ITUB20154663A1 - USE OF COMPOSITIONS OF SCOPOLAMINE DERIVATIVES IN THE LACTATION OF HERBIVE MAMMALS - Google Patents
USE OF COMPOSITIONS OF SCOPOLAMINE DERIVATIVES IN THE LACTATION OF HERBIVE MAMMALS Download PDFInfo
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- ITUB20154663A1 ITUB20154663A1 ITUB2015A004663A ITUB20154663A ITUB20154663A1 IT UB20154663 A1 ITUB20154663 A1 IT UB20154663A1 IT UB2015A004663 A ITUB2015A004663 A IT UB2015A004663A IT UB20154663 A ITUB20154663 A IT UB20154663A IT UB20154663 A1 ITUB20154663 A1 IT UB20154663A1
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- lactation
- veterinary compositions
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- compositions
- scopolamine
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- 239000000203 mixture Substances 0.000 title claims description 29
- 230000006651 lactation Effects 0.000 title claims description 18
- 241000124008 Mammalia Species 0.000 title claims description 7
- STECJAGHUSJQJN-VJQRDGCPSA-N chembl3084722 Chemical group C1([C@@H](CO)C(=O)O[C@@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-VJQRDGCPSA-N 0.000 title description 5
- 235000013336 milk Nutrition 0.000 claims description 17
- 239000008267 milk Substances 0.000 claims description 17
- 210000004080 milk Anatomy 0.000 claims description 17
- 241000283690 Bos taurus Species 0.000 claims description 14
- 241000282849 Ruminantia Species 0.000 claims description 12
- 238000004519 manufacturing process Methods 0.000 claims description 12
- YBCNXCRZPWQOBR-WVHCHWADSA-N butylscopolamine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)CCCC)=CC=CC=C1 YBCNXCRZPWQOBR-WVHCHWADSA-N 0.000 claims description 10
- 229930000680 A04AD01 - Scopolamine Natural products 0.000 claims description 9
- STECJAGHUSJQJN-GAUPFVANSA-N Hyoscine Natural products C1([C@H](CO)C(=O)OC2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-GAUPFVANSA-N 0.000 claims description 9
- STECJAGHUSJQJN-UHFFFAOYSA-N N-Methyl-scopolamin Natural products C1C(C2C3O2)N(C)C3CC1OC(=O)C(CO)C1=CC=CC=C1 STECJAGHUSJQJN-UHFFFAOYSA-N 0.000 claims description 9
- 125000000217 alkyl group Chemical group 0.000 claims description 9
- 229960002646 scopolamine Drugs 0.000 claims description 9
- 229950009846 scopolamine butylbromide Drugs 0.000 claims description 7
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims description 5
- 208000007976 Ketosis Diseases 0.000 claims description 3
- 230000004140 ketosis Effects 0.000 claims description 3
- 208000030159 metabolic disease Diseases 0.000 claims description 3
- LZCOQTDXKCNBEE-IKIFYQGPSA-N methscopolamine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)C)=CC=CC=C1 LZCOQTDXKCNBEE-IKIFYQGPSA-N 0.000 claims description 3
- 229960001383 methylscopolamine Drugs 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims 1
- 230000009467 reduction Effects 0.000 description 6
- 238000000034 method Methods 0.000 description 5
- 241000283707 Capra Species 0.000 description 4
- 241001494479 Pecora Species 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- 230000035935 pregnancy Effects 0.000 description 4
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 3
- 210000000481 breast Anatomy 0.000 description 3
- 208000004396 mastitis Diseases 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 238000011282 treatment Methods 0.000 description 3
- 239000002775 capsule Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- CXYRUNPLKGGUJF-OZVSTBQFSA-M pamine Chemical compound [Br-].C1([C@@H](CO)C(=O)OC2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)C)=CC=CC=C1 CXYRUNPLKGGUJF-OZVSTBQFSA-M 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 230000008929 regeneration Effects 0.000 description 2
- 238000011069 regeneration method Methods 0.000 description 2
- 150000003839 salts Chemical group 0.000 description 2
- 230000002048 spasmolytic effect Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 241000894006 Bacteria Species 0.000 description 1
- KORNTPPJEAJQIU-KJXAQDMKSA-N Cabaser Chemical compound C1=CC([C@H]2C[C@H](CN(CC=C)[C@@H]2C2)C(=O)N(CCCN(C)C)C(=O)NCC)=C3C2=CNC3=C1 KORNTPPJEAJQIU-KJXAQDMKSA-N 0.000 description 1
