10 results about "High plasma" patented technology

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 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.

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 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.