CN1543960A - Imipramine hydrochloride dripping pills and preparation - Google Patents
Imipramine hydrochloride dripping pills and preparation Download PDFInfo
- Publication number
- CN1543960A CN1543960A CNA2003101192091A CN200310119209A CN1543960A CN 1543960 A CN1543960 A CN 1543960A CN A2003101192091 A CNA2003101192091 A CN A2003101192091A CN 200310119209 A CN200310119209 A CN 200310119209A CN 1543960 A CN1543960 A CN 1543960A
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- CN
- China
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- imipramine hydrochloride
- preparation
- coolant
- polyethylene glycol
- imipramine
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract
The invention discloses am Imipramine Hydrochloride drop pill prepared through ultramicro disintegration and drop pills manufacturing technique, which has the advantages of improving collapse and dissolving speed, high dissolving rate, quick effect,increased medicament stability, oral or swallow administration, and good compliance.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically imipramine hydrochloride drop pill and preparation method thereof.
Background technology
Imipramine hydrochloride is a tricyclic antidepressant, and main effect is to block the reuptake of central nervous system to norepinephrine and these two kinds of neurotransmitteies of 5-hydroxy tryptamine, and these two kinds of neurotransmitter concentration increase in the synaptic space thereby make, the performance antidepressant effect.This product also has cholinolytic, anti-α
1Adrenoceptor and anti-H
1The histamine receptor effect, but very little to the dopamine receptor influence.
The imipramine hydrochloride oral absorption is good, bioavailability 29%~77%, protein binding rate 76%~95%, half-life (T
1/2) be 9~24 hours, distribution volume (V
d) 15~30L/kg.Mainly at liver metabolism, active metabolite is a desmethylimipramine.From renal excretion, can be secreted into milk, elderly patients descend to the metabolism and the discharge capacity of imipramine hydrochloride, and sensitivity strengthens, and should reduce consumption.List marketing at present tablet only arranged, clinically be used for various depressions.Because of having the effect of rousing oneself, be applicable to blunt type depression, but should not be used for agitating form depression or anxious depression.Also can be used for infantile enuresis.
Imipramine hydrochloride odorless or odorless almost, meet light gradual change color, easily molten in water, but the 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 imipramine hydrochloride therapeutical effect.
The present invention makes the imipramine hydrochloride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of imipramine hydrochloride sheet, and the therapeutical effect of imipramine hydrochloride is given full play to.
Summary of the invention
The imipramine 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 imipramine 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 imipramine hydrochloride is N among the present invention, N-dimethyl-10, and 11-dihydro-5H-dibenzo [b, f] azatropylidene-5-propylamin hydrochloride, structural formula is
Molecular formula is C
19H
24N
2HCl, molecular weight are 316.88.
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), 900ml is a solvent with hydrochloric acid solution (9 → 1000), 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 the about 10ml of solution, filter, get subsequent filtrate, according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 A), measure trap immediately, press C at the wavelength place of 251nm
19H
24N
2Absorptance (the E of HCl
1cm 1%) be 264 calculating stripping quantities.
Two, commercially available imipramine hydrochloride sheet testing result
1. disintegration time: 35 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 36.4 53.2 78.9 86.3
Three, example 1 sample detection result
1. the molten diffusing time: 2 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 51.4 93.6 99.7 98.4
Four, example 2 sample detection results
1. the molten diffusing time: 2 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 54.6 97.2 101.3 100.5
Five, example 3 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 45.9 89.2 97.6 98.3
Six, example 4 sample detection results
1. the molten diffusing time: 4 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 54.4 93.1 99.6 98.2
Seven, example 5 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 47.4 86.3 98.5 99.2
Eight, example 6 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate
Time (minute) 10 20 30 40
Dissolution (%) 58.7 90.5 98.6 97.2
The specific embodiment
One, example 1
Prescription:
Imipramine hydrochloride 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the imipramine 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:
Imipramine hydrochloride 5g
Macrogol 4000 15g
Make 1000
Method for making: the imipramine 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:
Imipramine hydrochloride 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the imipramine 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:
Imipramine hydrochloride 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the imipramine 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:
Imipramine hydrochloride 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the imipramine 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:
Imipramine hydrochloride 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that imipramine 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. imipramine hydrochloride drop pill and preparation method thereof is characterized in that: the imipramine 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 molecular formula of the described imipramine hydrochloride of claim 1 is C
19H
24N
2HCl, molecular weight are 316.88, 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 |
---|---|---|---|
CNA2003101192091A CN1543960A (en) | 2003-11-20 | 2003-11-20 | Imipramine hydrochloride dripping pills and preparation |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNA2003101192091A CN1543960A (en) | 2003-11-20 | 2003-11-20 | Imipramine hydrochloride dripping pills and preparation |
Publications (1)
Publication Number | Publication Date |
---|---|
CN1543960A true CN1543960A (en) | 2004-11-10 |
Family
ID=34338192
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNA2003101192091A Pending CN1543960A (en) | 2003-11-20 | 2003-11-20 | Imipramine hydrochloride dripping pills and preparation |
Country Status (1)
Country | Link |
---|---|
CN (1) | CN1543960A (en) |
-
2003
- 2003-11-20 CN CNA2003101192091A patent/CN1543960A/en active Pending
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C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
WD01 | Invention patent application deemed withdrawn after publication |