JP6117939B2 - ジクロフェナク組成物 - Google Patents
ジクロフェナク組成物 Download PDFInfo
- Publication number
- JP6117939B2 JP6117939B2 JP2015550212A JP2015550212A JP6117939B2 JP 6117939 B2 JP6117939 B2 JP 6117939B2 JP 2015550212 A JP2015550212 A JP 2015550212A JP 2015550212 A JP2015550212 A JP 2015550212A JP 6117939 B2 JP6117939 B2 JP 6117939B2
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- JP
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- Prior art keywords
- composition
- diclofenac
- solution
- sodium
- water
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims description 139
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 title claims description 74
- 229960001259 diclofenac Drugs 0.000 title claims description 64
- 239000000243 solution Substances 0.000 claims description 143
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 claims description 72
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 62
- JGMJQSFLQWGYMQ-UHFFFAOYSA-M sodium;2,6-dichloro-n-phenylaniline;acetate Chemical group [Na+].CC([O-])=O.ClC1=CC=CC(Cl)=C1NC1=CC=CC=C1 JGMJQSFLQWGYMQ-UHFFFAOYSA-M 0.000 claims description 61
- 229960001193 diclofenac sodium Drugs 0.000 claims description 59
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 claims description 50
- 239000007864 aqueous solution Substances 0.000 claims description 35
- 238000002347 injection Methods 0.000 claims description 34
- 239000007924 injection Substances 0.000 claims description 34
- 235000019445 benzyl alcohol Nutrition 0.000 claims description 24
- 229960004217 benzyl alcohol Drugs 0.000 claims description 24
- 208000002193 Pain Diseases 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 21
- 238000003756 stirring Methods 0.000 claims description 19
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 18
- 238000000034 method Methods 0.000 claims description 18
- 238000001356 surgical procedure Methods 0.000 claims description 15
- 239000002904 solvent Substances 0.000 claims description 13
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 claims description 12
- 229940001584 sodium metabisulfite Drugs 0.000 claims description 12
- 235000010262 sodium metabisulphite Nutrition 0.000 claims description 12
- 239000002738 chelating agent Substances 0.000 claims description 11
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 10
- 239000011734 sodium Substances 0.000 claims description 10
- 208000024891 symptom Diseases 0.000 claims description 10
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 9
- 239000003963 antioxidant agent Substances 0.000 claims description 9
- 235000006708 antioxidants Nutrition 0.000 claims description 9
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 9
- 239000003755 preservative agent Substances 0.000 claims description 9
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims description 9
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims description 8
- 239000004322 Butylated hydroxytoluene Substances 0.000 claims description 7
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 claims description 7
