CN1493274A - Vanillic aldehyde drip pill and its preparation method - Google Patents
Vanillic aldehyde drip pill and its preparation method Download PDFInfo
- Publication number
- CN1493274A CN1493274A CNA031592007A CN03159200A CN1493274A CN 1493274 A CN1493274 A CN 1493274A CN A031592007 A CNA031592007 A CN A031592007A CN 03159200 A CN03159200 A CN 03159200A CN 1493274 A CN1493274 A CN 1493274A
- Authority
- CN
- China
- Prior art keywords
- vanillin
- preparation
- coolant
- polyethylene glycol
- pill
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 title claims abstract description 35
- 239000006187 pill Substances 0.000 title claims abstract description 16
- 238000002360 preparation method Methods 0.000 title claims description 13
- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 claims description 33
- 235000012141 vanillin Nutrition 0.000 claims description 33
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 12
- 239000002826 coolant Substances 0.000 claims description 12
- 238000001035 drying Methods 0.000 claims description 9
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 8
- 239000000843 powder Substances 0.000 claims description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 8
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 6
- 229940008099 dimethicone Drugs 0.000 claims description 6
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims description 6
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 6
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 claims description 6
- 229960000502 poloxamer Drugs 0.000 claims description 6
- 229920001983 poloxamer Polymers 0.000 claims description 6
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 6
- 239000000758 substrate Substances 0.000 claims description 6
- 238000002156 mixing Methods 0.000 claims description 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 4
- 239000011159 matrix material Substances 0.000 claims description 4
- IQXJCCZJOIKIAD-UHFFFAOYSA-N 1-(2-methoxyethoxy)hexadecane Chemical compound CCCCCCCCCCCCCCCCOCCOC IQXJCCZJOIKIAD-UHFFFAOYSA-N 0.000 claims description 2
- 239000001828 Gelatine Substances 0.000 claims description 2
- 241000238631 Hexapoda Species 0.000 claims description 2
- 235000021355 Stearic acid Nutrition 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 230000001476 alcoholic effect Effects 0.000 claims description 2
- 229950009789 cetomacrogol 1000 Drugs 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 claims description 2
- 235000011187 glycerol Nutrition 0.000 claims description 2
- 229960005150 glycerol Drugs 0.000 claims description 2
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 claims description 2
- 229940057995 liquid paraffin Drugs 0.000 claims description 2
- -1 liquid paraffin Substances 0.000 claims description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 2
- 229940093430 polyethylene glycol 1500 Drugs 0.000 claims description 2
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims description 2
- 229940080350 sodium stearate Drugs 0.000 claims description 2
- 239000008117 stearic acid Substances 0.000 claims description 2
- 239000000126 substance Substances 0.000 claims description 2
- 235000015112 vegetable and seed oil Nutrition 0.000 claims description 2
- 239000008158 vegetable oil Substances 0.000 claims description 2
- 239000001993 wax Substances 0.000 claims description 2
- 238000000034 method Methods 0.000 abstract description 13
- 230000000694 effects Effects 0.000 abstract description 2
- 238000004090 dissolution Methods 0.000 description 19
- 238000001514 detection method Methods 0.000 description 6
- 239000000243 solution Substances 0.000 description 5
- 229940075507 glyceryl monostearate Drugs 0.000 description 4
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- 241000699670 Mus sp. Species 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- 206010010904 Convulsion Diseases 0.000 description 2
- 208000019505 Deglutition disease Diseases 0.000 description 2
- CWRVKFFCRWGWCS-UHFFFAOYSA-N Pentrazole Chemical compound C1CCCCC2=NN=NN21 CWRVKFFCRWGWCS-UHFFFAOYSA-N 0.000 description 2
- 238000004891 communication Methods 0.000 description 2
- 230000036461 convulsion Effects 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- DLYUQMMRRRQYAE-UHFFFAOYSA-N tetraphosphorus decaoxide Chemical compound O1P(O2)(=O)OP3(=O)OP1(=O)OP2(=O)O3 DLYUQMMRRRQYAE-UHFFFAOYSA-N 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 206010034759 Petit mal epilepsy Diseases 0.000 description 1
- 102000007562 Serum Albumin Human genes 0.000 description 1
- 108010071390 Serum Albumin Proteins 0.000 description 1
- 208000003554 absence epilepsy Diseases 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000008485 antagonism Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 239000002274 desiccant Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 206010015037 epilepsy Diseases 0.000 description 1
- 230000001037 epileptic effect Effects 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 230000000147 hypnotic effect Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000031891 intestinal absorption Effects 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000013558 reference substance Substances 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- SQMCFUSVGSBKFK-UHFFFAOYSA-M sodium;5-(cyclohexen-1-yl)-1,5-dimethylpyrimidin-3-ide-2,4,6-trione Chemical compound [Na+].O=C1N(C)C(=O)[N-]C(=O)C1(C)C1=CCCCC1 SQMCFUSVGSBKFK-UHFFFAOYSA-M 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000008925 spontaneous activity Effects 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A dripping pill of vanillic aldehyde and its preparing process are disclosed. Its advantages are high dissolving and disintegrating speed, high stripping percentage, quickly taking its curative effect, and low cost.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically vanillin drop pill and preparation method thereof.
Background technology
Animal experiment confirms that vanillin can significantly reduce the white mice spontaneous activity, and prolongs the hypnosis time of hexobarbitone sodium, can resist the convulsions that the white mice pentetrazole causes, but does not have the convulsions effect that antagonism mice galvanic shock causes; Can resist the epileptic electroencephalogram (eeg) ripple that the rabbit pentetrazole brings out.
