CN1569004A - Dripping pills of nefopam hydrochloride and its preparation method - Google Patents
Dripping pills of nefopam hydrochloride and its preparation method Download PDFInfo
- Publication number
- CN1569004A CN1569004A CNA2004100444403A CN200410044440A CN1569004A CN 1569004 A CN1569004 A CN 1569004A CN A2004100444403 A CNA2004100444403 A CN A2004100444403A CN 200410044440 A CN200410044440 A CN 200410044440A CN 1569004 A CN1569004 A CN 1569004A
- Authority
- CN
- China
- Prior art keywords
- nefopam hydrochloride
- coolant
- preparation
- nefopam
- 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.)
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Abstract
The invention relates to a Nefopam Hydrochloride drop pill prepared by utilizing ultramicro disintegration and drop pill manufacturing process, which has the advantages of improving collapse and dissolving speed, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use. It has good compliance, thus is especially suitable for children, the elderly, bedridden patients and dysphagia patients.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically nefopam hydrochloride drop pill and preparation method thereof.
Background technology
Nefopam hydrochloride is a kind of novel non-narcotic analgesics, has slight analgesic and flesh pine effect concurrently.Chemical constitution belongs to the cyclisation o-methyl-diphenhydramine, so do not have the characteristic of NSAID (non-steroidal anti-inflammatory drug), also non-opioid receptor agonist.Centering, severe pain are effective, the suitable 12mg morphine of intramuscular injection nefopam hydrochloride 20mg effect.Lighter to the respiration inhibition effect.To blood circulation unrestraint effect.There are not tolerance and dependency.
The nefopam hydrochloride oral absorption is rapid, T
MaxBe 1-3 hour, first pass effect is obvious.T
1/2Be 4-8 hour, plasma protein binding rate is 71%～76%.Lost pharmacologically active by hepatic metabolism, most of through renal excretion, original shape medicine less than 5% is discharged with feces on a small quantity.The oral formulations of list marketing at present only has tablet, clinical postoperative analgesia, the cancer pain, acute outer grieved of being used for.Also be used for visceral smooth muscle angor such as acute gastritis, ascariasis of biliary tract, ureteral calculus.
The nefopam hydrochloride mildly bitter flavor, molten in the water part omitted, its disintegration of tablet time is long, absorption difference, bioavailability is low, and 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 nefopam hydrochloride therapeutical effect.
The present invention makes the nefopam hydrochloride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of nefopam hydrochloride sheet, and the therapeutical effect of nefopam hydrochloride is given full play to.
Summary of the invention
The nefopam hydrochloride drop pill of making by using ultramicro communication technique and dropping pill formulation Technology not only have disintegrate molten loose fast, steady quality, the pill volume is little, and is easy to carry and use, and 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 nefopam hydrochloride 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 nefopam hydrochloride is 5-methyl isophthalic acid-phenyl-3,4,5 among the present invention, 6-tetrahydrochysene-1H-2, and the 5-paroxazine is also hot because of hydrochlorate, and molecular formula is C
17H
9NOHcl, molecular weight are 289.80, and 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
Disintegrate (molten loosing) time limit: check according to inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2000).
Two, commercially available nefopam hydrochloride sheet disintegration time testing result: 53 minutes
Three, example 1 sample disintegrate (molten loosing) time detecting result: 2 minutes
Four, example 2 sample disintegrates (molten loosing) time detecting result: 2 minutes
Five, example 3 sample disintegrates (molten loosing) time detecting result: 3 minutes
Six, example 4 sample disintegrates (molten loosing) time detecting result: 5 minutes
Seven, example 5 sample disintegrates (molten loosing) time detecting result: 8 minutes
Eight, example 6 sample disintegrates (molten loosing) time detecting result: 10 minutes
The specific embodiment
One, example 1
Prescription:
Nefopam hydrochloride 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the nefopam 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:
Nefopam hydrochloride 5g
Macrogol 4000 15g
Make 1000
Method for making: the nefopam 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:
Nefopam hydrochloride 5g
Polyethylene glycol 6000 10g
Macrogol 4000 5g
Make 1000
Method for making: the nefopam hydrochloride 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:
Nefopam hydrochloride 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the nefopam 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:
Nefopam hydrochloride 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the nefopam 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:
Nefopam hydrochloride 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that nefopam 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. nefopam hydrochloride drop pill and preparation method thereof is characterized in that: the nefopam 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 nefopam hydrochloride of claim 1 is 5-methyl isophthalic acid-phenyl-3,4,5,6-tetrahydrochysene-1H-2, and the 5-paroxazine is also hot because of hydrochlorate, and molecular formula is C
17H
9NOHcl, molecular weight are 289.80, and 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 |
|---|---|---|---|
| CNA2004100444403A CN1569004A (en) | 2004-05-13 | 2004-05-13 | Dripping pills of nefopam hydrochloride and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100444403A CN1569004A (en) | 2004-05-13 | 2004-05-13 | Dripping pills of nefopam hydrochloride and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1569004A true CN1569004A (en) | 2005-01-26 |
Family
ID=34481890
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2004100444403A Pending CN1569004A (en) | 2004-05-13 | 2004-05-13 | Dripping pills of nefopam hydrochloride and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1569004A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105687185A (en) * | 2009-12-15 | 2016-06-22 | 儿童医院 | Method of treating scars and beta-catenin-mediated disorders using Nefopam compounds |
| EP3854386A1 (en) * | 2020-01-21 | 2021-07-28 | Athena Pharmaceutiques SAS | An orally disintegrating pharmaceutical composition comprising nefopam and process for preparing the same |
-
2004
- 2004-05-13 CN CNA2004100444403A patent/CN1569004A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105687185A (en) * | 2009-12-15 | 2016-06-22 | 儿童医院 | Method of treating scars and beta-catenin-mediated disorders using Nefopam compounds |
| CN105687185B (en) * | 2009-12-15 | 2019-07-09 | 儿童医院 | The method of the disease of invasion fiber type tumor disease and beta-catenin mediation is treated using nefopam compound |
| EP3854386A1 (en) * | 2020-01-21 | 2021-07-28 | Athena Pharmaceutiques SAS | An orally disintegrating pharmaceutical composition comprising nefopam and process for preparing the same |
| AU2020286220B2 (en) * | 2020-01-21 | 2022-09-22 | Athena Pharmaceutiques Sas | An orally disintegrating pharmacutical composition comprising nefopam and process for preparing the same |
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|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |