20results about How to "Improve oral bioavailability" patented technology

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.

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 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.

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 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 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.

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 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 provides a compound as shown in a formula (I). The compound as a medicine has a good inverse agonistic effect on a CB1 receptor. Compared with the existing known CB1 receptor inverse agonist, the CB1 receptor inverse agonist has the following advantages: 1) the CB1 receptor inverse agonist has lower brain penetration capability, so that the CB1 receptor inverse agonist has better safety and can avoid or relieve neuropsychiatric side effects; and 2) the oral bioavailability is better.

The application belongs to the technical field of pharmaceutical chemistry, and particularly relates to a new mirinol crystal form, and particularly to a mirinol-adipic acid co-crystal and a preparation method and application thereof. The co-crystal has an X-ray diffraction spectrum expressed by 2theta using Cu-Kalpha radiation, and has characteristic peaks at least at 9.0+ / -0.2°, 15.7+ / -0.2°, 18.0+ / -0.2°, 24.0+ / -0.2°, 31.4+ / -0.2°, 31.6+ / -0.2°. The preparation method of the mirinol-adipic acid co-crystal is simple in operation, easy to control in crystallization process, and good in reproducibility.

The application belongs to the technical field of pharmaceutical chemistry, and particularly relates to a milrinone-citric acid dihydrate co-crystal. The application provides a new milrinone-citric acid dihydrate co-crystal and a preparation method thereof. The co-crystal has excellent properties, can significantly enhance the solubility and stability of milrinone, is helpful to improve the oral bioavailability, improve the clinical curative effect, has strong drug-making value, the preparation method is simple in operation and easy to control, and is suitable for industrial amplification.

The application belongs to the technical field of pharmaceutical chemistry, and particularly relates to a new crystal form of cabozantinib, a preparation method and application thereof. The new crystal form provided by the application is a cabozantinib-amino sulfonic acid-methanol co-crystal, wherein one molecule of cabozantinib, one molecule of amino sulfonic acid and one molecule of methanol form a basic unit of the crystal form, and great improvement is achieved in stability, solubility and the like, the preparation method is simple in operation, good in reproducibility and suitable for industrialized production.

The invention relates to a phenol polyethylene glycol derivative, a preparation method thereof and application of the phenol polyethylene glycol derivative in medicine. Specifically, the invention relates to a phenol polyethylene glycol derivative as shown in a general formula (A-I) or a stereoisomer, a tautomer or pharmaceutically acceptable salt thereof, and application in medicine, the structure of the compound as shown in the general formula (A-I) is shown in the specification, and the group definition of the compound is consistent with that of the specification.

The invention discloses an application of an RAR alpha specific antagonist in prevention and treatment of porcine reproductive and respiratory syndrome. According to the application, the fact that the RAR alpha specific antagonist ER 50891 has the anti-PRRSV effect is found for the first time, it is shown that the ER 50891 can remarkably inhibit replication and proliferation of the PRRSV, inhibit PRRSV N protein expression and reduce the PRRSV titer and has the remarkable antiviral effect, and the effect of the ER 50891 is dose-dependent. Meanwhile, the ER 50891 has a broad-spectrum antiviral effect on the PRRSV, and still has a relatively good antiviral effect on different strains and the high-pathogenicity PRRSV (HP-PRRSV). The invention discloses the new application of the ER 50891 in the anti-PRRSV aspect for the first time, a new candidate compound is provided for research and development of anti-PRRSV drugs, and a new strategy and means are also provided for clinical prevention and treatment of porcine reproductive and respiratory syndrome.

The application discloses aryl benzimidazole compounds of formula I, pharmaceutical compositions and applications thereof. The compounds and the pharmaceutical compositions have specific GLP-1 agonistic activity, and are agonists of glucagon-like peptide-1 receptor (GLP-1R). Therefore, the compounds can be used for preparing medicines for preventing and / or treating GLP-1 mediated diseases or related diseases.

The invention discloses a beta-lactamase inhibitor, which is selected from a compound with a structure shown as a formula I or pharmaceutically acceptable salts, isomers or deuterated substances of the compound. The invention discloses an application of the beta-lactamase inhibitor in preparation of the beta-lactamase inhibitor. The invention also discloses application of the beta-lactamase inhibitor in preparation of medicines for treating diseases related to bacterial infection. The bacteria are bacteria capable of producing beta-lactamase. The beta-lactamase inhibitor disclosed by the invention can quickly and completely release active metabolites such as avibactam, dulobactam, relebactam, nacchabactam and other diazabicyclo beta-lactamase inhibitors in vivo, and can quickly take effect, so that the oral bioavailability of the beta-lactamase inhibitor is effectively improved, the bioavailability of the beta-lactamase inhibitor is improved, and the bioavailability of the beta-lactamase inhibitor is improved. Therefore, the diazabicyclo beta-lactamase inhibitor can be orally taken, and the problem of low oral bioavailability of the diazabicyclo beta-lactamase inhibitor is solved.

The application discloses a series of glutarimide derivatives and application thereof, and specifically discloses a compound shown in formula (VI-1), a stereoisomer or a pharmaceutically acceptable salt thereof.