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WO2008039051A1 - Pharmaceutical composition for treating the excess weight and obesity which accompany dyslipidaemia - Google Patents

Pharmaceutical composition for treating the excess weight and obesity which accompany dyslipidaemia Download PDF

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Publication number
WO2008039051A1
WO2008039051A1 PCT/MX2007/000044 MX2007000044W WO2008039051A1 WO 2008039051 A1 WO2008039051 A1 WO 2008039051A1 MX 2007000044 W MX2007000044 W MX 2007000044W WO 2008039051 A1 WO2008039051 A1 WO 2008039051A1
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Prior art keywords
pharmaceutical composition
obesity
rosuvastatin
composition according
overweight
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Spanish (es)
French (fr)
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María Elena GARCÍA ARMENTA
Víctor Guillermo ALVAREZ OCHOA
Josefina Santos Murillo
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics

Definitions

  • the present invention is related to the pharmaceutical industry, and more specifically to the pharmaceutical industry of the manufacture of products for the control of overweight and obesity. Specifically it refers to a pharmaceutical composition for oral administration, which consists of a combination of a hydrogenated derivative of lipstatin or pharmacologically acceptable salts thereof and an HMG-CoA reductase inhibitor for the treatment of obesity and dyslipidemia.
  • Obesity is the result of a positive energy balance, as a result of an increase in the caloric recapture radius for energy expenditure.
  • the molecular factors that regulate food recapture and body weight balance have not been fully understood. Epidemiological studies have shown that the degree of overweight and obesity are important predictors for life expectancy.
  • Abdominal obesity has been linked with an increased risk of coronary artery disease and with three of its greatest risks, high blood pressure, diabetes that begins early and lipid elevation such as total cholesterol, LDL cholesterol and HDL cholesterol reduction.
  • Weight loss dramatically reduces these risks, a sustained weight loss of 5 to 10% has shown to improve the co-morbidities associated with obesity.
  • Treatments used to manage overweight and obesity include Orlistat, dexfenfluramine, sibutramine and phentermine; However, and in some cases, the side effects of these drugs may limit their use.
  • the treatments used for the management of dyslipidemias include all statins, pravastatin, simvastatin, lovastatin, fluvastatin, atorvastatin, cerivastatin and rosuvastatin, which also have the disadvantage of causing side effects.
  • the present invention focuses on this problem, providing a combination therapy comprising at least one lipstatin inhibitor and an HMG-CoA reductase inhibitor in a single dose unit, for the treatment of overweight and obesity that It is accompanied by dyslipidemia, the combination of these agents produces a synergy having a better therapeutic effect than when each of them are administered individually, on the other hand, lower concentrations of the active ingredients are used in combination, producing a lower risk of collateral events. .
  • compositions comprising at least one lipstatin inhibitor known as Orlistat and an HMG-CoA reductase inhibitor known as Rosuvastatin, in a single dose unit, containing lower dose concentration, which has a synergistic effect, providing greater therapeutic effect, with lower side effects for the treatment and control of overweight and obesity that is accompanied by dyslipidemia.
  • Pancreatic lipase and gastric lipase are two primary enzymes required for triglyceride hydrolysis and systemic absorption of the resulting free fatty acids and monoglycerides.
  • Orlistat is a potent lipase inhibitor gastric
  • Orlistat works in the intestine to block the absorption of approximately one third of all dietary fat. Due to the limiting effect of the absorption of dietary fat, the data has shown that orlistat promotes weight loss, maintenance of weight loss and prevention of weight gain in overweight and obese patients. Due to its mechanism of action, there is a potential for Orlistat to affect the absorption of other drugs, especially fat-soluble drugs. Numerous interaction studies have been carried out to evaluate the possible interactions between Orlistat and other medications, such as vitamins and alcohol, only some of these, such as vitamin E and beta carotenes, have been shown to reduce their absorption. HMG-CoA reductase inhibitors, such as pravastatin, simvastatin, lovastatin, atorvastatin, cerivastatin and preferably rosuvastatin, belong to the statin group.
  • Rosuvastatin has a favorable pharmacological profile, including its selective uptake by of liver cells, their hydrophilic nature and the absence of metabolism by the isoenzyme (CYP) 3A4 of cytochrome P450.
  • the latter property means that the potential for drug interactions mediated by CYP3A4 and, consequently, adverse events is low in patients who require concomitant treatment with a statin and agents metabolized by CYP3A4.
  • the pharmaceutical composition according to the invention comprises Orlistat 60 mg and calcium Rosuvastatin equivalent to 5 mg in a single dose unit and Orlistat 60 mg and calcium Rosuvastatin equivalent to 10 mg Rosuvastatin in a single dose unit.
  • Group 1 received the Orlistat 60 mg daily.
  • Group 2 received Rosuvastatin 5 mg and Group 3 received the combination Orlistat 60 mg and Rosuvastatin 5 mg daily and for 4 weeks.
  • the parameters to be evaluated were weight loss, reduction in body mass index and lipid profile evaluation, as well as adverse events.
  • Lipid profile was substantially modified to 170 mg / dl.
  • 24 female and male subjects between 18 and 70 years of age were included with a body mass index between 18 and 30 kg / m2 or an overweight of 20% of the ideal weight, which were accompanied by a total cholesterol elevation> 200 mg / dl.
  • the researchers received the informed consent letter signed by each patient.
  • the 24 subjects received the combination of Orlistat 60 mg and Rosuvastatin 10 mg daily for 4 weeks and was compared with the first study groups.