- WVVSZNPYNCNODU-CJBNDPTMSA-N Ergometrine Natural products C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@@H](CO)C)C2)=C3C2=CNC3=C1 WVVSZNPYNCNODU-CJBNDPTMSA-N 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- WVVSZNPYNCNODU-XTQGRXLLSA-N Lysergic acid propanolamide Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@H](CO)C)C2)=C3C2=CNC3=C1 WVVSZNPYNCNODU-XTQGRXLLSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 description 1
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 description 1
- 102000003946 Prolactin Human genes 0.000 description 1
- 108010057464 Prolactin Proteins 0.000 description 1
- BKRGVLQUQGGVSM-KBXCAEBGSA-N Revanil Chemical compound C1=CC(C=2[C@H](N(C)C[C@H](C=2)NC(=O)N(CC)CC)C2)=C3C2=CNC3=C1 BKRGVLQUQGGVSM-KBXCAEBGSA-N 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 235000019445 benzyl alcohol Nutrition 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 229960002802 bromocriptine Drugs 0.000 description 1
- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 description 1
- 229940088506 buscopan Drugs 0.000 description 1
- HOZOZZFCZRXYEK-GSWUYBTGSA-M butylscopolamine bromide Chemical compound [Br-].C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)CCCC)=CC=CC=C1 HOZOZZFCZRXYEK-GSWUYBTGSA-M 0.000 description 1
- 229960004596 cabergoline Drugs 0.000 description 1
- 244000309466 calf Species 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 210000003022 colostrum Anatomy 0.000 description 1
- 235000021277 colostrum Nutrition 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000002939 deleterious effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000003291 dopaminomimetic effect Effects 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229960001405 ergometrine Drugs 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 239000012456 homogeneous solution Substances 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000007972 injectable composition Substances 0.000 description 1
- 229940102223 injectable solution Drugs 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 229960003587 lisuride Drugs 0.000 description 1
- 210000005075 mammary gland Anatomy 0.000 description 1
- 229960004650 metergoline Drugs 0.000 description 1
- WZHJKEUHNJHDLS-QTGUNEKASA-N metergoline Chemical compound C([C@H]1CN([C@H]2[C@@H](C=3C=CC=C4N(C)C=C(C=34)C2)C1)C)NC(=O)OCC1=CC=CC=C1 WZHJKEUHNJHDLS-QTGUNEKASA-N 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 238000002156 mixing Methods 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
- 210000002445 nipple Anatomy 0.000 description 1
- 229940100688 oral solution Drugs 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 229940097325 prolactin Drugs 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000012027 sterile manufacturing Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000001131 transforming effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Emergency Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
“USO DI COMPOSIZIONI DI DERIVATI DELLA SCOPOLAMINA NELLA LATTAZIONE DI MAMMIFERI ERBIVORI” "USE OF COMPOSITIONS OF SCOPOLAMINE DERIVATIVES IN THE LACTATION OF HERBIVOROUS MAMMALS"
Campo deirinvenzione Field of the invention
La presente invenzione riguarda composizioni veterinarie per uso nella riduzione della produzione di latte e nella modulazione del picco di lattazione nei mammiferi erbivori, in particolare nei ruminanti, comprendenti un derivato alchilico quaternario della scopolamina, quale la butilscopolamina o metilscopolamina, al fine di permettere l’inizio del periodo di asciutta in modo rapido e fisiologico e di prevenire la chetosi e altre dismetabolie. The present invention relates to veterinary compositions for use in the reduction of milk production and in the modulation of the lactation peak in herbivorous mammals, in particular in ruminants, comprising a quaternary alkyl derivative of scopolamine, such as butylscopolamine or methylscopolamine, in order to allow the start of the dry period quickly and physiologically and to prevent ketosis and other metabolic disorders.
