105 results about "Rosiglitazone" patented technology

Rosiglitazone is a drug used to treat type 2 diabetes. Methods for the formation of amorphous rosiglitazone and formulations comprising the amorphous rosiglitazone are described. Other formulations include pulsed-release formulations and formulations for retention in the stomach and upper gastrointestinal tract. Controlled-release dosage form include those wherein the maximum plasma concentration of rosiglitazone occurs greater than one hour after administration to a human and / or wherein less than 75 percent by weight of the rosiglitazone is released at 1 hour after immersion in simulated gastric fluid.

Co-therapy of an anti-obesity agent, a statin, and a glitazone is disclosed along with fixed combinations thereof. Atorvastatin, rosiglitazone, and orlistat are preferred as the various components. Non-glitazone antidiabetic agents may be optionally added to the therapy and / or to the fixed combination product.

The invention relates to the technical field of medical science, in particular to new application of a ferroptosis inhibitor. The ferroptosis inhibitor is prepared from Liproxstatin-1, Ferrostatin-1,rosiglitazone, pioglitazone, troglitazone and Zileuton. The new application refers to that the inhibitor is applied to treating radiation-induced pulmonary injury diseases. The application has the advantages that (1) radioactive rays trigger radiation-induced pulmonary injury by mediating pulmonary alveoli epithelial cells to have ferroptosis, the ferroptosis specificity inhibitor can be used to prevent and treat radiation-induced pulmonary injury, and has the important meaning on development of new drug for preventing and treating radiation-induced pulmonary injury; and (2) it is found that radioactive rays can cause cell death through the mode of ferroptosis, and application of the ferroptosis inhibitor also has the significant theoretical meaning on guiding research for guiding radioactive rays to treat cancer mechanism.

The invention also provides methods, apparatuses and reagents useful for predicting future atherosclerosis based on expression levels of genes selected from the set of 68 genes with differential expression in response to pioglitazone and rosiglitazone. The invention also discloses reagent sets and biomarkers for predicting progression of atherosclerosis induced by anti-diabetic therapy in a subject. In one particular embodiment the invention provides a method for predict whether a compound will induce atherosclerosis using gene expression data from sub-acute treatments.

The invention provides a method for identifying whether a blood-glucose-lowering traditional Chinese medicine contains pioglitazone or rosiglitazone or not. The method comprises the following steps: carrying out thin layer chromatography on a blood-glucose-lowering traditional Chinese medicine to be detected; finding a suspected spot at a corresponding Rf value part of the pioglitazone and the rosiglitazone. The method is characterized by further comprising the following three steps: 1, collecting a series of one-dimensional surface enhanced Raman spectrums of the suspected spot to obtain a dynamic spectrum pattern of the blood-glucose-lowering traditional Chinese medicine to be detected; 2, pre-treating the dynamic spectrum pattern and drawing to obtain a two-dimensional correlation surface enhanced Raman spectrum of the blood-glucose-lowering traditional Chinese medicine to be detected; 3, judging whether the blood-glucose-lowering traditional Chinese medicine contains the pioglitazone or the rosiglitazone or not according to the two-dimensional correlation surface enhanced Raman spectrum of the blood-glucose-lowering traditional Chinese medicine to be detected. According to the technical scheme provided by the invention, whether the blood-glucose-lowering traditional Chinese medicine contains the pioglitazone or the rosiglitazone or not can be identified rapidly; the detection result is accurate and reliable, the cost is low and the operation is convenient.

The present invention relates to rosiglitazone and its pharmaceutically acceptable salts free of at least one of the process related impurities, in particular the dehydro and the succinic acid impurities of rosiglitazone, wherein said impurities are present in an amount of about 05 mg to not more than about 15 mg, and processes for their preparation.

