36 results about "Lubiprostone" patented technology

The invention discloses high-purity lubiprostone, a preparation method and application thereof. The high-purity lubiprostone has the chemical structural formula shown in the formula I, wherein HPLC (High Performance Liquid Chromatography) purity is more than 95 percent. The invention also provides a preparation method of the high-purity lubiprostone, which comprises the steps of: 1. sampling lubiprostone crude products to a chromatographic column for preparing the HPLC; 2. eluting eluent through the chromatographic column for preparing the HPLC; and 3. crystallizing with an organic solvent to obtain the high-purity lubiprostone.

The invention belongs to the technical field of pharmaceutical chemical engineering and particularly relates to a novel crystal form of lubiprostone, a preparation method of the crystal form and the application of the crystal form to medicine preparation. The crystal form is represented through X-ray powder diffraction, infrared spectrography and differential scanning calorimetry, has the advantages of high purity, high stability and easy preparation, is more suitable for storage and use, and can be better applied to preparation of lubiprostone drug substances and preparations.

The present invention relates to a lubiprostone crystal, the method for the preparation thereof, and a pharmaceutical composition or kit comprising the same, as well as the use of said crystal in the preparation of a medicament for the treatment of gastrointestinal tract diseases, especially constipation. The X-ray powder diffraction pattern of said crystal comprises characteristic peaks measured at the following 2θ reflection angles: 14.6±0.2°, 17.0±0.2° and 19.6±0.2°. As compared to amorphous lubiprostone, the crystal of the present invention has the advantages of relative high purity, stable properties and easy-for-storage and use.

The invention discloses a medicine composition for treating constipation and/or haemorrhoids and belongs to the field of medicines. Aiming at providing a medicine for treating constipation and/or haemorrhoids with a definite curative effect and specific ingredients, the invention discloses a medicine composition used for treating haemorrhoids, the medicine composition used for treating the haemorrhoids contains two ingredients, namely lubiprostone and ketorolac tromethamine, and the ratio of lubiprostone to ketorolac tromethamine is (0.02-10):1, preferably (0.1-5):1, and more preferably (0.5-2):1. A large number of experimental studies show that the medicine composition has an obvious treatment effect on anorectal diseases such as the haemorrhoids.

The invention relates to the field of pharmaceutical chemistry and provides a lubiprostone refining method. In comparison with existing lubiprostone preparation methods, the preparation method of the invention can be adopted to obtain high-purity lubiprostone more simply and with high yield through a recrystallization mode.

The invention relates to a method for synthesizing a 1R,2R,3R-substituted cyclopentanone compound. The method comprises: carrying out a reaction on a compound 1 and a halogenated alkane in an organicsolvent under the actions of a strong alkali and a cuprous salt to obtain a compound 3, carrying out ester hydrolysis on the compound 3 under the action of an alkali or pancreatin, and carrying out deprotection by using a fluorine reagent to obtain the product. According to the present invention, the synthesis method has characteristics of high yield, high product purity, good diastereoselectivity, easy reaction control and simple post-treatment, is suitable for industrial production, and can synthesize high-purity and high-yield alprostadil, lubiprostone, and the analogs of misoprostol and limaprost. The compound 1 is defined in the specification.

The present invention provides a lubiprostone solid dispersion and a preparation method thereof, wherein the lubiprostone solid dispersion comprises lubiprostone and a carrier, the carrier is a hydrophilic polymer carrier, a weight ratio of the lubiprostone to the carrier is 8:200000-400000, optionally the solid dispersion further comprises a surfactant, and a weight ratio of the lubiprostone to the carrier to the surfactant is 8:200000-400000:20000-40000. The preparation method comprises: dissolving lubiprostone, a carrier and/or a surfactant in an aqueous solvent, stirring to form a clarified solution, and carrying out freeze-drying or spray-drying to completely remove the aqueous solvent so as to prepare the solid dispersion. According to the present invention, the lubiprostone solid dispersion has advantages of improved water solubility, improved dissolution rate, promoted absorption by gastrointestinal tract and improved bioavailability.

The invention provides a pharmaceutical composition which utilizes lubiprostone as a main active ingredient and is capable of inducing hepatocyte proliferation and promoting liver regeneration after liver injury. The pharmaceutical composition can be a preparation based on oral administration, preferably, the pharmaceutical composition can be an oral solid preparation based on a tablet form or a capsule form. Furthermore, the pharmaceutical composition can be prepared into a lubiprostone unit preparation suitable for oral administration.

The invention discloses a preparation process of a lubiprostone intermediate. The preparation process comprises the following steps: firstly, carrying out reduction reaction on a lubi-initiator to obtain an intermediate 1; secondly, adding excessive weak base into a mixed solution of triphenylphosphonic acid bromide and absolute ether, then adding the intermediate 1 for complete reaction, then adjusting a pH value to 5 to 6, adding ethyl acetate for extracting, combining organic layers to obtain an organic phase, and carrying out vacuum concentration and drying on the organic phase to obtain an intermediate 2; thirdly, adding acetonitrile, diisopropylethylamine and benzyl bromide into the intermediate 2 for complete reaction, then carrying out vacuum concentration and drying, and adding the ethyl acetate and water for extracting and separating liquid; carrying out vacuum concentration and drying on the organic phase to obtain a crude product of an intermediate 3. The preparation process disclosed by the invention has the advantages of rapid and convenient synthesis route, high yield and relatively high economic value; the preparation process is quite suitable for scale production and provides another synthesis route with high economic benefits and high production efficiency for producing lubiprostone.

The invention discloses a soft capsule containing lubiprostone as well as a preparation method thereof. The capsule is a soft elastic capsule and consists of a capsule shell and a liquid composition accommodated in the capsule shell; the liquid composition comprises lubiprostone, a proper solvent and the like; and the capsule shell comprises the following components: gelatin, purified water, a plasticizer, a preservative, an antioxidant, an opacifying agent and a coloring agent. The soft capsule is short in disintegration time, rapid in dissolution, high in bioavailability, accurate in dosageand easy to absorb. The soft capsule containing the lubiprostone can effectively improve the stability and the bioavailability of the lubiprostone active component; and the preparation method is relatively simple and easy to produce, and has wide application prospect.