to claim 1 is characterized in that the medicine in the drug-reservoir is clathrate or the solid dispersion that contains 0.5～3g andrographolide.
3. the preparation method of the described andrographolide catablasm of claim 1 is characterized in that carrying out according to the following steps:
A. provide andrographolide 0.5～3g
B. prepare catablasm base material
A. get 0.1～0.5g polyvinyl alcohol and add water, make dissolving at 80～100 ℃;
B. get 0.4～0.6g sodium polyacrylate and pour in 1～3ml glycerol, stir;
C. with a and b gained solution mixing, be cooled to 50 ℃ and add 50% aqueous gelatin solution, 2～6ml, propylene glycol 1～5ml, sodium carboxymethyl cellulose 1～3.0g and 40%PVP aqueous solution 1～5ml, azone 1～3ml successively, fully stir, mix homogeneously gets substrate;
C. prepare cataplasma
Andrographolide 0.5～the 3.0g of steps A is joined in the substrate that the B step obtains, add Ca (OH)
20.1～0.4g or Al (0H)
30.1～0.4g crosslinking curing stirs, and is dry below 50 ℃, coats on the back lining materials, covers protective layer, cuts out packing.
4. the preparation method of the described andrographolide catablasm of claim 2 is characterized in that carrying out according to the following steps:
A. be equipped with andrographolide clathrate or solid dispersion by following either party's legal system
A. saturated water solution method-freeze-drying prepares the andrographolide clathrate: by medicine: beta-schardinger dextrin-is 1: 1～3 mol ratio, the alcoholic solution that will contain andrographolide 0.5～3g, slowly join in 50～70 ℃ the beta-schardinger dextrin-saturated aqueous solution, stir 3～5h, rotating speed is 300～800r.min
-1, stopping to heat the back and continue to stir 5～8h, stored refrigerated is spent the night, and lyophilization again gets white clathrate powder, weighs, and preserves standby;
B. solvent method prepares andrographolide solid dispersion: select PVP for use
K30Be carrier material, by medicine: the mass ratio of carrier material is 1: 1～6 preparations.At first, add PVP with medicine 0.5～3g dissolve with ethanol
K30Make dissolving, reclaim ethanol, lyophilization, standby;
C. fusion method prepares andrographolide solid dispersion: press medicine: the mass ratio of carrier material 1: 1～6 is with polyethylene glycol 6000 or Macrogol 4000 or poloxamer 188 heating and melting in 40～70 ℃ water-bath, the andrographolide fine powder 0.5～3g that added 120 mesh sieves while stirring, messenger drug object height degree dispersing and dissolving is in carrier material, wave diffusing ethanol, lyophilization, standby;
B. prepare catablasm base material
A. get 0.1～0.5g polyvinyl alcohol and add water, make dissolving at 80～100 ℃;
B. get 0.4～0.6g sodium polyacrylate and pour in 1～3ml glycerol, stir;
C. with a and b gained solution mixing, be cooled to 50 ℃ and add 50% aqueous gelatin solution, 2～6ml, propylene glycol 1～5ml, sodium carboxymethyl cellulose 1～3.0g and 40%PVP aqueous solution 1～5ml, azone 1～3ml successively, fully stir, mix homogeneously gets substrate;
C. prepare cataplasma
Clathrate that contains 0.5～3.0g andrographolide that steps A is obtained or solid dispersion join in the substrate that the B step obtains, and add Ca (OH)
20.1～0.4g or Al (OH)
30.1～0.4g crosslinking curing stirs, and is placed to room temperature, coats on the back lining materials, covers protective layer, and is dry below 50 ℃, cuts out packing.
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| CN103655479B (en) * | 2013-12-12 | 2015-12-09 | 成都乾坤动物药业有限公司 | A kind of andrographolide composition wettability solid dispersal powder and preparation method thereof |
| CN115068467A (en) * | 2021-03-15 | 2022-09-20 | 中国医学科学院药物研究所 | Medical application of andrographolide as LTB4 receptor inhibitor |
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