DK143438B - GEL-FORM OF VEGETABLE OIL BASED BARE FOR PREPARATIONS FOR TREATMENT OF MASTITIS OF Dairy animals - Google Patents
GEL-FORM OF VEGETABLE OIL BASED BARE FOR PREPARATIONS FOR TREATMENT OF MASTITIS OF Dairy animals Download PDFInfo
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- DK143438B DK143438B DK106175AA DK106175A DK143438B DK 143438 B DK143438 B DK 143438B DK 106175A A DK106175A A DK 106175AA DK 106175 A DK106175 A DK 106175A DK 143438 B DK143438 B DK 143438B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0041—Mammary glands, e.g. breasts, udder; Intramammary administration
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Description
143438 i o143438 in o
Den foreliggende opfindelse angår en gelformet, på vegetabilsk olie baseret bærer til præparater til behandling af mastitis hos malkedyr ved intramammal infusion.The present invention relates to a gel-shaped, vegetable oil-based carrier for preparations for treating mastitis in dairy animals by intramammal infusion.
Mastitis er en inflammationstilstand i mælkekirt-5 lerne, og den kan forekomme hos alle pattedyr, men bovin mastitis er af størst økonomisk betydning.Mastitis is an inflammatory condition of the mammary glands and it can occur in all mammals, but bovine mastitis is of the greatest economic importance.
Bovin mastitis er almindeligvis forårsaget af én eller flere mikroorganismer såsom Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus aureus, Aerobacter 10 aerogenes, Escherichia coll, Pseudomonas aeruginosa, Sal-monelle enteritidis, Clostridium perfingens og Coryne-bacterium pygenes, der trænger op i yveret gennem patteka-nalen og giver inflammation af det mælkeproducerende væv under dannelse af arvæv, som, når det en gang er dannet, kan 15 bevirke en permanent formindskelse af køers mælkeproduktion.Bovine mastitis is commonly caused by one or more microorganisms such as Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus aureus, Aerobacter 10 aerogenes, Escherichia coll, Pseudomonas aeruginosa, Salmonella enteritidis, Clostridium perfingens and Poryne -nal and causes inflammation of the milk-producing tissue to form scar tissue which, once formed, can cause a permanent decrease in the milk production of cows.
En infektion kan også ændre mælkens sammensætning, mængde, udseende og kvalitet.An infection can also change the composition, quantity, appearance and quality of the milk.
Ætiologien for mastitis gør overvindelsen af problemet afhængig af den kritiske diagnose af det specifikke 20 mikrobe-middel, korrektionen for mangelfuld pasning af dyrene og den velovervejede anvendelse af intrammamal terapi.The etiology of mastitis makes overcoming the problem dependent on the critical diagnosis of the specific microbial agent, the correction for inadequate care of the animals, and the deliberate use of intrammamal therapy.
Den foreliggende opfindelse er baseret på den erkendelse, at man kan opnå en meget kort udmalkningstid for anti-mastitismedikamentet efter intramammal infusion af et 25 anti-mastitismedikament, når dette er dispergeret i en spe ciel bærer. Denne specielle bærer er gelformet og baseret på vegetabilsk olie og ifølge opfindelsen er den ejendommelig ved, at den er baseret på jordnøddeolie, sesamolie, majsolie, bomuldsfrøolie, sojabønneolie eller olivenolie eller 30 blandinger deraf og indeholder mellem ca. 0,5 og ca. 5,0 vægt-% af en fedtsyreester af glycerol, hvori fedtsyren er en langkædet, mættet eller umættet monocarboxylsyre med 12-20 carbonatomer.The present invention is based on the recognition that a very short milking time for the anti-mastitis drug can be achieved after intramammal infusion of an anti-mastitis drug when dispersed in a special carrier. This particular carrier is gel-shaped and based on vegetable oil and according to the invention it is characterized in that it is based on peanut oil, sesame oil, corn oil, cotton seed oil, soybean oil or olive oil or mixtures thereof and contains between 0.5 and approx. 5.0% by weight of a fatty acid ester of glycerol, wherein the fatty acid is a long chain, saturated or unsaturated monocarboxylic acid having 12-20 carbon atoms.
