102 results about "Improved solubility" patented technology

The invention relates to a stevioside composition, which comprises at least one stevioside and at least one of siamenoside I, mogroside V, mogroside III-E and mogroside II-E, and is characterized in that the stevioside composition comprises at least one stevioside and at least one of siamenoside I, mogroside V, mogroside III-E and mogroside II-E; wherein the stevioside has a higher solubility in the composition than in an equivalent composition lacking siamenoside I, mogroside V, mogroside III-E, and mogroside II-E. The invention also relates to a method for preparing the stevioside composition. The composition may be an aqueous solution.

Provided are long-acting atrial natriuretic peptide (ANP) polypeptides that bind to natriuretic peptide receptors, such as NPR-A, thereby functioning as NPR-A agonists and that exhibit improved stability. The present invention provides atrial natriuretic peptides with specific structural features that result in polypeptides with sufficient activity at NPR-A and also possess a number of other beneficial attributes related to their potential development as therapeutic treatments, including improved solubility of the analogs in aqueous solution, improved chemical and physical formulation stability, an enhanced pharmacokinetic profile, and minimized potential immunogenicity.

The invention discloses an embedding method for stabilizing and slowly releasing beta-carotene. The embedding method comprises the following steps: selecting soybean oil; the stirring conditions are as follows: 300 r / min and 75 DEG C; preparing a water phase: stirring 80 kg of maltodextrin and 20 kg of cane sugar at 50 DEG C until 200 kg of distilled water is completely dissolved; the homogenizing conditions are as follows: the high-speed mixing and shearing emulsifying machine shears for 5 minutes at the speed of 17000 r / min, and the high-pressure homogenizing machine homogenizes for 2 minutes at the pressure of 20 MPa; the spray drying conditions are as follows: the pressure is 0.5 MPa, the inlet temperature is 170 DEG C, and the flow rate is 10 mL / min. The particle size D of the optimized beta-carotene microcapsule product is 95lt; according to the present invention, the prepared nano-particles have characteristics of uniform particle size, 300 nm, embedding rate of 94.2%, good stability in the 90-day storage period, and significantly improved solubility.

A method for improving drug solubility and a drug composite material having improved solubility. The method comprises preparing a silica colloidal suspension from silica nanoparticles having a diameter between 2 nm and 100 nm; rapidly evaporating a solvent by means of controlling the temperature and pressure, so as to obtain a porous surface material with ultra-high density silanol groups retained on the surface; and loading drug molecules. By controlling the size of nanoparticles and the density of silanol groups, drug molecules can be effectively adsorbed under anhydrous conditions, and rapidly desorbed and released in an aqueous environment.

The invention relates to an acid salt of a compound shown as a formula (I), in particular to a hydrochloride of the compound shown as a crystalline form (I) and a preparation method and application of the hydrochloride, and the compound is a PD-1 / PD-L1 inhibitor with the structure of the compound shown as the formula (I). The acid salt of the compound as shown in the formula (I) has improved dissolving capacity in a biological medium, and particularly, the crystalline compound hydrochloride has moderate hygroscopicity, good crystallinity, good solubility and stable physicochemical properties, which all meet the industrial production requirements and meet the development requirements of clinical pharmaceutical preparations. The acid salt or crystalline compound hydrochloride of the compound shown in the formula (I) can be widely applied to preparation of drugs for treating PD-1 / PD-L1 signal channel mediated tumors, immune related diseases and disorders, infectious diseases, infectious diseases or metabolic diseases.

This invention provides a highly water-soluble composition for promoting autophagy and its application. The composition comprises 5-hydroxyflavone, acetylhydroxyproline, and a suitable solvent. This composition is a unique vesicular composition that enables efficient delivery and synergistic effects of the two active ingredients. It promotes autophagy, has improved solubility, stability, and antioxidant properties, and can prevent and repair skin photodamage at its source. This invention also discloses a method for preparing this composition and its applications.