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The present invention concerns the pharmaceutical industry, and more specifically the pharmaceutical industry involved in manufacturing products for controlling excess weight and obesity. Specifically, it refers to a pharmaceutical composition for oral administration, which comprises a combination of a hydrogenated derivative of lipstatin or pharmacologically acceptable salts thereof and a HMG-CoA reductase inhibitor for the treatment of obesity and dyslipidaemia. The quantitative composition of this medicament would be Orlistat 60 mg and Rosuvastatin calcium equivalent to 10 mg of Rosuvastatin in a single dosage unit. The advantage of this medicament with respect to those of the prior art lies in the synergistic effect which has the effect of the combination, which achieves the same effect by lowering the dose and therefore has extremely diminished side effects.

Description

COMPOSICIÓN FARMACÉUTICA PARA EL TRATAMIENTO DEL SOBREPESO Y LA OBESIDAD QUE SE ACOMPAÑAN LA PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF OVERWEIGHT AND OBESITY ACCOMPANYING THE

DISLIPIDEMIA.Dyslipidemia

CAMPO DE LA INVENCIÓNFIELD OF THE INVENTION

La presente invención esta relacionada con la industria farmacéutica, y más específicamente con la industria farmacéutica de la manufactura de productos para el control de sobrepeso y obesidad. Específicamente se refiere a una composición farmacéutica para administración oral, que consiste en una combinación de un derivado hidrogenado de lipstatina o sales farmacológicamente aceptables de las mismas y un inhibidor de HMG-CoA reductasa para el tratamiento de la obesidad y la dislipidemia.The present invention is related to the pharmaceutical industry, and more specifically to the pharmaceutical industry of the manufacture of products for the control of overweight and obesity. Specifically it refers to a pharmaceutical composition for oral administration, which consists of a combination of a hydrogenated derivative of lipstatin or pharmacologically acceptable salts thereof and an HMG-CoA reductase inhibitor for the treatment of obesity and dyslipidemia.

ANTECEDENTESBACKGROUND

El sobrepeso y la obesidad es un problema de afectación mundial y que se ha incrementado en los últimos años, especialmente en México.Overweight and obesity is a problem of worldwide impact and has increased in recent years, especially in Mexico.

Es considerado un factor de gran importancia para el desarrollo de otros padecimientos como la, dislipidemia hipertensión arterial, la diabetes mellitus tipo 2 y el cáncer.It is considered a factor of great importance for the development of other conditions such as dyslipidemia. arterial hypertension, type 2 diabetes mellitus and cancer.

