CN1562001A - Carbazochrome sodium sulfoate dripping pill and its preparing method - Google Patents
Carbazochrome sodium sulfoate dripping pill and its preparing method Download PDFInfo
- Publication number
- CN1562001A CN1562001A CN 200410030367 CN200410030367A CN1562001A CN 1562001 A CN1562001 A CN 1562001A CN 200410030367 CN200410030367 CN 200410030367 CN 200410030367 A CN200410030367 A CN 200410030367A CN 1562001 A CN1562001 A CN 1562001A
- Authority
- CN
- China
- Prior art keywords
- sodium sulfonate
- carbazochrome sodium
- carbazochrome
- coolant
- sulfonate
- 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.)
- Pending
Links
- 239000006187 pill Substances 0.000 title claims abstract description 17
- 229960002631 carbazochrome Drugs 0.000 title claims 2
- XSXCZNVKFKNLPR-SDQBBNPISA-N carbazochrome Chemical compound NC(=O)N/N=C/1C(=O)C=C2N(C)CC(O)C2=C\1 XSXCZNVKFKNLPR-SDQBBNPISA-N 0.000 title claims 2
- 238000000034 method Methods 0.000 title description 12
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 title 1
- 229960004353 carbazochrome sodium sulfonate Drugs 0.000 claims abstract description 30
- HLFCZZKCHVSOAP-WXIWBVQFSA-M sodium;(5e)-5-(carbamoylhydrazinylidene)-1-methyl-6-oxo-2,3-dihydroindole-2-sulfonate Chemical compound [Na+].NC(=O)N\N=C/1C(=O)C=C2N(C)C(S([O-])(=O)=O)CC2=C\1 HLFCZZKCHVSOAP-WXIWBVQFSA-M 0.000 claims abstract description 30
- 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
- 238000002360 preparation method Methods 0.000 claims description 12
- 238000001035 drying Methods 0.000 claims description 8
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 8
- 239000000843 powder Substances 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
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 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
- PAYGMRRPBHYIMA-UHFFFAOYSA-N sodium;trihydrate Chemical compound O.O.O.[Na] PAYGMRRPBHYIMA-UHFFFAOYSA-N 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
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims 1
- 238000010298 pulverizing process Methods 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 description 20
- 238000001514 detection method Methods 0.000 description 6
- 239000008280 blood Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 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
- 238000005516 engineering process Methods 0.000 description 3
- 208000019505 Deglutition disease Diseases 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 238000004891 communication Methods 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
- 230000001225 therapeutic effect Effects 0.000 description 2
- 208000032843 Hemorrhage Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
A dripping pill of carbazochrome sodium sulfonate is prepared through superfine pulverizing and conventional steps for preparing dripping pills.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically carbazochrome sodium sulfonate drop pill and preparation method thereof.
Background technology
Carbazochrome sodium sulfonate can increase the resistance of blood capillary to damage, reduces the permeability of blood capillary, promotes the retraction of blood capillary fracture end and stops blooding.
Behind the oral carbazochrome sodium sulfonate 150mg of the man of health adult, in 0.5～1 hour blood Cmax greater than 25mg/ml, half-life (t
1/2) be 1.5 hours, it is the highest that oral back reached urine Chinese medicine concentration in 0.5～1 hour, and drainage in about 24 hours finishes.Clinical in hemorrhage.
The carbazochrome sodium sulfonate odorless, easily molten in hot water, molten in the water part omitted, its disintegration of tablet time is long, and dissolution and dissolution rate are low, absorption difference, bioavailability is low, and the supplementary product consumption ratio is big, and child, old people, bed patient and dysphagia patients are taken inconvenience, compliance is poor, has influenced the performance of carbazochrome sodium sulfonate therapeutical effect.
The present invention makes the carbazochrome sodium sulfonate drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of carbazochrome sodium sulfonate sheet, and the therapeutical effect of carbazochrome sodium sulfonate is given full play to.
Summary of the invention
The carbazochrome sodium sulfonate 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 carbazochrome sodium sulfonate 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 carbazochrome sodium sulfonate among the present invention (Carbazochrome Sodium Sulfonate) is 1-methyl-6-oxo-2,3,5,6-tetrahydro indole-5-semicarbazone-2-sulfonate sodium trihydrate, and structural formula is
Molecular formula is C
10H
11N
4NaO
5S3H
2O, molecular weight are 367.32.
