49results about How to "Improve oral bioavailability" patented technology

The present application belongs to the field of biomedicine technology, and specifically relates to a chondroitin sulfate oligosaccharide derivative and a preparation method and application thereof. The structure of the chondroitin sulfate oligosaccharide derivative is shown in Formula I, #imgabs0#Formula I, where R1 is SO3H, R2 is H or R1 is H, R2 is SO3H, and the polymerization degree of the chondroitin sulfate oligosaccharide derivative is equal to 8; the chondroitin sulfate oligosaccharide derivative has good promotion of chronic hepatitis repair and anti-inflammatory activity, and has a clear structure, and can be used for oral treatment of non-alcoholic fatty liver disease.

The invention belongs to the technical field of sustained-release microcapsules, and particularly discloses a ganoderma triterpenoid sustained-release microcapsule and a preparation method thereof.Bovine serum albumin and octenyl succinic anhydride modified starch are selected to prepare a Maillard product through a carbonyl ammonia condensation method to serve as a wall material, and a core material ganoderma triterpenoid is well wrapped in the wall material; the Maillard reaction product and the ganoderma triterpenoid are crosslinked, the structure of the freeze-dried microcapsule is not damaged, and the prepared granular microcapsule is complete in structure, high in embedding rate and good in stability. The sustained release performance of the ganoderma triterpenoids as an embedding material is improved, the water solubility of the ganoderma triterpenoids is improved, the dissolution speed and the intestinal mucosa permeability of the ganoderma triterpenoids are improved through conjugation change of polymer characteristics, the retention time is prolonged through biological adhesion, the oral bioavailability of the ganoderma triterpenoids is improved, and the bioavailability of the ganoderma triterpenoids is improved. The human body absorption and utilization degree of the ganoderma triterpenoids can be obviously improved.

The invention belongs to the technical field of medicines, and particularly relates to a flavonoid compound-meglumine co-amorphous substance and a preparation method thereof. The flavonoid compounds comprise baicalein, hesperetin, naringenin, kaempferol, quercetin, isoliquiritigenin and the like, and the co-amorphous substance consists of a single flavonoid compound and meglumine and is prepared by adopting a melting shock cooling method or a rotary evaporation method. The miscibility of the flavonoid compounds and the meglumine is screened through Hansen solubility. The crystal diffraction characteristics, thermodynamic properties and intermolecular interaction of the co-amorphous substance are measured through PXRD, DSC and FTIR, and it is shown that the six flavonoid compounds and meglumine successfully form a co-amorphous system. The solubility and the dissolution rate of the six flavonoid compound-meglumine co-amorphous substance are obviously superior to those of flavonoid bulk drugs, and the physical stability of the formed co-amorphous substance is obviously superior to that of a single amorphous drug, so that the co-amorphous substance shows good patent medicine performance.

The present invention discloses a method for preparing Lactobacillus casei and a preparation thereof. The Lactobacillus casei was deposited in the China General Microbiological Culture Collection Center on July 6, 2022, with a deposit number of CGMCC No. 25194. The preparation method of the double-layer emulsion probiotic preparation comprises the following steps: (1) vortexing Lactobacillus casei and a probiotic protective agent solution to uniformly disperse them to form an inner water phase W1; (2) dissolving ursolic acid in oil to form an oil phase O, and mixing the oil phase O with the inner water phase W1 by high-speed shearing to obtain an oil-in-water type colostrum W1 / O; (3) using a suspension of colloidal particles as an external water phase W2, adding the external water phase W2 to the colostrum W1 / O, and mixing by medium-speed shearing to obtain a double-layer emulsion probiotic preparation with a W1 / O / W2 type double emulsion structure.

