27 results about "Abiraterone acetate" patented technology

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 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 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.

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 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.

The present invention relates to oral suspension dosage form of Abiraterone Acetate. The invention also relates to provide patient-compliant, economical and technically advanced dosage form over existing dosage form. Moreover, the solubility and stability of the patient compliant Abiraterone Acetate formulation, prepared as per the present invention, is proven higher when compared to prior art inventions. Furthermore, the present invention also provides a suspension composition prepared by a process which is relatively simple, easy to commercially manufacture, and functionally reproducible.

This disclosure relates to a combination of abiraterone acetate and niraparib, to free-dose and fixed-dose combinations of abiraterone acetate and niraparib, and to methods of treating prostate cancer with such combinations.

This disclosure pertains to methods of treating prostate cancer in a subject, including, for example, metastatic prostate cancer, castrate-resistant prostate cancer, metastatic castrate-resistant prostate cancer, progressive metastatic castrate-resistant prostate cancer, castrate-sensitive prostate cancer, metastatic castrate-sensitive prostate cancer, prostate cancer naïve to novel hormonal agents (NHA), metastatic prostate cancer naïve to novel hormonal agents (NHA), castrate-resistant prostate cancer naïve to novel hormonal agents (NHA), castrate-sensitive prostate cancer naïve to novel hormonal agents (NHA), metastatic castrate-resistant prostate cancer naïve to novel hormonal agents (NHA), and metastatic castrate-sensitive prostate cancer naïve to novel hormonal agents (NHA), wherein the method comprises: (i) administering a compound of Formula (I), (I), or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X1, X2, X3, X4, and n are defined herein; and (ii) abiraterone, a pharmaceutically acceptable salt of abiraterone, abiraterone acetate, or a pharamaceutically acceptable sale of abiraterone acetate.

The invention relates to the technical field of drug detection, and discloses a method for detecting beta-lactam compound residues in a drug, which comprises the following steps of: extracting and diluting beta-lactam compounds in the drug through a uniform pretreatment process (adopting 50% acetonitrile) in combination with optimized LC-MS / MS conditions (including specific chromatographic columns, gradient elution procedures and mass spectrum parameters); synchronous quantitative detection of eight beta-lactam compounds (covering cephalosporin and penem) in five raw material medicines (exemestane, etoposide, abiraterone acetate, emtricitinib and cilnimod) with remarkable structural difference is realized, and the limit of quantitation is as low as 0.008 ppm. According to the method, the detection sensitivity is remarkably improved, the trace residue monitoring requirement is met, pretreatment steps are simple and universal, conditions do not need to be adjusted according to different raw material medicines, the detection efficiency and the method applicability are greatly improved, and the problems that the sensitivity is insufficient and the universality is poor in the prior art are effectively solved.