La obesidad es el resultado de un balance de energía positiva, como consecuencia de un aumento del radio de recaptura calórica para el gasto de energía. Los factores moleculares que regulan la recaptura de alimentos y el balance del peso corporal no han sido completamente entendidos . Los estudios epidemiológicos han demostrado que el grado de sobrepeso y obesidad son importantes predictores para la esperanza de vida.Obesity is the result of a positive energy balance, as a result of an increase in the caloric recapture radius for energy expenditure. The molecular factors that regulate food recapture and body weight balance have not been fully understood. Epidemiological studies have shown that the degree of overweight and obesity are important predictors for life expectancy.

Como hemos dicho, la obesidad y el sobrepeso, ocasionan muchos problemas de salud y especialmente está relacionada con el síndrome metabólico que puede llevar a la muerte prematura.As we have said, obesity and overweight cause many health problems and is especially related to the metabolic syndrome that can lead to premature death.

La obesidad abdominal se ha ligado con un mayor riesgo de enfermedad arterial coronaria y con tres de sus mayores riesgos, hipertensión arterial, diabetes que inicia en forma temprana y elevación de los lípidos como colesterol total, colesterol LDL y reducción del colesterol HDL.Abdominal obesity has been linked with an increased risk of coronary artery disease and with three of its greatest risks, high blood pressure, diabetes that begins early and lipid elevation such as total cholesterol, LDL cholesterol and HDL cholesterol reduction.

La pérdida de peso, reduce dramáticamente estos riesgos, una pérdida de peso sostenida del 5 al 10% ha mostrado mejorar las co-morbilidades asociadas con la obesidad.Weight loss dramatically reduces these risks, a sustained weight loss of 5 to 10% has shown to improve the co-morbidities associated with obesity.

Los tratamientos utilizados para el manejo del sobrepeso y la obesidad incluyen al Orlistat, dexfenfluramina, sibutramina y fentermina; sin embargo y en algunos casos, los efectos colaterales de estos fármacos pueden limitar su utilización.Treatments used to manage overweight and obesity include Orlistat, dexfenfluramine, sibutramine and phentermine; However, and in some cases, the side effects of these drugs may limit their use.

Por otra parte, los tratamientos utilizados para el manejo de las dislipidemias incluyen a todas las estatinas, pravastatina, simvastatina, lovastatina, fluvastatina, atorvastatina, cerivastatina y rosuvastatina, que también tienen la desventaja de producir efectos colaterales .On the other hand, the treatments used for the management of dyslipidemias include all statins, pravastatin, simvastatin, lovastatin, fluvastatin, atorvastatin, cerivastatin and rosuvastatin, which also have the disadvantage of causing side effects.

Existe una necesidad para nuevos métodos de tratamiento de la obesidad y el sobrepeso asociado con dislipidemia, que ofrezcan ventajas terapéuticas así como una mayor seguridad al reducir el riesgo de eventos colaterales .There is a need for new methods of treating obesity and overweight associated with dyslipidemia, which offer therapeutic advantages as well as greater safety by reducing the risk of collateral events.

La presente invención se enfoca a este problema, proporcionando una terapia de combinación que comprende al menos un agente inhibidor de lipstatina y un inhibidor de la HMG-CoA reductasa en una sola unidad de dosis, para el tratamiento del sobrepeso y obesidad que se acompaña de dislipidemia, la combinación de estos agentes produce una sinergia teniendo un mejor efecto terapéutico que cuando se administran cada uno de ellos en forma individual, por otra parte se utilizan menores concentraciones de los principios activos en forma combinada produciendo menor riesgo de eventos colaterales .The present invention focuses on this problem, providing a combination therapy comprising at least one lipstatin inhibitor and an HMG-CoA reductase inhibitor in a single dose unit, for the treatment of overweight and obesity that It is accompanied by dyslipidemia, the combination of these agents produces a synergy having a better therapeutic effect than when each of them are administered individually, on the other hand, lower concentrations of the active ingredients are used in combination, producing a lower risk of collateral events. .