Selv om bovin mastitis er af størst økonomiske be-35 tydning og der for nemheds skyld i det følgende i hovedsagen vil blive refereret dertil, vil det være klart, at 143438 2Although bovine mastitis is of the utmost economic importance and will be referred to for convenience in the following in the main proceedings, it will be clear that
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bæreren ifølge opfindelsen også er anvendelig til præparater til andre malkedyr.the carrier of the invention is also useful for preparations for other dairy animals.
Bæreren ifølge opfindelsen har vist sig at være særlig fordelagtig i præparater til behandling af masti-5 tis på grund af den overraskende korte tid, som dermed opnås for udmalkning af anti-mastitismedikamentet, dvs. det tidsrum, der skal hengå, før et anti-mastitismedikament er forsvundet fra yveret efter den sidste intramammale infusion. Denne egenskab er af overordentlig stor betydning, da mælk 10 forurenet med et anti-mastitismedikament ikke kan anvendes som konsummælk eller forhandles til osteproduktion.The carrier of the invention has been found to be particularly advantageous in compositions for the treatment of mastitis due to the surprisingly short time thus obtained for milking the anti-mastitis drug, ie. the amount of time that must elapse before an anti-mastitis drug has disappeared from the udder after the last intramammal infusion. This characteristic is of great importance, as milk 10 contaminated with an anti-mastitis drug cannot be used as human milk or negotiated for cheese production.
Virkningen af bæreren på udmalkningstiden for anti--mastitismedikamenter har længe været anset for yderst vigtig ved sammensætningen af infusionspræparater mod mastitis.The effect of the carrier on the milking time of anti - mastitis drugs has long been considered extremely important in the composition of infusions for mastitis.
15 Hidtil er anti-mastitismedikamenter til intramammal infusion almindeligvis blevet dispergeret i et oliemedium såsom en mineralolie eller en vegetabilsk olie indeholdende et trivalent metalstearat såsom aluminiumonostearat, f.eks. et jordnøddeoliemedium indeholdende 3% aluminiumonostearat.Hitherto, anti-mastitis drugs for intramammal infusion have generally been dispersed in an oil medium such as a mineral oil or a vegetable oil containing a trivalent metal stearate such as aluminum onostearate, e.g. a peanut oil medium containing 3% aluminum onostate.
20 En ulempe ved intramammale infusionspræparater indeholdende et sådant stearat er imidlertid, at udmalkningstiden for anti-mastitismedikamentet ved anvendelse af sådanne præparater er temmelig lang.However, one drawback of intramammal infusion preparations containing such stearate is that the milking time of the anti-mastitis drug using such preparations is rather long.
Med den anvendte betegnelse "anti-mastitismedika-25 ment" menes et hvilket som helst antimikrobielt middel, der er effektivt til behandling af mastitis. Eksempler på anti-mastitismedikamenter, der kan anvendes sammen med bæreren ifølge opfindelsen, er penicillin, neomycin, novobiocin, lincomycin, dihydrosteptomycin, streptomycin, erythro-30 mycin, polymyzin, tetracyclin, oxytetracyclin, chlortetra-cyclin, clindamycin, nitrofurazon, cephalosporiner, samt analoge og derivater deraf og deres farmaceutisk acceptable salte. Den anvendte mængde af anti-mastitismedikament vil selvfølgelig variere afhængende af, hvor alvorlig en masti-35 tis der er tale om,men almindeligvis vil de mængder, der hidtil har været anvendt til behandling af mastitis, være passende .The term "anti-mastitis drug" is used to mean any antimicrobial agent effective in treating mastitis. Examples of anti-mastitis drugs that can be used with the carrier of the invention are penicillin, neomycin, novobiocin, lincomycin, dihydrosteptomycin, streptomycin, erythromycin, polymyzin, tetracycline, oxytetracycline, chlorothetracycline, clindetracycline, clindetracycline, clindetracycline, clind analogs and derivatives thereof and their pharmaceutically acceptable salts. The amount of anti-mastitis drug used will, of course, vary depending on the severity of a mastitis, but generally the amounts heretofore used to treat mastitis will be appropriate.