This invention relates to isolated polypeptides that are analogs of human amylin. The disclosed amylin analog polypeptides have beneficial physicochemical properties relative to endogenous amylin, such as longer elimination half-lives (t1 / 2) and improved solubility and thermal stability. This invention also relates to methods of using presently disclosed amylin analog polypeptides in a variety of therapeutic indications, as well as methods of producing the same. The disclosed amylin analog polypeptides are particularly useful in methods of treating metabolic diseases or disorders, such as types 1 and 2 diabetes, and providing weight loss.

The present invention relates to a use of a methylated peptide as a therapeutic agent for degenerative brain diseases. Specifically, it has been confirmed that the methylated peptide according to the present invention exhibits improved solubility, bioavailability, phagocytosis by microglia, and anti-inflammatory efficacy compared to a conventional unmodified peptide, and exhibits excellent amyloid beta reduction efficacy compared to a conventional unmodified peptide in an animal model of degenerative brain diseases. Therefore, the methylated peptide according to the present invention can be usefully used as an active ingredient of a composition for preventing or treating degenerative brain diseases and cognitive impairment, learning disability, or memory impairment associated therewith.

Provided herein are compositions comprising a silicate, inositol, and optionally an amino acid, which have improved solubility and / or are crystalline. Also provided are methods of making the disclosed compositions, as well as methods of making beverages comprising the disclosed compositions.

Provided are substrates and methods for detecting enzymatic activity of various lysosomal storage enzymes. The molecules may be used as substrates with improved solubility.

The subject matter of the present invention is a creatine agglomerate with improved solubility characteristics in aqueous systems and improved handling, thus simplifying the intake of creatine. The agglomerate is characterized in that it contains 30 to 99.9 wt. % of ground creatine and / or ground creatine derivatives and / or ground creatine salts and 0.1 to 30 wt. % of a binder containing at least one oligosaccharide, in particular maltodextrin, based on the total weight of the agglomerate.

The present application belongs to the technical field of biological medicine, and discloses a salinomycin derivative, and a preparation method therefor and a use thereof. The salinomycin derivative comprises a general formula structure of formula (1), and compared with salinomycin, the activity of the salinomycin derivative is significantly improved. A group at the C-20 position contains a disulfide bond. By means of a replacement reaction of the disulfide bond, quick and efficient coupling with a polypeptide or an antibody can occur to obtain a GSH-sensitive salinomycin derivative containing the polypeptide or the antibody, or a salt thereof. The salinomycin derivative containing the polypeptide or the antibody, or the salt thereof has improved solubility, and also has enhanced targeting performance, has improved drug selectivity and biological activity, has a bystander effect, and in addition to being able to kill tumor cells highly expressing antigens, has a significant inhibitory effect on cells lowly expressing antigens. In addition, the salinomycin derivative or the salt thereof has the effects of reversing drug resistance in tumor cells and enhancing drug sensitization and can be used in combination with other drugs to further improve the efficacy.

The present application relates to ursolic acid with improved solubility and dispersibility, a method for producing same, and a method for improving the solubility of ursolic acid. In the present application, a complex of ursolic acid, an emulsifier, and a nonionic surfactant is formed and made into microparticles, thereby improving the solubility and dispersibility of poorly soluble ursolic acid and facilitating the utilization of ursolic acid as a nutritional material.

To provide glucose-dependent insulinotropic peptide (GIP)-derived peptide analogues which are antagonists of the GIP receptor.SOLUTION: The invention provides GIP-derived peptide analogues having specific sequences. The GIP peptide analogues are optimized by comprising amino acid substitutions A13Aib and / or N24E, and are fatty acid conjugated with / without a linker, thereby having improved solubility and / or physical stability.SELECTED DRAWING: None

Exemplary embodiments of the present technological advancement include pyridine-2,6-bis(phenylenephenolate) complexes that are useful as catalyst components for olefin polymerization and have enhanced solubility in non-aromatic hydrocarbons (e.g., isohexane). The improved solubility of these complexes was accomplished by the modification of the leaving group which generally leads to improved solubility, without adversely affecting the performance of the complex when used as a catalyst for olefin polymerizations.

The present disclosure provides cyclodextrin inclusion complexes of a β-cyclodextrin substituted host molecule wherein the guest is tirapazamine. The molar ratio of the tirapazamine guest to the cyclodextrin host ranges from about 14:1 to about 2:1, inclusive. The complexed tirapazamine has advantageous properties when compared to non-complexed tirapazamine in that the tirapazamine complex is water soluble and, at a molar ratio of the β-cyclodextrin substituted host molecule to the tirapazamine guest of 2:1, the pH of a 0.7-1 mg / mL solution of the inclusion complexes containing tirapazamine ranges from about pH 5.3 to about pH 6.4. The present disclosure also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier and cyclodextrin inclusion complexes of β-cyclodextrin substituted host molecules wherein the guest is tirapazamine. The pharmaceutical composition comprising the β-cyclodextrin-complexed tirapazamine demonstrates improved stability, improved solubility and reduced toxicity of the tirapazamine compared to non-complexed tirapazamine alone.

The present invention provides a crystal of a compound of formula I as a 3-hydroxy-5-pregnane-20-one derivative and a preparation method thereof. Specifically, the invention provides a crystal form G of a compound shown as a formula I and a preparation method thereof. The crystal form G of the present invention has significantly improved solubility, excellent storage stability at various temperatures, and low hygroscopicity, thereby improving druggability, and bringing very excellent effects for production, sales and transportation of drugs.

The present invention relates to a method for producing a plant protein extract comprising providing an aqueous suspension of a plant protein composition acidified to its isoelectric pH, adding an alkaline composition comprising a carbonate or bicarbonate salt to said suspension to correct the pH of said suspension to a pH ranging from 6.2 to 7.0, preferably 6.40 to 6.70, and heat treating the suspension at the corrected pH to form the plant protein extract. The invention also relates to a pea protein extract with a solubility, determined at 20°C and at pH 7, of greater than or equal to 50% and also with a reduced sodium content, and also to the use thereof for producing food products, in particular beverages.

A cyclocurcumin-based composition consisting of: a cyclocurcumin component present at 20 to 40 wt% of the total composition; a curcuminoid component present at 30 to 50 wt%, comprising 20 to 30 wt% curcumin, 5 to 10 wt% demethoxycurcumin, and 3 to 8 wt% bisdemethoxycurcumin; a solubilizer component present at 5 to 15 wt%, comprising polysorbate at 3 to 8 wt% and lecithin at 3 to 7 wt%; a complexing component present at 5 to 12 wt%, comprising cyclodextrin inclusion complexes; and a nanoparticulate component present at 3 to 10 wt%, comprising cyclocurcumin particles with a particle size in the range of 50 nm to 200 nm. consists of a polymer stabilizing component, which is present in an amount of 4 to 10 wt.-% is present and comprises polyvinylpyrrolidone or polyethylene glycol, a phospholipid complex component present in an amount of 3 to 8 wt% and consisting of phosphatidylcholine complexes, and an encapsulation component present in an amount of 2 to 6 wt% and containing maltodextrin or gum arabic, the composition being configured to ensure improved solubility, stability and bioavailability.

This invention provides urolithin A cocrystals, their preparation methods, compositions, and applications. Specifically, this invention provides a urolithin A cocrystal with high bioavailability, wherein the urolithin A cocrystal is selected from the group consisting of: urolithin A-proline cocrystals, urolithin A-carnitine cocrystals, urolithin A-nicotinamide cocrystals, or urolithin A-creatine cocrystals. Compared to urolithin itself, the urolithin A cocrystals of this invention exhibit high stability, a significantly lower melting point, and significantly improved solubility and bioavailability. Furthermore, the preparation method is simple, easy to control, and has good reproducibility, allowing for stable acquisition of the target cocrystal. The composition containing the cocrystal, prepared by grinding, has high yield, low cost, and is suitable for large-scale production.

The present invention relates to the field of pharmaceutical crystal forms, and specifically relates to crystal forms of 2-(4,4-difluoroazepin-1-yl)-N-(2-sulfamoylpyridin-4-yl)quinoline-3-carboxamide and a salt thereof, a pharmaceutical composition, and a use. The crystal forms of a compound of formula (I) and a salt thereof which are obtained in the present invention have excellent physical stability and chemical stability, and compared with free base crystal form K1 of the compound of formula (I), have significantly improved solubility, hygroscopicity and bioavailability, and are more conducive to clinical applications. Also disclosed in the present invention is a use of the crystal forms of the compound of formula (I) and the salt thereof as sodium ion channel Nav1.8 inhibitors for treating a wide range of pain.

