JP4537708B2 - プレウロムチリン誘導体を含有する微小球体 - Google Patents
プレウロムチリン誘導体を含有する微小球体 Download PDFInfo
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- JP4537708B2 JP4537708B2 JP2003546857A JP2003546857A JP4537708B2 JP 4537708 B2 JP4537708 B2 JP 4537708B2 JP 2003546857 A JP2003546857 A JP 2003546857A JP 2003546857 A JP2003546857 A JP 2003546857A JP 4537708 B2 JP4537708 B2 JP 4537708B2
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- 239000004005 microsphere Substances 0.000 title claims description 79
- ZRZNJUXESFHSIO-VYTKZBNOSA-N pleuromutilin Chemical class C([C@H]([C@]1(C)[C@@H](C[C@@](C)(C=C)[C@@H](O)[C@@H]2C)OC(=O)CO)C)C[C@]32[C@H]1C(=O)CC3 ZRZNJUXESFHSIO-VYTKZBNOSA-N 0.000 title claims description 19
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- UURAUHCOJAIIRQ-QGLSALSOSA-N tiamulin Chemical compound CCN(CC)CCSCC(=O)O[C@@H]1C[C@@](C)(C=C)[C@@H](O)[C@H](C)[C@@]23CC[C@@H](C)[C@]1(C)[C@@H]2C(=O)CC3 UURAUHCOJAIIRQ-QGLSALSOSA-N 0.000 description 8
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- UGMCXQCYOVCMTB-UHFFFAOYSA-K dihydroxy(stearato)aluminium Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[Al](O)O UGMCXQCYOVCMTB-UHFFFAOYSA-K 0.000 description 4
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- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 description 1
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- QZCLKYGREBVARF-UHFFFAOYSA-N Acetyl tributyl citrate Chemical compound CCCCOC(=O)CC(C(=O)OCCCC)(OC(C)=O)CC(=O)OCCCC QZCLKYGREBVARF-UHFFFAOYSA-N 0.000 description 1
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- OBUUFWIMEGVAQS-UHFFFAOYSA-N Pleuromutenol Natural products CC1C(O)C(C)(C=C)CC(O)C2(C)C(C)CCC31C2C(=O)CC3 OBUUFWIMEGVAQS-UHFFFAOYSA-N 0.000 description 1
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- 125000004190 benzothiazol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N=C(*)SC2=C1[H] 0.000 description 1
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- 238000010790 dilution Methods 0.000 description 1
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- HNPSIPDUKPIQMN-UHFFFAOYSA-N dioxosilane;oxo(oxoalumanyloxy)alumane Chemical compound O=[Si]=O.O=[Al]O[Al]=O HNPSIPDUKPIQMN-UHFFFAOYSA-N 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
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- 235000011852 gelatine desserts Nutrition 0.000 description 1