The invention relates to a separation, culture and induction differentiation method for precursor adipocyte in chicken muscle and belongs to the technical field of cytology. According to the method, hormone mixture 3-isobutyl-1-methylxanthine, dexamethasone and insulin are used, an induction differentiation system of external-source oleic acid and rosiglitazone is added, generation of oil drop ofprecursor adipocyte in the chicken muscle is induced, and an effective research means can be provided for the quality of poultry meat and particularly fat deposition in poultry muscle. By adopting themethod, intramuscular precursor adipocyte which is even in component and exuberant in proliferation and differentiation can be obtained, the effective induction differentiation system of adipocyte inthe chicken muscle is obtained, and the method has the advantages that the method is simple and convenient, easy to operate, low in cost, high in vigor and excellent in proliferation and differentiation capacity and can achieve acquirement of a large number of cells.

A method for predicting treatment response of a type II diabetes patient to rosiglitazone is provided. The method involves at least one sample from a patient having type II diabetes and analyzing biomarkers predictive of a patient who will respond to treatment with rosiglitazone. The biomarkers include, at least, interleukin-8, histidine, citrate. These biomarkers are identified in at least one classification analyses selected from the group consisting of a majority-vote based classifier and support-vector machine (SVM) classifier. Also provided is a method for predicting treatment response of a type II diabetes patient to glyburide at 8 weeks post-initiation of therapy. The method involves obtaining a sample from a type II diabetes patient who has been treated with glyburide for about 4 weeks and analyzing biomarkers predictive of a patient who will respond to treatment with glyburide at 8 weeks. The biomarkers useful in this method include, at least, sphingomyelin 23:1 and L-phenylalanine. Also provided are kits useful for the methods of the invention.

The invention discloses application of Lunasin polypeptide in the aspect of preparing substance with weight-reducing activity. Lunasin is substance with weight-reducing activity and is prepared by inhibiting differentiation of mouse preadipocyte (3T3-L1) through a PPAR gamma passage. The application includes: using an MTT method to detect influence, on 3T3-L1 adipocyte activity, of Lunasin at different dosages; detecting inhibiting effect, on adipocyte differentiation, of Lunasin at different dosages. Compared with current study conditions of Lunasin, the application has the advantages that the application shows that Lunasin can inhibit differentiation of insulin-induced 3T3-L1 cells, reduce accumulation of lipid droplets in lipid and inhibit mRNA expression of PPAR gamma, Lunasin presents dosage dependence, and effect of Lunasin with dosage higher than 50ug / mL is better than that of rosiglitazone of 5ug / mL; the application shows that Lunasin has potential weight-reducing effect.

There is provided a pharmaceutical composition that is adapted for pulmonary administration by inhalation, which composition comprises a glitazone, such as pioglitazone or rosiglitazone, and one or more pharmaceutically acceptable carriers and / or excipients, and wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer. There is also provided a use and kit.

The present invention relates to a kind of slow released preparation containing metformin hydrochloride and rosiglitazone and its preparation process. The preparation consists of slow released metformin hydrochloride and quickly released rosiglitazone. The extracorporeal leaching test shows that rosiglitazone is released in over 75 % in 30 min. The metformin hydrochloride is released in 15-40 % in the first 1 hr, 50-70 % in the first 4 hr, and over 75 % in the first 8 hr. The slow released preparation containing metformin hydrochloride and rosiglitazone has mild and lasting blood sugar reduction, capacity of avoiding hypoglycemia, gastrointestinal discomfort and other untoward reaction, decreased medicine taking times and raised compliance. The present invention also discloses the extracorporeal slow releasing characteristic and preparation process of the slow released preparation.

The invention relates to a detection method for qualitatively detecting whether thiazolidinedione medicines are doped in a Chinese patent medicine and a health food which have a hypoglycemic effect. The method comprises the following steps: 1, taking a sample to be measured, adding dichloromethane according to a case that 5-10mL of dichloromethane corresponds with 1g of the sample, strongly shaking for at least 40s, and filtering; 2, adding a small amount of a hydrochloric acid solution with the concentration of 0.08-0.12mol / L to a filtrate obtained in step 1, up-down overturning at least eight times, and standing for two-phase layering; and 3, adding a proper amount of a phosphomolybdic acid solution with the concentration of 0.04-0.1g / mL to an upper layer obtained in step 2 drop by drop. If deposition or turbidity appears, it shows that rosiglitazone or pioglitazone is doped in the sample. A corresponding kit comprises a reagent 1: dichloromethane; a reagent 2: the hydrochloric acid solution with the concentration of 0.08-0.12mol / L; and a reagent 3: the phosphomolybdic acid solution with the concentration of 0.04-0.1g / mL. The detection method of the invention has the advantages of accuracy and reliability, and the kit is convenient for carrying and carrying out onsite detection.

