The present invention belongs to the technical field of chemical drug crystallization. Disclosed are a menbutone sodium hydrate, a preparation method therefor, and a use thereof. The structure of the menbutone sodium hydrate is as shown in formula (I): The menbutone sodium hydrate has characteristic peaks at 2θ values of 10.3±0.2°, 10.7±0.2°, 12.0±0.2°, 14.3±0.2°, 15.1±0.2°, 16.5±0.2°, 18.9±0.2°, 25.2±0.2°, and 26.5±0.2° in an X-ray powder diffraction pattern measured using CuKa radiation. The menbutone sodium hydrate of the present invention has good solubility and dissolution rate, excellent formulation processability, high crystallization purity and good storage stability, and has broad prospects for clinical application.
C07C 59/90 - Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
C07C 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
2.
CRYSTAL FORM A, CRYSTAL FORM B AND CRYSTAL FORM C OF SODIUM SALT OF MENBUTONE, PREPARATION METHOD THEREFOR, AND USE THEREOF
Disclosed in the present invention are polymorphs of sodium salt of menbutone, a preparation method therefor, and the use thereof, which belong to the technical field of pharmaceutical crystal forms. Said polymorphs comprise a crystal form A, a crystal form B and a crystal form C of sodium salt of menbutone, the structure of the sodium salt of menbutone being as shown in the following formula [Formula 1]. The present invention provides the novel polymorphs of sodium salt of menbutone, and the polymorphs have good solubility and dissolution rate, exhibit better mixing performance during powder preparation processes, and have excellent formulation processability, high crystallization purity and good storage stability. A crystallization method for the crystal form A, crystal form B and crystal form C of sodium salt of menbutone provided by the present invention has a good removal effect on a specific impurity A in menbutone, involves a simple process and is easy to operate, and is thus suitable for industrial production.
C07C 59/90 - Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
C07C 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
3.
ANTI-PARASITIC INFECTION EXTERNAL PHARMACEUTICAL FORMULATION, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are an anti-parasitic infection external pharmaceutical formulation , a preparation method therefor and use thereof. The external pharmaceutical formulation comprises a first active ingredient and an aldehyde compound, the first active ingredient being an isoxazoline compound. The active ingredient aldehyde compound in the pharmaceutical formulation not only has insecticidal activity, but also can effectively improve the stability of the formulation. The transdermal rate of the external formulation is increased to improve the utilization rate of the pharmaceutically active ingredient.
C07D 261/04 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
The present invention provides an anti-parasitic infection oral pharmaceutical preparation, a method for preparing same, and use thereof. The oral pharmaceutical preparation comprises a filler, a flavoring agent, a phagostimulant, an excipient, a preservative, and an adhesive comprising a first active component. The first active component is an isoxazoline compound. In the anti-parasitic infection oral pharmaceutical preparation, a self-microemulsifying solution of the active component is used as the adhesive, such that the active component is uniformly distributed in the oral preparation, the drug release rate of the oral preparation can also be significantly increased, and the bioavailability of the active ingredient is improved.
Provided in the present invention are a derivative of an isoxazoline compound and the use thereof in the prevention and treatment of parasitic infections. The derivative of the isoxazoline compound has the following general structural formula: the derivative has obvious inhibitory and killing effects on most ectoparasites, and is suitable for preparing anti-parasitic animal drugs. The derivative has a high safety, low irritation, good therapeutic effects and obvious targeting effects, and also has broad application prospects in the prevention and treatment of animal ectoparasites, parasites in the external environment and agricultural pests.
C07D 261/04 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07C 251/48 - Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups bound to a carbon atom of a six-membered aromatic ring
C07C 25/24 - Halogenated aromatic hydrocarbons with unsaturated side chains
A01N 43/80 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
The present application relates to a crystal form of a valnemulin hydrochloride hydrate, a preparation method therefor, and a pharmaceutical composition containing the crystal form. Specifically, the present application relates to a crystal form of a valnemulin hydrochloride hydrate, wherein the crystal form shows characteristic peaks 2 θ at 9.2+/-0.2°, 9.5+/-0.2°, 10.3+/-0.2°, 11.8+/-0.2°, 12.3+/-0.2°, 12.8+/-0.2°, 15.1+/-0.2°, 17.5+/-0.2°, and 18.2+/-0.2° in an X-ray powder diffraction pattern. The crystal form of the valnemulin hydrochloride hydrate has a high bulk density, no hygroscopicity, and good stability. The present application also provides a method for preparing the above crystal form of the valnemulin hydrochloride hydrate and a pharmaceutical composition containing the crystal form, wherein the composition can be used for preparing various preparations, such as a soluble powder, an oral liquid, a sustained-release particle, an injection, and other dosage forms, and has broad clinical application prospects.
C07C 323/52 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
The present application relates to a doramectin polymorph. Specifically, the present application relates to doramectin crystal form A, crystal form B, and a preparation method thereof. The polymorph can be obtained by dissolving doramectin in a good organic solvent, followed by adding a poor solvent to precipitate crystals, cooling, filtering, and drying. The doramectin polymorph of the present application has the remarkable characteristics of stable physical and chemical properties, high purity, excellent fluidity, excellent yield of the preparation method, and suitability for industrial production.
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