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3 143A3 83 143A3 8
Til fremstilling af bæreren ifølge opfindelsen omdannes en af de nævnte vegetabilske olier til en gel ved behandling med fedtsyreesteren af glycerol. En foretrukken fedtsyreester er ifølge opfindelsen glycerylmonostearat, da 5 den er billig og let tilgængelig.For the preparation of the carrier of the invention, one of said vegetable oils is converted to a gel by treatment with the fatty acid ester of glycerol. A preferred fatty acid ester according to the invention is glyceryl monostearate as it is inexpensive and readily available.
Den mængde glycerylmonostearat eller anden fedtsyreester, der kan anvendes, ligger almindeligvis i området fra ca. 0,5 til ca. 5,0 vægt-% og fortrinsvis mellem 1,0 og 4,0 vægt-%. En gel dannet ved gelatinering af jordnøddeolie med 10 2,0 vægt-% glycerylmonostearat er en foretrukken bærer ifølge opfindelsen.The amount of glyceryl monostearate or other fatty acid ester that can be used is generally in the range of about 0.5 to approx. 5.0% by weight and preferably between 1.0 and 4.0% by weight. A gel formed by gelatinization of peanut oil with 2.0 wt% glyceryl monostearate is a preferred carrier of the invention.
Ifølge opfindelsen kan bæreren med fordel også indeholde mellem ca. 0,02 og ca. 0,15 vægt-% af natrium-, kaliumeller lithiumsaltet af en langkædet, mættet eller umættet 15 monocarboxylsyre med 12-20 carbonatomer, fortrinsvis kali-umstearat, da geleringen herved forbedres.According to the invention, the carrier can advantageously also contain between about 0.02 and approx. 0.15% by weight of the sodium, potassium or lithium salt of a long chain, saturated or unsaturated monocarboxylic acid of 12-20 carbon atoms, preferably potassium stearate, as the gelation is thereby improved.
En gel dannet ved gelatinering af jordnøddeolie med 2,0 vægt-% glycerylmonostearat og 0,12 vægt-% kaliumstearat udgør en særlig fremragende bærer ifølge opfindelsen.A gel formed by gelatinization of peanut oil with 2.0% by weight glyceryl monostearate and 0.12% by weight potassium stearate constitutes a particularly excellent carrier of the invention.
20 Til gelatinering af den vegetabilske olie opvarmes olien til en passende temperatur, der kan variere noget for de forskellige olier, men almindeligvis ligger under 100°C. Jordnøddeolie kan f.eks. let gelatineres ved opvarmning til 60-90°C og tilsætning af 2,0 vægt-% glycerylmonostearat ef-25 terfulgt af en køling til 25°C under omrøring. Der er ingen større risiko ved overhedning, forudsat at der ikke fremkaldes sønderdeling af olien. Opvarmede olier gelatineres med en fedtsyreester.For gelatinizing the vegetable oil, the oil is heated to a suitable temperature which may vary somewhat for the various oils, but is generally below 100 ° C. Peanut oil can e.g. is easily gelatinized by heating to 60-90 ° C and adding 2.0% by weight of glyceryl monostearate followed by cooling to 25 ° C with stirring. There is no major risk of overheating, provided that no oil decomposition is induced. Heated oils are gelatinized with a fatty acid ester.
I en række sammenligningsforsøg er der bestemt ud-30 malkningstiderne for antimastitis-medikamentet penicillin fra mælkegivende malkekøer efter intramammal infusion af penicillin og novobiocin, der var dispergeret i en jordnød-deolie-bærer geleret med henholdsvis aluminiumonostearat og glycerylmonostearat indeholdende en lille mængde kalium-35 stearat ("Tegin^).In a series of comparative experiments, the milking times of the antimastitis drug penicillin from lactating dairy cows were determined following intramammal infusion of penicillin and novobiocin dispersed in a peanut oil carrier gelled with aluminum monostearate and glyceryl monostearate, respectively. stearate ("Tegin ^).
