16 results about "High plasma" patented technology

The present invention provides a tetrazole compound, a pharmaceutical composition thereof and a use thereof. The compound of the present invention has a brand-new structure, a low clearance rate, high plasma exposure, good oral bioavailability, and good pharmacokinetic properties, and is conducive to drug development. The compound of the present invention or a pharmaceutically acceptable salt thereof can be used for preventing and / or treating pain, including neuropathic pain, etc.

The present application provides a kind of potassium channel regulator, its preparation method, pharmaceutical composition and application. Specifically provided are compounds as shown in formula V or pharmaceutically acceptable salts thereof. The potassium channel regulator compound of the present application has one or more of the following effect advantages: (1) novel structure; (2) good KCNQ2 / 3 channel opening activity; (3) weak KCNQ4, KCNQ5 opening activity, high KCNQ2 / 3 selectivity; (4) good in vivo efficacy, good protection effect on seizures; (5) low neuro-motor toxicity; (6) high brain-blood ratio; (7) high plasma, brain tissue concentration.

The invention provides a GK001 solid preparation as well as a preparation method and application thereof. The solid preparation comprises the following components: a GK001 amorphous solid dispersion, an excipient, a diluent, a disintegrating agent and a lubricant, the GK001 has a structure as shown in a formula I which is described in the specification. According to the invention, GK001 is creatively prepared into a solid preparation in the form of amorphous solid dispersion, and the solid preparation has excellent stability and fluidity and high oral availability. The preparation is moderate in hardness and stable in quality, the process requirements are met, and the friability and disintegration time limit both meet the requirements; the dissolution rate of the preparation is basically consistent with the drug content, the plasma exposure is high, and the oral dose of the drug and the plasma exposure are in a linear relationship.

Disclosed in the present invention are a radiolabeled compound of a risedronic acid derivative, and a precursor compound thereof, and a preparation method therefor and the use, which belong to the technical field of nuclear medicine. Provided in the present invention are a precursor compound of a radiolabeled compound of a risedronic acid derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and a radiolabeled compound of a risedronic acid derivative as shown in formula (II) or a pharmaceutically acceptable salt thereof. In the present invention, risedronic acid is creatively combined with a chelating agent to obtain NOTA-risedronic acid and DOTA-risedronic acid, and then a radionuclide is used for labelling. The radiolabeled product of the present invention has a relatively high water solubility, good in-vitro stability at room temperature, and a high plasma protein binding rate, and exhibits a relatively high and prolonged bone uptake in terms of imaging and in vivo distribution in mice; and compared to 68Ga-DOTA-ibandronic acid, the uptake of the compound of the present invention at the lesion site is twice as high.

The present application relates to an amide compound and its use, the amide compound is selected from the compound shown in formula (I), its tautomer, its endo racemate, its exo racemate, its enantiomer, its diastereoisomer, its atropisomer or its pharmaceutically acceptable salt. The present application develops a series of novel amide compounds, these amide compounds have excellent anti-HIV virus activity, and no obvious cytotoxicity, strong affinity to HIV-1 capsid protein, good specificity; suitable for intravenous administration, oral administration, subcutaneous administration, intramuscular administration mode, long half-life in vivo and high exposure; at the same time, the amide compound has no obvious inhibition to various CYP enzymes, shows high plasma protein binding, excellent safety and good metabolic stability in vivo, no potential off-target effect, high safety, and has the potential to develop into a clinical long-acting drug.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a novel glucocorticoid and a preparation method and application thereof, the novel glucocorticoid comprises a compound of a formula I, an optical isomer of the compound, a medicinal salt of the compound or a solvate of the compound, and the structural formula of the compound of the formula I is shown in the description. The compound provided by the invention has the advantages of high plasma removal rate, short half-life period, low systemic drug exposure and higher target selectivity to a glucocorticoid receptor (GR), and can obviously reduce side effects caused by systemic absorption of a glucocorticoid drug. The compound has remarkable anti-inflammatory activity on animal asthma, uveitis, xerophthalmia, inflammatory bowel disease, psoriasis and the like. The compound provided by the invention has good safety, no abnormal intraocular pressure is detected when the compound is continuously administered to the eyes of guinea pigs, and no obvious abnormal epidermal layer thickness occurs after the compound is continuously administered to the skin of rats.

The invention discloses a radioactive marker of a dithiophosphoric acid derivative, a precursor compound of the radioactive marker, a preparation method of the radioactive marker and application of the radioactive marker, and belongs to the technical field of nuclear medicine. The invention provides a precursor compound of a radiomarker of a dithiophosphoric acid derivative as shown in a structural formula (I) or a pharmaceutically acceptable salt of the precursor compound, and a radiomarker of a dithiophosphoric acid derivative as shown in a formula (II) or a pharmaceutically acceptable salt of the radiomarker. According to the invention, risedronic acid is creatively combined with a chelating agent to obtain NOTA-risedronic acid and DOTA-risedronic acid, and then radionuclides are used for labeling. The radiolabeled product disclosed by the invention is relatively high in water solubility, relatively good in-vitro stability at room temperature and high in plasma protein binding rate, and relatively high and relatively long-lasting skeleton uptake is shown in imaging and in-vivo distribution in mice; and compared with the 68Ga-DOTA-ibandronic acid, the intake of the compound disclosed by the invention at the focus part is twice of that of the 68Ga-DOTA-ibandronic acid.

The present invention relates to polymorphic forms of nepicastat acid addition salts, their preparation methods, and uses. The acid addition salts are selected from the group consisting of hydrochloride, sulfate, phosphate, mesylate, benzenesulfonate, p-toluenesulfonate, hydrobromide, maleate, tartrate, citrate, and fumarate, with hydrochloride being preferred. Nepicastat acid addition salts have high polymorphic stability, high solubility, high plasma concentration, high bioavailability, and excellent pharmacological activity, making them suitable for pharmaceutical preparations.

The invention belongs to the technical field of biomedical polypeptides, particularly relates to a frombesin polypeptide compound or a pharmaceutically acceptable salt thereof, and further relates to application of the polypeptide or the pharmaceutically acceptable salt thereof in medicines for treating diseases related to GRPR. The polypeptide provided by the invention has the characteristics of high affinity, high plasma stability and long plasma half-life period.

A solid dispersion, a preparation method therefor, and use thereof. The solid dispersion comprises an active ingredient: the compound of formula A or a derivative thereof, a crystal form thereof, an amorphous form thereof, or a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof, and comprises a carrier. The solid dispersion can significantly improve the oral bioavailability of the active ingredient and has good solid stability, causing the active ingredient to show higher plasma exposure in a rat.

The present invention provides a solid dispersion, its preparation method and use, which comprises an active ingredient, a compound of Formula A or a derivative thereof, in a crystalline form, an amorphous form, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and a carrier. The solid dispersion can significantly improve the oral bioavailability of the active ingredient, has good solid-state stability, and allows the active ingredient to exhibit high plasma exposure in rats.

Mammals typically heal with fibrotic scars. Treatments to regenerate human skin and hair without a scar remain elusive. Mice lacking C-X-C motif chemokine receptor 2 (CXCR2-KO) displayed robust and complete tissue regeneration across three different injury models, including skin, hair follicle, and cartilage. Remarkably, wild type mice receiving plasma from CXCR2-KO mice through parabiosis or injections healed wounds scarlessly. A comparison of circulating proteins using multiplex ELISA revealed a 24-fold higher plasma level of granulocyte-colony stimulation factor (G-CSF) in CXCR2-KO blood. Local injections of G-CSF into WT mouse wound beds reduced scar formation and increased hair follicle regeneration by 6-fold. G-CSF directly polarized macrophages into an anti-inflammatory phenotype, and both CXCR2-KO and G-CSF-treated mice recruited more anti-inflammatory macrophages into injured areas. These results improve our molecular understanding of scarless tissue regeneration and introduce a new therapeutic approach for cutaneous wounds and hair regeneration. Provided are compositions and methods relating to treating wound healing pathologies.

The present invention relates to a polymorphic form of a nepicastat acid addition salt, a preparation method therefor and a use thereof. The acid addition salt is selected from hydrochloride, sulfate, phosphate, mesylate, benzenesulfonate, p-toluenesulfonate, hydrobromate, maleate, tartrate, citrate, and fumarate, preferably hydrochloride. The nepicastat acid addition salt has high polymorphic form stability, high solubility, high plasma concentration, high bioavailability, and excellent pharmacological action, and therefore is suitable for pharmaceutical preparations.

The invention relates to a solid dispersion as well as a preparation method and application thereof. The solid dispersion comprises a compound as an active ingredient shown in a formula A or a derivative, a crystal form, an amorphous form, or pharmaceutically acceptable salt, hydrate or solvate thereof, and a carrier. The solid dispersion can significantly improve the oral bioavailability of the active component, and has good solid stability, so that the active component shows high plasma exposure in a rat body. # imgabs0 #

The invention provides a jet-spun yttrium-stabilized zirconia (YSZ) nanofiber sponge for portable plasma / serum separation, which has efficient plasma / serum separation performance, low hemolysis rate, high mechanical strength and good filtering efficiency, and is suitable for portable blood detection equipment. Zirconium n-propoxide and yttrium nitrate hexahydrate are used as precursors and are mixed with acetylacetone in ethyl alcohol, PVP is added, and stirring is performed to form a viscous solution. And micron fibers are spun through an airflow spinning device and are stacked into a porous sponge structure. And drying, pressurizing and densifying, and calcining at high temperature to remove organic components, thereby obtaining the pure white YSZ fiber sponge. The material overcomes the inconvenience of a traditional centrifugal method, has large-scale application potential, is uniform in fiber structure and high in porosity, and improves the blood separation efficiency and the material stability.

The present invention belongs to the field of biopharmaceutical polypeptide technology, specifically relating to a bombesin-like polypeptide compound or a pharmaceutically acceptable salt thereof, and further relates to the use of such a polypeptide or a pharmaceutically acceptable salt thereof in pharmaceuticals for treating GRPR-related conditions. The polypeptides of the present invention exhibit high affinity, high plasma stability, and a long plasma half-life.