DESCRIPCIÓN DETALLADA DEL INVENTODETAILED DESCRIPTION OF THE INVENTION

La presente invención proporciona composiciones que comprenden al menos un inhibidor de lipstatina conocido como Orlistat y un inhibidor de la HMG-CoA reductasa conocido como Rosuvastatina, en una sola unidad de dosis, conteniendo menor concentración de dosis, que tiene un efecto sinérgico, proporcionando mayor efecto terapéutico, con menores efectos secundarios para el tratamiento y control del sobrepeso y la obesidad que se acompaña de dislipidemia. La lipasa pancreática y la lipasa gástrica son dos enzimas primarias requeridas para la hidrólisis de triglicéridos y la absorción sistémica de los resultantes ácidos grasos libres y monoglicéridos . El Orlistat es un potente inhibidor de las lipasas gástricas .The present invention provides compositions comprising at least one lipstatin inhibitor known as Orlistat and an HMG-CoA reductase inhibitor known as Rosuvastatin, in a single dose unit, containing lower dose concentration, which has a synergistic effect, providing greater therapeutic effect, with lower side effects for the treatment and control of overweight and obesity that is accompanied by dyslipidemia. Pancreatic lipase and gastric lipase are two primary enzymes required for triglyceride hydrolysis and systemic absorption of the resulting free fatty acids and monoglycerides. Orlistat is a potent lipase inhibitor gastric

El Orlistat trabaja en el intestino para bloquear la absorción de aproximadamente una tercera parte de toda la grasa de la dieta. Por el efecto limitante de la absorción de la grasa de la dieta los datos han mostrado que el orlistat promueve la pérdida de peso, el mantenimiento de la pérdida de peso y la prevención de la ganancia de peso en pacientes con sobrepeso y obesos. Debido a su mecanismo de acción, existe un potencial para que el Orlistat afecte la absorción de otros fármacos, especialmente las drogas liposolubles . Numerosos estudios de interacción se han realizado para evaluar las posibles interacciones entre Orlistat y otros medicamentos, como las vitaminas y el alcohol, solamente algunas de estas como la vitamina E y los beta carotenos han mostrado reducir su absorción. Los inhibidores de HMG-CoA reductasa, como pravastatina, simvastatina, lovastatina, atorvastatina, cerivastatina y preferiblemente la rosuvastatina, pertenecen al grupo de las estatinas.Orlistat works in the intestine to block the absorption of approximately one third of all dietary fat. Due to the limiting effect of the absorption of dietary fat, the data has shown that orlistat promotes weight loss, maintenance of weight loss and prevention of weight gain in overweight and obese patients. Due to its mechanism of action, there is a potential for Orlistat to affect the absorption of other drugs, especially fat-soluble drugs. Numerous interaction studies have been carried out to evaluate the possible interactions between Orlistat and other medications, such as vitamins and alcohol, only some of these, such as vitamin E and beta carotenes, have been shown to reduce their absorption. HMG-CoA reductase inhibitors, such as pravastatin, simvastatin, lovastatin, atorvastatin, cerivastatin and preferably rosuvastatin, belong to the statin group.

La rosuvastatina tiene un perfil farmacológico favorable, incluyendo su captación selectiva por parte de las células hepáticas, su naturaleza hidrofílica y la ausencia de metabolismo por parte de la isoenzima (CYP) 3A4 del citocromo P450.Rosuvastatin has a favorable pharmacological profile, including its selective uptake by of liver cells, their hydrophilic nature and the absence of metabolism by the isoenzyme (CYP) 3A4 of cytochrome P450.