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- 150000004676 glycans Chemical class 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 239000001087 glyceryl triacetate Substances 0.000 description 1
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- 238000010438 heat treatment Methods 0.000 description 1
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- 150000003840 hydrochlorides Chemical class 0.000 description 1
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- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
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- 229910052744 lithium Inorganic materials 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 125000005397 methacrylic acid ester group Chemical group 0.000 description 1
- 125000005395 methacrylic acid group Chemical group 0.000 description 1
- XJRBAMWJDBPFIM-UHFFFAOYSA-N methyl vinyl ether Chemical compound COC=C XJRBAMWJDBPFIM-UHFFFAOYSA-N 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
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- 235000015097 nutrients Nutrition 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 125000000962 organic group Chemical group 0.000 description 1
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- 125000005498 phthalate group Chemical class 0.000 description 1
- LFSXCDWNBUNEEM-UHFFFAOYSA-N phthalazine Chemical compound C1=NN=CC2=CC=CC=C21 LFSXCDWNBUNEEM-UHFFFAOYSA-N 0.000 description 1
- 125000005936 piperidyl group Chemical group 0.000 description 1
- 235000021118 plant-derived protein Nutrition 0.000 description 1
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 1
- 229920000058 polyacrylate Polymers 0.000 description 1
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- 239000011148 porous material Substances 0.000 description 1
- OVARTBFNCCXQKS-UHFFFAOYSA-N propan-2-one;hydrate Chemical compound O.CC(C)=O OVARTBFNCCXQKS-UHFFFAOYSA-N 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 description 1
- 125000001453 quaternary ammonium group Chemical group 0.000 description 1
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- 229960002771 retapamulin Drugs 0.000 description 1
- STZYTFJPGGDRJD-NHUWBDDWSA-N retapamulin Chemical compound C([C@H]([C@@]1(C)[C@@H](C[C@@](C)(C=C)[C@@H](O)[C@@H]2C)OC(=O)CS[C@@H]3C[C@H]4CC[C@H](N4C)C3)C)C[C@]32[C@H]1C(=O)CC3 STZYTFJPGGDRJD-NHUWBDDWSA-N 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 125000005624 silicic acid group Chemical class 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
