34 results about "Tafluprost" patented technology

The invention provides a good-stability eye-drop preparation containing a PGF2alpha derivative. The eye-drop preparation comprises the PGF2alpha derivative serving as an active constituent and also comprises 15-hydroxy stearic acid polyglycol ester. It is surprised to find that after the 15-hydroxy stearic acid polyglycol ester serves as a solutizer of the PGF2alpha derivative (such as tafluprost) eye-drop preparation, the stability of active medicine is obviously improved; after the product is subjected to tests of the high temperature, the hard light, the acceleration stability and the long-term stability, compared with existing eye drops, the increase amount of related substances is obviously smaller, and the pharmacological activity and safety of the product are further guaranteed.

The invention provides eye drops containing tafluprost. The eye drops comprise tafluprost and a hydrophilic polymer, wherein the hydrophilic polymer is selected from polycarbophil or carbomer and the content of the hydrophilic polymer is 0.4-1.0%. Medicament storage formed by the eye drops plays a role of slowly releasing medicaments, prevents medicaments from being rapidly eliminated, and improves the bioavailability. The preparation method of the eye drops is simple and feasible and suitable for industrial production.

The present invention provides efficient, economical and environmental friendly methods for synthesis of prostaglandin analogs including tafluprost and intermediates thereof. The invention involves a selective oxidation using in situ boronate ester protection and a unique crystallization method to remove the undesired isomers of fluorinated intermediates.

The invention discloses a preparation method of Tafluprost. The preparation method comprises the following steps: adopting a compound of formula 1 as a raw material, and carrying out the steps of DIBAL-H reduction, a Wittig reaction and an esterification reaction, wherein alkaline amino acids are adopted for refining after the Wittig reaction. According to the preparation method disclosed by the invention, the total mass yield of the three-step reaction can reach 70%, the technology is stable, a prepared Tafluprost product is colorless or faint yellow thick oily liquid, and the purity reaches up to more than 99%.

The invention discloses a method for industrially preparing tafluprost. The method comprises the following steps: taking Corey lactone as an initial raw material, oxidizing, condensing, fluorinating,deprotecting, reducing, re-condensing, esterifying and refining to obtain the tafluprost, according to the method for large-scale preparation of the tafluprost provided by the invention, a reversed-phase and normal-phase preparative column purification technology is used, a molecular group evacuation technology is adopted, and a molecular group'evacuation agent 'is added into a mobile phase, so that a relatively good effect is achieved, in addition, a trichloroacetonitrile uric acid(TCCA)reagent is adopted in an oxidation method, and the yield of the tafluprost is improved. The use of variousreaction quenching agents is also the characteristic of the method, and the timely and reasonable quenching of the reaction has certain significance for reducing the generation of impurities.

The present application relates to amine salts of prostaglandin analogs and their uses for the preparation of substantially pure prostaglandin analogs. Specific embodiments relate to amine salts of tafluprost and their uses for the preparation of substantially pure tafluprost.

The invention belongs to the field of bio-medicine, and discloses a tafluprost eye drop agent and a preparation method thereof. The eye drop agent take tafluprost as an active ingredient, a hydrophilic gel skeleton material is used as a skeleton and a solubilizer, the tafluprost eye drop agent further includes an antioxidant and a stabilizer, and the antioxidant and the stabilizer are macromolecular compounds. A process of the tafluprost eye drop agent improves the asepsis level of a product, the characteristics of simple preparation composition, easy, convenient and quick operation, high compatibility for medicinal packaging materials, low cost, stable properties of liquid medicine and high quality standard are achieved, and the tafluprost eye drop agent is suitable for industrial production.

The invention discloses a preparation method of a tafluprost crude drug. The preparation method comprises the following steps: preparing and separating by adopting a high-performance preparation liquid phase, and pulping C6 to C8 alkane. The preparation method of the invention is stable in process, and high in operability. The total purity of the prepared Tafluprost is greater than 99.5 percent, the content of trans isomer impurities is less than 0.1 percent, and the content of other monomer impurities is less than 0.1 percent.

The present invention provides a new pharmaceutical application of a 15,15-difluoroprostaglandin F_2α derivative. As a result of intensive studies in order to find a new pharmaceutical application of a 15,15-difluoroprostaglandin F_2α derivative, it was found that, in a European Phase III clinical trial for tafluprost, one of the 15,15-difluoroprostaglandin F_2α derivatives, with patients with open-angle glaucoma or ocular hypertension, tafluprost has actions of growing eyelashes, making eyelashes thicker, and changing the color thereof, that is, has an effect of promoting the growth of hair (eyelashes). Therefore, a 15,15-difluoroprostaglandin F_2α derivative is useful as a hair growth promoting agent, and is expected to be useful as an active ingredient of a preventive or therapeutic agent for a disease associated with hair such as alopecia and a hair care product or a hair cosmetic product for regrowing hair, growing hair, increasing hair density, nourishing hair, or the like.

