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 - Composés non saturés contenant des groupes cétone contenant des groupes avec de l'oxygène lié par liaison simple
C07C 51/43 - SéparationPurificationStabilisationEmploi d'additifs par changement de l'état physique, p. ex. par cristallisation
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61P 1/16 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des troubles de la vésicule biliaire ou du foie, p. ex. protecteurs hépatiques, cholagogues, cholélitholytiques
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 - Composés non saturés contenant des groupes cétone contenant des groupes avec de l'oxygène lié par liaison simple
C07C 51/43 - SéparationPurificationStabilisationEmploi d'additifs par changement de l'état physique, p. ex. par cristallisation
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61P 1/16 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des troubles de la vésicule biliaire ou du foie, p. ex. protecteurs hépatiques, cholagogues, cholélitholytiques
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 - Composés hétérocycliques contenant des cycles oxazole-1, 2 ou oxazole-1, 2 hydrogéné non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique
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 - Composés hétérocycliques contenant des cycles oxazole-1, 2 ou oxazole-1, 2 hydrogéné non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique
C07D 413/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 413/10 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
C07C 251/48 - Oximes avec des atomes d'oxygène de groupes oxyimino liés à des atomes d'hydrogène ou à des atomes de carbone de radicaux hydrocarbonés non substitués avec l'atome de carbone d'au moins un des groupes oxyimino lié à un atome de carbone d'un cycle aromatique à six chaînons
C07C 25/24 - Hydrocarbures aromatiques halogénés à chaînes latérales non saturées
A01N 43/80 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec des atomes d'azote et des atomes d'oxygène ou de soufre, comme hétéro-atomes du cycle des cycles à cinq chaînons avec un atome d'azote et soit un atome d'oxygène, soit un atome de soufre, en 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, sulfures, hydropolysulfures ou polysulfures substitués par des halogènes, des atomes d'oxygène ou d'azote ou par des atomes de soufre ne faisant pas partie de groupes thio contenant des groupes thio et des groupes carboxyle liés au même squelette carboné ayant les atomes de soufre des groupes thio liés à des atomes de carbone acycliques du squelette carboné le squelette carboné étant acyclique et saturé
A61K 31/22 - Esters, p. ex. nitroglycérine, sélénocyanates d'acides carboxyliques d'acides acycliques, p. ex. pravastatine
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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