35 results about "Abiraterone acetate" patented technology

The invention provides abiraterone acetate and a preparation method thereof, and belongs to the technical field of organic synthesis. The preparation method comprises the following steps: mixing dehydroepiandrosterone, an aprotic polar solvent, an acylating agent and a first acid-binding agent, and carrying out first esterification reaction to obtain dehydroepiandrosterone acetate; mixing dehydroepiandrosterone acetate, a first solvent, a second acid-binding agent and halogen phosphate, and performing second esterification reaction to obtain an intermediate; and mixing the intermediate, a second solvent, 3-pyridine borate, a ligand, alkali and a metal catalyst, carrying out a coupling reaction, and carrying out post-treatment to obtain abiraterone acetate. According to the method, phosphate is obtained from halogen phosphate, so that the cost is low, the reagent toxicity is relatively low, and the yield is higher; phosphate ester is used as a coupling substrate, the reaction is stable, high-temperature conditions are not needed, energy consumption is low, impurities are few, and the yield is high. The result of the embodiment shows that the purity of the abiraterone acetate is higher than 99.35, and the yield is higher than 85%.

The present invention provides a method for preparing a high-purity and high-yield abiraterone acetate intermediate. The preparation method of the present invention comprises the steps of: (1) detecting the water content of raw material iodine: reacting zinc powder with iodine in solvent A, filtering and removing solids, and using Karl Fischer method to determine the water content N1 in the filtrate; performing a blank control experiment without iodine addition at the same time, using Karl Fischer method to determine the water content N2 in the filtrate in the blank control experiment, and calculating the water content of raw material iodine; (2) adding solvent B, iodine, and acetic anhydride to a container, stirring the reaction, adding tetramethylguanidine, adding dehydroepiandrosterone-17-hydrazone I, performing iodination reaction, and obtaining abiraterone acetate intermediate 17-iodo-androsta-5,16-diene-3β-alcohol II; the abiraterone acetate intermediate obtained by the method of the present invention has high yield and high purity.

The present invention belongs to the technical field of pharmaceutical preparations, and specifically relates to an abiraterone acetate suppository and a preparation method thereof. The abiraterone acetate suppository of the present invention comprises abiraterone acetate and a matrix. The matrix of the prescription amount is weighed, heated and melted, the abiraterone acetate of the prescription amount is added, stirred to dissolve, and filled on a suppository filling line to obtain the abiraterone acetate suppository. Compared with the prior art, the present invention greatly improves bioavailability, has a simple preparation process, and is suitable for large-scale industrial production.

Provided are methods and compositions, for treating prostate cancer by administering to a patient in need thereof a therapeutically effective amount of a PARP inhibitor, e.g., niraparib; a therapeutically effective amount of a CYP17 inhibitor, e.g., abiraterone acetate, and a therapeutically effective amount of a glucocorticoid, e.g., prednisone.

A method for preparing abiraterone acetate and an intermediate thereof are provided. In the method, in an organic solvent, in the presence of a metal catalyst, reacting a 3-site protected 17-hydroxy ester androst-5,16-diene-3β-hydroxy (ester) with a 3-substituted pyridine derivative to obtain abiraterone acetate or the intermediate thereof.

The present disclosure relates to niraparib and abiraterone acetate, plus prednisone or prednisolone; for use in a method of improving the efficacy of treatment of metastatic castration-resistant prostate cancer (mCRPC) in a patient with DNA-repair anomalies, in particular for improving the median radiographic progression-free survival (rPFS).

A nano abiraterone acetate composition, a preparation method therefor, and an oral tablet thereof. The composition comprises abiraterone acetate, a suspending aid, a surfactant, and a stabilizer in percentage by weight of 1:(0.1-4):(6-20):(0.01-0.1), and is prepared by wet grinding, drying, and dewatering. The oral bioavailability of the product is improved by adding a cholate absorption-promoting agent, such that the influence of food on drug absorption is reduced.

The application relates to a combination therapy for prostate cancer. The present invention provides methods and compositions for treating prostate cancer by administering to a patient in need thereof: a therapeutically effective amount of a PARP inhibitor, such as niraparib; a therapeutically effective amount of a CYP17 inhibitor, such as abiraterone acetate; and a therapeutically effective amount of a glycocortin, such as prednisone.

The invention discloses an abiraterone acetate self-nanoemulsion liquid-filled capsule as well as a preparation method and application thereof. The abiraterone acetate self-nanoemulsion liquid-filled capsule is good in self-nanoemulsion effect, controllable in preparation quality and remarkable in killing effect on prostate cancer cells, the bioavailability of the capsule is improved by 12.54 times compared with that of commercially available tablets, the influence of food on the bioavailability of drugs is reduced, the limitation of abiraterone tablets in clinical application is expected to be overcome, and the capsule is worthy of popularization and application. The research has important scientific significance and potential clinical application value.

Disclosed is abiraterone or a pharmaceutically acceptable salt thereof in a therapeutically effective amount for use in the treatment of Cushing's disease in dogs, wherein the pharmaceutically acceptable salt is preferably abiraterone acetate.

The present disclosure relates to a combination of abiraterone acetate and niraparib, free-dose and fixed-dose combinations of abiraterone acetate and niraparib, and methods of treatment of prostate cancer with said combinations.

The invention discloses a pharmaceutical composition containing abiraterone acetate and a preparation method thereof. The raw materials of the pharmaceutical composition include abiraterone acetate and a carrier, wherein the carrier is hydroxypropyl methylcellulose acetate succinate and methacrylic acid copolymer type C; or the carrier is hydroxypropyl methylcellulose acetate succinate. The pharmaceutical composition containing abiraterone acetate of the invention is an amorphous drug, which has high thermal stability, does not undergo crystal transformation for at least 45 days under accelerated conditions, and exists in a stable amorphous state; in the saliva and small intestine pH environment, it has higher instantaneous solubility and dissolution rate than abiraterone acetate, can be prepared into various forms of pharmaceutical preparations for administration, and has broad clinical application prospects.

The present application relates to the technical field of pharmaceutical preparation, and in particular to an abiraterone acetate enteric microcapsule and a preparation method thereof. The present application uses an emulsion diffusion method to prepare abiraterone acetate nanocapsules, then uses an enteric material to load the abiraterone acetate nanocapsules, and finally uses a spray drying technology to prepare abiraterone acetate oral enteric microcapsules. Through pharmacokinetic tests of a rat chylomicron blocking model, it is verified that the abiraterone acetate enteric microcapsules prepared by the present application are absorbed by the lymphatic pathway in the small intestine, so it is proved that the present application can enhance the permeability and solubility of abiraterone acetate in the body, improve the oral bioavailability thereof in the body, the preparation method is simple and controllable, has good repeatability, the particle size of the prepared nanocapsules is 182.3±5.7 nm, the Zeta potential is-15.0±1.1 mV, and the encapsulation rate is 92.4±1.7%.

This disclosure relates to methods of treating prostate cancer in a subject. This disclosure more specifically relates to methods for treating prostate cancer, such as metastatic castration-resistant prostate cancer, by administering to the subject olaparib and abiraterone acetate or a salt thereof.

The invention relates to the technical field of medicine detection, and discloses a method for detecting N-oxide impurities in abiraterone acetate medicine, which comprises the following steps: mixing an N-oxide impurity reference substance with acetonitrile to obtain a reference substance solution; the method comprises the following steps: mixing an abiraterone acetate medicine to be detected with acetonitrile to obtain a test solution; detecting the reference substance solution and the test solution by adopting a high performance liquid chromatography to obtain a chromatogram; in the detection process of the high performance liquid chromatography, mobile phases comprise a mobile phase A and a mobile phase B, the mobile phase A is acetonitrile, and the mobile phase B is water; and (4) analyzing by adopting an external standard method according to the chromatogram to obtain the content of the N-oxide impurity in the abiraterone acetate medicine. The method is high in detection sensitivity on the N-oxide impurities in the abiraterone acetate tablets, the method is good in durability, the N-oxide impurities in the abiraterone acetate tablets can be effectively controlled, and the controllability of the quality of the abiraterone acetate tablets is improved.

The present disclosure relates to niraparib and abiraterone acetate, plus prednisone or prednisolone: for use in a method of improving the efficacy of treatment of metastatic castration-resistant prostate cancer (mCRPC) in a patient with DNA-repair anomalies, in particular for improving the median radiographic progression-free survival (rPFS).

The application discloses a pharmaceutical composition containing abiraterone acetate and a preparation method and application thereof. An excipient of the pharmaceutical composition contains at least one oil phase, at least one emulsifier and at least one co-emulsifier. The pharmaceutical composition can significantly improve bioavailability and stability of a preparation. The pharmaceutical composition can be further prepared into a capsule.