Tecnica precedente Previous technique
Nei ruminanti, la lattazione, in generale, ha una durata tra i 5 e i 20 mesi, e in particolare dura circa 10 mesi per le vacche. In ruminants, lactation, in general, lasts between 5 and 20 months, and in particular it lasts about 10 months for cows.
Dopo questo periodo di lattazione, la mammella della vacca è messa a riposo produttivo per un periodo di tempo che dura tradizionalmente circa 60 giorni (noto come periodo di asciutta) fino al parto, dopo il quale ricomincia la produzione di latte (lattazione successiva). After this lactation period, the cow's udder is put to productive rest for a period of time that traditionally lasts about 60 days (known as the dry period) until calving, after which milk production resumes (subsequent lactation).
Il periodo di asciutta è utilizzato in genere - negli allevamenti per il benessere del ruminante. Questo periodo è particolarmente importante per la rigenerazione delle ghiandole mammarie, per evitare problemi di infiammazioni e infezioni durante la successiva lattazione e per ottenere una sufficiente produzione di colostro utile all’ immunità del vitello. The dry period is generally used - on farms for the welfare of the ruminant. This period is particularly important for the regeneration of the mammary glands, to avoid problems of inflammation and infections during subsequent lactation and to obtain sufficient production of colostrum useful for the immunity of the calf.
L’insorgenza di malattie, in particolare la mastite, durante la lattazione comporta una riduzione o il blocco della produzione di latte con notevoli danni economici. The onset of diseases, in particular mastitis, during lactation leads to a reduction or blockage of milk production with considerable economic damage.
Per queste ragioni, prodotti adatti a ridurre o bloccare in modo rapido la produzione di latte e favorire, con il periodo di asciutta, la involuzione mammaria o, durante la gestazione, le condizioni di rigenerazione, sono di estrema utilità terapeutica. For these reasons, products suitable for rapidly reducing or blocking the production of milk and favoring, with the dry period, breast involution or, during gestation, regeneration conditions, are extremely useful therapeutically.
Infatti, se la lattazione non termina in modo rapido e netto, permane in mammella una certa quantità di latte che mantiene beante il capezzolo, facilitando così l’ingresso di batteri mastidogeni che incontrano nel latte residuo il pabulum ideale per moltiplicarsi e causare una mastite o durante l’asciutta o durante la successiva lattazione. In fact, if lactation does not end quickly and clearly, a certain amount of milk remains in the breast which keeps the nipple open, thus facilitating the entry of mastidogenic bacteria which meet in the residual milk the ideal pabulum to multiply and cause mastitis or during dryness or during subsequent lactation.
Allo stato attuale sono noti prodotti derivati da ergotina ad azione dopaminergica, quali la Cabergolina, Metergolina, Lisuride, Bromocriptina, Ergometrina, che inibiscono la secrezione di prolattina con conseguente diminuzione o blocco della produzione di latte nei ruminanti (EP2349272-A1). At present, products derived from ergotine with dopaminergic action are known, such as Cabergoline, Metergoline, Lisuride, Bromocriptine, Ergometrine, which inhibit the secretion of prolactin with consequent decrease or block of milk production in ruminants (EP2349272-A1).
Si è ora sorprendentemente trovato che composizioni a base di derivati di sali quaternari della scopolamina, in particolare i derivati alchilici quaternari della scopolamina, quali la butilscopolamina bromidrato e la metilscopolamina bromidrato, sono in grado di diminuire o bloccare la produzione di latte nei mammiferi erbivori, in particolare nei ruminati, quali bovini, ovini, caprini, e quindi di indurre il periodo di asciutta. Gli stessi prodotti possono essere utilizzati in fase iniziale di lattazione al fine di modulare il picco di lattazione, prevenendo così l’insorgenza di chetosi ed altre dismetabolie che possono compromettere la salute della bovina e la sua redditività. It has now surprisingly been found that compositions based on derivatives of scopolamine quaternary salts, in particular the quaternary alkyl derivatives of scopolamine, such as butylscopolamine hydrobromide and methylscopolamine hydrobromide, are able to decrease or block milk production in herbivorous mammals, in particular in ruminates, such as cattle, sheep, goats, and therefore to induce the dry period. The same products can be used in the early lactation phase in order to modulate the lactation peak, thus preventing the onset of ketosis and other metabolic disorders that can compromise the health of the cow and its profitability.