Provided is a novel crystalline form of lifitegrast and a pharmaceutical composition containing the novel crystalline form of lifitegrast. The crystalline form of lifitegrast has improved solubility and excellent stability against heat and moisture, thereby being effectively used for preparing a pharmaceutical composition.

To provide a unit dose detergent article having improved solubility.SOLUTION: Provided is a multi-compartment water-soluble unit dose detergent article including a plurality of compartments in a generally superposed relationship. The water-soluble unit dose detergent article 1 includes a water-soluble film wrapping a fabric care or household care detergent composition. The detergent composition includes a detersive surfactant. The water-soluble film includes a first film 2 including a specific polyvinyl alcohol polymer blend.SELECTED DRAWING: Figure 1

This invention relates to multimers containing a plurality of target peptide sequences which permit high levels of expression and improved solubility for ease of downstream processing and purification.

This patent document discloses compositions, containers, and methods related to anionic cannabinoids that contain oxide substituents. The anionic cannabinoids may be prepared from cannabinoid molecules, for example, by contacting the cannabinoid molecules with a strong base. The anionic cannabinoids generally display improved solubility in water.

The present invention provides a paliperidone cocrystal, and a preparation method therefor and a use thereof. The cocrystal former of the paliperidone cocrystal is nicotinic acid. The paliperidone cocrystal is obtained by dissolving paliperidone and nicotinic acid in an aqueous organic solvent and then evaporating to dryness under reduced pressure. The paliperidone cocrystal of the present invention has high purity and stable quality, is suitable for commercial storage, has greatly improved solubility and dissolution rate, and is more suitable for the development of paliperidone preparations.

The invention relates to a crystalline compound or a basic salt thereof as well as a preparation method and application of the crystalline compound or the basic salt. The compound is a PD-IIIPD-L1 inhibitor with a compound structure as shown in a formula (1). The crystalline compound has moderate hygroscopicity, improved solubility, good crystallinity and stable physicochemical properties, the crystalline compound basic salt has good crystallinity, good solubility and stable physicochemical properties, industrial production requirements are met, and clinical pharmaceutical preparation development needs are met. The crystalline compound or the basic salt thereof can be widely applied to preparation of drugs for treating tumors mediated by a PD-IIIPD-L1 signal channel, immune related diseases and disorders, infectious diseases, infectious diseases or metabolic diseases.

The invention belongs to the technical field of crystal form drug molecules, and particularly relates to salts of abiraterone derivatives, in particular to glutarate of L-valine abiraterone. The glutarate of L-valine abiraterone provided by the invention has characteristic peaks at the positions of 8.2 + / -0.2 degrees, 8.9 + / -0.2 degrees, 9.9 + / -0.2 degrees, 16.5 + / -0.2 degrees, 17.0 + / -0.2 degrees, 17.8 + / -0.2 degrees and 19.8 + / -0.2 degrees in an X-ray diffraction spectrum represented by 2 theta. The glutarate has improved dissolution and dissolution performance, can play a therapeutic role more effectively, and is good in stability, small in adhesiveness and convenient to store and process.

Exemplary embodiments of the present technological advancement include pyridine-2,6-bis(phenylenephenolate) complexes that are useful as catalyst components for olefin polymerization and have improved solubility in non-aromatic hydrocarbons (e.g. isohexane). The improved solubility of these complexes was accomplished by the modification of the ligand framework at a specific position that led to improved solubility, but did not adversely affect the performance of the complex when used as a catalyst for olefin polymerizations.

The present invention relates to a pharmaceutical formulation comprising at least one active pharmaceutical ingredient (API) having low aqueous solubility or a pharmaceutically acceptable salt thereof in the form of particles of a size between 1 and 800 nm, wherein said particles are encapsulated within a large microparticle of a size between 1 and 100 μm formed by a matrix comprising at least an excipient. Therefore, the API is entrapped or encapsulated in the microparticles of excipients. This pharmaceutical formulation contains the pharmaceutical active ingredient having improved solubility and subsequently supra-bioavailability.