Til forsøgene anvendtes holstenske malkekøer (i 3. lactationsperiode eller ældre) i forskellige produktionssta-For the experiments, Holstein dairy cows (during the 3rd lactation period or older) were used in different production stages.
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4 143438 dier, og de blev alle maskinmalket to gange om dagen.4,144,383, and they were all milked twice a day.
KØerne blev straks efter en normal malkning inflaseret i yveret med 10 ml af præparaterne indeholdende 100.000 J.U. procain-penicillin, 50 mg chlorbutanol og varierende 5 mængde natriumnovobiocin, generelt ved tre successive malkninger med 12 timer mellem de enkelte behandlinger, men i to tilfælde fik køerne to infusioner med 24 timers mellemrum.After a normal milking, the cows were infused into the udder with 10 ml of the preparations containing 100,000 J.U. procaine-penicillin, 50 mg of chlorobutanol and varying 5 amounts of sodium novobiocin, generally at three successive milks with 12 hours between the individual treatments, but in two cases the cows received two infusions at 24 hour intervals.
Mælken opsamledes fra hver ko for hver malkning efter behandlingen, og i deraf udtagne prøver bestemtes 10 restindholdet af penicillin efter den metode, der er angivet af A. Kirshbaum et al. i "Assay Methods for Antibiotics in Milk, Dairy Products, and Animal Tissue", U.S.D.H.E.W., F.D.A., Washington, D.C. revideret 1967.The milk was collected from each cow for each milking after treatment, and in samples taken the residual penicillin content was determined according to the method set forth by A. Kirshbaum et al. in "Assay Methods for Antibiotics in Milk, Dairy Products, and Animal Tissue", U.S.D.H.E.W., F.D.A., Washington, D.C. revised 1967.
De opnåede resultater er anført i følgende tabel, 15 hvor angivelserne "2% AMPOG", "1% AIIPOG", 0,5% AMPOG" refererer til jordnøddeolie geleret med henholdsvis 2, 1 og 0,5% aluminiumonostearat, medens betegnelserne "2%The results obtained are listed in the following table, 15 where the terms "2% AMPOG", "1% AIIPOG", 0.5% AMPOG "refer to peanut oil gelled with 2, 1 and 0.5% aluminum onostate respectively, while the terms" 2 %
GlyPOG" og "1% GlyPOG" refereret til jordnødeolie geleret med henholdsvis 2 og 1% af det ovenfor beskrevne "Tegin"®.GlyPOG "and" 1% GlyPOG "refer to peanut oil gelled with 2 and 1%, respectively, of the" Tegin "® described above.
20 Resultaterne viser, at udmalkningstiderne for penicillin er betydelig kortere, når der som bærer for penicillinet er anvendt jordnøddeolie geleret med glycerylmo-nostearat plus lidt kaliumstearat, end når der som bærer er anvendt jordnøddeolie geleret med aluminiumonostearat.The results show that the milking times for penicillin are significantly shorter when peanut oil gelled with glyceryl monostearate plus a little potassium stearate is used as carrier for the penicillin than when peanut oil gelled with aluminum monostearate is used.
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De følgende eksempler skal tjene til nærmere illustrering af opfindelsen.The following examples are intended to further illustrate the invention.
Eksempel 1.Example 1.
5 Et præparat til behandling af mastitis og inde holdende bæreren ifølge opfindelsen fremstilles på følgende måde; 100 g jordnøddeolie opvarmes til 60-90°C, og der tilsættes 1,00 g glycerylmonostearat, hvorefter der afkø-10 les til 25°C under omrøring. Derpå tilsættes 1,00 g natrium-novobiocin og 500.000 enheder af procain-penicillin G vinder omrøring, hvorefter det hele ledes gennem en kolloid-mølle. Det færdige præparat kommes på én-gangs mastitis--sprøjter i doser på 10 g.A composition for treating mastitis and containing the carrier of the invention is prepared as follows; Heat 100 g of peanut oil to 60-90 ° C and add 1.00 g of glyceryl monostearate, then cool to 25 ° C with stirring. Then, 1.00 g of sodium novobiocin and 500,000 units of procaine-penicillin G are added stirring, after which it is all passed through a colloid mill. The finished preparation is placed on one-time mastitis - syringes in doses of 10 g.
