CN1562027A - Trimetazidine hydrochloride dripping pill and its preparing method - Google Patents
Trimetazidine hydrochloride dripping pill and its preparing method Download PDFInfo
- Publication number
- CN1562027A CN1562027A CN 200410030370 CN200410030370A CN1562027A CN 1562027 A CN1562027 A CN 1562027A CN 200410030370 CN200410030370 CN 200410030370 CN 200410030370 A CN200410030370 A CN 200410030370A CN 1562027 A CN1562027 A CN 1562027A
- Authority
- CN
- China
- Prior art keywords
- trimetazidine hydrochloride
- trimetazidine
- coolant
- hydrochloride
- polyethylene glycol
- 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
- UHWVSEOVJBQKBE-UHFFFAOYSA-N Trimetazidine Chemical compound COC1=C(OC)C(OC)=CC=C1CN1CCNCC1 UHWVSEOVJBQKBE-UHFFFAOYSA-N 0.000 title claims abstract description 32
- 229960001177 trimetazidine Drugs 0.000 title claims abstract description 32
- 239000006187 pill Substances 0.000 title claims abstract description 17
- 238000000034 method Methods 0.000 title description 12
- 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
- 239000000758 substrate Substances 0.000 claims description 7
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 6
- 229940008099 dimethicone Drugs 0.000 claims description 6
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 6
- 235000013870 dimethyl polysiloxane Nutrition 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
- 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
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 4
- 239000011159 matrix material Substances 0.000 claims description 3
- 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
- CVVIJWRCGSYCMB-UHFFFAOYSA-N hydron;piperazine;dichloride Chemical compound Cl.Cl.C1CNCCN1 CVVIJWRCGSYCMB-UHFFFAOYSA-N 0.000 claims description 2
- -1 liquid paraffin Substances 0.000 claims description 2
- 229940057995 liquid paraffin Drugs 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
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 238000010298 pulverizing process Methods 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 description 19
- 238000001514 detection method Methods 0.000 description 6
- 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
- 230000017531 blood circulation Effects 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- 210000004165 myocardium Anatomy 0.000 description 3
- 208000019505 Deglutition disease Diseases 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 238000004891 communication Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 230000000302 ischemic effect Effects 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
- 206010002383 Angina Pectoris Diseases 0.000 description 1
- 206010002660 Anoxia Diseases 0.000 description 1
- 241000976983 Anoxia Species 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- 206010061216 Infarction Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000007953 anoxia Effects 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000004087 circulation Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 230000007849 functional defect Effects 0.000 description 1
- 230000007574 infarction Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 210000002464 muscle smooth vascular Anatomy 0.000 description 1
- 230000002107 myocardial effect Effects 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 230000036284 oxygen consumption Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
A dripping pill of trimetazidine hydrochloride is prepared through superfine pulverizing and conventional steps for preparing dripping pill.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically Trimetazidine Hydrochloride drop pill and preparation method thereof.
Background technology
Trimetazidine Hydrochloride can directly act on vascular smooth muscle, reduces vascular resistance, and blood flow around coronary blood flow increasing reaches can alleviate the heart working amount, thereby reduces myocardial oxygen consumption, to guarantee the supply of myocardium oxygen under the anoxia condition.Can also promote the ischemic myocardium side to prop up circulation and form, quicken the ischemic myocardium restoration of blood flow, alleviate the extent of damage of infarction.
The Trimetazidine Hydrochloride onset is slower, and action time is comparatively lasting.Clinical acute and chronic arteria coronaria functional defect, angina pectoris, the old myocardial infarction of being used for.
The Trimetazidine Hydrochloride Tablets in healthy disintegration 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 Trimetazidine Hydrochloride therapeutical effect.
The present invention makes the Trimetazidine Hydrochloride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of Trimetazidine Hydrochloride Tablets in healthy, and the therapeutical effect of Trimetazidine Hydrochloride is given full play to.
Summary of the invention
The Trimetazidine Hydrochloride 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 Trimetazidine Hydrochloride fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, fully mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
The chemical name of Trimetazidine Hydrochloride among the present invention (Trimetazidine Hydrochloride) is 1-(2,3, a 4-trimethoxy benzyl) piperazine dihydrochloride, and molecular formula is C
14H
22N
2O
32HCl, molecular weight are 339.26.
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), with 0.05mol/L sulfuric acid solution 600ml is solvent, and rotating speed is that per minute 100 changes, 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), wavelength place at 232nm measures trap, presses C
14H
22N
2O
3Absorptance (the E of 2HCL
1cm 1%) be 286 calculating stripping quantities.
