JP2011213726A - 水溶性メロキシカム顆粒 - Google Patents
水溶性メロキシカム顆粒 Download PDFInfo
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- JP2011213726A JP2011213726A JP2011137557A JP2011137557A JP2011213726A JP 2011213726 A JP2011213726 A JP 2011213726A JP 2011137557 A JP2011137557 A JP 2011137557A JP 2011137557 A JP2011137557 A JP 2011137557A JP 2011213726 A JP2011213726 A JP 2011213726A
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- meloxicam
- granule
- meglumine
- granules
- granule according
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- 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 66
- 229960001929 meloxicam Drugs 0.000 title claims abstract description 63
- 239000008187 granular material Substances 0.000 title claims abstract description 55
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims abstract description 21
- 229960003194 meglumine Drugs 0.000 claims abstract description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 241001465754 Metazoa Species 0.000 claims abstract description 12
- 239000011230 binding agent Substances 0.000 claims abstract description 12
- 235000003599 food sweetener Nutrition 0.000 claims abstract description 12
- 239000003765 sweetening agent Substances 0.000 claims abstract description 12
- 235000000346 sugar Nutrition 0.000 claims abstract description 11
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims abstract description 8
- 239000011734 sodium Substances 0.000 claims abstract description 8
- 229910052708 sodium Inorganic materials 0.000 claims abstract description 8
- 239000003651 drinking water Substances 0.000 claims abstract description 7
- 235000020188 drinking water Nutrition 0.000 claims abstract description 7
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229910052700 potassium Inorganic materials 0.000 claims abstract description 6
- 239000011591 potassium Substances 0.000 claims abstract description 6
- 150000003863 ammonium salts Chemical class 0.000 claims abstract description 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 4
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 3
- 238000000034 method Methods 0.000 claims description 12
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 11
- 229960001031 glucose Drugs 0.000 claims description 11
- 239000007788 liquid Substances 0.000 claims description 11
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 10
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 10
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 10
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 10
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 8
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 7
- 239000013543 active substance Substances 0.000 claims description 7
- 239000008103 glucose Substances 0.000 claims description 7
- 239000008101 lactose Substances 0.000 claims description 7
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 7
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 7
- 235000012907 honey Nutrition 0.000 claims description 5
- 208000023504 respiratory system disease Diseases 0.000 claims description 5
- 239000007921 spray Substances 0.000 claims description 5
- LICPKMHUPOIPDE-WZTVWXICSA-N 4-hydroxy-2-methyl-n-(5-methyl-1,3-thiazol-2-yl)-1,1-dioxo-1$l^{6},2-benzothiazine-3-carboxamide;(2r,3r,4r,5s)-6-(methylamino)hexane-1,2,3,4,5-pentol Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=NC=C(C)S1 LICPKMHUPOIPDE-WZTVWXICSA-N 0.000 claims description 4
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 4
- 235000009499 Vanilla fragrans Nutrition 0.000 claims description 4
- 244000263375 Vanilla tahitensis Species 0.000 claims description 4
- 235000012036 Vanilla tahitensis Nutrition 0.000 claims description 4
- 235000010358 acesulfame potassium Nutrition 0.000 claims description 4
- 230000037396 body weight Effects 0.000 claims description 4
- 239000000796 flavoring agent Substances 0.000 claims description 4
- 235000019634 flavors Nutrition 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 4
- 239000000600 sorbitol Substances 0.000 claims description 4
- 238000005507 spraying Methods 0.000 claims description 4
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical group OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims description 3
- 108010011485 Aspartame Proteins 0.000 claims description 3
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 3
- 239000002202 Polyethylene glycol Substances 0.000 claims description 3
- 206010037660 Pyrexia Diseases 0.000 claims description 3
- 239000000605 aspartame Substances 0.000 claims description 3
- 235000010357 aspartame Nutrition 0.000 claims description 3
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 3
- 229960003438 aspartame Drugs 0.000 claims description 3
- 239000011248 coating agent Substances 0.000 claims description 3
- 238000000576 coating method Methods 0.000 claims description 3
- 239000003205 fragrance Substances 0.000 claims description 3
- 238000010438 heat treatment Methods 0.000 claims description 3
- 229920001223 polyethylene glycol Polymers 0.000 claims description 3
- 229940069328 povidone Drugs 0.000 claims description 3
- 229940085605 saccharin sodium Drugs 0.000 claims description 3
- 238000003756 stirring Methods 0.000 claims description 3
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 2
- 108010010803 Gelatin Proteins 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 235000011430 Malus pumila Nutrition 0.000 claims description 2
- 235000015103 Malus silvestris Nutrition 0.000 claims description 2
- 229930195725 Mannitol Natural products 0.000 claims description 2
- 208000002193 Pain Diseases 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 2
- 229930006000 Sucrose Natural products 0.000 claims description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 2
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 239000008273 gelatin Substances 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- 235000011852 gelatine desserts Nutrition 0.000 claims description 2
- 235000001727 glucose Nutrition 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 230000007774 longterm Effects 0.000 claims description 2
- 239000000594 mannitol Substances 0.000 claims description 2
- 235000010355 mannitol Nutrition 0.000 claims description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- 239000005720 sucrose Substances 0.000 claims description 2
- 239000000811 xylitol Substances 0.000 claims description 2
- 235000010447 xylitol Nutrition 0.000 claims description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 2
- 229960002675 xylitol Drugs 0.000 claims description 2
- 235000013305 food Nutrition 0.000 abstract description 3
- 150000003839 salts Chemical class 0.000 abstract description 3
- 239000000126 substance Substances 0.000 abstract 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- -1 N-methyl-D-glucamine salt Chemical class 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 229960003511 macrogol Drugs 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 2
- 206010012735 Diarrhoea Diseases 0.000 description 2
- 241000283086 Equidae Species 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- 208000016285 Movement disease Diseases 0.000 description 2
- 206010052904 Musculoskeletal stiffness Diseases 0.000 description 2
- 241000282887 Suidae Species 0.000 description 2
- 239000000619 acesulfame-K Substances 0.000 description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 230000035622 drinking Effects 0.000 description 2
- 208000004396 mastitis Diseases 0.000 description 2
- 239000002304 perfume Substances 0.000 description 2
- 239000011550 stock solution Substances 0.000 description 2
- 239000013589 supplement Substances 0.000 description 2
- 241000283690 Bos taurus Species 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000428 dust Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000006193 liquid solution Substances 0.000 description 1
- 244000144972 livestock Species 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 239000005022 packaging material Substances 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000004549 water soluble granule Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Biophysics (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Fodder In General (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Non-Alcoholic Beverages (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
【解決手段】メロキシカム、メロキシカムのメグルミン、ナトリウム、カリウム、又はアンモニウムの塩形成剤、結合剤、砂糖又は甘味料、キャリア、任意に用いてよい香料、及び任意に用いてよい他の賦形剤を含む、水に素早く溶解するメロキシカム顆粒。
【選択図】なし
Description
したがって、本発明は、メロキシカム、メロキシカムのメグルミン、ナトリウム、カリウム、又はアンモニウムの塩形成剤、結合剤、砂糖又は甘味料、キャリア、任意に用いてよい香料、及び任意に用いてよい賦形剤、を含む水溶解性顆粒に関する。
本発明のメロキシカム顆粒は現存する製品よりも多くの利点を有する。
a)結合剤、任意に用いてよい砂糖又は甘味料、メロキシカム、メグルミン及び/又は香料を含む、水性顆粒形成用液体を製造する工程。
b)50℃から80℃、好ましくは65℃の一定の温度で供給される空気流を用いた上方噴霧流動床法により、キャリア上に顆粒形成用の液体を噴霧する工程。
c)続いて、上方噴霧流動床法により結合剤、砂糖又は甘味料及び/又は香料を含む水性顆粒形成用液体をコーティングする工程。
本発明のメロキシカム顆粒の特徴は、室温下で専用の包装に保存した場合、24ヶ月以上の長期間安定性を有するということである。
特に好ましいメロキシカム顆粒の製造物には、メロキシカム、メグルミン、ヒドロキシプロピルメチルセルロース、ポビドン、及びグルコースモノハイドレートを含む。
さらに、本発明は、動物における痛み、炎症、発熱、急性乳腺炎、下痢、凝り、運動障害及び呼吸器疾患、好ましくは急性乳腺炎、下痢、凝り、運動障害及び呼吸器疾患、最も好ましくは運動障害及び呼吸器疾患を処置する医薬組成物の製造のためのメロキシカム顆粒の使用に関する。
本発明の調合物は動物、好ましくは哺乳類に、特に豚、馬、牛、犬、又は猫などの家庭内ペット又は家畜、さらに好ましくは豚又は馬の処置に好適である。
本発明のメロキシカム顆粒は、活性物質の一回の投与量を体重1キロg当たり0.2〜1.0mgの範囲、好ましくは体重1キロg当たり0.4〜0.8mg、好ましくは体重1キロg当たり0.5〜0.7mg、さらに好ましくは体重1キロg当たり0.6mgとして用いるのが好適である。
本発明のメロキシカム顆粒を用いて、飲料水中及び補助飼料としても投与することのできる医薬組成物を製造するのも良い。
メグルミンの割合はメロキシカム顆粒中、0.035%と2.8パーセントの間、好ましくは0.07%から1.4%、好ましくは0.21%から1.05%、さらに好ましくは0.28%から0.7%、とくに約0.42%である。ナトリウム、カリウム、及びアンモニウムの可能な濃度は、それに応じて計算してよい。
結合剤の濃度は、顆粒1g中、20〜80mgの範囲、好ましくは30〜70mg、好ましくは40〜60mg、最も好ましくは50mgとしてよい。
砂糖の濃度は、顆粒1g中、50〜150mgの範囲、好ましくは75〜125mg、さらに好ましくは約100mgとしてよい。
甘味料の濃度は、顆粒1g中、1〜10mgの範囲、好ましくは2〜5mg、さらに好ましくは約3mgとしてよい。
キャリアの濃度は、顆粒1g中、800〜985mgの範囲、好ましくは900〜960mg、さらに好ましくは約930mgとしてよい。
香料の濃度は、顆粒1g中、0.1〜10mgの範囲、好ましくは0.2〜1.0mg、さらに好ましくは約0.5mgとしてよい。
0.6%メロキシカム顆粒
処方: g/100g
メロキシカム 0.6
メグルミン 0.42
ヒドロキシプロピルメチルセルロース 3.00
ポビドン 2.00
グルコースモノハイドレート 93.98
≪実施例2≫
1.2%メロキシカム顆粒
メロキシカム 1.2
メグルミン 0.84
ヒドロキシプロピルメチルセルロース 3.00
コーリドン25 2.0
グルコースモノハイドレート 92.96
≪実施例3≫
0.6%メロキシカム顆粒
メロキシカム 0.6
メグルミン 0.42
ファーマコート606(Pharmacoat 606) 4.0
マクロゴル6000 1.0
アセスルフェイムK(Acesulfame K) 0.3
ラクトース 93.68
≪実施例4≫
0.6%メロキシカム顆粒
メロキシカム 0.6
メグルミン 0.42
ファーマコート606 4.75
マクロゴル6000 0.25
アセスルフェイムK 0.3
液体バニラ香料 0.05
ラクトース 93.63
顆粒を、25℃、相対湿度60%下に3ヶ月間保存する。活性物質の含有量、水分の含有量(Karl-Fische法による)、見た目の溶解度特性、脱塩水中におけるpH、及び見た目の湿潤性に関して、重要な変化はまったく見られなかった。見た目の溶解度特性を決定するために、室温下で顆粒5gを脱塩水に溶解させた。約1分後、澄んだ黄色の溶液が得られた。