I derivati quaternari della scopolamina agiscono a livello dei recettori muscarinici e sono in genere usati sia in terapia umana che veterinaria come spasmolitici. The quaternary derivatives of scopolamine act at the level of muscarinic receptors and are generally used in both human and veterinary therapy as spasmolytics.
In particolare la n-Butilscopolamina è in commercio da molti anni come medicinale col nome di Buscopan, ad azione spasmolitica. In particular, n-Butylscopolamine has been on the market for many years as a medicine under the name of Buscopan, with a spasmolytic action.
Questi composti quaternari perdono l'attività a livello del SNC a causa della scarsa capacità di penetrare attraverso la barriera emato-encefalica. These quaternary compounds lose their CNS activity due to their poor ability to penetrate the blood-brain barrier.
DESCRIZIONE DELL’INVENZIONE DESCRIPTION OF THE INVENTION
La presente invenzione ha per oggetto composizioni veterinarie per uso nella riduzione della produzione di latte nei mammiferi erbivori, in particolare nei ruminanti, comprendenti un derivato alchilico quaternario della scopolamina, comprendenti un derivato alchilico quaternario della scopolamina, in particolare la butilscopolamina bromidrato e la metilscopolamina bromidrato The present invention relates to veterinary compositions for use in the reduction of milk production in herbivorous mammals, in particular in ruminants, comprising a quaternary alkyl derivative of scopolamine, comprising a quaternary alkyl derivative of scopolamine, in particular butylscopolamine hydrobromide and methylscopolamine hydrobromide
f f
R = n-Butile, Metile R = n-Butyl, Methyl
Secondo l'invenzione, queste sostanze sono somministrate come composizioni farmaceutiche in quantità terapeuticamente efficaci, come unico trattamento o più trattamenti, al fine di indurre una riduzione della produzione di latte. According to the invention, these substances are administered as pharmaceutical compositions in therapeutically effective amounts, as a single treatment or several treatments, in order to induce a reduction in milk production.
Le composizioni dell’invenzione presentano una serie di aspetti vantaggiosi, sia dal punto di vista del benessere dell’animale sia - come diretta conseguenza - in termini economici per l’allevatore. Infatti esse: The compositions of the invention have a number of advantageous aspects, both from the point of view of animal welfare and - as a direct consequence - in economic terms for the breeder. In fact they:
- possono essere somministrate durante la gestazione dei ruminanti senza causare alcun effetto deleterio o abortivo sulla gestazione; - non influiscono sulla quantità e sulla qualità del latte nel successivo periodo di lattazione; - they can be administered during the gestation of ruminants without causing any deleterious or abortive effect on gestation; - they do not affect the quantity and quality of milk in the subsequent lactation period;
- assicurano una diminuzione del rischio di mastiti nei ruminanti. Le composizioni veterinarie secondo la presente invenzione possono essere somministrate secondo modi di somministrazione noti e adattatati al trattamento delle varie specie di ruminanti, quali bovine, ovini e caprini, pecore. - ensure a decrease in the risk of mastitis in ruminants. The veterinary compositions according to the present invention can be administered according to known methods of administration adapted to the treatment of the various species of ruminants, such as cattle, sheep and goats, sheep.
Tali composizioni possono essere somministrate per via orale, cutanea e parenterale, preferibilmente per via parenterale, in particolare endovenosa o intramuscolare. Such compositions can be administered orally, cutaneously and parenterally, preferably parenterally, in particular intravenously or intramuscularly.
Le composizioni dell’invenzione possono quindi essere sotto forma di una soluzione iniettabile oppure orale, in forma di polvere, capsule, granuli, compressa rivestita, capsula, spray, pillola, pillole, compresse, o paste. The compositions of the invention can therefore be in the form of an injectable or oral solution, in the form of powder, capsules, granules, coated tablet, capsule, spray, pill, pills, tablets, or pastes.
La composizione veterinaria è preferibilmente somministrata in una singola dose iniettabile. The veterinary composition is preferably administered in a single injectable dose.
