CN1546034A - Dripping pills of meloxicam and its preparation - Google Patents
Dripping pills of meloxicam and its preparation Download PDFInfo
- Publication number
- CN1546034A CN1546034A CNA200310121922XA CN200310121922A CN1546034A CN 1546034 A CN1546034 A CN 1546034A CN A200310121922X A CNA200310121922X A CN A200310121922XA CN 200310121922 A CN200310121922 A CN 200310121922A CN 1546034 A CN1546034 A CN 1546034A
- Authority
- CN
- China
- Prior art keywords
- meloxicam
- preparation
- coolant
- polyethylene glycol
- drop pill
- 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
- ZRVUJXDFFKFLMG-UHFFFAOYSA-N Meloxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=NC=C(C)S1 ZRVUJXDFFKFLMG-UHFFFAOYSA-N 0.000 title claims abstract description 32
- 229960001929 meloxicam Drugs 0.000 title claims abstract description 32
- 239000006187 pill Substances 0.000 title claims abstract description 17
- 238000002360 preparation method Methods 0.000 title claims description 13
- 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
- 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
- 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
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 4
- 239000002253 acid 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
- 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
- -1 liquid paraffin Substances 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
- 238000004519 manufacturing process Methods 0.000 abstract description 4
- 208000019505 Deglutition disease Diseases 0.000 abstract description 3
- 239000003814 drug Substances 0.000 abstract description 2
- 239000002671 adjuvant Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 description 10
- 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
- 238000004891 communication Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 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
- 101150071146 COX2 gene Proteins 0.000 description 1
- 101100114534 Caenorhabditis elegans ctc-2 gene Proteins 0.000 description 1
- 208000000857 Hepatic Insufficiency Diseases 0.000 description 1
- 206010019663 Hepatic failure Diseases 0.000 description 1
- 101150000187 PTGS2 gene Proteins 0.000 description 1
- 208000001647 Renal Insufficiency Diseases 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000002917 arthritic effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 210000002249 digestive system Anatomy 0.000 description 1
- 150000002085 enols Chemical class 0.000 description 1
- 210000003608 fece Anatomy 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 201000006370 kidney failure Diseases 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 210000002381 plasma Anatomy 0.000 description 1
- 238000005057 refrigeration Methods 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 238000002636 symptomatic treatment Methods 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention relates to a meloxicam 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 meloxicam drop pill and preparation method thereof.
Background technology
Meloxicam is the enol acid NSAID (non-steroidal anti-inflammatory drug), has antiinflammatory, analgesia and refrigeration function.Optionally suppress Cycloxygenase-2 (Cox-2), a little less than the inhibitory action to Cycloxygenase-1, so untoward reaction such as digestive system is few.
Meloxicam is oral, rectally is drawn and received well, and after the oral absorption, the medicine in the blood plasma more than 99% combines with plasma protein, and the half-life is about 20 hours.Metabolite about 50% is discharged from urine, and all the other are discharged from feces.When hepatic insufficiency or light, moderate renal insufficiency, pharmacokinetic parameter does not have significant change.Be applicable to the arthritic symptomatic treatment of rheumatoid arthritis and painful.
The meloxicam tablet disintegration time is long, absorption difference, and bioavailability is low, and the supplementary product consumption ratio is big, and child, old people, bed patient and dysphagia patients are taken inconvenience, and compliance is poor, has influenced the performance of meloxicam therapeutical effect.
The present invention makes the meloxicam drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of meloxicam tablet, and the therapeutical effect of meloxicam is given full play to.
Summary of the invention
The meloxicam 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, 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 has working condition and production equipment is simple, production cost is low, compares the advantage that supplementary product consumption reduces with tablet, has 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 meloxicam 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 structural formula of meloxicam among the present invention (Meloxicam) 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 meloxicam tablet disintegration time testing result: 59 minutes
Three, example 1 sample disintegrate (molten loosing) time detecting result: 2 minutes
Four, example 2 sample disintegrates (molten loosing) time detecting result: 3 minutes
Five, example 3 sample disintegrates (molten loosing) time detecting result: 2 minutes
Six, example 4 sample disintegrates (molten loosing) time detecting result: 6 minutes
Seven, example 5 sample disintegrates (molten loosing) time detecting result: 9 minutes
Eight, example 6 sample disintegrates (molten loosing) time detecting result: 8 minutes
The specific embodiment
One, example 1
Prescription:
Meloxicam 7.5g
Polyethylene glycol 6000 12g
Make 1000
Method for making: the meloxicam 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:
Meloxicam 7.5g
Macrogol 4000 12g
Make 1000
Method for making: the meloxicam 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:
Meloxicam 7.5g
Polyethylene glycol 6000 2g
Macrogol 4000 10g
Make 1000
Method for making: the meloxicam 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:
Meloxicam 7.5g
Glyceryl monostearate 12g
Make 1000
Method for making: the meloxicam 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:
Meloxicam 7.5g
Polyethylene glycol 6000 10g
Poloxamer 2g
Make 1000
Method for making: the meloxicam 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:
Meloxicam 7.5g
Glyceryl monostearate 11g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that meloxicam 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. meloxicam drop pill and preparation method thereof is characterized in that: the meloxicam fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, and abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
2. the structural formula of the described meloxicam Meloxicam of claim 1 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 |
|---|---|---|---|
| CNA200310121922XA CN1546034A (en) | 2003-12-08 | 2003-12-08 | Dripping pills of meloxicam and its preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200310121922XA CN1546034A (en) | 2003-12-08 | 2003-12-08 | Dripping pills of meloxicam and its preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1546034A true CN1546034A (en) | 2004-11-17 |
Family
ID=34338573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA200310121922XA Pending CN1546034A (en) | 2003-12-08 | 2003-12-08 | Dripping pills of meloxicam and its preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1546034A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013056684A3 (en) * | 2011-10-18 | 2013-06-13 | 华东理工大学 | Thiazole derivative as dhodh inhibitor and use thereof |
-
2003
- 2003-12-08 CN CNA200310121922XA patent/CN1546034A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013056684A3 (en) * | 2011-10-18 | 2013-06-13 | 华东理工大学 | Thiazole derivative as dhodh inhibitor and use thereof |
| CN103998434A (en) * | 2011-10-18 | 2014-08-20 | 华东理工大学 | Thiazole derivative as DHODH inhibitor and use thereof |
| CN103998434B (en) * | 2011-10-18 | 2016-10-12 | 华东理工大学 | Thiazole and application thereof as DHODH inhibitor |
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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 |