http://rdf.ncbi.nlm.nih.gov/pubchem/patent/BR-0102287-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_412a7c5c70ef101299d6bdc6405f8186 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4184 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P33-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-365 |
| filingDate | 2001-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8c398e996b65f68e508f17ea07cc49e0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2050a14431e5153495b5074b51c02d34 |
| publicationDate | 2002-05-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | BR-0102287-A |
| titleOfInvention | Injectable veterinary compositions formed by the combination of sulphoxides derived from benzimidazoles or an acidic or basic salt with macrocyclic lactones indicated for the treatment of internal and external parasites of cattle, sheep, pigs and goats |
| abstract | "INJECTIBLE VETERINARY COMPOSITIONS FORMED BY THE ASSOCIATION OF BENZIMIDAZOLE-DERIVED SULPHOXIDES OR AN ACID OR BASIC SALT WITH MACROCYCLICAL LACTONES INDICATED FOR THE TREATMENT OF INTERNAL AND EXTERNAL CATTLE. The present invention relates to the new veterinary injectable pharmaceutical compositions formed by the association of <UM> type A <MV> compounds, the sulfoxides derived from Benzimidazoles (figure 1) with <UM> type B <MV> compounds, the macrocyclic lactones being represented by Avermectins: Ivermectins, Abamectins, Doramectin, Moxidectin, Milbemycins and derivatives of these compounds; this veterinary injectable composition can be presented in the following forms: 1 - An injectable solution in which both active ingredients composed of <UM> type A and B <MV>, are dissolved in the solvent (s) that compose the formulation. II - An injectable suspension in which one of the active ingredients composed of <UM> type A or B <MV> is dissolved in the solvent (s) that make up the formulation and the other active ingredient composed of <UM> type A or B <MV> is in coated or uncoated suspension. III - An injectable suspension in which both active ingredients composed of <UM> type A and B <MV> are in suspension. IV - An extemporaneous injectable solution whose preparation is carried out at the time of its application, by adding the solution of one of the active ingredients composed of <UM> type A <MV>, a solution previously prepared or prepared at the moment of its application over the solution of the other active ingredient <UM> type B <MV> compounds in appropriate solvent (s). V - An extemporaneous injectable emulsion whose preparation takes place at the moment of its application, formed by the addition of the solution of one of the active ingredients composed of the <UM> type A <MV> dissolved in a solvent or in the mixture of appropriate solvents-on the solution of another active ingredient compounds of <UM> type B <MV> dissolved in a suitable solvent or mixture of solvents; the emuition is formed because the solvents that make up the solution of the <UM> type A <MV> compounds are not miscible with the solvents that make up the solution of the type B compounds. VI - An extemporaneous emulsion whose preparation is carried out at the moment application; the solution of <UM> type A <MV> compounds is prepared at that time by adding the solvent (s) over a salt (acid or alkali) of a <UM> type A <MV> compound or adding the solutions of acids or alkalis on type A compounds in powder or suspension in appropriate solvent (s); then this freshly prepared solution is mixed with a solution of <UM> type B <MV> compounds, the emulsion is formed because the solvents that make up the solution of <UM> type A <MV> compounds are not miscible with solvents that make up the solution of the <UM> type B <MV> compounds; and VII - An extemporaneous injectable emulsion whose preparation is carried out at the moment of its application. Initially, we have a mixture formed by the suspension of <UM> type A <MV> compounds in solvents immiscible with the solvents that are dissolving the <UM> type B <MV> compounds, when the application is added, the mixture previously described, a solution of an acid or base dissolved in water and stirred until a stable emulsion or microemulsion is formed by the solution of <UM> type A <MV> compounds with the solution of <UM> type B compounds <MV>; the structure of <UM> type A <MV> compounds is as follows: (figure 1) where R ^ 1 ^ is an alkyl or phenylalkyl chain and R ^ 2 ^ is an alkyl chain, as well as their acid salts or basics used in various injectable formulations in order to increase the solubility of SULPHOXIDES DERIVED FROM A BENZIMIDAZOLE; as an example we have Albendazole Sulfoxide, where R ^ 1 ^ is propyl and R ^ 2 ^ methyl, Oxfendazole where R ^ 1 ^ is phenyl and R ^ 2 ^ methyl; as salts derived from these examples we have the albendazole sulfoxide hydrochloride, the albendazole sulfoxide methanesulfonate, the albendazole sulfoxide sodium salt, the albendazole sulfoxide potassium salt and etc .; for the structure, and characterization of <UM> type B <MV> compounds, we can refer to the widely available technical and commercial literature: for Avermectins, Ivermectin and Abamectin, reference can be made, for example, to the work <UM > Ivermectin and Abamectin <MV>, 1989 by MH Fischer and H. Mrozik, Willian C. Campbell ed. Springer Verlag or Albers Sch รท nberg et al. (1981) <UM> Avermectins Structure Deternlination <MV>. J. Am. Chem. Soc. 103: 4216-4221; for Doramectin we can consult notably <UM> Veterinary Parasitology <MV> vol. 49 N <0> 1, July 1993: 5-15; for Milbemycins, we can refer, among others, to Davies H. G. et. al. 1986, <UM> Avermectins and Milbemvcins <MV>; nat. Prod. Rep. 3: 87-121, Mrozik H et al, 1983, <UM> Synthesis of Milbemycins from Avermectins <MV>, <UM> Tetrahedron Lett <MV>. 24: 5333-5336, as well as US-A-4 134 973; the resulting solutions can be administered to cattle, sheep, pigs and goats infected by internal and / or external parasites in a single dose; the concentration of the active ingredients varies from 2.5% to 15% for SULFOXIDE DERIVED FROM BENZIMIDAZOLES (type A compounds) and from 0.4% to 1.5% MACROCYCLIC LACTONES (type B compounds) in the final composition of veterinary pharmaceutical specialty; the pharmaceutical composition for use is also provided; The dose of the active ingredients by body weight is as follows: - For BENZIMIDAZOLES-DERIVED SULFOXIDES (compounds of <UM> type A <MV>) ranges from 1.5 mg per kilo of body weight to 6.0 mg per kilo of body weight. - For MACROCYCLIC LACTONES (compounds of <UM> type B <MV>) it varies from 0.1 mg per kilogram of body weight to 0.4 mg per kilogram of body weight. |
| priorityDate | 2001-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 40.