NL8603150A - PREVENTIVE AND THERAPEUTIC PREPARATION AGAINST PARASITES AND METHOD FOR PREPARING THESE. - Google Patents
PREVENTIVE AND THERAPEUTIC PREPARATION AGAINST PARASITES AND METHOD FOR PREPARING THESE. Download PDFInfo
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- NL8603150A NL8603150A NL8603150A NL8603150A NL8603150A NL 8603150 A NL8603150 A NL 8603150A NL 8603150 A NL8603150 A NL 8603150A NL 8603150 A NL8603150 A NL 8603150A NL 8603150 A NL8603150 A NL 8603150A
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- preparation
- preventive
- sheep
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- therapeutic preparation
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
-1- t Λ ï-1- t Λ ï
Kenm.: 86-37. Int.Class.: A 01 N.Ref .: 86-37. Int.Class .: A 01 N.
Aanvrager: Barend Willem Hak, te Giessen.Applicant: Barend Willem Hak, in Giessen.
Preventief en therapeutisch preparaat tegen parasieten, alsmede werkwijze ter bereiding daarvan.Preventive and therapeutic preparation against parasites and a method for their preparation.
De onderhavige uitvinding heeft betrekking op de bereiding van een preventief en therapeutisch preparaat ter bestrijding van endoparasieten en ectoparasieten bij rundvee, schapen, geiten en varkens.The present invention relates to the preparation of a preventive and therapeutic composition for the control of endoparasites and ectoparasites in cattle, sheep, goats and pigs.
Een zodanig preparaat,dat een breedspectrum-werking heeft en als zodanig 5 zowel oraal als parenteraal kan worden toegepast,was nog niet bekend.Such a preparation, which has a broad spectrum effect and as such can be used both orally and parenterally, was not yet known.
Daar besmetting met ectoparasieten veelal het optreden van endoparasieten tot gevolg heeft, en het tijdstip van noodzakelijke therapie bij sommige dieren moeilijk te onderkennen is, vormt een preparaat met zodanige toepassingsmogelijkheden een uitkomst voor de veterinaire practijk.Since contamination with ectoparasites often results in the occurrence of endoparasites, and the time of necessary therapy in some animals is difficult to recognize, a preparation with such application possibilities is a solution for veterinary practice.
10 Als voorbeeld van een gevaarlijke runder- en schapenziekte diene de distomatose (leverbotziekte).10 An example of a dangerous bovine and sheep disease is distomatosis (liver fluke disease).
De zuigworm Fasciola hepatica treedt als larve in het leverbotslakje op, de cercariae encysteren zich op het gras, vooral op drassige weilanden, waardoor zij met het gras in rund en schaap geraken.The sucking worm Fasciola hepatica acts as a larva in the liver fluke, the cercariae encyst on the grass, especially on marshy meadows, so that they get into cattle and sheep with the grass.
15 De zuigworm komt dan in de galgangen voor, tast het epitheel aan en veroorzaakt leverbeschadiging.The suction worm then occurs in the bile ducts, attacks the epithelium and causes liver damage.
Gevonden werd een veterinair-farmaceutisch product met de brede eigenschappen als in de aanhef vermeld, dat in de vorm van een suspensie kan worden toegepast, en dat wordt bereid door 2,3,5,6-tetrahydro-6-fenyl-20 imidazo-2,1-thiazol-hydrochloride (benzimidazol) fijn verdeeld te mengen in een gewichtsverhouding van 2:1 met N-5-chloor-4-06-(4-chloorfenyl)-Λ-cyanomethyl-2-methylfenyl-2-hydroxy-3,5-dijodobenzamiiie> (Salicylanilide).A veterinary pharmaceutical product with the broad properties as mentioned in the preamble has been found, which can be used in the form of a suspension, and which is prepared by 2,3,5,6-tetrahydro-6-phenyl-20 imidazo Mix 2,1-thiazole hydrochloride (benzimidazole) in a 2: 1 weight ratio with N-5-chloro-4-06- (4-chlorophenyl) -Λ-cyanomethyl-2-methylphenyl-2-hydroxy- 3,5-diodobenzamyl (Salicylanilide).
Het benzimidazol heeft een verlammende werking op nematoden en longwormen.The benzimidazole has a paralyzing effect on nematodes and lungworms.
De wormen worden met de faeces uitgescheiden.The worms are excreted in the faeces.
25 De paralytische werking wordt toegeschreven aan een blokkering van een enzym^dat vereist is voor het metabolisme van de parasiet, (inhibitie van adenosinetrifosfaat), zonder dat het zoogdier schade ondervindt, omdat een in zoogdieren inactieve metaboliet wordt gevormd, die zonder problemen wordt afgescheiden.The paralytic activity is attributed to a blocking of an enzyme required for the metabolism of the parasite (inhibition of adenosine triphosphate), without harm to the mammal, because a metabolite which is inactive in mammals is formed and which is released without problems. .