The invention relates to dexcamphanol or fenchol ester derivatives of 2-hydroxynicotinic acid and pharmaceutical application of the dexcamphanol or fenchol ester derivatives, and belongs to the technical field of biological medicine. The structural general formula of the derivative disclosed by the invention is # imgabs0 #, wherein R1 is selected from-H,-Cl, alkyl with 1 to 8 carbon atoms,-CF3,-CF2H,-CN,-SCH3,-OH,-CHO,-CH2OH,-CH2NH2,-COOH, halogenated phenyl or-NR4R5; r4 and R5 are independently selected from-H or-CH3; r2 is selected from-H, alkyl with 1-6 carbon atoms, and acyl or carbamoyl with 2-7 carbon atoms; r3 is selected from # imgabs1; # X is selected from-CH = or-N =. The derivative disclosed by the invention has a good inflammation inhibition effect; and under the condition of high concentration, the compound has lower cytotoxicity and is safer. The compound can be used for preparing medicines for treating inflammation and inflammation-related diseases such as cerebral apoplexy, neuropathic pain, depression and senile dementia.

The invention discloses a nutritional food capable of improving a night vision function and a preparation method of the nutritional food. The composition is prepared from anthocyanin-sterculia nobilis acid nano-particles, fucoxanthin-vitamin A-resveratrol nano-particles and zinc taurate. The functions of retinal rod cells can be remarkably improved, the blood microcirculation of eyes can be promoted, and the vision sensitivity and the asthenopia resistance in dark environments such as night, weak light and low visibility can be remarkably improved; the product can be prepared into capsules, tablets, electuary, oral liquid or beverage.

This invention belongs to the technical field of medicinal chemistry and provides a milrinone-tartaric acid cocrystal. Using Cu-Kα radiation, its X-ray diffraction pattern (expressed as 2θ) exhibits characteristic peaks at at least 10.0±0.2°, 13.2±0.2°, 20.4±0.2°, 24.7±0.2°, 26.2±0.2°, 26.7±0.2°, and 34.3±0.2°. The cocrystal of this invention has high solubility and good stability. Using this cocrystal to prepare formulations avoids the use of large amounts of excipients and auxiliaries in existing technologies, reducing both production costs and clinical safety risks. The preparation method of the milrinone-tartaric acid cocrystal provided by this invention is simple to operate, the crystallization process is easy to control, and it has good reproducibility.

The invention belongs to the technical field of crystal form drug molecules, and particularly relates to a preparation method and application of an axitinib-fumaric acid-acetic acid eutectic crystal. According to the axitinib-fumaric acid-acetic acid eutectic crystal, a basic unit of a crystal form is composed of one molecule of axitinib, one molecule of fumaric acid and one molecule of acetic acid, the stability, solubility, permeability and the like are greatly improved, and the preparation method is easy to operate, good in reproducibility and suitable for industrial production.

This invention discloses a chitosan-Chlamydomonas reinhardtii protein composite carrier, its preparation method, and its application. The composite carrier has a triple network structure, comprising: a three-dimensional network backbone formed by cross-linking chitosan and sodium tripolyphosphate, constituting the first network; a functional enhancing phase, including Chlamydomonas reinhardtii protein, which is embedded and anchored in the three-dimensional network backbone through a first physical interaction, constituting the second network, thereby forming a chitosan-Chlamydomonas reinhardtii protein complex with an interpenetrating network structure; and a structure-directing agent, including a hydrophobic active substance, which self-assembles and embeds into the hydrophobic microregions of the chitosan-Chlamydomonas reinhardtii protein complex through a second physical interaction, constituting the third network. The composite carrier provided by this invention is prepared using electrospinning technology, achieving high loading capacity and high encapsulation efficiency, constructing a multi-layered antioxidant defense network, and can serve as a highly efficient and stable multifunctional carrier for the preparation of functional food delivery materials.