The purpose of the present invention is to provide a simple and efficient method for purifying tafluprost that can be scaled up in proportion. The present invention relates to the method for purifying tafluprost, which comprises a step for purifying a crude product of tafluprost by silica gel column chromatography and collecting a component containing tafluprost by HPLC analysis. In addition, the present invention also relates to a method for producing tafluprost, which comprises the aforementioned method for purifying tafluprost.

The present invention provides a cocrystal composite composed of resveratrol and a prostaglandin analog and a pharmaceutical composition comprising the same. The cocrystal composite and the composition are characterized in that the prostaglandin analog is one selected from the latanoprost, travoprost, bimatoprost, tafluprost and Latanoprostene Bunod. The cocrystal composite can generate synergistic inhibit effects (with CI being less than 1) on cell proliferation of various cells of cancer such as lung cancer and gastric cancer.

The invention discloses a high-efficiency herbal eye drop, and belongs to the field of pharmaceutical chemicals. The high-efficiency herbal eye drop contains the following components in parts by weight: 80-100 parts of water, 50-60 parts of polycarbophil AA, 30-40 parts of oxytetracycline, 25-30 parts of tafluprost, 20-25 parts of timclol maleate, 18-23 parts of herba houttuyniae extract, 16-21 parts of flos lonicerae extract, 13-18 parts of semen cassiae extract, 11-16 parts of rhizoma coptidis extract, 9-13 parts of sodium chloride, 6-11 parts of edetate disodium, 6-9 parts of poloxamer, 5-8parts of tyloxapol, 4-8 parts of timclol maleate, 4-6 parts of brinzolamide, 2-5 parts of mannitol, 2-5 parts of citric acid, 2-4 parts of sodium citrate, 1-3 parts of benzene, and 1-3 parts of a preservative. The high-efficiency herbal eye drop solves the problems that a traditional herbal eye drop has poor absorption and a poor effect, and a chemical preparation eye drop hurts eyes.

The invention belongs to the technical field of medicine, and relates to a preparation method of Tafluprost and analogs thereof and a related intermediate compound. The preparation method is characterized in that (4-carboxybutyl)triphenylphosphonium bromide having a structure shown below is used as a witting reaction reagent, wherein R is alkyl or aryl. The method is simple, feasible and convenient for industrial production; and the Tafluprost and analogs thereof which are basically free of omega chain trans-isomers can be prepared.

The invention provides a crystal form of (3aR,4R,5R,6aS)-4-((E)-3,3-difluoro-4-phenoxylbutyl-1-alkyl-1-yl)-2-oxohexahydro-2H-cyclopentane[b]furan-5-benzoate (a tafluprost intermediate, a difluorination product 2), and a preparation method of corresponding crystals of the crystal form. Crystal form parameters comprise characteristic peak values (2theta) of the XRPD spectrum of the crystals, and DSC and IR characteristic atlas parameters. White crystal powder of the product 2 is obtained through single solvent or mixed solvent recrystallization by adopting a simple crystallization method, the primary crystallization purity is greater than 90% generally, the highest purity after secondary crystallization reaches 99.8%, and the proportion of each of all unimodal impurities is lower than 0.1%, so the purification process of tafluprost synthesized by using the product 2 as a raw material is substantially simplified.

The invention provides a medicine composition containing an effective dosage of puerarin and an effective dosage of dorzolamide or brinzolamide or prostaglandin, such as latanoprost, tafluprost and the like or/ and an effective dosage of water-retaining agent or wetting agent or antixerophthalmic ingredients, and application in preparation of medicines, including eye-purpose medicines used for preventing or treating intraocular pressure or elevated intraocular pressure, glaucoma, fundi diseases, optic nerve protection, dry eyes or xerophthalmia or dry eye syndromes of the human being or mammals. The medicine disclosed by the invention has a better curative effect or a smaller side effect or better treatment compliance or a better treatment mode.

The invention provides a method for synthesizing tafluprost, and relates to the technical field of tafluprost synthesis. The method for synthesizing the tafluprost comprises the following specific preparation steps: S1, primary reaction, S2, secondary reaction, S3, third reaction, S4, fourth reaction, S5, fifth reaction and S6, final reaction. The invention provides the method for synthesizing tafluprost. According to the method for synthesizing tafluprost, racemic Corey lactone diol is used as a raw material, the tafluprost is obtained through oxidation, condensation, fluorination, reduction, recondensation and esterification reaction, the total mass yield of six-step reaction of the preparation method can reach 22%, the process is stable, the prepared tafluprost product is colorless viscous oily liquid, and the purity of the tafluprost product is up to 99% or above.

The invention provides a preparation method of tafluprost. According to the method, a fluorinated raw material is obtained at first, and then, HWE reaction is carried out to form double bonds; and therefore, the double bond addition side reaction during fluorination can be avoided. Therefore, the method disclosed by the invention can be used for obtaining the fluorinated product with high yield and high purity, so that the preparation cost of the tafluprost can be reduced, and the economic benefit of the tafluprost can be improved.