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 7
- 206010061218 Inflammation Diseases 0.000 claims description 7
- 208000004550 Postoperative Pain Diseases 0.000 claims description 7
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- 235000010354 butylated hydroxytoluene Nutrition 0.000 claims description 7
- 229940095259 butylated hydroxytoluene Drugs 0.000 claims description 7
- 230000004054 inflammatory process Effects 0.000 claims description 7
- PJUIMOJAAPLTRJ-UHFFFAOYSA-N monothioglycerol Chemical compound OCC(O)CS PJUIMOJAAPLTRJ-UHFFFAOYSA-N 0.000 claims description 7
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 7
- 208000005171 Dysmenorrhea Diseases 0.000 claims description 6
- 206010013935 Dysmenorrhoea Diseases 0.000 claims description 6
- QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 claims description 6
- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 claims description 6
- QPCDCPDFJACHGM-UHFFFAOYSA-N N,N-bis{2-[bis(carboxymethyl)amino]ethyl}glycine Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CC(O)=O QPCDCPDFJACHGM-UHFFFAOYSA-N 0.000 claims description 6
- 230000001154 acute effect Effects 0.000 claims description 6
- 230000003078 antioxidant effect Effects 0.000 claims description 6
- 235000010385 ascorbyl palmitate Nutrition 0.000 claims description 6
- 229940075557 diethylene glycol monoethyl ether Drugs 0.000 claims description 6
- 210000003205 muscle Anatomy 0.000 claims description 6
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 claims description 6
- 229940035024 thioglycerol Drugs 0.000 claims description 6
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 5
- 206010006811 Bursitis Diseases 0.000 claims description 5
- 201000005569 Gout Diseases 0.000 claims description 5
- 208000012659 Joint disease Diseases 0.000 claims description 5
- 208000019695 Migraine disease Diseases 0.000 claims description 5
- 208000023178 Musculoskeletal disease Diseases 0.000 claims description 5
- 208000010040 Sprains and Strains Diseases 0.000 claims description 5
- 208000000491 Tendinopathy Diseases 0.000 claims description 5
- 206010043255 Tendonitis Diseases 0.000 claims description 5
- 239000002221 antipyretic Substances 0.000 claims description 5
- 229940125716 antipyretic agent Drugs 0.000 claims description 5
- 229940072107 ascorbate Drugs 0.000 claims description 5
- 235000010323 ascorbic acid Nutrition 0.000 claims description 5
- 239000011668 ascorbic acid Substances 0.000 claims description 5
- 239000006184 cosolvent Substances 0.000 claims description 5
- GUBNMFJOJGDCEL-UHFFFAOYSA-N dicyclomine hydrochloride Chemical compound [Cl-].C1CCCCC1C1(C(=O)OCC[NH+](CC)CC)CCCCC1 GUBNMFJOJGDCEL-UHFFFAOYSA-N 0.000 claims description 5
- 229940110321 dicyclomine hydrochloride Drugs 0.000 claims description 5
- 206010027599 migraine Diseases 0.000 claims description 5
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 5
- 201000008482 osteoarthritis Diseases 0.000 claims description 5
- 229960005489 paracetamol Drugs 0.000 claims description 5
- 230000002335 preservative effect Effects 0.000 claims description 5
