57 results about "Ramelteon" patented technology

The invention relates the technical field of medicinal preparations and discloses a tablet containing ramelteon and copovidone. Through use of copovidone, the tablet solves the problem of low bioavailability of the ramelteon preparation prepared by the prior art. Through common preparation methods, ramelteon, copovidone and other required components are mixed according to a preset ratio and the mixture is pressed to form the tablet. A preparation method of the tablet comprises the following steps of mixing ramelteon, copovidone and a needed excipient in a granulator to obtain a uniform mixture, adding a needed binder into the granulator, carrying out granulation, taking out the granules, carrying out drying, carrying out screening to obtain powder having required granule sizes, adding magnesium stearate and a required disintegrating agent into the powder of which the granule sizes are adjusted and carrying out mixing to obtain particles to be tabletted. The tablet provided by the invention has greatly improved in-vitro bioavailability.

The invention relates to a preparation method of a Ramelteon intermediate. The Ramelteon intermediate is prepared by taking 4,5-dibromo-1,2,6,7-tetrahydro-8H-indeno[5,4-b]furan-8-one as a raw material, and then subjecting the raw material to a series of simple reactions so as to obtain the Ramelteon intermediate. The preparation method of the Ramelteon intermediate has the advantages of high yield, high product purity, simple operation, low cost, and suitability for mass production.

The invention belongs to the technical field of medicines and relates to ramelteon oral disintegrating tablets and a preparation method thereof. When being disintegrated, the ramelteon oral disintegrating tablets provided by the invention are wholly disintegrated within 60 seconds according to Chinese Pharmacopoeia Standards and have no hard cores. Raw drugs are sensitive to humidity so that dry-process granulation is used for replacing traditional wet-process granulation. The ramelteon oral disintegrating tablets provided by the invention are prepared from ramelteon and auxiliary components including a disintegrating agent, a filling agent, a binding agent, a sweetness flavoring agent and the like, and a dry-process granulation process is adopted. The ramelteon oral disintegrating tablets have the overall effects of high disintegrating speed, simple process steps, low cost, convenience for taking, good mouth feel, stable quality, reliable curative effect and the like; after the ramelteon oral disintegrating tablets are orally taken, the ramelteon oral disintegrating tablets are rapidly dispersed into fine particles or powder in an oral cavity, so that the ramelteon oral disintegrating tablets are particularly suitable for patients who cannot easily orally take the tablets and have insomnia; when the preparation reaches gastrointestinal tracts, the preparation exists in a form of fine particles, and thus the dissolving rate of the medicine is accelerated; and the medicine is widely distributed in the gastrointestinal tracts and a plurality of absorption points exist, so that the bioavailability can be improved.

The invention discloses a porcine oocyte in-vitro maturation culture solution as well as a preparation method and application thereof and belongs to the technical field of oocyte in-vitro maturation culture. In order to solve the problems of low porcine oocyte in-vitro maturation rate and development rate at present, the invention provides the porcine oocyte in-vitro maturation culture solution aswell as the preparation method and application thereof. The culture solution comprises a base culture solution TCM-199, penicillin, streptomycin, NaHCO3, 4-hydroxyethylpiperazine ethane sulfonic acid, polyvinyl alcohol, sodium pyruvate, insulin, cysteine, an epidermal growth factor, a porcine follicular fluid, pregnant mare serum gonadotropin, human chorionic gonadotropin and ramelteon. The culture solution can increase the oocyte in-vitro maturation quality, the cumulus cell diffusion index, the glutathione level, the parthenogenetic embryo blastocyst rate and blastocyst total cell number, the in-vitro fertilization embryo cleavage rate, the blastocyst rate and blastocyst total cell number and decrease the ROS level of oocytes.

The invention relates to a method for synthesizing Ramelteon. In the method, a compound I is selected as a starting substance, and Ramelteon is obtained by substitution, chiral separation, reduction, substitution, nucleophilic reaction and other reactions. Compared with the prior art, the method provided by the invention has the advantages that the entire process is environment-friendly, and the yield and purity of the product are high.

The invention provides a Ramelteon composition. The Ramelteon is composed of the following components, by weight part, 5-8 parts of Ramelteon and 0.5-3 parts of polyvidone. The invention also discloses a Ramelteon tablet. The Ramelteon tablet is composed of the following components including, by weight part, 5-8 parts of Ramelteon, 0.5-3 parts of polyvidone, 80-110 parts of filling agent, 3-10 parts of disintegrating agent and 0.5-1.5 parts of lubricant. The Ramelteon tablet is high in dissolution rate and stability and is prepared through a conventional method, which is simple in process, easy to operate, low in requirements on micronizing equipment, low in production cost and applicable to industrial mass production.

The invention provides a resolution method of a ramelteon intermediate, which comprises the following steps: (1) carrying out salification reaction on a compound (I) 2,2-(1,6,7,8-tetrahydro-2H-indeno[5,4-B]furyl-8-yl)ethylamine and a resolution reagent L-pyroglutamic acid in a methanol-containing organic solvent at 20-100 DEG C to obtain a ramelteon intermediate compound (II) crude product; and (2) recrystallizing the ramelteon intermediate compound (II) crude product in an organic solvent, and dissociating under the action of alkali to obtain the target product ramelteon intermediate compound (II). The reaction route of the method is disclosed in the specification.

The invention discloses a preparation method of ramelteon, which comprises the following steps: by using a compound IV as a starting material, carrying out reduction, chiral resolution and acylation reaction to obtain the ramelteon. The product II obtained by using a chiral resolving agent has very high chiral purity and yield, the resolution yield reaches 45% or above, and the highest resolutionyield in the existing literature technology is about 30%; the finally obtained ramelteon product is high in purity, repeated recrystallization purification is not needed, the total yield reaches 42% or above, the synthesis steps are short, and the operation process is simple.

The invention discloses a synthetic preparation method for a key intermediate of ramelteon 1,2,6,7-tretrahydro-8H-indeno[5,4-b]furan-8-one. According to the preparation method, by taking 2,3-dihydrobenzofuran-4-formaldehyde as an initial raw material, the key intermediate of ramelteon 1,2,6,7-tretrahydro-8H-indeno[5,4-b]furan-8-one is synthesized through Grignard reaction, oxidizing reaction and Nazarov cyclization reaction. The preparation method has the advantages of being high in reaction selectivity, few in side effects, high in total yield and quality, environmental-friendly, simple and convenient in process operation, high in stability and controllability and the like, and is suitable for industrial large-scaled production.