Esta última propiedad significa que el potencial de interacciones farmacológicas mediadas por la CYP3A4 y, por consiguiente de eventos adversos es bajo en los pacientes que requieren tratamiento concomitante con una estatina y agentes metabolizados por la CYP3A4. La composición farmacéutica de acuerdo con la invención comprende al Orlistat 60 mg y Rosuvastatina calcica equivalente a 5 mg en una sola unidad de dosis y Orlistat 60 mg y Rosuvastatina calcica equivalente a 10 mg de Rosuvastatin en una sola unidad de dosis .The latter property means that the potential for drug interactions mediated by CYP3A4 and, consequently, adverse events is low in patients who require concomitant treatment with a statin and agents metabolized by CYP3A4. The pharmaceutical composition according to the invention comprises Orlistat 60 mg and calcium Rosuvastatin equivalent to 5 mg in a single dose unit and Orlistat 60 mg and calcium Rosuvastatin equivalent to 10 mg Rosuvastatin in a single dose unit.

Ejemplo 1:Example 1:

Se realizó un estudio para evaluar el grado de efectividad y la posible interacción de la combinación. Se incluyeron 24 sujetos femeninos y masculinos entre 18 y 70 años de edad con un índice de masa corporal entre 18 y 30mkg/m2 o un sobrepeso del 20% del peso ideal, que estuvieran acompañados de una elevación del colesterol total > 200 mg/dl. Los investigadores recibieron la carta de consentimiento informado firmado por cada paciente.A study was conducted to assess the degree of effectiveness and the possible interaction of the combination. 24 female and male subjects between 18 and 70 years of age were included with a body mass index between 18 and 30mkg / m2 or an overweight of 20% of the ideal weight, which were accompanied by a total cholesterol elevation> 200 mg / dl . Investigators They received the informed consent letter signed by each patient.

Los sujetos fueron divididos en tres grupos el Grupo 1 recibió el Orlistat 60 mg diariamente. El Grupo 2 recibió la Rosuvastatina 5 mg y el Grupo 3 recibió la combinación Orlistat 60 mg y Rosuvastatina 5 mg diariamente y por 4 semanas .The subjects were divided into three groups Group 1 received the Orlistat 60 mg daily. Group 2 received Rosuvastatin 5 mg and Group 3 received the combination Orlistat 60 mg and Rosuvastatin 5 mg daily and for 4 weeks.

Los parámetros a evaluar fueron la pérdida de peso, la reducción en el índice de masa corporal y la evaluación del perfil de lípidos., así como, eventos adversos.The parameters to be evaluated were weight loss, reduction in body mass index and lipid profile evaluation, as well as adverse events.

Resultados :Results:

Los 24 pacientes terminaron el estudio y fueron evaluados al término del mismo.The 24 patients finished the study and were evaluated at the end of it.

Pacientes del Grupo 1 el 85% tuvieron una pérdida de peso del 5% y una reducción del índice de masa corporal del 3%, el perfil de lípidos se modificó con un promedio de colesterol total de 185 mg/dl.Group 1 patients 85% had a weight loss of 5% and a reduction in body mass index of 3%, the lipid profile was modified with an average total cholesterol of 185 mg / dl.

Pacientes del Grupo 2 el 100% no tuvieron una pérdida de peso ni reducción del índice de masa corporal, el perfil de lípidos se modificó sustancialmente a 170 mg/dl .Group 2 patients 100% had no weight loss or reduction in body mass index, the Lipid profile was substantially modified to 170 mg / dl.

Pacientes del Grupo 3 el 100% tuvo una pérdida de peso del 10% y una reducción del índice de masa corporal del 10%, el perfil de lípidos se modificó aún mas que en el Grupo 2 a 150 mg/dl.Patients of Group 3 100% had a weight loss of 10% and a reduction in body mass index of 10%, the lipid profile was modified even more than in Group 2 at 150 mg / dl.

En ningún caso se presentaron efectos adversos en los que fuera necesario suspender el tratamiento.In no case there were adverse effects in which it was necessary to suspend the treatment.

