18 results about "Ezetimibe" patented technology

The present disclosure relates to stable pharmaceutical compositions comprising fixed dose combination of obicetrapib and ezetimibe, or their salts, solvates or derivatives thereof. The disclosure further describes the use of ezetimibe and obicetrapib, e.g. in the form of such fixed dose combinations, for preparation of medicaments and method of treatment of subjects requiring reduction in LDL-cholesterol or those suffering from hyperlipidemia or mixed dyslipidemia.

A method of lowering LDL-C levels, reducing cardiovascular risk and / or treatment of a cardiovascular disease, comprising administering to a subject in need thereof, a first amount of AZD0780 or a pharmaceutically acceptable salt thereof and a second amount of ezetimibe or a pharmaceutically acceptable salt thereof, wherein the first amount and the second amount together comprise a therapeutically effective amount.

The invention discloses an ezetimibe pharmaceutical composition and a preparation, a preparation method and application thereof, the composition comprises a therapeutically effective amount of ezetimibe and a composite solubilizer, and the composite solubilizer is composed of vitamin E polyethylene glycol succinate, lauric acid polyethylene glycol glyceride Gelucire50 / 13 and Gelucire48 / 16. By adopting the composite solubilizer and cooperating with conventional auxiliary materials, under the condition of not depending on a high-risk organic solvent or a strong-irritation surfactant, the problems of slow dissolution and poor oral absorption caused by poor water solubility of ezetimibe are solved, and the dual improvement of the absorption speed and degree is realized. The method is simple and stable in process and suitable for industrial production. The prepared ezetimibe tablet is quick in dissolution and high in bioavailability, can realize low-dose efficient treatment, provides a better choice for clinical treatment of primary hypercholesteremia, and has important clinical value and application prospect.

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses an ezetimibe and rosuvastatin calcium tablet and a preparation method thereof. According to the ezetimibe and rosuvastatin calcium tablet and the preparation method thereof, the ultrasonic modified microcrystalline cellulose with high specific surface area and high relative water retention value is added into the ezetimibe and rosuvastatin calcium tablet, ezetimibe can be well coated, in addition, the ultrasonic modified microcrystalline cellulose has more hydroxyl groups, and can form hydrogen bonds with the hydroxyl groups in the ezetimibe, so that the ezetimibe and rosuvastatin calcium tablet can be used for preparing the ezetimibe and rosuvastatin calcium tablet. The ezetimibe stably exists in the pore diameter of the ultrasonic modified microcrystalline cellulose, and the solubility of the ezetimibe can be effectively improved in the drug release process.

The present invention relates to a pharmaceutical combination preparation, which comprises all of ezetimibe, rosuvastatin and empagliflozin as active ingredients, and thus can be administered as a single drug, and not through co-administration, in the simultaneous treatment of dyslipidemia and diabetes, thereby increasing patient dosing convenience, minimally affecting dissolution between drugs, ensuring biological equivalence, and providing excellent stability of the active ingredients.

The present invention relates to a pharmaceutical combination preparation comprising ezetimibe and losartan. When the pharmaceutical combination preparation is dissolved in a solution of pH 4.0 to 5.0 for 10 minutes, the amount of losartan dissolved is 5,700 µg or less, and the amount of ezetimibe dissolved is 270 µg or more. Dissolution in a solution of pH 4.0 to 5.0 is carried out under conditions of a temperature of 37°C and a paddle method of 50 rpm in 500 mL of acetate pH regulator in accordance with the United States Pharmacopeia for the preparation of a pharmaceutical combination comprising 20 mg of ezetimibe and 183 mg of losartan.

This invention relates to a modified ezetimibe having the structure of Formula (I) or a pharmaceutically acceptable salt thereof for use in the treatment of cancer by oral administration through inhibition of HDM2 / HDM4-mediated suppression of p53, wherein the binding affinity and oral bioavailability of the modified ezetimibe for targeting of HDM2, HDM4 (also known as HDMX) and more particularly, both HDM2 and HDM4 is enhanced compared with unmodified ezetimibe.

The invention relates to solid pharmaceutical compositions comprising or essentially consisting of (A) an intragranular phase comprising or essentially consisting of (i) ezetimibe, a pharmaceutically acceptable salt and / or solvate thereof; (ii) one or more intragranular diluents; (iii) one or more intragranular binders; (iv) optionally, one or more intragranular disintegrants; and (v) optionally, one or more intragranular surfactants; and (B) an extragranular phase comprising or essentially consisting of (vi) pitavas-tatin, a pharmaceutically acceptable salt and / or solvate thereof; (vii) one or more extragranular diluents; (viii) optionally, one or more extragranular disintegrants; and (ix) optionally, one or more extragranular lubricants. The invention further relates to an oral dosage form comprising the solid pharmaceutical composition suitable for oral administration.

The present disclosure relates to combinations of obicetrapib and ezetimibe, or their salts, solvates or derivatives thereof. The disclosure further describes the use of ezetimibe and obicetrapib, e.g. in the form of a fixed dose combination product, for preparation of medicaments and method of treatment of subjects requiring reduction in LDL-cholesterol or those suffering from hyperlipidemia or mixed dyslipidemia.

A solid oral pharmaceutical composition, comprising: a first active ingredient, which is pitavastatin or a pharmaceutically acceptable salt thereof, and a second active ingredient, which is a pharmaceutically acceptable salt thereof; the second active ingredient is ezetimibe or a pharmaceutically acceptable salt of the ezetimibe; and at least one excipient comprising a diluent, a stabilizer, a disintegrating agent, an adhesive, a sweetener, a lubricant, a glidant, a perfume, a colorant or a combination thereof.

