CN1137687C - 口服托三嗪砜的半固体含水制剂 - Google Patents
口服托三嗪砜的半固体含水制剂 Download PDFInfo
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- CN1137687C CN1137687C CNB998069302A CN99806930A CN1137687C CN 1137687 C CN1137687 C CN 1137687C CN B998069302 A CNB998069302 A CN B998069302A CN 99806930 A CN99806930 A CN 99806930A CN 1137687 C CN1137687 C CN 1137687C
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- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
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Abstract
本发明涉及托三嗪砜的口服糊剂，除防腐剂和润湿剂之外，该糊剂还含有浓度为0.1-20%(重量)、粒度为1-10·10-6m的活性物质和聚合度为约3·106、浓度为0.1-5%(重量)的聚丙烯酸，剩余部分由加至总量100%的水组成。
Description
本发明涉及口服半固体含水制剂，其中含有1-甲基-3-[4-[(三氟甲基)磺酰基]苯氧基]-间甲苯基]-s-三嗪-2，4，6(1H，3H，5H)-三酮(＝托三嗪砜)作为活性成分。
托三嗪砜在动物球虫病和类似疾病的组合物中用作活性化合物(US-P 4219552，DE-P 2718799)。
通常，该组合物为活性成分的溶液，活性成分经用水稀释后，通过动物饮水给药(EP-A 116175)。该组合物还可以是粉末和颗粒形式，该粉末和颗粒与未经治疗的动物的饲料混合在一起。
如果活性化合物仅仅是微溶于水中，则用合适的悬浮剂制备活性化合物的水悬浮液。为此，需将活性化合物经湿法研磨微粉化并与悬浮剂和水混合。然后通过加入增稠剂由该悬浮液制备半固体或糊状制剂。托三嗪砜经湿法研磨微粉化后得到的产品无法进一步加工。因此，采用常规方法不可能制得稳定的托三嗪砜悬浮液。因此，同样不可能以常规方法制得含有托三嗪砜作为活性化合物的糊剂。
如果托三嗪砜通过干法微粉化，则活性化合物预期的粒度将使得仅仅使用非常高浓度的悬浮剂才可能制得活性化合物的稳定水悬浮液。
然而，直接服用而无需进一步稀释的组合物例如口服糊剂应当使用尽可能少的添加剂进行制备。但是，以常规方法制备的托三嗪砜糊剂除了添加剂之外，含有高浓度的悬浮剂。
本发明涉及托三嗪砜的口服糊剂，其特征在于：
a)含有粒度为1·10-6m至最大50·10-6m、含量为0.1-20％(重量)的活性化合物，
b)含有其中丙烯酸含量为56％至68％(重量)、分子量为约3·106并用碱金属或碱土金属碱中和的、含量为0.1-5％(重量)的聚丙烯酸，
c)任选地含有含量为5-30％(重量)的润湿剂，
d)任选地含有含量为0.01-0.5％(重量)的防腐剂，
e)以及加余量水至100％。
在本发明的制剂中，活性化合物的含量优选为5％-20％(重量)、更优选10％-15％(重量)。
聚丙烯酸优选用碱金属氢氧化物或碱土金属碳酸盐中和。本发明的制剂含有浓度为0.2％-1％、优选0.5％(重量)的聚丙烯酸。这些聚丙烯酸是可以购买到并且在药典中已知的，例如商品名为Carbomer 934P的聚丙烯酸。
优选的防腐剂是对羟基苯甲酸酯(parabenes)例如4-羟基苯甲酸甲酯、4-羟基苯甲酸乙酯或4-羟基苯甲酸丙酯。为了达到足够的防腐效果，防腐剂可以单独使用或者结合使用。通常防腐剂的浓度为0.01-5％(重量)。
该制剂还可以任选地含有润湿剂例如甘油或1，2-丙二醇。润湿剂的使用浓度为5％-30％、优选10％-20％(重量)。
所含活性化合物的粒度为1-10·10-6m、优选1-5·10-6m。粒度最大为50·10-6m、优选为30·10-6m。
通过干法研磨得到所需的活性化合物的粒度分布。
为此，例如，在扁圆柱体空气喷射式碾磨机中，使用加压空气以5-6巴的压力，每小时将20千克活性化合物微粉化。
通过将每种成分混合得到本发明的组合物。通过增加或减少水的含量可以调节其稠度。所需稠度是糊状稠度。这使得该组合物可以用适宜的给药器例如注射器、管、药刀等口服给药。
本发明组合物特别适用于对抗许多哺乳动物的球虫病和类似的疾病，所述哺乳动物是例如马科(如马、驴等)、反刍动物(例如牛、绵羊、山羊、骆驼或相关的物种等)、猪、狗、猫、兔子、啮齿动物或其他哺乳动物。可以治疗所有年龄组的上述动物。球虫病和类似的疾病应理解为是被处于传染期的各球虫种例如艾美球虫属(Eimeria)，等孢子球虫属(isospora)，Castoisospora，Sarkocystis，弓形体属(Toxoplasma)，新孢子球虫属(Neospora)或Cryptosporidae传染。所治疗的动物可以是最终的宿主或是中间宿主。所产生的疾病可以不同(例如多数球虫病表现为腹泻、在EPM的情况下表现为运动系统紊乱、流产等)。因此，很难给出建议用量。通常，以每千克体重最高30mg活性化合物的剂量一次或重复给药是有效的。
本发明的糊剂还可以与动物饲料混合。
实施例1
口服或与动物饲料混合的糊剂
组合物：
托三嗪砜 15克
聚丙烯酸 0.5克
氢氧化钠 0.1克
1，2-丙二醇 20克
对羟基苯甲酸丙酯 0.02克
对羟基苯甲酸甲酯 0.14克
水 适量至100克制备
将各组分在一起搅拌。形成可以装填到适当施药器中的半固体含水制剂。
Claims (3)
1.托三嗪砜的口服糊剂，其特征在于：
a)含有粒度为1·10-6m至最大50·10-6m、含量为0.1-20％(重量)的活性化合物，
b)含有其中丙烯酸含量为56％至68％(重量)、分子量为约3·106并用碱金属或碱土金属碱中和的、含量为0.1-5％(重量)的聚丙烯酸，
c)任选地含有含量为5-30％(重量)的润湿剂，
d)任选地含有含量为0.01-0.5％(重量)的防腐剂，
e)以及加余量水至100％。
2.权利要求1的糊剂在制备口服治疗动物球虫病的药物中的应用。
3.制备权利要求1的糊剂的方法，其特征在于将活性化合物微粉化并与其他组分混合。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19824483.5 | 1998-06-02 | ||
| DE19824483A DE19824483A1 (de) | 1998-06-02 | 1998-06-02 | Halbfeste wäßrige Zubereitungen für orale Applikation von Toltrazuril-Sulfon |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1304310A CN1304310A (zh) | 2001-07-18 |
| CN1137687C true CN1137687C (zh) | 2004-02-11 |
Family
ID=7869584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB998069302A Expired - Lifetime CN1137687C (zh) | 1998-06-02 | 1999-05-20 | 口服托三嗪砜的半固体含水制剂 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US6436935B1 (zh) |
| EP (1) | EP1091740B1 (zh) |
| JP (1) | JP4958336B2 (zh) |
| KR (1) | KR100717832B1 (zh) |
| CN (1) | CN1137687C (zh) |
| AT (1) | ATE279926T1 (zh) |
| AU (1) | AU756372B2 (zh) |
| BR (1) | BR9910936B1 (zh) |
| CA (1) | CA2333680C (zh) |
| DE (2) | DE19824483A1 (zh) |
| DK (1) | DK1091740T3 (zh) |
| ES (1) | ES2232143T3 (zh) |
| HK (1) | HK1038702B (zh) |
| HU (1) | HU228500B1 (zh) |
| NZ (1) | NZ508513A (zh) |
| PL (1) | PL193534B1 (zh) |
| PT (1) | PT1091740E (zh) |
| WO (1) | WO1999062519A1 (zh) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6150361A (en) * | 1998-12-22 | 2000-11-21 | Bayer Corporation | Triazineone compounds for treating diseases due to sarcosystis, neospora and toxoplasma |
| DE10040174A1 (de) * | 2000-08-17 | 2002-02-28 | Bayer Ag | Verwendung von Triazintrion-Sulfonen zur Bekämpfung von Coccidiosen |
| DE10040110A1 (de) * | 2000-08-17 | 2002-02-28 | Bayer Ag | Verwendung von Triazintrion-Sulfoxiden zur Bekämpfung von Coccidiosen |
| DE102004001558A1 (de) * | 2004-01-10 | 2005-08-18 | Bayer Healthcare Ag | Arzneimittel zur topischen Applikation bei Tieren |
| DE102007025908A1 (de) | 2007-06-01 | 2008-12-04 | Bayer Healthcare Ag | Formulierungen enthaltend Triazinone und Eisen |
| SI22751A (sl) * | 2008-04-03 | 2009-10-31 | Krka, D.D., Novo Mesto | Toltrazuril z izboljĺ animi lastnostmi za raztapljanje |
| DE102009012423A1 (de) * | 2009-03-10 | 2010-09-16 | Bayer Animal Health Gmbh | Zubereitung auf Ölbasis |
| EP2740469A1 (en) | 2012-12-07 | 2014-06-11 | Ceva Sante Animale | New treatments with triazines |
| EP2740492A1 (en) | 2012-12-07 | 2014-06-11 | Ceva Sante Animale | Triazine formulations with a second active ingredient and surfactant(s) |
| EP2740470A1 (en) | 2012-12-07 | 2014-06-11 | Ceva Sante Animale | Treatment of Coccidiosis with intramuscular triazine composition |
| EP3578182A1 (en) | 2018-06-05 | 2019-12-11 | Bayer Animal Health GmbH | Formulations containing triazinones and iron with a low amount of free iron ions |
| EP3578181A1 (en) | 2018-06-05 | 2019-12-11 | Bayer Animal Health GmbH | Formulation for use in the simultaneous treatment of coccidial infections and iron deficiencies |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2718799A1 (de) * | 1977-04-27 | 1978-11-09 | Bayer Ag | 1-(4-phenoxy-phenyl)-1,3,5-triazin- derivate, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel und wachstumsfoerderer |
| DE3300793A1 (de) * | 1983-01-12 | 1984-07-12 | Bayer Ag, 5090 Leverkusen | Coccidiosemittel |
| US4755386A (en) * | 1986-01-22 | 1988-07-05 | Schering Corporation | Buccal formulation |
| DE19519821A1 (de) | 1995-05-31 | 1996-12-05 | Bayer Ag | Mittel gegen parasitäre Protozoen |