' £ f . ? * Λ -2-£ f. ? * Λ -2-
Het salicylanilide heeft een doeltreffende werking tegen uiteenlopende soorten van parasieten, zoals nematoden, trematoden, doch ook arthnopoden, bij rundvee en schapen.Salicylanilide is effective against a wide variety of parasites, such as nematodes, trematodes, but also arthhnopods, in cattle and sheep.
Het bleek doelmatig ter bestrijding van leverbot (Fasciola hepatica, 5 Fasciola gigantica en Fascioloides magna), tegen bloedzuigende nematoden (Haemonchus, Oesophagostomum, Bunostomum en Strongyloides).It proved effective against liver flukes (Fasciola hepatica, 5 Fasciola gigantica and Fascioloides magna), against bloodsucking nematodes (Haemonchus, Oesophagostomum, Bunostomum and Strongyloides).
Het bleek nu ook zeer effectief te zijn bij de bestrijding van vormen van Haemonchus, die resistent zijn tegen benzimidazol.It has now also been found to be very effective in controlling forms of Haemonchus, which are resistant to benzimidazole.
Daar nu het salicylanilide naast deze eigenschap ook de larven van de 10 schapenvlieg (Oestrus ovis) en de rundervlieg (Hypoderma bovis) binnen enkele dagen doodt, werd het idee geboren de beide verbindingen te mengen, waarmede dan uit- en inwendige bestrijding bij het vee mogelijk bleek.Since the salicylanilide now also kills the larvae of the sheep fly (Oestrus ovis) and the bovine fly (Hypoderma bovis) in a few days in addition to this property, the idea was born to mix the two compounds, with which external and internal control in the cattle possibly turned out.
Het salicylanilide bleek vervolgens goede resultaten te hebben bij de bestrijding der larven van teken en luis (Boophilus microplus, Boophilus 15 decoloratus en Dermacentor), schapenvliegen (Cochliomya hominovorax) en het legsel van mijten (Psoroptes, Chorioptes en Sarcoptes).The salicylanilide subsequently appeared to have good results in the control of the larvae of ticks and lice (Boophilus microplus, Boophilus 15 decoloratus and Dermacentor), sheep flies (Cochliomya hominovorax) and the clutch of mites (Psoroptes, Chorioptes and Sarcoptes).
Ook deze verbinding remt het metabolisme van de parasieten, vooral van larven, terwijl de zoogdieren daarvan geen schade ondervinden.This compound also inhibits the metabolism of the parasites, especially larvae, while the mammals are not harmed.
Het salicylanilide wordt bereid door reactie van 2-nitro-4-chloortolueen 20 met chloorbenzyl-4-cyanide in alkalisch medium, het reactieproduct te reduceren tot 4-amino-2-chloor-{)C-4-chloorfenyl-5-methylfenylacetonitril, en dit met fosfor-trichloride om te zetten tot fosfaat,dat reageert met 3,5-dijodosalicylzuur tot N-5-chloor-4-06· (4-chloorfenyl) -Cx^cyanomethyl·^ methylfenyl-2— hydroxy-3,5-di jodobenzamicle.The salicylanilide is prepared by reacting 2-nitro-4-chlorotoluene 20 with chlorobenzyl-4-cyanide in alkaline medium, reducing the reaction product to 4-amino-2-chloro {{C-4-chlorophenyl-5-methylphenylacetonitrile, and converting it to phosphate with phosphorus trichloride, which reacts with 3,5-dijodosalicylic acid to N-5-chloro-4-06 · (4-chlorophenyl) -Cx ^ cyanomethyl · methyl-2-hydroxy-3, 5-di iodobenzamicle.
25 Het preparaat volgens de onderhavige uitvinding werd geformuleerd door een suspensie te bereiden van 100 g van het bovenvermelde benzimidazol en 50 g van het boven vermelde salicylanilide, en op te vullen tot 1 1 met propyieénglycoJL-ti aqua deskill at'Zt*^ zodat e^n ml van het preparaat 100 mg van het benzimidazol-hydrochloride en 50 mg van het salicylanilide 30 bevat.The composition of the present invention was formulated by preparing a suspension of 100 g of the above-mentioned benzimidazole and 50 g of the above-mentioned salicylanilide, and filling to 1 l with propylene glyco-Jl-ti aqua deskill at 2 ^ n ml of the preparation contains 100 mg of the benzimidazole hydrochloride and 50 mg of the salicylanilide 30.
Het preparaat wordt in ampullen van 100 ml afgevuld en is dan gereed voor subcutane injectie.The preparation is filled into 100 ml ampoules and is then ready for subcutaneous injection.
Het kan ook oraal worden gebruikt als .suspensie of als tablet (bolus).It can also be used orally as a suspension or as a tablet (bolus).