Ejemplo 2:Example 2:

Se realizó un estudio para evaluar el grado de efectividad y la posible interacción de la combinación.A study was conducted to assess the degree of effectiveness and the possible interaction of the combination.

Se incluyeron 24 sujetos femeninos y masculinos entre 18 y 70 años de edad con un índice de masa corporal entre 18 y 30 kg/m2 o un sobrepeso del 20% del peso ideal, que estuvieran acompañados de una elevación del colesterol total > 200 mg/dl. Los investigadores recibieron la carta de consentimiento informado firmado por cada paciente. Los 24 sujetos recibieron la combinación de Orlistat 60 mg y Rosuvastatina 10 mg diariamente durante 4 semanas y se comparó con los grupos del primer estudio .24 female and male subjects between 18 and 70 years of age were included with a body mass index between 18 and 30 kg / m2 or an overweight of 20% of the ideal weight, which were accompanied by a total cholesterol elevation> 200 mg / dl. The researchers received the informed consent letter signed by each patient. The 24 subjects received the combination of Orlistat 60 mg and Rosuvastatin 10 mg daily for 4 weeks and was compared with the first study groups.

Resultados:Results:

Los 24 pacientes terminaron el estudio y fueron evaluados al término del mismo.The 24 patients finished the study and were evaluated at the end of it.

El 100% de los pacientes tuvo una pérdida de peso del 11% y una reducción del índice de masa corporal del 10%, el perfil de lípidos se modificó aún más que en el primer estudio a 135 mg/dl de colesterol total.100% of the patients had a weight loss of 11% and a reduction in body mass index of 10%, the lipid profile was modified even more than in the first study at 135 mg / dl of total cholesterol.

En ningún caso se presentaron efectos adversos en los que fuera necesario suspender el tratamiento.In no case there were adverse effects in which it was necessary to suspend the treatment.

El invento ha sido descrito suficientemente como para que una persona con conocimientos medios en la materia pueda reproducir y obtener los resultados que mencionamos en la presente invención. Sin embargo cualquier persona hábil en el campo de la técnica que compete el presente invento puede ser capaz de hacer modificaciones no descritas en la presente solicitud, no obstante si para la aplicación de estas modificaciones en una composición determinada o en el proceso de manufactura del mismo, se requiere de la materia reclamada en las siguientes reivindicaciones, dichas estructuras deberán ser comprendidas dentro del alcance de la invención. The invention has been described sufficiently that a person with average knowledge in the field can reproduce and obtain the results mentioned in the present invention. However, any skilled person in the field of the art that is in charge of the present invention may be able to make modifications not described in the present application however, if the material claimed in the following claims is required for the application of these modifications in a particular composition or in the manufacturing process thereof, said structures must be included within the scope of the invention.