Vanillin is mainly through intestinal absorption, and absorbance is more than 98%, and serum albumin combination rate 71% ± 1% is easily by blood brain barrier, mainly through renal excretion.The clinical petit mal epilepsy that is used for, and the adjuvant drug of various epilepsy.List marketing at present the vanillin sheet only arranged.
Vanillin (Vanillin) has fragrance, to photo-labile, slightly soluble in water, vanillin sheet disintegration time is long, and dissolution and dissolution rate are low, absorption difference, bioavailability is low, and supplementary product consumption is big, and child, old people, bed patient and dysphagia patients are taken inconvenience, compliance is poor, has influenced the performance of vanillin therapeutical effect.
The present invention makes the vanillin drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of vanillin sheet, and the therapeutical effect of vanillin is given full play to.
Summary of the invention
The vanillin drop pill of making by using ultramicro communication technique and dropping pill formulation Technology not only have disintegrate molten loose fast, dissolution and dissolution rate improve, steady quality, the pill volume is little, both can swallow also can buccal, easy to carry and use, onset is rapid, compliance is good, be particularly suitable for the characteristics that child, old people, bed patient and dysphagia patients are taken, but also have working condition and production equipment is simple, production cost is low, compare the advantage that supplementary product consumption reduces with tablet, demonstrated fully the new drug research exploitation spirit that people-oriented.
For achieving the above object, the present invention by the following technical solutions: the vanillin fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
The chemical name of vanillin is 4-hydroxyl-3-methoxyl group-benzaldehyde among the present invention, and molecular formula is C
8H
8O
3, molecular weight is 152.15, structural formula is:
Substrate among the present invention includes but not limited to polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.
Coolant among the present invention includes but not limited to dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution etc.
Below through detecting to beneficial effect of the present invention as directed
One, detects index and method
1. disintegrate (molten loosing) time limit: check according to inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2000).
2. dissolution rate: lucifuge operation.Sample thief, according to dissolution method (two XC second methods of Chinese Pharmacopoeia version in 2000), with water 200ml is solvent, and rotating speed is that per minute 50 changes, operation in accordance with the law, in the time of 5,10,20,30 and 45 minutes, get solution and filter, it is an amount of that precision is measured subsequent filtrate, adds water and quantitatively be diluted to the solution that contains vanillin 8 μ g among every 1ml, according to spectrophotography (two IVA of Chinese Pharmacopoeia version in 2000), measure trap at the wavelength place of 280nm; In addition to take by weighing with the phosphorus pentoxide be desiccant to precision, and 3 hours vanillin reference substance of drying under reduced pressure is an amount of, be dissolved in water and quantitatively dilution make the solution that contains 8 μ g among every 1ml, measure trap with method, calculate stripping quantity.
Two, commercially available vanillin sheet testing result
1. disintegration time: 50 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 25.3 36.7 55.5 72.6 84.6
Three, example 1 sample detection result
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 45.4 67.8 92.5 99.6 98.7
Four, example 2 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 40.3 58.9 88.6 97.4 99.5
Five, example 3 sample detection results
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 50.3 75.2 93.6 99.7 101.2
Six, example 4 sample detection results
1. the molten diffusing time: 9 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 45.7 68.9 89.3 95.6 99.7
Seven, example 5 sample detection results
1. the molten diffusing time: 12 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 38.5 52.3 81.9 92.3 98.4
Eight, example 6 sample detection results
1. the molten diffusing time: 17 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 40.3 51.2 63.9 88.6 98.7
The specific embodiment
One, example 1
Prescription:
Vanillin 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the vanillin fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused polyethylene glycol 6000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Two, example 2
Prescription:
Vanillin 5g
Macrogol 4000 15g
Make 1000
Method for making: the vanillin fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused Macrogol 4000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Three, example 3
Prescription:
Vanillin 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the vanillin fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused Macrogol 4000 and the polyethylene glycol 6000 mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Four, example 4
Prescription:
Vanillin 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the vanillin fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused glyceryl monostearate substrate, and mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.
Five, example 5
Prescription:
Vanillin 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the vanillin fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused polyethylene glycol 6000 and the poloxamer mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Six, example 6
Prescription:
Vanillin 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that vanillin and poloxamer cross 200 mesh sieves through micronizing and be added in the fused glyceryl monostearate substrate, mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.
Claims (4)
1. vanillin drop pill and preparation method thereof is characterized in that: the vanillin fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, and abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
2. the chemical name of the described vanillin of claim 1 is 4-hydroxyl-3-methoxyl group-benzaldehyde, and molecular formula is C
8H
8O
3, molecular weight is 152.15, structural formula is:
3. the described substrate of claim 1 includes but not limited to polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.
4. the described coolant of claim 1 includes but not limited to dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution etc.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031592007A CN1493274A (en) | 2003-09-10 | 2003-09-10 | Vanillic aldehyde drip pill and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031592007A CN1493274A (en) | 2003-09-10 | 2003-09-10 | Vanillic aldehyde drip pill and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1493274A true CN1493274A (en) | 2004-05-05 |
Family
ID=34240936
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031592007A Pending CN1493274A (en) | 2003-09-10 | 2003-09-10 | Vanillic aldehyde drip pill and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1493274A (en) |
-
2003
- 2003-09-10 CN CNA031592007A patent/CN1493274A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |