Abstract

Provided are a controlled-release ticagrelor tablet and a preparation method therefor, wherein the controlled-release tablet comprises a tablet core and a film-controlled coating system, the tablet core comprises ticagrelor accounting for 30‑60 wt％ of the total weight of the tablet core, and the controlled-release tablet is provided with two or more drug release holes. The controlled-release ticagrelor tablet is mild and long-lasting in release, can be released almost completely within 20 h, can have a good release effect on ticagrelor of different crystal forms, and is also stable in performance, can be stored for a long time, and has a simple preparation process and is suitable for industrial production.

IPC Classes  ?

• A61K 9/44 - Pills, lozenges or tablets printed, embossed, grooved, or perforated
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 47/38 - CelluloseDerivatives thereof
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

Abstract

Disclosed is an oral controlled-release brivaracetam preparation and a preparation method therefor. The controlled-release preparation is a single-chamber osmotic pump controlled-release preparation, and is composed of a drug tablet core and a membrane-controlled coating system. The controlled-release preparation has a drug-release hole, the drug tablet core comprises 30-60％ parts by weight of brivaracetam, and the membrane-controlled coating accounts for 3-34 (w/w, %) of the total weight of the drug tablet core. The controlled-release preparation has an in-vitro zero-level constant-speed drug release curve, can form a spherical preparation after water absorption swelling, and is not prone to being adhered to the wall of a digestive tract, which results in the local concentration of a drug being too high.

IPC Classes  ?

• A61K 9/44 - Pills, lozenges or tablets printed, embossed, grooved, or perforated
• A61K 9/36 - Organic coatings containing carbohydrates or derivatives thereof
• A61K 9/32 - Organic coatings containing solid synthetic polymers
• A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
• A61P 25/08 - AntiepilepticsAnticonvulsants

Abstract

Disclosed are a method for preparing PF06651600 and an intermediate used therein. The method for preparing PF06651600 comprises the following processes: compound 5 and acryloyl chloride undergo an aminolysis reaction to obtain compound PF06651600; compound 4 is subjected to debenzylation by means of catalytic hydrogenation to obtain compound 5; furthermore, compound 2 and compound 3 undergo a nucleophilic substitution reaction to obtain compound 4.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system