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: sample thief, according to dissolution method (two appendix XC first methods of Chinese Pharmacopoeia version in 2000), 600ml is a solvent with phosphate buffer (pH7.0), and rotating speed is per 100 commentaries on classics, operation in accordance with the law, in the time of 10,20,30,40 minutes, get solution 10ml, filter, get filtrate, according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 A), measure absorption receipts degree at the wavelength place of 363nm, press C
10H
11N
4NaO
5Absorptance (the E of S
1cm 1%) be 862 calculating dissolution rates.
Two, commercially available carbazochrome sodium sulfonate sheet testing result
1. disintegration time: 62 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 23.6 35.4 53.5 74.5
Three, example 1 sample detection result
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 49.6 81.3 94.5 98.2
Four, example 2 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 43.4 84.5 92.3 97.6
Five, example 3 sample detection results
1. the molten diffusing time: 4 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 47.4 84.5 90.3 96.2
Six, example 4 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 41.4 82.3 90.6 99.1
Seven, example 5 sample detection results
1. the molten diffusing time: 8 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 38.5 84.4 93.1 97.2
Eight, example 6 sample detection results
1. the molten diffusing time: 12 minutes
2. dissolution rate
Time (minute) 10 20 30 40
Dissolution (%) 41.4 82.3 91.5 96.7
The specific embodiment
One, example 1
Prescription:
Carbazochrome sodium sulfonate 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the carbazochrome sodium sulfonate 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:
Carbazochrome sodium sulfonate 5g
Macrogol 4000 15g
Make 1000
Method for making: the carbazochrome sodium sulfonate 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:
Carbazochrome sodium sulfonate 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the carbazochrome sodium sulfonate 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:
Carbazochrome sodium sulfonate 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the carbazochrome sodium sulfonate 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:
Carbazochrome sodium sulfonate 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the carbazochrome sodium sulfonate 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:
Carbazochrome sodium sulfonate 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that carbazochrome sodium sulfonate 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. carbazochrome sodium sulfonate drop pill and preparation method thereof is characterized in that: the carbazochrome sodium sulfonate 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 carbazochrome sodium sulfonate Carbazochrome of claim 1 Sodium Sulfonate is 1-methyl-6-oxo-2,3,5,6-tetrahydro indole-5-semicarbazone-2-sulfonate sodium trihydrate, and structural formula is
Molecular formula is C
10H
11N
4NaO
5S3H
2O, molecular weight are 367.32.
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 |
|---|---|---|---|
| CN 200410030367 CN1562001A (en) | 2004-03-29 | 2004-03-29 | Carbazochrome sodium sulfoate dripping pill and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410030367 CN1562001A (en) | 2004-03-29 | 2004-03-29 | Carbazochrome sodium sulfoate dripping pill and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1562001A true CN1562001A (en) | 2005-01-12 |
Family
ID=34481094
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410030367 Pending CN1562001A (en) | 2004-03-29 | 2004-03-29 | Carbazochrome sodium sulfoate dripping pill and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1562001A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104127388A (en) * | 2014-02-21 | 2014-11-05 | 杭州长典医药科技有限公司 | Special ultrafine carbazochrome sodium sulfonate powder freeze-dried preparation and preparation method thereof |
| CN104473864A (en) * | 2014-11-25 | 2015-04-01 | 陈长潭 | Carbazochrome sodium sulfonate semisolid preparation and preparation method thereof |
-
2004
- 2004-03-29 CN CN 200410030367 patent/CN1562001A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104127388A (en) * | 2014-02-21 | 2014-11-05 | 杭州长典医药科技有限公司 | Special ultrafine carbazochrome sodium sulfonate powder freeze-dried preparation and preparation method thereof |
| CN104473864A (en) * | 2014-11-25 | 2015-04-01 | 陈长潭 | Carbazochrome sodium sulfonate semisolid preparation and preparation method thereof |
| CN104473864B (en) * | 2014-11-25 | 2017-02-22 | 陈长潭 | Carbazochrome sodium sulfonate semisolid preparation and preparation method thereof |
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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 |