Two, commercially available Trimetazidine Hydrochloride Tablets in healthy testing result
1. disintegration time: 56 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 21.6 37.5 48.3 59.4
Three, example 1 sample detection result
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 46.7 75.3 96.5 99.0
Four, example 2 sample detection results
1. the molten diffusing time: 2 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 41.4 82.6 93.5 98.7
Five, example 3 sample detection results
1. the molten diffusing time: 4 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 39.6 78.3 95.3 96.7
Six, example 4 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 41.5 72.3 89.4 97.2
Seven, example 5 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 36.7 84.5 92.3 99.1
Eight, example 6 sample detection results
1. the molten diffusing time: 8 minutes
2. dissolution rate
Time (minute) 10 20 30 40
Dissolution (%) 46.7 83.5 96.6 99.8
The specific embodiment
One, example 1
Prescription:
Trimetazidine Hydrochloride 3g
Polyethylene glycol 6000 17g
Make 1000
Method for making: the Trimetazidine Hydrochloride 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:
Trimetazidine Hydrochloride 3g
Macrogol 4000 17g
Make 1000
Method for making: the Trimetazidine Hydrochloride 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:
Trimetazidine Hydrochloride 3g
Polyethylene glycol 6000 5g
Macrogol 4000 12g
Make 1000
Method for making: the Trimetazidine Hydrochloride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added to fused Macrogol 4000 and the polyethylene glycol 6000 elder brother closes in the substrate, stirs evenly, and be coolant with the dimethicone, the dropping preparation method pill, drying, promptly.
Four, example 4
Prescription:
Trimetazidine Hydrochloride 3g
Glyceryl monostearate 17g
Make 1000
Method for making: the Trimetazidine Hydrochloride 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:
Trimetazidine Hydrochloride 3g
Polyethylene glycol 6000 12g
Poloxamer 5g
Make 1000
Method for making: the Trimetazidine Hydrochloride 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:
Trimetazidine Hydrochloride 3g
Glyceryl monostearate 15g
Poloxamer 2g
Make 1000
Method for making: get the mixing fine powders that Trimetazidine Hydrochloride 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. Trimetazidine Hydrochloride drop pill and preparation method thereof is characterized in that: the Trimetazidine Hydrochloride fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, fully mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
2. the chemical name of the described Trimetazidine Hydrochloride Trimetazidine of claim 1 Hydrochloride is 1-(2,3, a 4-trimethoxy benzyl) piperazine dihydrochloride, and molecular formula is C
14H
22N
2O
32HCl, molecular weight are 339.26.
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 200410030370 CN1562027A (en) | 2004-03-29 | 2004-03-29 | Trimetazidine hydrochloride dripping pill and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410030370 CN1562027A (en) | 2004-03-29 | 2004-03-29 | Trimetazidine hydrochloride dripping pill and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1562027A true CN1562027A (en) | 2005-01-12 |
Family
ID=34481097
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410030370 Pending CN1562027A (en) | 2004-03-29 | 2004-03-29 | Trimetazidine hydrochloride dripping pill and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1562027A (en) |
-
2004
- 2004-03-29 CN CN 200410030370 patent/CN1562027A/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1562027A (en) | Trimetazidine hydrochloride dripping pill and its preparing method | |
| CN1493298A (en) | Ginseng stem leaf total saponin drip pill and its preparation method | |
| CN1528281A (en) | Rhododeudron molle toxin drop pill and preparing method thereof | |
| CN1528287A (en) | Herba lysionoti extract drop pill and preparing method thereof | |
| CN1562001A (en) | Carbazochrome sodium sulfoate dripping pill and its preparing method | |
| CN1546022A (en) | Dripping pills of luteanine hydrochloride and its preparation | |
| CN1528294A (en) | Indolol drop pill and preparing method thereof | |
| CN1582943A (en) | Clomipramine hydrochloride drops and their preparation | |
| CN1493276A (en) | Ferulaic acid sodium drip pill and its preparation method | |
| CN1526393A (en) | Hydralazine hydrochloride guttate pills and the prepn | |
| CN1528318A (en) | Herba adonidis aglycone drop pill and preparing method thereof | |
| CN1493290A (en) | Ferulaic acid piperazine drip pill and its preparation method | |
| CN1493288A (en) | Hanfangchin A drip pill and its preparation method | |
| CN1602875A (en) | MolsidominE dripping pills and its preparation process | |
| CN1582908A (en) | Tramadol hydrochloride drops and their preparation | |
| CN1602868A (en) | Dripping pills of ketotifen fumarate and its preparation method | |
| CN1493287A (en) | Shishan alkaloid drip pill and its preparation method | |
| CN1528272A (en) | Agrimophol drop pill and preparing method thereof | |
| CN1582940A (en) | Calmazine hydrochloride drops and their preparation | |
| CN1490005A (en) | Berberine or berberine salts drops and their preparation | |
| CN1562039A (en) | Moricizine hydrochloride dripping pill and its preparing method | |
| CN1528298A (en) | Isocarboxazid drop pill and preparing method thereof | |
| CN1543967A (en) | Benproperine phosphate dripping pills and preparation | |
| CN1582939A (en) | Dioxyimipramine hydrochloride drops and their preparation | |
| CN1562043A (en) | Epristeride dripping pills and its preparing method |
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 |