A novel process for the preparation of a compound of the formula (II), which is useful as intermediate compound for the preparation of thiazolidinedione derivatives, such as rosiglitazone, pioglitazone, troglitazone and ciglitazone, is disclosed. The novel process comprising reacting a compound of the formula (III) with a compound of the formula (IV) in a mixture of a non-polar water immiscible organic solvent and water (two phase system) with an alkali metal hydroxide or an alkali metal carbonate as a base in the presence of a phase transfer catalyst. In the first aspect of the present invention comprising reacting 2-(N-methyl-N-(2- pyridyl) ethanol with 4-fluorobenzaldehyde in the mixture of a non-polar water immiscible organic solvent, preferably toluene, and water with an alkali metal hydroxide or an alkali metal carbonate as a base, preferably potassium hydroxide, in the presence of a phase transfer catalyst, e.g. tetra n-butylammonium hydrogensulphate or benzyltriethylammonium chloride, to obtain 4-[2-(N-methyl-N-(2- pyridyl)amino)ethoxy]benzaldehyde, which is the key intermediate for preparing rosiglitazone and its salts, e.g. maleate salt or phosphate salt, useful in the treatment of Type II diabetes.

A compound of the formula: wherein A represents a ring group connected to the oxygen atom by a C1 to C6 hydrocarbon chain, R is hydrogen or a C1-C4 alkyl, and Q is hydrogen, or an amine protecting group such as acetyl, trifluoroacetyl, benzoyl, benzyl, or trityl, is useful in making thiazolidinedione derivatives such as pioglitazone, rosiglitazone and troglitazone.

The invention provides a traditional Chinese medicine for curing type II diabete, which is Hubei dwarf lilyturf tuber hetetopolysaccharide extracted by taking Hubei dwarf lilyturf tuber as a raw material. The traditional Chinese medicine has obvious effects of reducing blood sugar of mice with the type II diabete, obvious effects of reducing insulin resistance and the effect strength of the traditional Chinese medicine has no statistical difference from that of rosiglitazone. Compared with the rosiglitazone, the hetetopolysaccharide can better reduce blood total cholesterol and triglycercide, improve ratio of high-density lipoprotein to low-density lipoprotein, and effectively prevent and curing arteriosclerosis and thrombosis.

The invention discloses a qualitative analysis detection method for illegally mixed high-polar chemical anti-diabetic components in anti-diabetic traditional Chinese medicine products. The method comprises the following steps that: 1) high efficient liquid phase chromatography conditions: an ammonium acetate-triethylamine-acetonitrile moving phase system and a C18 chromatographic column with certain specification are used, the wavelength is detected by ultraviolet, and the flow rate is 1.0ml / min; 2) analysis result: glibenclamide, glipizide, gliclazide, glimepiride, gliquidone, repaglinide, nateglinide, rosiglitazone and pioglitazone hydrochloride can realize the complete separation; 3) result judgment: when retention time of a chromatographic peak in an anti-diabetic traditional Chinese medicine product is consistent with that of anti-diabetic medicine in the step 2) and the apparent absorption is shown out, which indicate that the anti-diabetic medicine is contained in the sample to be tested. The method has the advantages of quickness, simplicity, convenience, high sensitivity, strong specialization, broad coverage and so on.

The invention provides a differentiation inducing agent and method for murine preadipocytes 3T3-L1. The differentiation inducing agent is prepared from 3-isobutyl-1-methylxanthine, insulin, dexamethasone, rosiglitazone and FBS. The differentiation inducing method comprises the steps that 3T3-L1 cells are cultured in a high-glucose DMEM culture solution containing the differentiation inducing agentafter routine resuscitation culture, then cultured in a high-glucose DMEM culture solution containing insulin and 10% FBS and then cultured in a high-glucose DMEM culture solution containing 10% FBSby means of a half-solution change method. By means of the method, the differentiation cycle is short and is only 6-7 days, the conversion rate of the preadipocytes is high, the cell differentiation is uniform, and the development of studies on fat metabolism diseases is greatly promoted.