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Het product heeft als mengsel van een benzimidazol en een salicylanilide een breedspectrum-werking ten opzichte van elke van soortgelijke verbindingen als zodanig, als gevolg van de elkaar aanvullende werking van de twee componenten.The product, as a mixture of a benzimidazole and a salicylanilide, has a broad spectrum action relative to any of similar compounds per se, due to the complementary action of the two components.
5 Het is bestemd voor rundvee, varkens, schapen en geiten.5 It is intended for cattle, pigs, sheep and goats.
860 31 5 0 *860 31 5 0 *
Claims (3)
Priority Applications (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
NL8603150A NL8603150A (en) | 1986-12-11 | 1986-12-11 | PREVENTIVE AND THERAPEUTIC PREPARATION AGAINST PARASITES AND METHOD FOR PREPARING THESE. |
EP87201320A EP0272706B1 (en) | 1986-12-11 | 1987-07-13 | Method for manufacturing a veterinary medicine, and process for putting it into pharmaceutically applicable forms |
ES87201320T ES2052547T3 (en) | 1986-12-11 | 1987-07-13 | PROCEDURE FOR THE PRODUCTION OF A VETERINARY HEALING AND THERAPEUTIC AGENT, AS WELL AS PREPARATION TO GIVE PHARMACEUTICALLY APPLICABLE FORMS. |
DE8787201320T DE3782408D1 (en) | 1986-12-11 | 1987-07-13 | METHOD FOR PRODUCING A VETERINARY MEDICINAL PRODUCT AND PROCESSING IN PHARMACEUTICAL APPLICABLE FORMS. |
IE220187A IE60375B1 (en) | 1986-12-11 | 1987-08-18 | A method for producing a veterinary curative and for processing it into a pharmaceutically acceptable form |
GR920402462T GR3006126T3 (en) | 1986-12-11 | 1992-11-02 | |
NL930076C NL930076I1 (en) | 1986-12-11 | 1993-06-17 | Method of extending a veterinary drug |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
NL8603150 | 1986-12-11 | ||
NL8603150A NL8603150A (en) | 1986-12-11 | 1986-12-11 | PREVENTIVE AND THERAPEUTIC PREPARATION AGAINST PARASITES AND METHOD FOR PREPARING THESE. |
Publications (1)
Publication Number | Publication Date |
---|---|
NL8603150A true NL8603150A (en) | 1988-07-01 |
Family
ID=19848979
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
NL8603150A NL8603150A (en) | 1986-12-11 | 1986-12-11 | PREVENTIVE AND THERAPEUTIC PREPARATION AGAINST PARASITES AND METHOD FOR PREPARING THESE. |
NL930076C NL930076I1 (en) | 1986-12-11 | 1993-06-17 | Method of extending a veterinary drug |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
NL930076C NL930076I1 (en) | 1986-12-11 | 1993-06-17 | Method of extending a veterinary drug |
Country Status (6)
Country | Link |
---|---|
EP (1) | EP0272706B1 (en) |
DE (1) | DE3782408D1 (en) |
ES (1) | ES2052547T3 (en) |
GR (1) | GR3006126T3 (en) |
IE (1) | IE60375B1 (en) |
NL (2) | NL8603150A (en) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2801791B1 (en) * | 1999-12-03 | 2003-05-30 | Elpronat | COMPOSITION FOR ANIMALS CONTAINING METHYL SALICYLATE |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU527154B2 (en) * | 1978-12-15 | 1983-02-17 | Pitman-Moore Australia Limited | Composition and process |
-
1986
- 1986-12-11 NL NL8603150A patent/NL8603150A/en not_active Application Discontinuation
-
1987
- 1987-07-13 ES ES87201320T patent/ES2052547T3/en not_active Expired - Lifetime
- 1987-07-13 EP EP87201320A patent/EP0272706B1/en not_active Expired - Lifetime
- 1987-07-13 DE DE8787201320T patent/DE3782408D1/en not_active Expired - Lifetime
- 1987-08-18 IE IE220187A patent/IE60375B1/en not_active IP Right Cessation
-
1992
- 1992-11-02 GR GR920402462T patent/GR3006126T3/el unknown
-
1993
- 1993-06-17 NL NL930076C patent/NL930076I1/en unknown
Also Published As
Publication number | Publication date |
---|---|
IE60375B1 (en) | 1994-07-13 |
IE872201L (en) | 1988-06-11 |
GR3006126T3 (en) | 1993-06-21 |
EP0272706A3 (en) | 1990-02-07 |
NL930076I1 (en) | 1993-09-16 |
EP0272706A2 (en) | 1988-06-29 |
ES2052547T3 (en) | 1994-07-16 |
DE3782408D1 (en) | 1992-12-03 |
EP0272706B1 (en) | 1992-10-28 |
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