9 results about "Pranlukast" patented technology

The present invention relates to a pharmaceutical composition for improving the bioavailability of pranlukast and a method for preparing the same, and more particularly, to a pharmaceutical composition for improving the bioavailability of pranlukast, which comprises 0.1 to 10 parts by weight of a water-soluble polymer and 0.1 to 5 parts by weight of a flow aid such as silicon dioxide, relative to 15 to 25 parts by weight of pranlukast, so that the composition of the present invention exhibits bioequivalent or even superior pharmacokinetic characteristics to a commercially available preparation even when the content of pranlukast is reduced to 50 mg or less per tablet (1 tablet per time, twice a day), thereby improving the medication compliance of patients and reducing side effects caused by the intake of an excessive amount of pranlukast, and a method for preparing the same.

Disclosed is a pharmaceutical composition comprising bepotastine or a pharmaceutically acceptable salt thereof, pranlukast or a pharmaceutically acceptable salt thereof, or a hydrate thereof as a main ingredient, and capable of inhibiting the generation of related substances by using an antioxidant.

The present invention relates to a pharmaceutical composition having improved bioavailability of pranlukast, and a preparation method therefor, and, more specifically, to a pharmaceutical composition and a preparation method therefor, the composition comprising, on the basis of 15-25 parts by weight of pranlukast, 0.1 to 10 parts by weight of a water-soluble polymer and 0.1 to 5 parts by weight of a silica-based superplasticizer, thereby exhibiting drug efficacy that is at least clinically equal to that of commercially available formulations even if the amount of pranlukast is reduced to 50 mg / tablet or less (1 tablet taken twice per day), and thus improves patient drug compliance and reduces side effects caused by taking an excessive amount of pranlukast.

The invention belongs to the technical field of biology, and discloses application of pranlukast in preparation of drugs for preventing and / or treating fatty liver diseases, diabetes and obesity. The invention proves that pranlukast has the effect of relieving fat accumulation in vivo and in vitro; the pranlukast can obviously reduce lipid droplet accumulation in liver cells at an in-vitro cellular level, obviously reduce the weight of a metabolism-related fatty liver disease (MASLD) model mouse induced by a high-fat feed in vivo, and improve pathological abnormalities such as liver functions, glucose and lipid metabolism disorder, insulin resistance and liver fatty degeneration; it shows potential in preventing or treating diseases accompanied by the metabolic syndrome. Meanwhile, the invention further provides a medicine which contains pranlukast and is used for preventing and / or treating the diseases.

The present invention provides a method for preparing a pranlukast intermediate. Using compound C as a raw material, the pranlukast intermediate is obtained after reaction. The pranlukast intermediate prepared by the present invention has a high yield, and has the advantages of relatively mild reaction conditions, convenient operation, high purity and high yield of the obtained pranlukast intermediate, and is suitable for industrial production. Therefore, it provides a more valuable synthetic route for the preparation of pranlukast, which can bring good social and economic benefits and has great economic value potential.

The application provides a method for determining the content of pranlukast, which is suitable for the technical field of quality control of organic chemical synthetic bulk drugs, and especially suitable for accurate content detection in the production process of pranlukast bulk drugs. The analysis method overcomes the limitations of tailing and asymmetry of pranlukast chromatographic peak in the prior art, optimizes the composition of the mobile phase and the chromatographic conditions, shortens the analysis time, and improves the detection sensitivity and accuracy. The application adopts high performance liquid chromatography, the chromatographic column is a silica gel bonded octadecylsilane column, the ultraviolet detector is used, the mobile phase is a phosphate buffer solution containing ion pair reagent sodium heptanesulfonate and an organic solvent acetonitrile, and the separation and detection are carried out in an isocratic elution mode. The method has good separation degree, strong specificity, high precision and good repeatability, and meets the methodological verification requirements of the content determination of pranlukast.

The present invention relates to a pharmaceutical composition for improving the bioavailability of pranlukast and a method for preparing the same, and more particularly, to a pharmaceutical composition comprising 0.1 to 10 parts by weight of a water-soluble polymer and 0.1 to 5 parts by weight of a silica-based flow aid relative to 15 to 25 parts by weight of pranlukast, thus, even if the pranlukast content is reduced to 50 mg / tablet or less (one tablet each time, twice a day), the composition of the present invention can exhibit bioequivalent or even better pharmacokinetic characteristics than commercially available preparations in the human body, thereby improving the medication compliance of patients and improving the compliance of the patients. The side effect caused by excessive taking of pranlukast is reduced. The invention also discloses a preparation method of the pharmaceutical composition.

The invention discloses an application of pranlukast in preparing a medicine for resisting clostridium difficile infection. A small-molecule inhibitor aiming at a toxin B (TcdB) receptor binding domain is screened by adopting an artificial intelligence auxiliary method. The research finds that the pranlukast has very high affinity (-35 kcal / mol) with TcdB. In-vitro experiment results show that pranlukast has no toxic effect on cells, but can obviously inhibit the cytotoxic effect induced by TcdB. After the I-EV-P is wrapped by EV (I-EV) from intestinal epithelial cells, the I-EV-P can remarkably recover the body weight of the gerbil, the survival rate reaches up to 100%, and the I-EV-P can also reduce the TcdB load after challenge of clostridium difficile and relieve intestinal tract lesions. The invention proves that pranlukast has excellent characteristics for the first time, is a promising non-antibiotic small molecular therapeutic agent, and can relieve pathological injury induced by TcdB and relieve infection of clostridium difficile.

The invention discloses a preparation method of a pharmaceutical composition containing pranlukast and the pharmaceutical composition prepared by the preparation method.