The invention provides a composition for improving the thrombolysis capacity of a human body, a preparation method and application thereof.The composition is prepared from, by weight, 5-30 parts of earthworm protein, 30-120 parts of hippophae rhamnoides total flavone extract, 50-150 parts of silymarin extract, 20-80 parts of maltodextrin and 15-60 parts of pregelatinized starch, the earthworm protein activates a fibrinolytic system to promote t-PA to release and dissolve thrombus, and the hippophae rhamnoides total flavone extract activates the fibrinolytic system to promote t-PA to release and dissolve thrombus; the hippophae rhamnoides total flavonoids regulate the ratio of PGI2 / TXA2 to inhibit platelet aggregation and reduce blood fat, the silymarin protects the liver function to enhance LDL-C metabolism clearing, the hippophae rhamnoides total flavonoids, the silymarin and the hippophae rhamnoides total flavonoids cooperate to form a thrombolysis-antithrombosis-metabolism regulation three-dimensional intervention system, a whole-course low-temperature mixing direct tabletting process is adopted

A probiotic microsphere with in-situ proliferation, its preparation method and application. The microsphere is prepared by a two-step Pickering double emulsion method, encapsulating probiotics and panax notoginseng saponins, and then mixed with sodium alginate and cross-linked by calcium ions. The structure significantly improves the survival rate of probiotics in simulated gastric juice, intestinal juice, heat treatment and antibiotic environment, and maintains high viable cell count during long-term storage. Co-encapsulated PNS and double emulsion stabilizer natural polysaccharide-protein nanocomposite can promote the proliferation of probiotics in-situ, increase their activity. In addition, the microsphere can effectively promote the colonization and proliferation of probiotics in the intestinal tract, enhance the oral bioavailability of bioactive ingredients, and is suitable for functional food, feed, biological medicine field, especially as 3D printing special medical food for dysphagia population and prevention and treatment of intestinal inflammatory diseases.

The present application provides a series of substituted 1,2,4-triazole derivatives and their applications, and specifically provides a compound shown in formula (I) and a pharmaceutically acceptable salt thereof.

The invention discloses a dendrobium officinale flavone nano-liposome with uric acid reducing activity as well as a preparation method and application thereof. The nano-liposome is prepared based on a sterol substance, a phospholipid substance and a cationic lipid. Wherein the sterol substance comprises phytosterol ester and cholesterol, the phospholipid substance is dipalmitoyl phosphatidylcholine (DPPC), and the cationic lipid is (2, 3-dioleoyl-propyl)-trimethylamine (DOTAP); and a functional active substance dendrobium officinale flavone is encapsulated. The dendrobium officinale flavone nano-liposome is prepared by adopting an ethanol injection method, and the nano-liposome can reduce the content of uric acid and xanthine oxidase, inhibit the level of inflammatory factors and relieve kidney and liver injury, so that hyperuricemia is relieved.

The invention discloses a celecoxib solid self-emulsifying nano-microsphere and a preparation method and application thereof. The celecoxib solid self-emulsifying nano-microsphere of the invention comprises an outer shell and an inner core arranged in the outer shell, wherein the raw materials for preparing the outer shell comprise: a polymer and a solvent; and the raw materials for preparing the inner core comprise: celecoxib, an oil phase, an emulsifier, an emulsifier and a precipitation inhibitor. The celecoxib solid self-emulsifying nano-microsphere has the advantages of good dispersibility, uniform particle size and large drug loading, and can be rapidly emulsified when encountering an aqueous environment of the gastrointestinal tract, significantly improving the dissolution rate and oral bioavailability of celecoxib. In addition, the preparation process of the invention is simple, there is no heating process, and the obtained product has stable quality, and is suitable for industrial production.

The invention relates to a polysubstituted indole compound as well as a preparation method and application thereof. Specifically, the invention discloses a compound as shown in a formula (I), or a pharmaceutically acceptable salt thereof, or a prodrug thereof, the compound is a complement factor B inhibitor, has a significant inhibitory effect on complement factor B, and is high in bioavailability and excellent in pharmacokinetics.

The present invention provides a JAK inhibitor having high oral bioavailability, characterized in that the JAK inhibitor comprises: a Formula I compound, or a stereoisomer, geometric isomer, tautomer, hydrate, solvate, or pharmaceutically acceptable salt thereof as an active ingredient. The JAK inhibitor with high oral bioavailability provided by the present invention can overcome the problem that existing JAK inhibitors have low oral bioavailability, and involves further modifying a chemical compound so as to change the physicochemical characteristics of one or several small molecule compounds, thus increasing the in-vivo cell absorption performance of said compound(s), greatly improving the bioavailability of the medication and providing new possibilities for drug delivery and utilization for said compound medication.