- 201000004415 tendinitis Diseases 0.000 claims description 5
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 4
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 claims description 4
- 206010027646 Miosis Diseases 0.000 claims description 4
- UEEJHVSXFDXPFK-UHFFFAOYSA-N N-dimethylaminoethanol Chemical compound CN(C)CCO UEEJHVSXFDXPFK-UHFFFAOYSA-N 0.000 claims description 4
- 208000014677 Periarticular disease Diseases 0.000 claims description 4
- 206010037660 Pyrexia Diseases 0.000 claims description 4
- 208000016247 Soft tissue disease Diseases 0.000 claims description 4
- 229960004308 acetylcysteine Drugs 0.000 claims description 4
- 235000019282 butylated hydroxyanisole Nutrition 0.000 claims description 4
- 229960004515 diclofenac potassium Drugs 0.000 claims description 4
- KXZOIWWTXOCYKR-UHFFFAOYSA-M diclofenac potassium Chemical compound [K+].[O-]C(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl KXZOIWWTXOCYKR-UHFFFAOYSA-M 0.000 claims description 4
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 claims description 4
- HXQVQGWHFRNKMS-UHFFFAOYSA-M ethylmercurithiosalicylic acid Chemical compound CC[Hg]SC1=CC=CC=C1C(O)=O HXQVQGWHFRNKMS-UHFFFAOYSA-M 0.000 claims description 4
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims description 4
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims description 4
- 229960002216 methylparaben Drugs 0.000 claims description 4
- 230000003547 miosis Effects 0.000 claims description 4
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 claims description 4
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 claims description 4
- 229960003415 propylparaben Drugs 0.000 claims description 4
- UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 0.000 claims description 4
- 229960002569 versetamide Drugs 0.000 claims description 4
- AXFGWXLCWCNPHP-UHFFFAOYSA-N versetamide Chemical compound COCCNC(=O)CN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC(=O)NCCOC AXFGWXLCWCNPHP-UHFFFAOYSA-N 0.000 claims description 4
- 239000003109 Disodium ethylene diamine tetraacetate Substances 0.000 claims description 3
- 208000003456 Juvenile Arthritis Diseases 0.000 claims description 3
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims description 3
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 claims description 3
- 208000009621 actinic keratosis Diseases 0.000 claims description 3
- 239000004480 active ingredient Substances 0.000 claims description 3
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 3
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 3
- 239000011575 calcium Substances 0.000 claims description 3
- 229910052791 calcium Inorganic materials 0.000 claims description 3
- 239000001201 calcium disodium ethylene diamine tetra-acetate Substances 0.000 claims description 3
- 235000011188 calcium disodium ethylene diamine tetraacetate Nutrition 0.000 claims description 3