A seconda delle formulazioni e delle sostanze, le composizioni dell’invenzione possono comprendere ingredienti farmaceutici convenzionali per le formulazioni ad uso orale o parenterale. Inoltre, nel caso di formulazioni orali, queste possono essere somministrate direttamente ai ruminanti o possono essere mescolate nel cibo. Depending on the formulations and substances, the compositions of the invention may include conventional pharmaceutical ingredients for formulations for oral or parenteral use. Furthermore, in the case of oral formulations, these can be administered directly to ruminants or can be mixed into food.
Le composizioni iniettabili sono preparate mescolando un sale quaternario alchilico della scopolamina con un solvente, un regolatore di pH, un conservante e trasformando la miscela con un processo tradizionale per iniezione intramuscolare, cutanea o endovenosa. The injectable compositions are prepared by mixing an alkyl quaternary salt of scopolamine with a solvent, a pH regulator, a preservative and transforming the mixture by a traditional process for intramuscular, skin or intravenous injection.
La dose da somministrare può variare in funzione del ruminante (bovino o caprino) o del modo di somministrazione (orale, parenterale). The dose to be administered may vary according to the ruminant (bovine or goat) or the method of administration (oral, parenteral).
Quando somministrate a un bovino, le composizioni della presente invenzione conterranno il derivato alchilico quaternario della scopolamina a una dose che può variare da un minimo di 40 mcg/Kg a un massimo di 1200 mcg/kg. When administered to a bovine, the compositions of the present invention will contain the quaternary alkyl derivative of scopolamine at a dose that can vary from a minimum of 40 mcg / kg to a maximum of 1200 mcg / kg.
Quando somministrate a un ovino o caprino, le composizioni della presente invenzione conterranno il derivato alchilico quaternario della scopolamina a una dose che può variare da un minimo di 40 mcg/Kg a un massimo di 1200 mcg/kg. When administered to a sheep or goat, the compositions of the present invention will contain the quaternary alkyl derivative of scopolamine at a dose that can vary from a minimum of 40 mcg / kg to a maximum of 1200 mcg / kg.
Preferibilmente la composizione è somministrata per via endovenosa in dose singola tra 200 e 600 mcg/kg per ottenere una riduzione della quantità di latte tra il 30 e l’80% nell’ intervallo di 6 giorni dalla somministrazione della dose unica. Preferably, the composition is administered intravenously in a single dose between 200 and 600 mcg / kg to obtain a reduction in the quantity of milk between 30 and 80% in the interval of 6 days from the administration of the single dose.
I seguenti esempi illustrano la presente invenzione ma non ne limitano il campo di applicazione. The following examples illustrate the present invention but do not limit its field of application.
ESEMPI EXAMPLES
Esempio 1 Example 1
Preparazione iniettabile Injectable preparation
A 9,5 litri di soluzione acquosa per iniettabili si aggiungono 200g di alcol benzilico e si agita fino a ottenimento di una soluzione omogenea. To 9.5 liters of aqueous solution for injections, 200g of benzyl alcohol are added and stirred until a homogeneous solution is obtained.
Alle soluzione si aggiungono 200 g di n-butilscopolamina bromidrato, si mantiene in agitazione per circa 30 minuti e si porta a volume di 10 litri con acqua per iniettabili. Il pH deve essere compreso tra 3.7 - 6.5. To the solution are added 200 g of n-butylscopolamine hydrobromide, it is kept under stirring for about 30 minutes and it is brought to a volume of 10 liters with water for injections. The pH must be between 3.7 - 6.5.
La soluzione viene sterilizzata per filtrazione con i normali metodi di produzione per sterili. The solution is filter sterilized using standard sterile manufacturing methods.
Si ottiene una soluzione iniettabile contenente 20 mg/ml di n-butilscopolamina bromidrato. A solution for injection is obtained containing 20 mg / ml of n-butylscopolamine hydrobromide.
Esempio 2 Example 2
Studio clinico di efficacia nella bovina. Clinical efficacy study in cattle.
Lo studio è stato effettuato somministrando la composizione dell’ esempio 1 in 10 bovine gravide al 7° mese di gravidanza, prossime all’asciutta. The study was carried out by administering the composition of example 1 to 10 pregnant cows in the 7th month of pregnancy, close to dryness.