The invention discloses an abiraterone borane carrying agent with prostatic cancer targeting property as well as a preparation method and application of the abiraterone borane carrying agent. The abiraterone borane compound comprises abiraterone borane and abiraterone acetate borane. According to the embodiment of the invention, based on abiraterone acetate and prostatic cancer targeting and safety of abiraterone, a borane group is introduced into structures of abiraterone acetate and abiraterone acetate, and a novel boron carrying agent is obtained and is used for BNCT treatment of prostatic cancer. The novel boron carrying agent not only retains the CYP17 enzyme inhibitory activity of abiraterone and abiraterone acetate, but also provides the possibility of targeting prostate cancer cells for BNCT by introducing a 10B isotope. Through the innovative medicine design, the curative effect and selectivity of BNCT in prostatic cancer treatment can be remarkably improved, damage to normal tissue is reduced, and a safer and more effective treatment choice is provided for prostatic cancer patients.

The present invention discloses a preparation method of abiraterone acetate and its intermediate. The preparation method includes the steps: (1) in a solvent, in the presence of a metal catalyst, a ligand and a base, 3 - protected 17 - hydroxyester androst - 5,16 - diene - 3β - hydroxy (ester) reacts with diethyl(3 - pyridyl)borane to obtain abiraterone acetate or its intermediate, and the intermediate is converted to obtain abiraterone acetate. The preparation method of the present invention has simple operation and is suitable for large - scale industrial production.

1.The name of the design product: poster (abiraterone acetate tablet). 2.The use of the design product: for poster. 3.The design points of the design product: in the combination of shape and pattern. 4.The picture or photo that best indicates the design points: front view. 5.The design product is a flat product, and the rear view, left view, right view, top view and bottom view are omitted.

The invention relates to an oral suspension dosage form of abiraterone acetate. The invention also relates to providing patient compliant, economical and technically advanced dosage forms over existing dosage forms. Besides, compared with the prior art, the abiraterone acetate preparation with patient compliance, which is prepared according to the invention, is proved to have higher solubility and stability. In addition, the present invention provides a suspension composition prepared by a relatively simple, readily commercially producible and functionally reproducible method.

Methods and compositions are provided for treating prostate cancer by administering to a patient in need thereof a therapeutically effective amount of a PARP inhibitor, e.g., niraparib, a therapeutically effective amount of a CYP17 inhibitor, e.g., abiraterone acetate, and a therapeutically effective amount of a glucocorticoid, e.g., prednisone.

The present disclosure relates to methods of treating prostate cancer in a subject. More specifically, the present disclosure relates to methods of treating prostate cancer, e.g., metastatic castration-resistant prostate cancer, by administering to a subject olaparib and abiraterone acetate or a salt thereof.

The present disclosure relates to a pharmaceutical product having at least one batch indication, wherein the pharmaceutical product comprises niraparib and abiraterone acetate.

A drug composition containing abiraterone acetate, and a preparation method therefor and an application thereof. Excipients thereof comprise at least one oil phase, at least one emulsifier, and at least one co-emulsifier. The dug composition can obviously improve the bioavailability and the stability of a preparation. The drug composition can be further prepared as capsules.

The invention relates to the technical field of pharmaceutical preparations, in particular to an abiraterone acetate self-emulsifying soft capsule and a preparation method thereof. The abiraterone acetate self-emulsifying soft capsule comprises a content and a capsule shell, the content is prepared from the following components in percentage by mass: 5 percent to 7.5 percent of abiraterone acetate, 22.5 percent to 48.75 percent of a surfactant, 25 percent to 42.13 percent of a cosurfactant, 10 percent to 30 percent of an oil phase and 0.005 percent to 0.02 percent of an antioxidant; the average particle size of the microemulsion formed by diluting the content with a hydrochloric acid solution with the pH value of 1.2 is 80-100 nm. The abiraterone acetate self-emulsifying soft capsule has good long-term storage stability and high bioavailability, drug absorption is not affected by food intake, and medication compliance of patients can be improved.

The present invention relates to a pharmaceutical composition comprising solid dispersion of amorphous abiraterone acetate and one or more pharmaceutically acceptable excipients, having improved solubility, stability, bioavailability, and no positive food effect. The present invention also relates to a method for its preparation, a dosage form comprising such compositions, and the use of the said composition or dosage form as a medicament for the treatment of prostate cancer.

The present invention relates to a dispersible tablet comprising at least 70% w / w of abiraterone acetate based on the total weight of the tablet and at least one pharmaceutically excipient selected from group consisting of diluents, binders, surfactants, glidants, disintegrants, lubricants, sweeteners and flavorants and further relates to the process for the preparation thereof.