- SHWNNYZBHZIQQV-UHFFFAOYSA-L calcium;disodium;2-[2-[bis(carboxylatomethyl)azaniumyl]ethyl-(carboxylatomethyl)azaniumyl]acetate Chemical compound [Na+].[Na+].[Ca+2].[O-]C(=O)C[NH+](CC([O-])=O)CC[NH+](CC([O-])=O)CC([O-])=O SHWNNYZBHZIQQV-UHFFFAOYSA-L 0.000 claims description 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 3
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 claims description 3
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims description 3
- 229960003330 pentetic acid Drugs 0.000 claims description 3
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 claims description 3
- 235000010265 sodium sulphite Nutrition 0.000 claims description 3
- 235000010384 tocopherol Nutrition 0.000 claims description 3
- 229930003799 tocopherol Natural products 0.000 claims description 3
- 239000011732 tocopherol Substances 0.000 claims description 3
- 229960001295 tocopherol Drugs 0.000 claims description 3
- 238000011541 total hip replacement Methods 0.000 claims description 3
- 206010019233 Headaches Diseases 0.000 claims description 2
- 206010068319 Oropharyngeal pain Diseases 0.000 claims description 2
- 201000007100 Pharyngitis Diseases 0.000 claims description 2
- 229940087168 alpha tocopherol Drugs 0.000 claims description 2
- 229940035676 analgesics Drugs 0.000 claims description 2
- 235000001465 calcium Nutrition 0.000 claims description 2
- 238000007865 diluting Methods 0.000 claims description 2
- 231100000869 headache Toxicity 0.000 claims description 2
- 230000002757 inflammatory effect Effects 0.000 claims description 2
- 239000012299 nitrogen atmosphere Substances 0.000 claims description 2
- 230000002980 postoperative effect Effects 0.000 claims description 2
- 235000013772 propylene glycol Nutrition 0.000 claims description 2
- GNBVPFITFYNRCN-UHFFFAOYSA-M sodium thioglycolate Chemical compound [Na+].[O-]C(=O)CS GNBVPFITFYNRCN-UHFFFAOYSA-M 0.000 claims description 2
- 229940046307 sodium thioglycolate Drugs 0.000 claims description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-M succinate(1-) Chemical compound OC(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-M 0.000 claims description 2
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 claims description 2
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- UGDAWAQEKLURQI-UHFFFAOYSA-N 2-(2-hydroxyethoxy)ethanol;hydrate Chemical compound O.OCCOCCO UGDAWAQEKLURQI-UHFFFAOYSA-N 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical class CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- FJKROLUGYXJWQN-UHFFFAOYSA-N 4-hydroxybenzoic acid Chemical compound OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims 1
- 241000694440 Colpidium aqueous Species 0.000 claims 1
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- LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 description 10
- 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 description 9
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- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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Description
ジクロフェナクまたはその塩を含んで成る、経済的でありながら生理学的に有効な組成物を提供することが本発明の目的である。
本発明は、治療有効量のジクロフェナクまたはその塩を含んで成る医薬組成物を提供する。さらに本発明は、抗炎症剤、鎮痛剤、及び/または解熱剤から選定される他の医薬活性成分との組み合わせとしてジクロフェナクを含んで成る組成物を提供する。特に本発明は、ジクロフェナクナトリウム及びトランスクトール(Transcutol)を主溶媒としての水と共に含んで成る組成物を提供する。