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- 239000002600 sunflower oil Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 239000004753 textile Substances 0.000 description 1
- 150000003557 thiazoles Chemical class 0.000 description 1
- CBDKQYKMCICBOF-UHFFFAOYSA-N thiazoline Chemical compound C1CN=CS1 CBDKQYKMCICBOF-UHFFFAOYSA-N 0.000 description 1
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- 229960002622 triacetin Drugs 0.000 description 1
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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
- A61K9/14—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
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K20/00—Accessory food factors for animal feeding-stuffs
- A23K20/10—Organic substances
- A23K20/195—Antibiotics
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K40/00—Shaping or working-up of animal feeding-stuffs
- A23K40/20—Shaping or working-up of animal feeding-stuffs by moulding, e.g. making cakes or briquettes
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K40/00—Shaping or working-up of animal feeding-stuffs
- A23K40/25—Shaping or working-up of animal feeding-stuffs by extrusion
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K40/00—Shaping or working-up of animal feeding-stuffs
- A23K40/30—Shaping or working-up of animal feeding-stuffs by encapsulating; by coating
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K50/00—Feeding-stuffs specially adapted for particular animals
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K50/00—Feeding-stuffs specially adapted for particular animals
- A23K50/60—Feeding-stuffs specially adapted for particular animals for weanlings
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
Landscapes
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Polymers & Plastics (AREA)
- Engineering & Computer Science (AREA)
- Health & Medical Sciences (AREA)
- Food Science & Technology (AREA)
- Zoology (AREA)
- Animal Husbandry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Fodder In General (AREA)
- Medicinal Preparation (AREA)
Description
d)−CH2−S−(CH2)k−N(R5)(R6)(式中、kは2から5の整数であり;R5およびR6は、それぞれが互いに独立して、C1〜6アルキルである);
e)−CH2−S−C(CH3)2−CH2−NH−C(O)−R7(式中、R7は、−NH2により置換されるC1〜6アルキルであるか、あるいは、−S−および−NH−から選択される1つまたは2つのヘテロ原子を含有する飽和した5員複素環である);
f)−CH2−S−C(CH2)l−R8(式中、lは0または1であり;R8は、下記の基:
g)−CH3、−CH2Cl、CH2Br、−CH2SCN、−CH2−NH2、−CH2−N3、−CO−OH、−CH2−OCOCH3、または下記の基:
の1つであり;
(B)二重結合が炭素原子1と炭素原子2との間に存在し、RaおよびRbがHであり、Tが、下記の群i:
i)−CH2−CO−R12(式中、R12は、非置換または置換の窒素含有の5員複素環または6員複素環、非置換または置換のアリール基、あるいは、基−CH2−R13であり、R13はハロゲンまたは−SR14であり、R14は、アミノ−C1〜6アルキル、あるいは、非置換または置換の窒素含有の5員複素環または6員複素環、あるいは、非置換または置換のアリール基であり、前記複素環基またはアリール基に対する置換基は、OH、CN、NO2、N3、C1〜6アルキル、C1〜6アルコキシ、C1〜6アルコキシ−C1〜6アルキル、ジ−N−C1〜6アルキルアミノ、C1〜6アシルアミノ、C1〜6アシルカルボニルアミノ、C1〜6アシルオキシ、C1〜6カルバモイル、モノ−N−C1〜6アルキルカルバモイル、ジ−N−C1〜6アルキルカルバモイル、C1〜6アシルオキシカルボニル、C1〜6アルキルスルホニル、C1〜6アルキルスルフィニルおよびベンジルからなる群から選択される1個から3個の基である)
であり;
(C)単結合が炭素原子1と炭素原子2との間に存在し、RaがHまたはOHまたはFであり、かつRbがHであり、あるいは、RaがHであり、かつRbがFであり、Tが、下記の群k:
k)−CH2−CO−R12(式中、R12は、群iについて定義される通りである)
である)
が好ましく、これには、その生理学的に許容され得る酸付加塩および四級アンモニウム塩が含まれる。
R1がビニルであり;単結合が炭素原子1と炭素原子2との間に存在し;
RaおよびRbがHであり;そして
Tが−CH2−S−(CH2)k−N(R5)(R6)(式中、kは2から5の整数であり;R5およびR6は、それぞれが互いに独立して、C1〜6アルキルである)である。その群において、Tが−CH2−S−(CH2)2−N(C2H5)(C2H5)であるプレウロムチリン誘導体が非常に特に好ましい。
R1がビニルであり;単結合が炭素原子1と炭素原子2との間に存在し;
RaおよびRbがHであり、Tが−CH2−S−C(CH3)2−CH2−NH−C(O)−R7(式中、R7は、−NH2により置換されるC1〜6アルキルであるか、あるいは、−S−および−NH−から選択される1つまたは2つのヘテロ原子を含有する飽和した5員複素環である)である。その群において、Tが−CH2−S−C(CH3)2−CH2−NH−C(O)−R7(式中、R7は、−NH2により置換されるC1〜6アルキルである)であるプレウロムチリン誘導体が好ましく、特に、Tが−CH2−S−C(CH3)2−CH2−NH−C(O)−CH(NH2)−CH(CH3)2であるプレウロムチリン誘導体が好ましい。
欧州特許第0165577号は、飼料と混合された後、またはペレット化されたとき、改善された安定性を有し、長期間の貯蔵を可能にする、亜鉛バシトラシンを含む飼料添加物の提供に関する。改善された安定性は、亜鉛バシトラシンを含む飼料添加物にポリマー被覆を施すことによって達成され、この場合、多糖類、ポリアクリラート、脂肪、脂肪様化合物またはワックスなどのポリマーが被覆剤として使用されている。
Shigeru Goto他、Journal of Microencapsulation、1986、第3巻第4号、293〜305;
Shigeru Goto他、Journal of Microencapsulation、1986、第3巻第4号、305〜316、または米国特許第3714065号(これはドイツ国特許第2105039号に対応する)。
(a)セラックと、セルロース、アクリル酸もしくはメタクリル酸、無水マレイン酸、ポリビニルピロリドンまたはポリビニルアルコールに基づくポリマーとからなる群から選択される、微小球体に対するマトリックスの形成に好適なポリマーの溶液を、適する場合には水の添加とともに、パラフィン油またはシリコーン油に対する親和性が低く、誘電率が約10〜約40である有機溶媒に前記セラックまたは前記ポリマーを溶解することによって調製すること;
(b)プレウロムチリン誘導体をそのようなセラック溶液またはポリマー溶液に撹拌しながら導入し、その結果、パラフィン油またはシリコーン油と混和しない第1の有機相を形成させること;
(c)その第1の相を、パラフィン油またはシリコーン油からなる第2の油相に、例えば、静的ミキサーまたは高圧ホモジナイザーを使用して激しく撹拌しながら導入し、そして、溶媒をエバポレーションまたは除去したときにプレウロムチリン誘導体を含む微小球体が形成されるまで、得られた混合物の撹拌を続けること;
(d)微小球体を単離し、そして適する場合には洗浄および乾燥すること。
80gの活性物質(バルネムリン)を3920gの従来の粉砕および均質化された子ブタ用乾燥飼料に加え、スパイラルミキサーを使用して十分に混合する。それによって、4000gのプレミックスが得られる。この4000gのプレミックスを、100リットルのスパイラルミキサーにおいて、さらに36kgの従来の粉砕および均質化された子ブタ用乾燥飼料に加え、同様に十分に混合する。得られた40kgの部分混合物を、その後、さらに360kgの従来の粉砕および均質化された子ブタ用乾燥飼料に加えて、押し出し機に移し、長さが約10mmで、幅さが約6mmの棒形状の飼料ペレットに、68℃〜72℃および10kbar〜100kbarの圧力で圧縮成形する。圧縮成形プロセスの間、蒸気(2bar、136℃)が使用される。押し出し機の加熱部分における滞留時間は約75秒で設定される。完成したペレットは、それぞれが25kgの袋に充填される。
調製例2に従って、3タイプの子ブタ用飼料ペレット(A、BおよびC)が、異なる前処理を受けた有効成分ではあるが、同一量の有効成分を使用して調製される。タイプAのペレットは50%の市販ECONOR(登録商標)(有効成分:バルネムリン)を含み、この場合、有効成分はヒドロキシプロピルメチルセルロース(HPMC)で被覆される。タイプBのペレットは純粋な有効成分(バルネムリン)を塩酸塩の形態で含む。タイプCのペレットは、埋め込まれたバルネムリン塩酸塩を含む、調製例1に従って調製された微小球体を含む。
Claims (15)
- 下記の式I:
a)−CH 2 −OH;
b)下記の基:
d)−CH 2 −S−(CH 2 ) k −N(R 5 )(R 6 )(式中、kは2から5の整数であり;R 5 およびR 6 は、それぞれが互いに独立して、C 1〜6 アルキルである);
e)−CH 2 −S−C(CH 3 ) 2 −CH 2 −NH−C(O)−R 7 (式中、R 7 は、−NH 2 により置換されるC 1〜6 アルキルであるか、あるいは、−S−および−NH−から選択される1つまたは2つのヘテロ原子を含有する飽和した5員複素環である);
f)−CH 2 −S−C(CH 2 ) l −R 8 (式中、lは0または1であり;R 8 は、下記の基:
g)−CH 3 、−CH 2 Cl、CH 2 Br、−CH 2 SCN、−CH 2 −NH 2 、−CH 2 −N 3 、−CO−OH、−CH 2 −OCOCH 3 、または下記の基:
i)−CH 2 −CO−R 12 (式中、R 12 は、非置換または置換の窒素含有の5員複素環または6員複素環、非置換または置換のアリール基、あるいは、基−CH 2 −R 13 であり、R 13 はハロゲンまたは−SR 14 であり、R 14 は、アミノ−C 1〜6 アルキル、あるいは、非置換または置換の窒素含有の5員または6員複素環、あるいは、非置換または置換のアリール基であり、前記複素環基またはアリール基に対する置換基は、OH、CN、NO 2 、N 3 、C 1〜6 アルキル、C 1〜6 アルコキシ、C 1〜6 アルコキシ−C 1〜6 アルキル、ジ−N−C 1〜6 アルキルアミノ、C 1〜6 アシルアミノ、C 1〜6 アシルカルボニルアミノ、C 1〜6 アシルオキシ、C 1〜6 カルバモイル、モノ−N−C 1〜6 アルキルカルバモイル、ジ−N−C 1〜6 アルキルカルバモイル、C 1〜6 アシルオキシカルボニル、C 1〜6 アルキルスルホニル、C 1〜6 アルキルスルフィニルおよびベンジルからなる群から選択される1個から3個の基である);または
k)−CH 2 −CO−R 12 (式中、R 12 は、群iについて定義される通りである)から選択される基である)
を有するプレウロムチリン(pleuromutilin)誘導体を含む微小球体であって、前記プレウロムチリン誘導体が、平均サイズ1μmから5000μmの、ほとんどが球状のポリマーマトリックス粒子からなる微小球体に包まれ、前記微小球体全体に固体形態または液体形態で高度に分散されている前記微小球体。 - 式Iにおいて、
R1がエチルまたはビニルであり;
(A)単結合が炭素原子1と炭素原子2との間に存在し、RaおよびRbがHである場合は、Tが、請求項1に記載の基a〜iのいずれか1つであり;
(B)二重結合が炭素原子1と炭素原子2との間に存在し、RaおよびRbがHである場合は、Tが、請求項1に記載の基iであり;
(C)単結合が炭素原子1と炭素原子2との間に存在し、RaがHまたはFであり、かつRbがHであり、あるいは、RaがHであり、かつRbがFである場合は、Tが下記の基kであるプレウロムチリン誘導体またはその生理学的に許容され得る酸付加塩および四級アンモニウム塩を含む、請求項1に記載の微小球体。 - R1がビニルであり、単結合が炭素原子1と炭素原子2との間に存在し、RaおよびRbが水素またはハロゲンであり、Tが、式Iについて定義される通りであるプレウロムチリン誘導体またはその生理学的に許容され得る酸付加塩および四級アンモニウム塩を含む、請求項1に記載の微小球体。
- R1がビニルであり;単結合が炭素原子1と炭素原子2との間に存在し;RaおよびRbがHであり、Tが−CH2−S−(CH2)k−N(R5)(R6)(式中、kは2から5の整数であり;R5およびR6は、それぞれが互いに独立して、C1〜6アルキルである)であるプレウロムチリン誘導体またはその生理学的に許容され得る酸付加塩および四級アンモニウム塩を含む、請求項3に記載の微小球体。
- Tが−CH2−S−(CH2)2−N(C2H5)(C2H5)である、請求項4に記載の微小球体。
- R1がビニルであり;単結合が炭素原子1と炭素原子2との間に存在し;RaおよびRbがHであり、Tが−CH2−S−C(CH3)2−CH2−NH−C(O)−R7(式中、R7は、−NH2により置換されるC1〜6アルキルであるか、あるいは、−S−および−NH−から選択される1つまたは2つのヘテロ原子を含有する飽和した5員複素環である)であるプレウロムチリン誘導体またはその生理学的に許容され得る酸付加塩および四級アンモニウム塩を含む、請求項3に記載の微小球体。
- R1がビニルであり;単結合が炭素原子1と炭素原子2との間に存在し;RaおよびRbがHであり、Tが−CH2−S−C(CH3)2−CH2−NH−C(O)−R7(式中、R7は、−NH2により置換されるC1〜6アルキルである)であるプレウロムチリン誘導体またはその生理学的に許容され得る酸付加塩および四級アンモニウム塩を含む、請求項6に記載の微小球体。
- R1がビニルであり;単結合が炭素原子1と炭素原子2との間に存在し;RaおよびRbがHであり、Tが−CH2−S−C(CH3)2−CH2−NH−C(O)−CH(NH2)−CH(CH3)2であるプレウロムチリン誘導体またはその生理学的に許容され得る酸付加塩および四級アンモニウム塩を含む、請求項7に記載の微小球体。
