CN1493290A - Ferulaic acid piperazine drip pill and its preparation method - Google Patents
Ferulaic acid piperazine drip pill and its preparation method Download PDFInfo
- Publication number
- CN1493290A CN1493290A CNA031576672A CN03157667A CN1493290A CN 1493290 A CN1493290 A CN 1493290A CN A031576672 A CNA031576672 A CN A031576672A CN 03157667 A CN03157667 A CN 03157667A CN 1493290 A CN1493290 A CN 1493290A
- Authority
- CN
- China
- Prior art keywords
- piperazine
- preparation
- coolant
- piperazine ferulate
- acid
- 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
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A dripping pill of piperazine ferulate and its superfine pulverizing process for preparing it are disclosed. Its advantages are high dissolving and disintegrating speed, high stripping percentage, quickly taking its effect, high stability and low cost.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically drop pills of piperazine ferulic acid and preparation method thereof.
Background technology
Piperazine ferulate has anticoagulant, antiplatelet aggregation, expansion blood capillary, increases coronary flow, vasospasmolytic effect.
Piperazine ferulate oral absorption blood medicine peak time is 29 minutes, distribution phase half-life (t
1/2α) be 27 minutes, eliminate phase half-life (t
1/2 β) be 5.5 hours.Piperazine ferulate is distributed more widely in vivo, in liver, kidney blood, distribute more, it is also more to distribute in stomach, small intestinal fat, mainly discharges from urine, feces.Can see through placental barrier.List marketing at present have only the piperazine ferulate sheet, dosage form is single.The clinical renal glomerular disease that is used for all kinds of with microscopic hematuria and hypercoagulability is as the auxiliary treatment of nephritis, chronic nephritis, nephrotic syndrome early stage uremia and coronary heart disease, cerebral infarction, vasculitis etc.
Piperazine ferulate is insoluble in water, and piperazine ferulate sheet disintegration time is long, and dissolution and dissolution rate are low, the supplementary product consumption ratio is big, child, old people, bed patient and dysphagia patients are taken inconvenience, and compliance is poor, have influenced the performance of piperazine ferulate therapeutical effect.
The present invention makes the drop pills of piperazine ferulic acid agent by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of piperazine ferulate sheet, and the therapeutical effect of piperazine ferulate is given full play to.
Summary of the invention
The drop pills of piperazine ferulic acid 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 piperazine ferulate 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 piperazine ferulate is 3-methoxyl group-4-Hydroxycinnamic Acid piperazine among the present invention, and molecular formula is C
4H
10N
2C
10H
10O
4, molecular weight is 474.51, structural formula:
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 appendix XC first methods of Chinese Pharmacopoeia version in 2000), is a solvent with water 1000ml, rotating speed is 50 commentaries on classics, and operation in accordance with the law is in the time of 5,10,20,30 and 45 minutes, get solution 10ml, filter, it is an amount of that precision is measured subsequent filtrate, adds water and quantitatively be diluted to the solution that contains piperazine ferulate 6 μ g among every 1ml approximately, shake up, according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 A), measure trap at the wavelength place of 310nm, press C
4H
10N
22C
10H
10O
4Absorptance (E
1cm 1%) be 653 calculating stripping quantities.