本発明は、ジクロフェナクまたはその塩を含んで成る組成物を提供する。ジクロフェナク塩は、ジクロフェナクナトリウム、ジクロフェナクカリウム、ジクロフェナクジエチルアミン、ジクロフェナクジエタノールアミンまたはジクロフェナクβ−ジメチルアミノエタノールから選定される。従来の製剤化ジクロフェナクナトリウム注射液は、筋肉内投与に限定される。かかる限定は、静脈内の安全性プロファイルのためではなく、主に薬物の物理化学的特性に起因するものである。ジクロフェナクのナトリウム塩の水溶解性は乏しく、特に水溶液及び有機性溶液から結晶化しがちである。本発明は、様々な経路により投与するのに適した、水性組成物中の治療有効量のジクロフェナク、またはその塩を提供する。
対照として使用した他の市販のジクロフェナク組成物DYNAPAR AQ(Troika Indian 特許第231479号;米国特許第20080153914号対応)に対して、本発明に従い調製した製品(本明細書において“発明/試験品”と称す)の一つの薬物動態研究を行った。対照品として使用されるDYNAPAR AQは、ジクロフェナク(75mg)、グリコフロール及びベンジルアルコールを含んで成る。本発明に従い調製したサンプル(試験品)は、以下の組成物:ジクロフェナクナトリウム:7.5%(すなわち75mg)、トランスクトール:20%、ベンジルアルコール:2%、pH:7.5〜9.0を有する。生物学的同等性研究は、臨床研究施設で行った。
Claims (19)
- 5〜50%(wt/v)のジエチレングリコールモノエチルエーテルと主溶媒としての水との溶液中に、25〜200mg/mLのジクロフェナクまたはその塩を含んで成り、30℃で約1〜約5cpsの間の粘性を有する注射用の水性組成物。
- 前記ジクロフェナク塩が、ジクロフェナクナトリウム、ジクロフェナクカリウム、ジクロフェナクジエチルアミン、ジクロフェナクジエタノールアミンまたはジクロフェナクβ−ジメチルアミノエタノールから選定される、請求項1に記載された組成物。
- 前記組成物が、ベンジルアルコールを3%(v/v)以下の濃度で含んで成る、請求項1に記載された組成物。
- 前記組成物が、溶媒/共溶媒及び防腐剤をさらに含んで成る、請求項1に記載された組成物。
- 前記溶媒/共溶媒及び防腐剤が、アルコール、パラベン、メタ重亜硫酸ナトリウム、重亜硫酸ナトリウム、亜硫酸ナトリウム、プロピレングリコール、チオメロサール(thiomerosal)、グリセロール及びチオグリセロールまたはその組み合わせ、パルミチン酸アスコルビル、アスコルビン酸塩、トコフェロールα、α−トコフェロール水素コハク酸塩及びトコフェロール誘導体の混合物、及びチオグリコール酸ナトリウムから成る群から選定される、請求項4に記載された組成物。
- 前記防腐剤が、メタ重亜硫酸ナトリウムであり、且つ0.1〜1%の間の濃度で存在する、請求項1に記載された組成物。
- 前記組成物が、ナトリウムEDTA(エチレンジアミン四酢酸)、ジナトリウムEDTA、カルシウムジナトリウムEDTA、カルシウムベルセタミド(versetamide)Na、カルテリドール、及びDTPA(ジエチレントリアミンペンタ酢酸)から成る群から選定されるキレート剤を含んで成る、請求項1に記載された組成物。
- 前記使用されるキレート剤の量が、0.01〜0.05%の間である、請求項7に記載された組成物。
- 前記組成物が、投与用に、単位投与ボーラス注射液または複数の投与バイアルとして調製される、請求項1〜8のいずれか1項に記載された組成物。
- 前記組成物が、1〜5mL、好適には1〜3mLの溶液において調製され、且つ使用に先立ちさらに希釈されてもよい、請求項1〜9のいずれか1項に記載された組成物。
- 前記組成物が、1mLの溶液中に、25〜200mgのジクロフェナクまたはその塩、及び5〜50%(wt/v)のトランスクトールを主溶媒としての水と組み合わせて含んで成る、請求項1〜10のいずれか1項に記載された組成物。
- 前記組成物のpHが、7.5〜9.0の間である、請求項1〜11のいずれか1項に記載された組成物。
- 前記組成物が、抗炎症剤、鎮痛剤、及び/または解熱剤から選定される治療有効量の他の医薬活性成分をさらに含んで成る、請求項1に記載された組成物。
- 前記組成物が、チオグリセロール、アセチルシステイン、ブチル化ヒドロキシアニソール(BHA)及びブチル化ヒドロキシトルエン(BHT)、アスコルビン酸塩、パルミチン酸アスコルビル、メチルパラベン、プロピルパラベン、チオメルサール及び混合トコフェロール成分から成る群から選定される抗酸化物質をさらに含んで成る、請求項1に記載された組成物。
- 前記組成物が、治療有効量の塩酸ジシクロミンをさらに含んで成る、請求項1に記載された組成物。
- 前記組成物が、治療有効量のパラセタモールをさらに含んで成る、請求項1に記載された組成物。
- ジクロフェナクまたはその塩及びジエチレングリコールモノエチルエーテルを含んで成る注射用の水性組成物の調製方法であって、且つ
a.5〜50%(wt/v)のジエチレングリコールモノエチルエーテルに30〜50%の水を添加することにより水溶液を調製し;
b.窒素雰囲気下で、撹拌しながら、25mg〜200mgのジクロフェナクを前記水溶液中に添加し;
c.前記溶液のpHを7.5〜9.0の範囲に調節し;そして
d.前記溶液を希釈し、前記溶液中に所望の濃度のジクロフェナクを得ることを含んで成る方法。 - 頭痛、咽頭痛等の疼痛及び/または炎症症状、関節リウマチ、変形性関節症、強直性脊椎炎等の様々な筋骨格及び関節障害、滑液包炎及び腱炎等の関節周囲障害、捻挫及び筋違え等の軟部組織障害、腎疝痛、急性痛風、月経困難症、片頭痛及びいくつかの外科手術等の痛みを伴う症状を治療または予防するため;光線性角化症、発熱、手術後の疼痛、若年性特発性関節炎、急性の手術後の疼痛、手術中の縮瞳を管理するため;手術後の炎症を治療するため;又は、全人工股関節置換の疼痛を管理するための、5〜50%(wt/v)のジエチレングリコールモノエチルエーテルと主溶媒としての水との中に、25mg〜200mg/mLのジクロフェナクまたはその塩を含んで成る組成物。
- 手術後疼痛、滑液包炎、捻挫及び筋違え、腱炎、筋骨格及び関節障害に関連した疼痛及び炎症、急性痛風、月経困難症、腎疝痛、関節リウマチを治療または予防するため;手術後または手術中の炎症を治療するため;又は、全人工股関節置換の疼痛を管理するための、5〜50%(wt/v)のジエチレングリコールモノエチルエーテルと主溶媒としての水との中に、25mg〜200mg/mLのジクロフェナクまたはその塩を含んで成る組成物。
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IN3704/MUM/2012 | 2012-12-28 | ||
IN3704MU2012 | 2012-12-28 | ||