A Panax notoginseng polysaccharide iron nanoparticle preparation, its preparation method, and its application are disclosed. This invention can effectively prepare Panax notoginseng polysaccharide iron nanoparticles, solving the application problem in the preparation of drugs for treating iron deficiency anemia, inflammatory bowel disease-related anemia, iron deficiency anemia-related colitis, inflammatory anemia, or inflammatory bowel disease. The specific steps are as follows: The crude Panax notoginseng polysaccharide solution is purified using conventional purification methods to obtain purified Panax notoginseng polysaccharide. This purified polysaccharide is dissolved in ultrapure water, and an iron source is added under inert gas protection. After co-precipitation and chemical reduction reactions, the pH value is adjusted, and iron nanoparticles are loaded onto the Panax notoginseng polysaccharide to obtain Panax notoginseng polysaccharide-coated iron nanoparticles. The preparation method of this invention is simple, uses abundant raw materials, and has low production costs. It represents a major innovation in drugs for treating iron deficiency anemia and inflammatory bowel disease-related iron deficiency anemia, and has practical application value.

The invention discloses an absorption enhancer and preparation method for improving the oral bioavailability of polypeptides, relates to the field of biological health care technology, including arginine grafted hyaluronic acid complex, enzyme inhibitor, and promotion auxiliary agent; the mass fraction of arginine grafted hyaluronic acid complex in the absorption enhancer for improving the oral bioavailability of polypeptides is 60-65%; the mass fraction of enzyme inhibitor in the absorption enhancer for improving the oral bioavailability of polypeptides is 5-8%; the rest are: promotion auxiliary agent; the enzyme inhibitor is pepstatin; the absorption enhancer for improving the oral bioavailability of polypeptides prepared by the method of the present invention is remarkable for the absorption effect of polypeptide oral liquid. The absorption enhancer prepared by the present invention is mainly capable of improving the absorption of components such as protein polypeptides by the gastrointestinal tract, making it easier to enter the physiological system circulation through the physiological barrier of the intestinal tract, improving absorption efficiency, and then improving oral bioavailability.

The application belongs to the field of medicine, and discloses a rebamipide volorabine salt, which has a structure shown in formula (I), wherein the structure of formula (I) is as follows: the application discloses a preparation method of the rebamipide volorabine salt and application of the rebamipide volorabine salt in preparation of a medicine for treating and / or preventing a gastric acid related disease or a helicobacter pylori infection disease.

The invention discloses a polygonatum polysaccharide hydrogel preparation of dihydromyricetin. In the preparation process of the polygonatum polysaccharide hydrogel preparation of dihydromyricetin, polygonatum polysaccharide is used as an adhesive, food-grade low-molecular organic acid is used as a pH regulator and a preservative, and a food-grade calcium chloride ion cross-linking agent is used as a gel structure control agent. The polygonatum sibiricum polysaccharide hydrogel of dihydromyricetin prepared by the invention is a good sustained-release preparation, has better hydrophilic effect, gastrointestinal stability effect, permeability effect and sustained-release effect on dihydromyricetin, and enhances the bioavailability of dihydromyricetin. Meanwhile, the natural bioactive substance, namely, the dihydroxyenzyme, has the characteristics of low side effect and easiness in obtaining, so that the implementation of the invention is of great significance to the development of chronic disease targeted drugs and the prevention and treatment of chronic diseases in the future by the dihydroxyenzyme.