The invention relates to a sustained-release preparation of compound metformin hydrochloride rosiglitazone and a preparation method thereof; wherein, rosiglitazone and metformin hydrochloride have slow releasing characteristic in an in-vitro dissolution test, the rosiglitazone is released by 10-30 percent for a first hour, and is released by 60-80 percent for a fourth hour, and is released by morethan 80 percent for an eighth hour; the metformin hydrochloride is released by 15-40 percent for a first hour, is released by 50-70 percent for a fourth hour, and is released by more than 75 percentfor an eighth hour. The formula is mild and has prolonged action of glucose reduction, so as to avoid adverse reaction such as hypoglycemia and gastrointestine malaise, reduce taking times (one or twotimes each day), and improve compliance of a patient. The invention discloses the in-vitro drug-releasing characteristic of the sustained-release preparation and the preparation method thereof.

The invention discloses a CBH culture medium for inducing the chicken preadipocyte differentiation and a differentiation method thereof. The CBH culture medium is prepared by adding the following components into a conventional culture medium: bovine insulin (20[mu]g / mL), dexamethasone (1[mu]M), 3-isobutyl-1-methyl xanthine (0.5mM), and rosiglitazone (5[mu]M). The differentiation method comprises the following steps: separating and culturing chicken primary preadipocyte; when cells reach 50% confluence in a growth culture medium, dividing cells into a control group and an induction group; culturing the control group in the growth culture medium, while culturing the induction group in a CBH culture medium, respectively changing the cultures every day, and carrying out induction for six days. The result shows that the lipid droplets of the cells in the induction group deposit, GPDH activity and expression levels of aP2, G0S2, and PPAR[gamma]mRNA of the induction group are prominently higher than those of the control group, and the result show that CBH culture medium can induce chicken preadipocyte differentiation.

The present invention relates to slow released medicine preparation, and is especially one kind of slow released rosiglitazone tablet and its preparation process. The slow released rosiglitazone tablet consists of core tablet and coating layer, the core tablet consists of solid rosiglitazone dispersion, sodium alginate, hypromellose and magnesium stearate, the coating layer consists of rosiglitazone, sodium alginate, microcrystalline cellulose, hypromellose and magnesium stearate, and the solid rosiglitazone dispersion consists of rosiglitazone and polyglycol-6000. The slow released rosiglitazone tablet has less medicine taking times, relatively long period of maintaining certain blood medicine concentration in human body, long period for body to maintain sensitivity on insulin, and raised medicine safety, effectiveness and adaptability.

The invention discloses a medicine composition for treating diabetes mellitus and complications thereof, and in particular relates to a medicine composition comprising arctigenin and rosiglitazone or pharmaceutically acceptable salts thereof, and application of the composition in preparation of a medicine for treating diabetes mellitus, diabetes mellitus complications and diseases relative to thediabetes mellitus.

The invention relates to the field of the biotechnology, in particular to an adipogenesis induction culture medium and an adipogenic differentiation method. The adipogenesis induction culture medium comprises 3-isobutyl-1-methylxanthine, insulin, indomethacin, dexamethasone, rosiglitazone, PRP (Platelet Rich Plasma) and a basic culture medium. The invention provides an adipogenic differentiation method which enables various inducing factors to be subjected to combined application to act on mesenchymal stem cells including GMSCs and like, has a synergistic effect and can effectively induce the adipogenic differentiation of the mesenchymal stem cells, and the adipogenic differentiation effect of the adipogenic differentiation method is obviously superior to that of an existing conventional induction method. The GMSCs autologous materials are abundant, are easy in expansion in vitro and can be used for autotransplantation so as to avoid immunological rejection reaction.

The present invention provides a compound of the formula (I): wherein A represents a ring group connected to the oxygen atom by a C1 to C6 hydrocarbon chain, R is hydrogen or a C1-C4 alkyl, and Q is hydrogen, or an amine protecting group such as acetyl, trifluoroacetyl, benzoyl, benzyl, or trityl, is useful in making thiazolidinedione derivatives (formula (II)), such as pioglitazone, rosiglitazone and troglitazone.