Two, commercially available piperazine ferulate sheet testing result
1. disintegration time: 38 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 21.2 35.3 48.6 65.2 78.3
Three, example 1 sample detection result
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 54.5 75.2 89.6 99.7 98.2
Four, example 2 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 60.3 78.2 86.5 98.4 99.2
Five, example 3 sample detection results
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 61.2 80.5 95.3 101.2 100.4
Six, example 4 sample detection results
1. the molten diffusing time: 10 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 50.3 72.5 85.4 99.7 99.6
Seven, example 5 sample detection results
1. the molten diffusing time: 12 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 48.3 64.5 80.3 97.6 98.2
Eight, example 6 sample detection results
1. the molten diffusing time: 16 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 45.2 67.3 82.5 98.9 99.1
The specific embodiment
One, example 1
Prescription:
Piperazine ferulate 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the piperazine ferulate 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:
Piperazine ferulate 5g
Macrogol 4000 15g
Make 1000
Method for making: the piperazine ferulate 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:
Piperazine ferulate 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the piperazine ferulate 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:
Piperazine ferulate 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the piperazine ferulate 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:
Piperazine ferulate 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the piperazine ferulate 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:
Piperazine ferulate 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that piperazine ferulate 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. drop pills of piperazine ferulic acid and preparation method thereof is characterized in that: the piperazine ferulate 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 piperazine ferulate of claim 1 is 3-methoxyl group-4-Hydroxycinnamic Acid piperazine, and molecular formula is C
4H
10N
2C
10H
10O
4, molecular weight is 474.51, structural formula:
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 |
|---|---|---|---|
| CNA031576672A CN1493290A (en) | 2003-09-06 | 2003-09-06 | Ferulaic acid piperazine drip pill and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031576672A CN1493290A (en) | 2003-09-06 | 2003-09-06 | Ferulaic acid piperazine drip pill and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1493290A true CN1493290A (en) | 2004-05-05 |
Family
ID=34240894
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031576672A Pending CN1493290A (en) | 2003-09-06 | 2003-09-06 | Ferulaic acid piperazine drip pill and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1493290A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1872064B (en) * | 2005-06-01 | 2010-09-29 | 天津天士力制药股份有限公司 | Drop pills of piperazine ferulic acid, and preparation method |
-
2003
- 2003-09-06 CN CNA031576672A patent/CN1493290A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1872064B (en) * | 2005-06-01 | 2010-09-29 | 天津天士力制药股份有限公司 | Drop pills of piperazine ferulic acid, and preparation method |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1493290A (en) | Ferulaic acid piperazine drip pill and its preparation method | |
| CN1493298A (en) | Ginseng stem leaf total saponin drip pill and its preparation method | |
| CN1493295A (en) | Oleanolic acid drip pill and its preparation method | |
| CN1528321A (en) | Rhizoma gastrodiae extract drop pill and preparing method thereof | |
| CN1562001A (en) | Carbazochrome sodium sulfoate dripping pill and its preparing method | |
| CN1528287A (en) | Herba lysionoti extract drop pill and preparing method thereof | |
| CN1493276A (en) | Ferulaic acid sodium drip pill and its preparation method | |
| CN1528298A (en) | Isocarboxazid drop pill and preparing method thereof | |
| CN1526393A (en) | Hydralazine hydrochloride guttate pills and the prepn | |
| CN1546022A (en) | Dripping pills of luteanine hydrochloride and its preparation | |
| CN1582908A (en) | Tramadol hydrochloride drops and their preparation | |
| CN1528281A (en) | Rhododeudron molle toxin drop pill and preparing method thereof | |
| CN1528294A (en) | Indolol drop pill and preparing method thereof | |
| CN1602848A (en) | Ambroxol hydrochloride drop pills and its preparation method | |
| CN1582937A (en) | Amiloride hydrochloride drops and their preparation | |
| CN1528301A (en) | Nicorandic drop pill and preparing method thereof | |
| CN1602868A (en) | Dripping pills of ketotifen fumarate and its preparation method | |
| CN1493280A (en) | Mezereum drip pill and its preparation method | |
| CN1602845A (en) | Fenfluramine hydrochloride drop pills and its preparation method | |
| CN1528318A (en) | Herba adonidis aglycone drop pill and preparing method thereof | |
| CN1526379A (en) | Sibutramine hydrochloride dripping pill and its prepn | |
| CN1493288A (en) | Hanfangchin A drip pill and its preparation method | |
| CN1543967A (en) | Benproperine phosphate dripping pills and preparation | |
| CN1543961A (en) | Oxazepam dripping pills and preparation thereof | |
| CN1562039A (en) | Moricizine hydrochloride dripping pill 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 |