PCT/IN2013/000805 WO2014102824A1 (en) | 2012-12-28 | 2013-12-27 | Diclofenac composition |
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US (1) | US20140187635A1 (ja) |
EP (1) | EP2938325B8 (ja) |
JP (1) | JP6117939B2 (ja) |
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HK (1) | HK1211858A1 (ja) |
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KR101524473B1 (ko) * | 2014-12-22 | 2015-06-02 | 주식회사 한국팜비오 | 주사제 조성물 |
WO2016170401A1 (en) * | 2015-04-20 | 2016-10-27 | Umedica Laboratories Pvt. Ltd | Novel injectable composition of diclofenac sodium |
US11110073B2 (en) | 2017-03-24 | 2021-09-07 | Cadila Healthcare Limited | Storage stable aqueous injectable solution comprising diclofenac |
GB201720992D0 (en) * | 2017-12-15 | 2018-01-31 | Hooper Mark | A medical use |
GR1009729B (el) * | 2018-08-02 | 2020-05-15 | Win Medica Φαρμακευτικη Ανωνυμη Εταιρεια | Σταθερος ενεσιμος συνδυασμος |
KR20210093256A (ko) * | 2018-11-16 | 2021-07-27 | 세이가가쿠 고교 가부시키가이샤 | 의약 조성물 |
US20220280463A1 (en) | 2019-09-09 | 2022-09-08 | Ftf Pharma Private Limited | Pharmaceutical formulations comprising diclofenac |
US11707443B2 (en) | 2019-09-26 | 2023-07-25 | Rk Pharma Inc. | Storage stable aqueous parenteral solutions comprising diclofenac |
TW202140062A (zh) * | 2020-02-18 | 2021-11-01 | 丹麥商諾佛 儂迪克股份有限公司 | Glp-1組成物及其用途 |
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DE3324193A1 (de) | 1983-07-05 | 1985-01-17 | Troponwerke Gmbh & Co Kg | Depot-antiphlogistika |
DE3446873A1 (de) | 1984-12-21 | 1986-07-10 | Merckle Gmbh | Fluessige diclofenac-zubereitungen |
US5283067A (en) * | 1987-01-30 | 1994-02-01 | Ciba-Geigy Corporation | Parenteral suspensions |
EP0661050A1 (en) * | 1991-07-04 | 1995-07-05 | Taisho Pharmaceutical Co. Ltd | Analgesic |
US5389681A (en) | 1992-10-22 | 1995-02-14 | Ciba-Geigy Corporation | Parenteral solutions for diclofenac salts |
ZA949182B (en) | 1993-12-02 | 1995-07-26 | South African Druggists Ltd | Pharmaceutical composition |
JP4542743B2 (ja) * | 2002-12-26 | 2010-09-15 | Kdl株式会社 | ピリドン誘導体の溶液状医薬組成物 |
AU2004226323A1 (en) * | 2003-03-26 | 2004-10-14 | Becton, Dickinson And Company | Use of benzyl alcohol, and other phenolic preservatives to reduce pain during intradermal injection |
WO2005027977A2 (en) | 2003-09-22 | 2005-03-31 | Agis Industries (1983) Ltd. | Diclofenac compositions for the treatment of skin disorders |
US20050238674A1 (en) | 2004-03-10 | 2005-10-27 | Shimoda Biotech (Pty) Ltd. | Stable injectable compositions |
US20050214230A1 (en) * | 2004-03-23 | 2005-09-29 | J. B. Chemicals & Pharmaceuticals Ltd. | Novel stomatological gel |
US8809393B2 (en) * | 2005-02-01 | 2014-08-19 | Troikaa Pharmaceuticals Ltd | Injectable preparations of diclofenac and its pharmaceutically acceptable salts |
KR20080016689A (ko) * | 2005-05-27 | 2008-02-21 | 파나세아 바이오테크 리미티드 | 약물주사가 가능한 새로운 형태의 조성물 및 이러한조성물을 위한 조제방법 |
EA201100863A1 (ru) | 2008-11-28 | 2011-12-30 | Эдванс Холдингз Лимитед | Фармацевтическая композиция, включающая диклофенак и сложный эфир гидроксижирной кислоты и полиоксиалкилена |
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