The application belongs to the technical field of medical nutritional foods, and particularly relates to a composite peptide nutritional composition for promoting wound healing and a preparation process and application thereof. The composite peptide nutritional composition for promoting wound healing is prepared from raw materials including fish collagen peptide 15%-25%, bovine spleen peptide 0.03%-0.05%, blood protein oligopeptide 0.10%-0.30%, albumin peptide 0.10%-0.30%, ginseng powder 0.01%-0.03%, composite fermentation extract 15%-20%, plant extract 10%-20%, prebiotic 20%-25%, and whey protein matrix supplementing the rest to 100% by weight percentage. The application improves the content of healing-promoting peptide segments and various active ingredients such as anti-inflammatory repair by using self-made fish collagen peptide, composite fermentation extract and other raw materials, and improves the bioavailability of plant extract through embedding technology, thereby significantly improving the wound healing rate and quality.

This invention relates to a method for preparing resveratrol nanoparticles, belonging to the field of traditional Chinese medicine technology. Addressing the problems of low oral bioavailability and lack of colonic targeting of resveratrol, this invention provides a nanoparticle formulation composed of resveratrol, zein, and xylan. The formulation is prepared by dissolving resveratrol and zein in an organic phase, adding them dropwise to an aqueous xylan phase, and then evaporating the organic solvent. This invention utilizes the hydrophobic effect of zein to improve drug encapsulation efficiency and leverages the colonic degradation characteristics and anti-inflammatory activity of xylan to achieve synergistic effects, enabling precise release of resveratrol at sites of intestinal inflammation.

The invention discloses an asenapine maleate oral adhesion film preparation as well as a preparation method and application thereof, belongs to the field of pharmaceutical preparations, and particularly relates to an asenapine maleate self-nanoemulsion oral adhesion film and an asenapine maleate nanocrystal oral adhesion film preparation. The self-nanoemulsion can improve the solubility of asenapine maleate, the lower surface tension of the self-nanoemulsion is beneficial to penetrating through a mucous membrane hydration layer and enhancing mucous membrane absorption, and the nanocrystal can improve the solubility and dissolution rate of API, increase the drug concentration gradient near the oral mucosa and promote diffusion and oral absorption of drugs. The oral cavity adhesion film can adhere to the sublingual part and rapidly release the medicine, the medicine is absorbed by rich submucosal blood vessels and directly enters systemic circulation, metabolism of the gastrointestinal tract and the liver is avoided, and then oral bioavailability is enhanced.

The present application relates to the field of medicine, and specifically, to a GLP-1 analog oral delivery composition. The GLP-1 analog oral delivery composition provided in the present application includes a GLP-1 analog and a delivery agent, and the delivery agent includes lauroyl-L-carnitine and sodium caprate. The composition shown in the present invention has excellent oral bioavailability. The composition shown in the present invention has good hypoglycemic and weight loss effects, and can be used to prepare drugs for treating or preventing diabetes or obesity. The preparation process of the composition shown in the present invention is simple, which is conducive to industrial production.

The present invention discloses a trimethyl chitosan-modified sodium alginate multivesicular liposome and a preparation method and application thereof. The preparation method comprises: (1) dissolving a lipid component in an organic solvent as an oil phase; dissolving sodium alginate in an aqueous solution containing an osmotic pressure regulator as an inner aqueous phase; (2) adding the oil phase to the inner aqueous phase, and ultrasonically forming colostrum; (3) adding the colostrum to an outer aqueous phase containing an osmotic pressure regulator and an auxiliary emulsifier, and homogenizing to form a double emulsion; (4) rotary evaporating the double emulsion to remove the organic solvent, centrifuging to remove the free drug, and dispersing the precipitate in a solvent to obtain sodium alginate multivesicular liposome; (5) synthesizing trimethyl chitosan, and uniformly coating to obtain trimethyl chitosan-modified sodium alginate multivesicular liposome. The liposome prepared by the present invention has a high drug encapsulation rate, and the use of trimethyl chitosan modification can further promote oral absorption, improve the oral bioavailability of the drug, reduce the number of drug use times, and improve patient compliance. Furthermore, the trimethyl chitosan-modified sodium diester alginate multivesicular liposomes have uniform particle size and stable morphology, so as to exert anticoagulation and platelet aggregation inhibition effects and be applied to the treatment of thrombosis-related diseases.

