Provided are a pharmaceutical composition comprising an allopregnanolone derivative and the use thereof. The pharmaceutical composition comprises the following components in percentage by mass: 30% to 70% of allopregnanolone derivative, 15% to 62% of filler, 5% to 20% of binder, 1% to 2.5% of glidant, 0.2% to 1.2% of lubricant and 0 to 10% of disintegrant. The pharmaceutical composition has excellent stability and a rapid dissolution rate, and is suitable for preparing solid preparations such as quick-release capsules, granules, and tablets. Also provided is a method for preparing a capsule preparation by using the pharmaceutical composition.
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A compound represented by formula I, a racemate, a stereoisomer, a tautomer, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof are provided. In formula I, R2 and R4 are independently selected from H or D, respectively; R1 and R3 are independently selected from CH3, CH2D, CHD2 or CD3, respectively; and the compound of formula I contains at least one deuterium atom. While retaining the pharmacological activity of the allopregnanolone, an allopregnanolone derivative that is suitable for oral administration is obtained by means of the structural modification on the hydroxyl group of the allopregnanolone.
A compound represented by formula I, a racemate, a stereoisomer, a tautomer, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof are provided. In formula I, R2 and R4 are independently selected from H or D, respectively; R1 and R3 are independently selected from CH3, CH2D, CHD2 or CD3, respectively; and the compound of formula I contains at least one deuterium atom. While retaining the pharmacological activity of the allopregnanolone, an allopregnanolone derivative that is suitable for oral administration is obtained by means of the structural modification on the hydroxyl group of the allopregnanolone.
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
C07B 59/00 - Introduction of isotopes of elements into organic compounds
3.
SALT FORM AND POLYCRYSTALLINE FORM OF ALLOPREGNANOLONE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
The present invention provides various salt forms of an allopregnanolone derivative, including hydrochloride, phosphate, L-malate, maleate, p-toluenesulfonate, benzoate and the like. The present invention further provides a plurality of crystal forms and amorphous forms of the hydrochloride of the allopregnanolone derivative, including a crystal form I, a crystal form II, a crystal form III, and a crystal form IV. Both the hydrochloride and the phosphate of the allopregnanolone derivative have good stability, and the preparation method is simple and easy to operate, is suitable for scale-up production, and has good industrial application value.
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61P 25/00 - Drugs for disorders of the nervous system
The present invention provides a pharmaceutical composition for injection, comprising deoxycholic acid, lidocaine, a cosolvent, a buffering agent, an osmotic pressure regulating agent, and water. The pharmaceutical composition has good stability and is convenient to use, and pharmacodynamic tests prove that compared with a deoxycholic acid single preparation, the pharmaceutical composition can greatly reduce irritant side effects such as pain and swelling, and can remarkably improve the compliance and the treatment satisfaction of a patient.
A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A pharmaceutical composition comprising trifarotene, comprising trifarotene, a grease, an emulsifier, and water, wherein the grease is selected from at least one of caprylic capric triglyceride, caprylic triglyceride, isopropyl myristate, and mineral oil; the emulsifier is selected from at least one of sorbitan oleate and oleic acid polyethylene glycol glyceride. The addition of the emulsifier causes the composition to have a uniform texture and greatly improves the stability of trifarotene in the grease, thus effectively stabilizing the physical and chemical properties of the pharmaceutical composition, reducing irritation, and effectively improving the safety of drug use and the skin comfort.
A pirfenidone topical formulation is provided, comprising a therapeutically effective amount of pirfenidone, water, and at least one cosolvent, the cosolvent being selected from a combination of dimethyl sulfoxide and an alcohol solvent. The formulation exhibits high skin permeability, good stability, no irritation, excellent skin tolerance, and ease of use. The formulation can be used in the preparation of drugs for preventing or treating diseases related to excessive proliferation of skin or connective tissues and chronic skin injuries.
maxmax, is good in druggability, and can be used for preventing and/or treating androgen-related disorders. The compound provided by the invention also has a good hair growth promoting effect, and can effectively increase the number of hair follicles and the growth length of hair.
C07C 49/577 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings containing ether groups, groups, groups, or groups
C07C 49/533 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings to a three- or four-membered ring
C07C 49/537 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings to a five-membered ring
C07C 49/543 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings to a six-membered ring
C07C 49/547 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings to a seven- to twelve-membered ring
C07C 49/557 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings having unsaturation outside the rings
The present invention relates to the field of medicinal chemistry, and in particular, to a malate salt of a xanomeline derivative, the malate salt having a structure as shown in formula (I). The malate salt of the compound of formula (I) has excellent effects on at least one aspect of physical stability, solubility, hygroscopicity, biological activity, safety, bioavailability, toxic and side effects, etc.
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups
C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
C07C 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
241332233, respectively; and the compound of formula I contains at least one deuterium atom. According to the present invention, on the premise of retaining the pharmacological activity of the allopregnanolone, an allopregnanolone derivative that is suitable for oral administration is obtained by means of the structural modification on the hydroxyl group of the allopregnanolone, and has a good physical/chemical stability.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
patents