Claims (16)
- メロキシカム、結合剤、砂糖又は甘味料、キャリア、メロキシカムのメグルミン、ナトリウム、カリウム、又はアンモニウムの塩形成剤、任意に用いてよい香料、及び任意に用いてよい他の賦形剤を含む、水溶性の顆粒。
- 前記塩形成剤がメグルミンである、請求項1記載のメロキシカム顆粒。
- 前記結合剤が、ヒドロキシプロピル−メチルセルロース、ポリビニルピロリドン、ゼラチン、スターチ、及びポリエチレングリコールエーテルの中から選ばれる、請求項1又は2記載のメロキシカム顆粒。
- 前記砂糖又は甘味料が、サッカリンナトリウム、アスパルテーム、及びSunett(登録商標)の中から選ばれる、請求項1〜3のいずれか1項に記載のメロキシカム顆粒。
- 前記香料が、バニラ、蜂蜜味、リンゴ味、及びコントラマルムの中から選ばれる、請求項1〜4のいずれか1項に記載のメロキシカム顆粒。
- 前記キャリアが、ラクトース、グルコース、マンニトール、キシリトール、スクロース、及びソルビトールの中から選ばれる、請求項1〜5のいずれか1項に記載のメロキシカム顆粒。
- メロキシカムを0.05〜4%の割合で含む、請求項1〜6のいずれか1項に記載のメロキシカム顆粒。
- メグルミン及びメロキシカムを、モル比率9:8〜12:8で含む、請求項1〜7のいずれか1項に記載の顆粒。
- メグルミン及びメロキシカムを、モル比率10:8で含む、請求項1〜8のいずれか1項に記載の顆粒。
- 以下の工程a)〜c)が連続的に行われる、請求項1〜9のいずれか1項に記載の顆粒の製造方法。
a)結合剤、砂糖又は甘味料、メロキシカム、メグルミン及び/又は香料を含む、水性顆粒形成用液体を製造する工程。
b)50℃〜80℃の一定の温度で供給される空気流を用いた上方噴霧流動床法により、キャリア上に前記顆粒形成用液体を噴霧する工程。
c)続いて、上方噴霧流動床法により、結合剤、砂糖又は甘味料及び/又は香料を含む水性顆粒形成用液体をコーティングする工程。 - 前記顆粒形成用液体が、成分を70℃〜100℃で加熱、攪拌することにより製造される、請求項10記載の工程。
- 室温下で専用の包装に保存した場合、24ヶ月以上の長期間安定性を有する、請求項1〜9のいずれか1項に記載の顆粒。
- メロキシカム、メグルミン、ヒドロキシプロピルメチルセルロース、ポビドン、及びグルコースモノハイドレートを含む、請求項1〜9又は12のいずれか1項に記載の顆粒。
- 動物の、痛み、炎症、発熱、及び呼吸器疾患を処置する医薬品組成物を調整する、請求項1〜9又は12のいずれか1項に記載のメロキシカム顆粒の使用。
- 活性物質の一回の投与量を体重1キロg当たり0.2〜1.0mgの範囲とする、請求項13に記載のメロキシカム顆粒の使用。
- 飲料水中及び補助飼料として投与する医薬組成物を製造するための、請求項12又は13に記載のメロキシカム顆粒の使用。
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DE10250081A DE10250081A1 (de) | 2002-10-25 | 2002-10-25 | Wasserlösliche Meloxicam Granulate |
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DE10250081A1 (de) * | 2002-10-25 | 2004-05-13 | Boehringer Ingelheim Vetmedica Gmbh | Wasserlösliche Meloxicam Granulate |
EP1568369A1 (en) | 2004-02-23 | 2005-08-31 | Boehringer Ingelheim Vetmedica Gmbh | Use of meloxicam for the treatment of respiratory diseases in pigs |
DE102004030409A1 (de) * | 2004-06-23 | 2006-01-26 | Boehringer Ingelheim Vetmedica Gmbh | Neue Verwendung von Meloxicam in der Veterinärmedizin |
CN1680427B (zh) * | 2005-02-01 | 2010-08-11 | 杨喜鸿 | 易于水溶解的匹多莫德复盐及其制备方法 |
CN101222911A (zh) * | 2005-07-15 | 2008-07-16 | 特瓦制药工业有限公司 | 新的制粒方法及由此制备的颗粒 |
AU2006298895B9 (en) * | 2005-09-30 | 2013-01-24 | Boehringer Ingelheim Vetmedica Gmbh | Pharmaceutical preparation containing meloxicam |
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US7772255B2 (en) * | 2005-12-13 | 2010-08-10 | Supratek Pharma, Inc. | Method of treating tumors with azaxanthones |
KR100791160B1 (ko) * | 2006-05-30 | 2008-01-02 | 조선대학교산학협력단 | 멜록시캄의 에탄올아민염 및 이를 함유하는 약제학적조성물 |
JP2010083826A (ja) * | 2008-10-01 | 2010-04-15 | Nihon Generic Co Ltd | オキシカム系化合物を含む固形製剤を製造する方法 |
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CN102647971B (zh) | 2009-10-12 | 2016-03-16 | 贝林格尔.英格海姆维特梅迪卡有限公司 | 用于包含美洛昔康的组合物的容器 |
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RU2465892C1 (ru) * | 2011-09-21 | 2012-11-10 | Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Новосибирский национальный исследовательский государственный университет (НГУ)" | Способ получения высокодисперсного мелоксикама |
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US9526734B2 (en) * | 2014-06-09 | 2016-12-27 | Iceutica Pty Ltd. | Formulation of meloxicam |
WO2016086114A1 (en) * | 2014-11-25 | 2016-06-02 | Artdem, Llc | Sports drink formulation |
US20170281640A1 (en) * | 2016-04-04 | 2017-10-05 | Productos Maver, S.A. De C.V. | Pharmaceutical Compositions Containing a Muscle Relaxant and a Nonsteroidal Anti-Inflammatory Drugs (NSAID) |
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