Provided herein are compounds of formula (I) wherein Ra, Rb, Rc, A and p have the meanings given in the specification, as defined in formula (I), as well as pharmaceutically acceptable salts and solvates thereof, which are useful in the treatment of diseases in which pan-immune proteasome inhibition is desired or desired, and in particular in the treatment of cancer.

The present application discloses a flurana nanostructured lipid carrier and a preparation method thereof, which belongs to the technical field of insecticide preparation. The flurana nanostructured lipid carrier semisolid cream can be administered orally or externally, and is used for preventing and treating ectoparasitic diseases of pets such as dogs and cats. The present application improves the performance of the nanostructured lipid carrier by adding a quantitative polyol to the aqueous phase and compounding with lipids, which not only makes the nanostructured lipid carrier system more stable and has a high encapsulation rate, but also improves the release and absorption of the main drug in the nanostructured lipid carrier, solves the solubility of flurana, and improves the bioavailability, promotes the drug to better exert its therapeutic effect in the body, enables pets to improve the therapeutic effect while reducing the dosage of the drug, improves the safety of the drug, reduces the damage to the pet, and has significant clinical application value.

The invention relates to a semaglutide nanoparticle preparation, and relates to the field of pharmaceutical preparations. The semaglutide nanoparticle preparation is characterized in that an active component semaglutide-carboxylated dextrade-40 compound is entrapped in a nanoparticle, and the semaglutide-carboxylated dextrade-40 compound is obtained by blending semaglutide and carboxylated dextrade-40 in a water phase solvent. According to the semaglutide nano preparation, a semaglutide pC-DEX40 compound is prepared by virtue of an electrostatic compression effect, so that the capacity of semaglutide for resisting adverse factors in a preparation forming process is improved; the Sml-pC-DEX40 is entrapped in the nano particles to obtain the nano particles loaded with the Sml-pC-DEX40, so that the oral delivery efficiency and the bioavailability of semaglutide are improved.

The invention belongs to the field of chemical drugs, and discloses a BTK protein degradation agent taking a silicon-containing group as a hydrophobic label, and a preparation method, a pharmaceutical composition and application thereof. The structure of the BTK protein degradation agent with the silicon-containing group as the hydrophobic label is shown in a formula I, and linker is a saturated aliphatic chain, an unsaturated aliphatic chain, a connecting structure composed of an aromatic ring and a saturated aliphatic chain or a connecting structure composed of an aromatic ring and an unsaturated aliphatic chain; r is a specific silicon-containing group as a hydrophobic label. The BTK protein degradation agent with the silicon-containing group as the hydrophobic label is obtained, the preparation process is simple and easy to implement, and the obtained BTK protein degradation agent has high liver microsome metabolism stability and considerable oral bioavailability, shows an efficient treatment effect in an in-vivo experiment, has a certain inhibition effect on proliferation of various tumor cells, and has a good application prospect. The compound is suitable for developing drugs for treating leukemia and other cancers. # imgabs0 #

The invention belongs to the field of chemical medicines, and discloses an EGFR (epidermal growth factor receptor) protein degradation agent taking a silicon-containing group as a hydrophobic label as well as a preparation method, a pharmaceutical composition and application of the EGFR protein degradation agent. The structure of the EGFR protein degradation agent with the silicon-containing group as the hydrophobic label is shown as a formula I, and linker is a saturated aliphatic chain, an unsaturated aliphatic chain, a connecting structure composed of an aromatic ring and a saturated aliphatic chain or a connecting structure composed of an aromatic ring and an unsaturated aliphatic chain; r is a specific silicon-containing group as a hydrophobic label. The EGFR protein degradation agent with the silicon-containing group as the hydrophobic label is obtained, the preparation process is simple and easy to implement, and the obtained EGFR protein degradation agent has high liver microsome metabolism stability and considerable oral bioavailability, shows an efficient treatment effect in an in-vivo experiment, has a certain inhibition effect on proliferation of various tumor cells, and has a good application prospect. The method is suitable for developing medicines for treating lung cancer and the like. # imgabs0 #