A composite medicine for treating polycystic kidney disease contains the epoxidase 2(COX-2) specific depressant and the thiazolidbione-type medicine.

The invention relates to a culture medium and method for quickly inducing the differentiation of human mesenchymal stem cells to obtain fat. According to the method, at first, an IMDM culture medium is improved: FBS, penicillin, streptomycin, dexamethasone, diluted insulin, 3-isobutyl-1-methylxanthine and rosiglitazone are added into the IMDM culture medium in sequence to obtain an inducing culture medium; primary human mesenchymal stem cells are subjected to subculture; then the inducing culture medium is used to culture human mesenchymal stem cells, and finally the human mesenchymal stem cells are differentiated to obtain fat cells. In the inducing culture medium, dexamethasone, insulin, 3-isobutyl-1-methylxanthine and rosiglitazone all have a fat differentiating inducing function. The provided culture medium and method can accelerate the induced differentiation, shorten the experiment time, increase the induced differentiation rate at the same time, reduce the chance that cells arepolluted, and guarantee the activity of cells.

The invention discloses a method for preparing rosiglitazone tartrate, relates to a method for preparing a novel medicinal compound, namely 5-[4-[2-methyl-N-(2-pyridyl) amino] ethoxy] thiazolidine-2,4-diketone tartrate, and belongs to the field of medicinal chemistry. The method comprises the following steps of: adding 5-[4-[2-methyl-N-(2-pyridyl) amino] ethoxy] thiazolidine-2,4-diketone into a polar solvent, adding tartaric acid with heating to dissolve the 5-[4-[2-methyl-N-(2-pyridyl) amino] ethoxy] thiazolidine-2,4-diketone, refluxing, cooling to room temperature after the reaction is finished, filtering, drying, and thus obtaining a product. The method is high in yield, short in reaction time, very simple in post treatment and convenient for industrialized production. The prepared compound can be used for treating type II diabetes and multiple diabetic complications, and is high in bioavailability and quick in response; and the pharmacokinetics of the compound is not affected by age.

The invention discloses a diabetes treating compound medicine for reducing side effect of rosiglitazone and a preparation method thereof, and belongs to the field of medicine preparation. The compound medicine consists of rosiglitazone and a diuretic medicine, wherein the ratio of rosiglitazone to the diuretic medicine by weight is 1:(0.04-1). The diabetes treating compound medicine is compounded and matched with any one of spirolactone, amiloride, compound amiloride, ergosterol, triamterene, ethacrynic acid, hydroflumethiazide and bumetanide which can better eliminate side effect of rosiglitazone with rosiglitazone so as to form the compound medicine which not only can reduce the side effect of rosiglitazone, but also better treats diabetes.

The invention discloses a tartaric acid rogridone dispersing tablet for curing II type diabetes mellitus and a preparation method thereof. The water-solubility of the tartaric acid rogridone is inferior, the absorption thereof is slow after taking orally, the bioavailability is low and no tartaric acid rogridone dispersing tablet is marketed at home and abroad. The tartaric acid rogridone dispersing tablet of the invention is prepared by using 0.5 to 15% of tartaric acid rogridone, 10 to 90% of filler, 1 to 10% of disintegrating agent, 0.1 to 30% of adhesive and 0.5 to 6% of lubricating agent. The invention not only widens the dosage form scope of the tartaric acid rogridone but also can rapidly disintegrate the dispersing tablet, quickly absorb and promote the bioavailability and blood concentration so as to promote the curative effect of the drug and conveniently take.

The invention discloses a drug combination which can lower blood sugar, containing guava leaf extract and rosiglitazone or pioglitazone. The drug combination of the invention can not only put the sugar lowering function of guava leaf extract and rosiglitazone or pioglitazone into fullplay so as to lead to the synergetic effect of the two medicines, but also can reduce adverse reaction and give full play to the advantages of definite curative effect and rapid onset time of chemical drugs as well as the functions of balancing the human body and lowering toxicity of traditional Chinese medicines.