15;15;
Eksempel 2.Example 2.
Et andet præparat til behandling af mastitis og indeholdende bæreren ifølge opfindelsen fremstilles på følgende måde: 20 100 g jordnøddeolie opvarmes til 60-90°C og tilsæt tes 1,425 g glycerylmonostearat og 0,075 g kaliumstearat, hvorefter der køles til 25°C under omrøring. Derpå tilsættes under omrøring 1,5 g natriumnovobiocin og 1.500.000 enheder af procain-penicillin G, og produktet ledes gennem 25 en kolloidmølle. Det færdige præparat kommes på én-gangs mastitis-sprøjter i doser på 10 g.Another preparation for treating mastitis and containing the carrier of the invention is prepared as follows: 20 100 g of peanut oil are heated to 60-90 ° C and 1.425 g of glyceryl monostearate and 0.075 g of potassium stearate are added, then cooled to 25 ° C with stirring. Then, with stirring, 1.5 g of sodium novobiocin and 1,500,000 units of procaine-penicillin G are added and the product is passed through a colloid mill. The finished preparation is applied to disposable mastitis syringes at doses of 10 g.
Eksempel 3.Example 3
Et præparat til behandling af mastitis og indehol-30 dende bæreren ifølge opfindelsen fremstilles på følgende måde: 100 g jordnøddeolie opvarmes til 60-90°C og tilsættes 2,0 g glycerylmonostearat, hvorpå der afkøles til 25°C under omrøring. Derpå tilsættes under omrøring 2,0 g linco-35 mycin-hydrochlorid, og produktet ledes gennem en kolloidmølle. Det· formalede produkt kommes i én-gangs mastitis--sprøjteri doser på 10 g.A composition for treating mastitis and containing the carrier of the invention is prepared as follows: 100 g of peanut oil are heated to 60-90 ° C and 2.0 g of glyceryl monostearate is added, then cooled to 25 ° C with stirring. Then, with stirring, 2.0 g of linco-mycin hydrochloride is added and the product is passed through a colloid mill. The · ground product comes in one-time mastitis - spraying doses of 10 g.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45603074A | 1974-03-29 | 1974-03-29 | |
| US45603074 | 1974-03-29 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| DK106175A DK106175A (en) | 1975-09-30 |
| DK143438B true DK143438B (en) | 1981-08-24 |
| DK143438C DK143438C (en) | 1981-12-21 |
Family
ID=23811160
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK106175A DK143438C (en) | 1974-03-29 | 1975-03-14 | GEL SHEET, ON VEGETABLE OIL BASED BEARS FOR PREPARATIONS FOR TREATMENT OF MASTITIS OF Dairy animals |
Country Status (8)
| Country | Link |
|---|---|
| BE (1) | BE827361A (en) |
| CA (1) | CA1052697A (en) |
| DE (1) | DE2512391C2 (en) |
| DK (1) | DK143438C (en) |
| FR (1) | FR2265408B1 (en) |
| GB (1) | GB1456349A (en) |
| NL (1) | NL7502808A (en) |
| ZA (1) | ZA751451B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1988000059A1 (en) * | 1986-07-01 | 1988-01-14 | Drilletten Ab | A controlled-release composition for a biologically active material dissolved or dispersed in an l2-phase |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1547164A (en) * | 1975-08-14 | 1979-06-06 | Beecham Group Ltd | Veterinary compositions |
| IT1190445B (en) * | 1985-11-08 | 1988-02-16 | Fatro Spa | VETERINARY COMPOSITIONS BASED ON ANTIMICROBIAL AGENTS AND THEIR USE |
