CN1526392A - Cetirizine hydrochloride guttate pills and the prepn - Google Patents
Cetirizine hydrochloride guttate pills and the prepn Download PDFInfo
- Publication number
- CN1526392A CN1526392A CNA031595588A CN03159558A CN1526392A CN 1526392 A CN1526392 A CN 1526392A CN A031595588 A CNA031595588 A CN A031595588A CN 03159558 A CN03159558 A CN 03159558A CN 1526392 A CN1526392 A CN 1526392A
- Authority
- CN
- China
- Prior art keywords
- cetirizine hydrochloride
- coolant
- polyethylene glycol
- cetirizine
- preparation
- 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
- ZKLPARSLTMPFCP-UHFFFAOYSA-N Cetirizine Chemical compound C1CN(CCOCC(=O)O)CCN1C(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZKLPARSLTMPFCP-UHFFFAOYSA-N 0.000 title claims abstract description 34
- 229960004342 cetirizine hydrochloride Drugs 0.000 title claims abstract description 33
- 239000006187 pill Substances 0.000 title claims abstract description 18
- 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
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 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
- 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
- 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
- -1 liquid paraffin 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
- 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
- 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
- 238000000034 method Methods 0.000 abstract description 13
- 208000019505 Deglutition disease Diseases 0.000 abstract description 3
- 238000004519 manufacturing process Methods 0.000 abstract description 3
- 230000029087 digestion Effects 0.000 abstract 2
- 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
- 238000005516 engineering process Methods 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 238000004891 communication Methods 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000009472 formulation 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
- 102000004506 Blood Proteins Human genes 0.000 description 1
- 108010017384 Blood Proteins Proteins 0.000 description 1
- IHTYTYHXCRAMAV-UHFFFAOYSA-N acetic acid;dihydrochloride Chemical compound Cl.Cl.CC(O)=O IHTYTYHXCRAMAV-UHFFFAOYSA-N 0.000 description 1
- 230000001705 anti-serotonergic effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 210000005098 blood-cerebrospinal fluid barrier Anatomy 0.000 description 1
- 229960001803 cetirizine Drugs 0.000 description 1
- 230000003153 cholinolytic effect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 239000000938 histamine H1 antagonist Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 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
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000013558 reference substance Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention is Cetirizine hydrochloride dripping pill prepared through superfine crushing and dripping pill producing process. The Cetirizine hydrochloride dripping pill has raised disintegrating and dissolving speed, high digestion rate and digestion degree, fast acting, high stability, reduced supplementary material consumption, low production cost and easy carrying about and taking. It may be haven in mouth or swallowed, has excellent conformity and is especially suitable for children, the aged and other patients with dysphagia.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically cetirizine hydrochloride drop pill and preparation method thereof.
Background technology
Cetirizine hydrochloride is the selectivity histamine H
1Receptor antagonist.Zoopery shows that it does not have obvious cholinolytic and antiserotonergic effect, is difficult for acting on maincenter H by blood-cerebrospinal fluid barrier
1Central inhibitory action is stronger when receptor, clinical use.
The oral back of cetirizine hydrochloride is by gastrointestinal absorption.The once oral 10mg cetirizine of health adult, peak reaching time of blood concentration (t
Max) be 30～60 minutes, the blood peak concentration of drug is 300ng/ml, with the plasma protein binding rate height, plasma half-life is about 10 hours, about 70% with the original shape medicine with urine excretion, on a small quantity from defecate.
The cetirizine hydrochloride odorless, bitter in the mouth, have draw moist, in water very easily the dissolving, but its tablet or capsule disintegration time are long, dissolution and dissolution rate are low, absorption difference, and bioavailability is 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 cetirizine hydrochloride therapeutical effect.
The present invention makes the cetirizine hydrochloride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes Cetirizine hydrochloride Tablets and capsular above defective, and the therapeutical effect of cetirizine hydrochloride is given full play to.
Summary of the invention
The cetirizine 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 child, the old people, the characteristics that bed patient and dysphagia patients are taken, but also have working condition and production equipment is simple, production cost is low, with tablet or capsule and compare the advantage that supplementary product consumption reduces, 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 cetirizine 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 cetirizine hydrochloride among the present invention (Cetirizine Hydrochloride) is (±)-2-[2-[4-[(4-chlorphenyl) benzyl]-the 1-piperazinyl] ethyoxyl] the acetic acid dihydrochloride, molecular formula is C
21H
25ClN
2O
32HCl, 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
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 water is solvent, rotating speed is that per minute 100 changes, operation in accordance with the law in the time of 5,10,20,30 and 45 minutes, is got solution and is filtered, get subsequent filtrate according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 A), measure trap at the wavelength place of 231nm; Other precision takes by weighing through 105 ℃ of cetirizine hydrochloride reference substances that are dried to constant weight an amount of, is dissolved in water, and makes the solution that contains 10 μ g among every 1ml, with the method operation, calculates stripping quantity.
Two, commercially available Cetirizine hydrochloride Tablets testing result
1. disintegration time: 34 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 2 6.4 45.6 68.5 82.3 90.5
Three, example 1 sample detection result
1. the molten diffusing time: 1 minute
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 63.4 76.5 89.2 99.6 101.3
Four, example 2 sample detection results
1. the molten diffusing time: 2 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 58.4 72.5 90.3 98.7 97.6
Five, example 3 sample detection results
1. the molten diffusing time: 2 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 64.5 85.6 92.4 97.8 98.9
Six, example 4 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 54.2 81.3 8 8.6 97.8 97.2
Seven, example 5 sample detection results
1. the molten diffusing time: 6 minutes
2. dissolution rate:
Time (minute) 5 10 20 30 45
Dissolution (%) 50.6 78.1 8 2.5 98.7 96.4
Eight, example 6 sample detection results
1. the molten diffusing time: 8 minutes
2. dissolution rate
Time (minute) 5 10 20 30 45
Dissolution (%) 53.5 72.3 86.4 98.9 99.1
The specific embodiment
One, example 1
Prescription:
Cetirizine hydrochloride 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the cetirizine 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:
Cetirizine hydrochloride 5g
Macrogol 4000 15g
Make 1000
Method for making: the cetirizine 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:
Cetirizine hydrochloride 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the cetirizine 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:
Cetirizine hydrochloride 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the cetirizine 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:
Cetirizine hydrochloride 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the cetirizine 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:
Cetirizine hydrochloride 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that cetirizine 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. cetirizine hydrochloride drop pill and preparation method thereof is characterized in that: the cetirizine 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 described cetirizine hydrochloride molecular formula of claim 1 is C
21H
25ClN
2O
32HC1, 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 |
|---|---|---|---|
| CNA031595588A CN1526392A (en) | 2003-09-23 | 2003-09-23 | Cetirizine hydrochloride guttate pills and the prepn |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031595588A CN1526392A (en) | 2003-09-23 | 2003-09-23 | Cetirizine hydrochloride guttate pills and the prepn |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1526392A true CN1526392A (en) | 2004-09-08 |
Family
ID=34287333
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031595588A Pending CN1526392A (en) | 2003-09-23 | 2003-09-23 | Cetirizine hydrochloride guttate pills and the prepn |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1526392A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104069086A (en) * | 2014-07-22 | 2014-10-01 | 周有财 | Flunarizine hydrochloride composition capsule and preparation method thereof |
-
2003
- 2003-09-23 CN CNA031595588A patent/CN1526392A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104069086A (en) * | 2014-07-22 | 2014-10-01 | 周有财 | Flunarizine hydrochloride composition capsule 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 |