- 微小球体が、セラックと、セルロース、アクリル酸もしくはメタクリル酸、無水マレイン酸、ポリビニルピロリドンまたはポリビニルアルコールに基づくポリマーとからなる群から選択される、微小球体の形成に好適なポリマーからなる、請求項1から8のいずれか一項に記載の微小球体。
- (a)セラックと、セルロース、アクリル酸もしくはメタクリル酸、無水マレイン酸、ポリビニルピロリドンまたはポリビニルアルコールに基づくポリマーとからなる群から選択される、微小球体に対するマトリックスの形成に好適なポリマーの溶液を、適する場合には水の添加とともに、パラフィン油またはシリコーン油に対する親和性が低く、誘電率が10から40である有機溶媒に前記セラックまたは前記ポリマーを溶解することによって調製すること、
(b)プレウロムチリン誘導体をそのようなセラック溶液またはポリマー溶液に撹拌しながら導入し、その結果、パラフィン油またはシリコーン油と混和しない第1の有機相を形成させること、
(c)そのような第1の相を、パラフィン油またはシリコーン油からなる第2の油相に、激しく撹拌しながら導入し、そして、溶媒をエバポレーションまたは除去したときにプレウロムチリン誘導体を含む微小球体が形成されるまで、得られた混合物の撹拌を続けること、
(d)微小球体を単離し、そして適する場合には洗浄および乾燥すること
を含む、請求項1から9のいずれか一項に記載されるプレウロムチリン誘導体を含む微小球体を調製するための方法。 - 粉砕された植物系乾燥飼料および/または動物系乾燥飼料のほかに、タンパク質、ビタミンおよびミネラルなどの添加物を伴うか、または伴うことなく、請求項1から9のいずれか一項に記載されるプレウロムチリン誘導体を含む微小球体の効果的な量を含む動物飼料ペレット。
- 飼育動物および生産用家畜における感染性疾患を処置する方法において使用される請求項11に記載の動物飼料ペレット。
- 飼育動物および生産用家畜における感染性疾患を処置するための動物飼料ペレットの調製における、請求項1から9のいずれか一項に記載の微小球体の使用。
- 微小球体の形態にある請求項1から9のいずれか一項に記載の微小球体を、粉砕および均質化された有機飼料成分と十分に混合すること、5重量%から10重量%の水または蒸気で湿らし、60℃から80℃の高温で棒状物に圧縮成形すること、そして、そのような棒状物を飼料ペレットに分割することを含む、請求項1から9のいずれか一項に記載の微小球体を含む動物飼料ペレットを調製する方法。
- 微小球体が、前記ポリマーに基づいて3重量%から10重量%の可塑剤を含有する、請求項9に記載のプレウロムチリン誘導体を含む微小球体。
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2007
- 2007-07-19 CY CY20071100963T patent/CY1106745T1/el unknown
Also Published As
Publication number | Publication date |
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KR100965017B1 (ko) | 2010-06-21 |
WO2003045354A1 (en) | 2003-06-05 |
RU2296004C2 (ru) | 2007-03-27 |
ATE363270T1 (de) | 2007-06-15 |
BR0214521A (pt) | 2004-10-26 |
WO2003045354A8 (en) | 2004-08-26 |
AU2002356740A1 (en) | 2003-06-10 |
CN1592608A (zh) | 2005-03-09 |
RU2004119815A (ru) | 2006-01-10 |
JP2005523243A (ja) | 2005-08-04 |
CY1106745T1 (el) | 2012-05-23 |
ES2284980T3 (es) | 2007-11-16 |
US20050070486A1 (en) | 2005-03-31 |
DK1450767T3 (da) | 2007-08-13 |
EP1450767A1 (en) | 2004-09-01 |
NZ533085A (en) | 2005-10-28 |
CA2466671C (en) | 2011-03-29 |
AR038367A1 (es) | 2005-01-12 |
CN100348185C (zh) | 2007-11-14 |
BR0214521B1 (pt) | 2014-05-27 |
KR20040058334A (ko) | 2004-07-03 |
CA2466671A1 (en) | 2003-06-05 |
PT1450767E (pt) | 2007-09-05 |
US8236851B2 (en) | 2012-08-07 |
DE60220436D1 (de) | 2007-07-12 |
DE60220436T2 (de) | 2008-01-31 |
MXPA04005186A (es) | 2004-08-11 |
AU2002356740B2 (en) | 2006-06-15 |
EP1450767B1 (en) | 2007-05-30 |
ZA200403801B (en) | 2006-05-31 |
CO5390081A1 (es) | 2004-04-30 |
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