12 results about "Sirolimus" patented technology

The present invention relates to nanoparticles comprising sirolimus and albumin, a pharmaceutical composition comprising the same for subcutaneous administration, and a method for preparing the same. In the case of using the preparation method of the present invention, nanoparticles comprising sirolimus and albumin having excellent stability of particle size distribution can be prepared, the prepared nanoparticles can be prepared as a pharmaceutical composition suitable for subcutaneous injection, and the increase in administration dose and the convenience of administration can be improved.

The application discloses a method for simultaneously and rapidly detecting the concentration of four immunosuppressants, comprising the following steps: mixing a blood sample with an internal standard solution containing ascomycin, cyclosporine-d4, sirolimus-d3 and everolimus-d4, adding a precipitant and centrifuging to obtain a sample to be detected; injecting into a liquid chromatography-tandem mass spectrometry system for analysis to obtain original data containing the retention time window and mass spectrum response signal of four analytes; searching the original data based on an interferent database, wherein the interferent database contains a plurality of compounds that can possibly generate mass spectrum signal interference and characteristic ion information thereof; inputting the original data and the searched potential interferent information into a machine learning model to output a net mass spectrum response value after interference correction; and calculating the concentration of tacrolimus, cyclosporine, sirolimus and everolimus in the blood sample according to the obtained net mass spectrum response value, the mass spectrum response value of the corresponding internal standard and a pre-established standard curve.

The present application provides a suspension of sirolimus, which comprises sirolimus, a stabilizer, an osmotic pressure regulator, a suspending agent, a pH regulator and water; wherein the sirolimus is suspended in the water in the form of solid. The preparation process of the inhalation suspension provided by the present application is simple, and the selected excipients are suitable for use in drugs, so that the preparation provided by the present application is not only safe and reliable, but also low in production cost. The inhalation suspension provided by the present application can be stored at room temperature, and after long-term storage, the particle size of sirolimus in the preparation changes little, and the impurity content is low. The bioavailability of the suspension provided by the present application is much higher than that of oral preparations.

The application relates to the field of medicine preparation, in particular to a sirolimus enteric microcapsule granule and a preparation method thereof. The sirolimus enteric microcapsule granule comprises the following components in parts by weight: 0.1-0.5 parts of sirolimus, 50-80 parts of microcrystalline cellulose, 5-10 parts of an inner layer coating material and 3-8 parts of an outer layer coating material; the inner layer coating material comprises carboxymethylcellulose, and the outer layer coating material comprises Eudragit L100-55. The application is characterized in that the outer layer coating is composed of Eudragit L100-55, so that the granule can smoothly pass through the stomach and reach the intestines; the inner layer coating material is composed of carboxymethylcellulose, after the outer layer coating is dissolved in the intestines, the carboxymethylcellulose absorbs water and expands to form a viscous gel layer, so that the drug release is delayed, and the blood drug concentration can be maintained for a long time.

The present application relates to the field of medicine, and particularly relates to application of sirolimus combined with immune checkpoint inhibitors in anti-tumor treatment. The present application discloses use of a combination of sirolimus or a derivative thereof and an immune checkpoint inhibitor in preparation of a medicament for treating tumors, a pharmaceutical composition and a kit comprising the combination, and a method for treating tumors by administering a therapeutically effective amount of the pharmaceutical composition or the kit to a tumor patient in need. The combination of the present application has a synergistic effect and is suitable for treating cancer.

This application relates, in certain embodiments, to a method and composition for treating soft tissue sarcomas (STS, e.g., spindle cell sarcoma, solitary fibrous tumor, or leiomyosarcoma) using a composition comprising nanoparticles containing an mTOR inhibitor (e.g., limus drugs, e.g., sirolimus or its derivatives) and albumin in combination with a multityrosine kinase inhibitor (e.g., pazopanib).

The disclosure relates in part to the discovery that slow-flow vascular malformations (which can be venous and / or lymphatic) can be treated using direct intralesional delivery of an active drug, such as but not limited to a mTOR inhibitor, such as but not limited to temsirolimus, or a salt or solvate thereof.

The application discloses a sirolimus albumin composition and a preparation method thereof. The preparation method of the application adds an incubation step before evaporation and removal of a solvent from a material liquid after high-pressure homogenization, which not only makes nanoparticles more uniform, but also further improves the physical stability of a nanosuspension and the chemical stability of a preparation without adding any stabilizer. Compared with a marketed product, the sirolimus albumin composition disclosed by the application can be completely dissolved in 1-3 min, the reconstitution operation is more convenient, and the nanosuspension after reconstitution can be stable at 30 DEG C for 24 h, which is more convenient for clinical use. Moreover, the composition of the application can be stored at room temperature, is convenient for transportation, and has a longer effective period.

An intravascular device including a transferable drug coating adhered to an exposed outer surface on the device, the drug coating comprising an anti-proliferative active ingredient and a xanthophyll excipient. The xanthophyll may be selected from the group consisting of lutein, astaxanthin, zeaxanthin, meso zeaxanthin, cryptotaxanthin, tunaxanthin, salmoxanthin, and parasiloxanthin, and mixtures thereof. The anti-proliferative active ingredient may be selected from the group consisting of sirolimus, everolimus, zotarolimus, bioliimus, tacrolimus, pimecrolimus, paclitaxel, and mixtures thereof. The device may be used in the treatment of eye disease.

To provide effective therapeutic agents for the treatment of refractory lymphatic and vascular diseases. Provided is a therapeutic agent for the treatment of refractory lymphatic and vascular diseases which contains sirolimus as an active ingredient. The administration of the therapeutic agent is initiated by oral or tube administration at a dosage determined according to parameters related to the pharmacokinetics of sirolimus in a patient having the disease and the weight and age of the patient.

Provided are methods of treating cancer (e.g, a cancer that comprises one or more cancer cells that express a KRAS G12C mutant protein and / or have at least one mTOR-activating aberration) in an individual that comprise administering a composition comprising nanoparticles that comprise an mTOR inhibitor (such as a limus drug, e.g, sirolimus or a derivative thereof) and an albumin in combination with a KRAS G12C inhibitor to the individual. Also provided are related kits.