| DK16290D0 (en) * | 1990-01-19 | 1990-01-19 | Spindel & Spinnfluegelfab Veb | PATTERN TREATMENT NAME NECESSARY TO FIGHT MASTITIS |
| DE69319134D1 (en) * | 1992-12-08 | 1998-07-16 | Bimeda Res Dev Ltd | AQUEOUS ANTIBIOTIC COMPOSITION FOR VETERINARY USE |
| JP2001501181A (en) * | 1996-09-06 | 2001-01-30 | ミネソタ マイニング アンド マニュファクチャリング カンパニー | Antimicrobial composition |
| CA2274796C (en) | 1996-12-18 | 2006-12-05 | Bimeda Research & Development Limited | Antiinfective free intramammary veterinary composition |
| FR2833500A1 (en) * | 2001-12-17 | 2003-06-20 | Veyron Et Froment Lab | New anhydrous, oily gel for use in the manufacture of e.g. cosmetics, oral dental products or pharmaceuticals |
| NZ519112A (en) * | 2002-05-22 | 2004-12-24 | Interag | Drug delivery device for administration of active agent to mammary gland cavity |
| US7842791B2 (en) | 2002-12-19 | 2010-11-30 | Nancy Jean Britten | Dispersible pharmaceutical compositions |
| US20040197422A1 (en) * | 2002-12-20 | 2004-10-07 | Pfizer Inc | Veterinary compositions for treating mastitis |
| GB0229642D0 (en) * | 2002-12-20 | 2003-01-22 | Pfizer Ltd | Veterinary compositions for treating mastitis |
| RU2369356C2 (en) | 2004-02-02 | 2009-10-10 | Баймеда Рисерч энд Дивелопмент Лимитед | Device for treatment of mammillary canal of mammal |
| EP2962660A1 (en) | 2004-02-02 | 2016-01-06 | Bimeda Research & Development Limited | Device for treating a teat canal of an animal |
| CN101547698B (en) | 2006-10-10 | 2014-01-08 | 威斯康星旧生研究基金会 | Intra-mammary teat sealant formulation and method of using same to reduce or eliminate visual defects in aged cheeses |
| KR20120005497A (en) * | 2009-04-08 | 2012-01-16 | 위스콘신 얼럼나이 리서어치 화운데이션 | Intra-mammary teat sealant formulation and method of using same to reduce or eliminate visual defects in aged cheeses |
-
1975
- 1975-03-06 CA CA221,421A patent/CA1052697A/en not_active Expired
- 1975-03-10 ZA ZA00751451A patent/ZA751451B/en unknown
- 1975-03-10 NL NL7502808A patent/NL7502808A/en not_active Application Discontinuation
- 1975-03-14 DK DK106175A patent/DK143438C/en not_active IP Right Cessation
- 1975-03-21 DE DE2512391A patent/DE2512391C2/en not_active Expired
- 1975-03-28 FR FR7509948A patent/FR2265408B1/fr not_active Expired
- 1975-03-28 BE BE154927A patent/BE827361A/en not_active IP Right Cessation
- 1975-04-01 GB GB1331075A patent/GB1456349A/en not_active Expired
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1988000059A1 (en) * | 1986-07-01 | 1988-01-14 | Drilletten Ab | A controlled-release composition for a biologically active material dissolved or dispersed in an l2-phase |
Also Published As
| Publication number | Publication date |
|---|---|
| DE2512391A1 (en) | 1975-10-02 |
| DE2512391C2 (en) | 1986-10-09 |
| FR2265408A1 (en) | 1975-10-24 |
| AU7909675A (en) | 1976-09-16 |
| DK143438C (en) | 1981-12-21 |
| DK106175A (en) | 1975-09-30 |
| BE827361A (en) | 1975-09-29 |
| CA1052697A (en) | 1979-04-17 |
| GB1456349A (en) | 1976-11-24 |
| FR2265408B1 (en) | 1978-08-04 |
| NL7502808A (en) | 1975-10-01 |
| ZA751451B (en) | 1976-02-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PBP | Patent lapsed |