Methods are presented for improving atherosclerotic plaque characteristics in a patient with atherosclerotic cardiovascular disease (ASCVD). The method comprises administering an effective amount of obicetrapib, or pharmaceutically acceptable salt, solvate, or co-crystal thereof, and optionally co-administering an effective amount of ezetimibe, or pharmaceutically acceptable salt or solvate thereof, to the patient. Methods are also provided for reducing coronary artery inflammation in a patient with atherosclerotic cardiovascular disease (ASCVD). The method comprises administering an effective amount of obicetrapib, or pharmaceutically acceptable salt, solvate, or co-crystal thereof, and optionally co-administering an effective amount of ezetimibe, or pharmaceutically acceptable salt of solvate thereof, to the patient. In preferred embodiments, obicetrapib is administered as amorphous obicetrapib hemicalcium. In particularly preferred embodiments, amorphous obicetrapib hemicalcium and ezetimibe are administered daily in a fixed dose combination (FDC) oral dosage form.

Disclosed is a new compound of formula (I) or a pharmaceutically acceptable salt thereof, which binds tightly to the hydrophobic binding pocket of Mdm2, thereby preventing Mdm2 from binding to the tumor suppressor p53 and increasing p53 levels. Also disclosed is the use of the compound or a pharmaceutically acceptable salt thereof for the treatment of Mdm2 cancer and its use in the manufacture of a medicament.

The present disclosure relates to combinations of obicetrapib and ezetimibe, or their salts, solvates or derivatives thereof. The disclosure further describes the use of ezetimibe and obicetrapib, e.g. in the form of a fixed dose combination product, for preparation of medicaments and method of treatment of subjects requiring reduction in LDL-cholesterol or those suffering from hyperlipidemia or mixed dyslipidemia.

The invention belongs to the technical field of pharmaceutical analysis, and particularly relates to a method for determining chiral isomers in rosuvastatin calcium ezetimibe tablets. The invention provides a method for determining a chiral isomer in a rosuvastatin calcium ezetimibe tablet, which comprises the following steps: changing an isocratic elution mode into a gradient elution mode, establishing an effective pretreatment method, optimizing a test solution solvent and a high performance liquid chromatography with specific parameters, and determining the chiral isomer in the rosuvastatin calcium ezetimibe tablet. The problems that the solubility difference of rosuvastatin calcium and ezetimibe is large, rosuvastatin calcium is unstable to acid, ezetimibe is unstable to alkali, isocratic elution time is too long and the like are solved. The quality of chiral isomers of rosuvastatin calcium and ezetimibe, which are recorded in European Pharmacopoeia and United States Pharmacopoeia, is controlled; establishing sensitivity and system applicability requirements; the retention time and correction factors of specific impurities are marked, so that the detection result is more accurate.

This invention relates to a modified ezetimibe having the structure of Formula (I) or a pharmaceutically acceptable salt thereof for use in the treatment of cancer by oral administration through inhibition of HDM2 / HDM4-mediated suppression of p53, wherein the binding affinity and oral bioavailability of the modified ezetimibe for targeting of HDM2, HDM4 (also known as HDMX) and more particularly, both HDM2 and HDM4 is enhanced compared with unmodified ezetimibe. (I)

This invention relates to the field of pharmaceutical analysis technology and discloses a method for detecting the content of ezetimibe and rosuvastatin calcium tablets using a reversed-phase chromatography system. The method employs high-performance liquid chromatography (HPLC) with 0.1% trifluoroacetic acid solution as mobile phase A, acetonitrile as mobile phase B, and methanol as mobile phase C. Gradient elution is performed using an octadecylsilane-bonded silica column. The detection wavelength is 242 nm, and the injection volume is 10 μL. The content of ezetimibe and rosuvastatin calcium is calculated using the external standard method. This method can effectively separate the two main components from various degradation impurities, exhibiting good peak shape and excellent resolution. It meets the requirements for pharmaceutical quality control in terms of specificity, limit of quantitation, limit of detection, linear range, precision, accuracy, repeatability, and robustness. The system is stable and provides a reliable technical solution for the quality detection of ezetimibe and rosuvastatin calcium tablets.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a rosuvastatin ezetimibe preparation and a preparation method thereof. Comprising the following steps: (1) dissolving an ezetimibe raw material in a solvent to obtain an ezetimibe solution, taking sulfobutyl-beta-cyclodextrin, adding purified water, mixing, adding the ezetimibe solution, and drying at low temperature to obtain an ezetimibe inclusion compound; (2) premixing a rosuvastatin calcium raw material, a filling agent and a flow aid, then sieving the premixed material, the ezetimibe clathrate compound, a disintegrating agent and the filling agent, adding a lubricating agent, and mixing to obtain rosuvastatin and ezetimibe total mixed powder; (3) tabletting the total mixed powder of the rosuvastatin and the ezetimibe to obtain a rosuvastatin and ezetimibe substrate; and (4) carrying out film coating on the rosuvastatin ezetimibe substrate to obtain the rosuvastatin ezetimibe tablet. The method is simple in process, good in production continuity, high in mechanization degree and suitable for industrial production, the obtained preparation is stable in quality and accurate in dosage, and the quality of the preparation is consistent with that of an original developed preparation.