| DE19603984A1 (de) * | 1996-02-05 | 1997-08-07 | Bayer Ag | Granulate von Triazinen |
| US5883095A (en) * | 1997-08-07 | 1999-03-16 | University Of Kentucky Research Foundation | Formulations and methods to treat and prevent equine protozoal myeloencephalitis |
| BR9808114A (pt) * | 1997-03-31 | 2000-03-08 | David Granstrom | Formulação de ração para cavalos utilizável para tratar epm, processos para tratar pm em um cavalo que necessita deste tratamento, para prevenir infecção com s. neutrona em cavalos, e, para exterminar s. neurona em cavalos |
-
1998
- 1998-06-02 DE DE19824483A patent/DE19824483A1/de not_active Withdrawn
-
1999
- 1999-05-20 EP EP99926343A patent/EP1091740B1/de not_active Expired - Lifetime
- 1999-05-20 US US09/701,087 patent/US6436935B1/en not_active Expired - Lifetime
- 1999-05-20 DK DK99926343T patent/DK1091740T3/da active
- 1999-05-20 WO PCT/EP1999/003462 patent/WO1999062519A1/de not_active Application Discontinuation
- 1999-05-20 NZ NZ508513A patent/NZ508513A/xx not_active IP Right Cessation
- 1999-05-20 AT AT99926343T patent/ATE279926T1/de active
- 1999-05-20 PL PL99344329A patent/PL193534B1/pl unknown
- 1999-05-20 PT PT99926343T patent/PT1091740E/pt unknown
- 1999-05-20 CA CA002333680A patent/CA2333680C/en not_active Expired - Lifetime
- 1999-05-20 JP JP2000551775A patent/JP4958336B2/ja not_active Expired - Lifetime
- 1999-05-20 CN CNB998069302A patent/CN1137687C/zh not_active Expired - Lifetime
- 1999-05-20 KR KR1020007012499A patent/KR100717832B1/ko not_active IP Right Cessation
- 1999-05-20 AU AU43642/99A patent/AU756372B2/en not_active Expired
- 1999-05-20 BR BRPI9910936-0A patent/BR9910936B1/pt not_active IP Right Cessation
- 1999-05-20 HU HU0102007A patent/HU228500B1/hu unknown
- 1999-05-20 ES ES99926343T patent/ES2232143T3/es not_active Expired - Lifetime
- 1999-05-20 DE DE59910906T patent/DE59910906D1/de not_active Expired - Lifetime
-
2002
- 2002-01-16 HK HK02100359.3A patent/HK1038702B/zh not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| HK1038702A1 (en) | 2002-03-28 |
| ATE279926T1 (de) | 2004-11-15 |
| AU756372B2 (en) | 2003-01-09 |
| JP2002516862A (ja) | 2002-06-11 |
| ES2232143T3 (es) | 2005-05-16 |
| EP1091740A1 (de) | 2001-04-18 |
| US6436935B1 (en) | 2002-08-20 |
| JP4958336B2 (ja) | 2012-06-20 |
| PL193534B1 (pl) | 2007-02-28 |
| AU4364299A (en) | 1999-12-20 |
| EP1091740B1 (de) | 2004-10-20 |
| CA2333680C (en) | 2009-05-19 |
| KR20010043453A (ko) | 2001-05-25 |
| HK1038702B (zh) | 2004-12-10 |
| HUP0102007A2 (hu) | 2001-11-28 |
| BR9910936A (pt) | 2001-03-06 |
| DE59910906D1 (de) | 2004-11-25 |
| BR9910936B1 (pt) | 2010-11-16 |
| HU228500B1 (en) | 2013-03-28 |
| CN1304310A (zh) | 2001-07-18 |
| PT1091740E (pt) | 2004-12-31 |
| PL344329A1 (en) | 2001-10-22 |
| KR100717832B1 (ko) | 2007-05-11 |
| CA2333680A1 (en) | 1999-12-09 |
| HUP0102007A3 (en) | 2003-10-28 |
| WO1999062519A1 (de) | 1999-12-09 |
| NZ508513A (en) | 2002-09-27 |
| DE19824483A1 (de) | 1999-12-09 |
| DK1091740T3 (da) | 2005-01-24 |
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