Claims

REIVINDICACIONES 1.- Una composición farmacéutica caracterizada porgue contiene como sustancias activas Orlistat 60 mg y Rosuvastatina calcica equivalente a 5 mg de Rosuvastatina en una sola unidad de dosis.1.- A pharmaceutical composition characterized by Porgue contains as active substances Orlistat 60 mg and Rosuvastatin calcium equivalent to 5 mg Rosuvastatin in a single dose unit. 2. - Una composición farmacéutica de conformidad con la reivindicación 1 porque contiene como sustancias activas Orlistat 60 mg y Rosuvastatina calcica equivalente a 10 mg de Rosuvastatina en una sola unidad de dosis .2. - A pharmaceutical composition according to claim 1 because it contains as active substances Orlistat 60 mg and Rosuvastatin calcium equivalent to 10 mg Rosuvastatin in a single dose unit. 3. - Una composición farmacéutica de conformidad con la reivindicación 1 y 2 porque son utilizadas en pacientes con sobrepeso y obesidad que se acompaña de dislipidemia .3. - A pharmaceutical composition according to claim 1 and 2 because they are used in overweight and obese patients accompanied by dyslipidemia. 4.- Una composición farmacéutica caracterizada porque pueden ser utilizadas otras sustancias activas como las estatinas, pravastatina, simvastatina, lovastatina, atorvastatina, cerivastatina, fluvastatina y preferiblemente la rosuvastatina.4.- A pharmaceutical composition characterized in that other active substances such as statins, pravastatin, simvastatin, lovastatin, atorvastatin, cerivastatin, fluvastatin and preferably rosuvastatin. 5. - Una composición farmacéutica de conformidad con la reivindicación 1 en la cual se utilizan menores concentraciones de Orlistat y de Rosuvastatina calcica.5. - A pharmaceutical composition according to claim 1 in which lower concentrations of Orlistat and Rosuvastatin calcium are used. 6. - Una composición farmacéutica de conformidad con la reivindicación 1, 2, 3, 4 ó 5 en la cual se pueden utilizar otras sustancias que son útiles para el tratamiento, prevención y control de desórdenes que están asociados con sobrepeso y obesidad, como, diabetes mellitus tipo 2 como agonistas PPARγ como pioglitazona y rosiglitazona, biguanidas como metformina, fenformina, sulfonilureas como glimepirida, glibenclamida, glipizida, gliburida, repaglinida, nateglinida, tolbutamida, pueden ser utilizadas insulinas .6. - A pharmaceutical composition according to claim 1, 2, 3, 4 or 5 in which other substances that are useful for the treatment, prevention and control of disorders that are associated with overweight and obesity can be used, such as, Type 2 diabetes mellitus as PPARγ agonists such as pioglitazone and rosiglitazone, biguanides such as metformin, fenformin, sulfonylureas such as glimepiride, glibenclamide, glipizide, glyburide, repaglinide, nateglinide, tolbutamide, insulins may be used. 7. - Una composición farmacéutica de conformidad con la reivindicación 1, 2, 3, 4, 5 ó 6 en la cual se pueden utilizar otras sustancias que son útiles para el tratamiento prevención y control de desórdenes que están asociados con sobrepeso y obesidad como insulinas .7. - A pharmaceutical composition according to claim 1, 2, 3, 4, 5 or 6 in which other substances that are useful for the treatment of prevention and control of disorders that are associated with overweight and obesity can be used as insulins 7. - Una composición farmacéutica de conformidad con la reivindicación 1, 2, 3, 4, 5 ó 6 en la cual se pueden utilizar otras sustancias que son útiles para el tratamiento prevención y control de desórdenes que están asociados con sobrepeso y obesidad como hipertensión como antagonistas de los canales de calcio como Amlodipino, felodipino, nimodipino . Inhibidores de la enzima convertidora de angiotensina como captopril, enalapril, losinopril. Antagonistas del receptor de angiotensina como losartan, candesartan y telmisartan. Bloqueadores alfa adrenérgicos . 7. - A pharmaceutical composition according to claim 1, 2, 3, 4, 5 or 6 in which other substances that are useful for the treatment of prevention and control of disorders that are associated with overweight and obesity such as hypertension can be used as calcium channel antagonists such as Amlodipine, felodipine, nimodipine. Angiotensin-converting enzyme inhibitors such as captopril, enalapril, losinopril. Angiotensin receptor antagonists such as losartan, candesartan and telmisartan. Alpha adrenergic blockers.
PCT/MX2007/000044 2006-09-25 2007-04-02 Pharmaceutical composition for treating the excess weight and obesity which accompany dyslipidaemia Ceased WO2008039051A1 (en)

Priority Applications (1)

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ARP070104239A AR062988A1 (en) 2006-09-25 2007-09-25 PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF OVERWEIGHT AND OBESITY ACCOMPANIED WITH DISLIPIDEMIA

Applications Claiming Priority (2)

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MXPA06010973A MXPA06010973A (en) 2006-09-25 2006-09-25 Pharmaceutical composition for treating the excess weight and obesity which accompany dyslipidaemia.
MXPA/A/2006/010973 2006-09-25

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MXPA06010973A (en) 2009-02-18
AR062988A1 (en) 2008-12-17

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