Le bovine sono state trattate per endovena con una dose di 40 mg/ 100 Kg p.v. (400 mcg/kg corrispondenti a 2 ml/quintale p.v.) in somministrazione unica subito dopo la mungitura serale. The cows were treated intravenously with a dose of 40 mg / 100 kg b.w. (400 mcg / kg corresponding to 2 ml / quintal bw) in single administration immediately after the evening milking.
Nel giorno successivo alla somministrazione (T0) e per i successivi 5 giorni (T5) sono state pesate le quantità di latte prodotto per giornata (somma di mungitura mattutina e serale). On the day following administration (T0) and for the following 5 days (T5) the quantities of milk produced per day were weighed (sum of morning and evening milking).
I risultati sono riportati in Tabella e in Figura, che mostra un grafico che riporta in ordinate i litri di latte per singole vacche. The results are shown in the Table and in the Figure, which shows a graph showing the liters of milk for individual cows in ordinates.
I risultati dimostrano che la somministrazione di una sola dose della formulazione di butilscopolamina ha determinato una riduzione media della produzione di latte del 52% al 6°giorno dalla somministrazione unica. The results demonstrate that the administration of a single dose of the butylscopolamine formulation resulted in an average reduction in milk production of 52% on the 6th day of the single administration.
Tabella Table
Matricola TF di<'>] Media Media j % dj lattazioni giornaliera giornaliera decremento tra il primo e del primo dell'ultimo l'ultimo giorno giorno (L) giorno (L) TF serial number of <'>] Average Average j% dj daily lactation daily decrease between the first and the first of the last day on the last day (L) day (L)
6969 2 7 3 -57% 6969 2 7 3 -57%
0633 1 5 0 65 -87% 0633 1 5 0 65 -87%
0927 2 6 3 -50% 0927 2 6 3 -50%
8721 2 8 3.25 -59% 8721 2 8 3.25 -59%
8637 3 9.5 6.5 -32% 8637 3 9.5 6.5 -32%
0376 2 30.5 5,8 -45% 0376 2 30.5 5.8 -45%
8725 3 9.75 6 5 -33% 8725 3 9.75 6 5 -33%
0364 2 6.75 2.5 -63% 0364 2 6.75 2.5 -63%
5000 3 6.25 3 -52% ! 5000 3 6.25 3 -52%!
8739 2 5 1 -80% 8739 2 5 1 -80%
MEDIA 7.38 3.52 -52% AVERAGE 7.38 3.52 -52%
Claims (9)
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Non-Patent Citations (4)
| Title |
|---|
| D K AARON ET AL: "Reducing Milk Production in Ewes at Weaning Using Restricted Feeding and Methscopolamine Bromide 1 Introduction", J. ANIM. SCI, 1 January 1996 (1996-01-01), pages 1434 - 1442, XP055276992, Retrieved from the Internet <URL:https://www.animalsciencepublications.org/publications/jas/pdfs/75/6/1434> [retrieved on 20160601] * |
| DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 1988, OIWA, YOKO ET AL: "Pharmacokinetic studies of oxitropium bromide (Ba 253 BR)(2). Enterohepatic circulation, transfer into milk , placental transfer and protein binding in rats", XP002758293, retrieved from STN Database accession no. 1989:107527 * |
| M R POWELL ET AL: "A Potential Strategy for Decreasing Milk Production in the Ewe at Weaning Using a Growth Hormone Release Blocker1/'", JOURNAL OF ANIMAL SCIENCE, 11 December 2014 (2014-12-11), pages 1901 - 1905, XP055276991, Retrieved from the Internet <URL:https://www.animalsciencepublications.org/publications/jas/pdfs/73/7/1901> [retrieved on 20160601] * |
| OIWA, YOKO ET AL: "Pharmacokinetic studies of oxitropium bromide (Ba 253 BR)(2). Enterohepatic circulation, transfer into milk , placental transfer and protein binding in rats", YAKURI TO CHIRYO (1973-2000) , 16(12), 4785-93 CODEN: YACHDS; ISSN: 0386-3603, 1988 * |
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