106results about How to "Improve oral bioavailability" patented technology

The invention discloses an amorphous solid form of a compound as shown in a formula (I), an X-ray powder diffraction pattern of the amorphous solid form has no characteristic diffraction peak within the 2 theta angle range of 0-40 degrees, the amorphous solid form as shown in the figure 1 has good stability, the dissolution rate of tablets prepared from the amorphous solid form can reach 95% or above within 10 min, and the dissolution rate of the tablets can reach 95% or above within 10 min. Meanwhile, excellent dissolution uniformity is achieved, high solubility can be achieved in the human physiological pH environment, and the oral bioavailability of the tigorazan is greatly improved. The preparation method of the amorphous solid comprises the following steps: adding the following formula (I) into an organic solvent, heating, dissolving, cooling, adding a poor solvent, and crystallizing to obtain the amorphous solid. The method is simple in step, easy to operate, capable of effectively reducing cost and suitable for industrial large-scale production. # imgabs0 #

The invention belongs to the technical field of biological medicine, and particularly 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 the formula I # imgabs0 #, in the formula I, R1 is SO3H and R2 is H or R1 is H and R2 is SO3H, and the polymerization degree of the chondroitin sulfate oligosaccharide derivative is equal to 8; the chondroitin sulfate oligosaccharide derivative has good chronic hepatitis repair promotion and anti-inflammatory activity, is clear in structure, and can be orally taken to treat the non-alcoholic fatty liver disease.

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 relates to the technical field of oral solid preparations, in particular to a high-bioavailability coenzyme Q10 tablet and a preparation method thereof. The coenzyme Q10 tablet comprises an active component coenzyme Q10, a filler, an adhesive, a disintegrating agent, a lubricant and a high polymer material, compared with the prior art, hydroxyethyl methylcellulose and hydroxypropyl methylcellulose succinate are mixed according to a certain mass ratio to serve as a high polymer carrier material, the prepared coenzyme Q10 tablet can be rapidly dissolved out in vitro, and the coenzyme Q10 tablet has the advantages that the preparation process is simple, and the cost is low. Moreover, the stability of the medicine can be improved, the medicine can be rapidly absorbed in vivo after being orally taken, the oral bioavailability of the coenzyme Q10 is greatly improved, and a preparation process of the preparation is simple to operate, good in reproducibility and suitable for industrial production.

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 discloses a fluralan nanostructure lipid carrier and a preparation method thereof, and belongs to the technical field of insecticide preparation, fluralan nanostructure lipid carrier semisolid cream can be orally taken or externally applied and is used for preventing and treating ectoparasitic diseases of pets such as dogs and cats; quantitative polyol is added into the water phase to be compounded with the lipid, so that the performance of the nano-structure lipid carrier is improved, the nano-structure lipid carrier system is more stable and high in encapsulation efficiency, release and absorption of a main drug in the nano-structure lipid carrier are improved, the problem of solubility of the fluralana is solved, bioavailability is improved, and the preparation method is suitable for industrial production. The traditional Chinese medicine composition promotes the medicine to play a better curative effect in vivo, so that the treatment effect is improved while the dosage of pets is reduced, the safety of the medicine is improved, the damage to the pets is reduced, and the traditional Chinese medicine composition has remarkable clinical application value.

The invention discloses a crystal form of a compound as well as a preparation method and application thereof, the compound has a structure as shown in a formula I. The crystal form has higher crystal purity, lower hygroscopicity, better solid stability and better solubility, is beneficial to preparation and storage of pharmaceutical preparations, and has very good application value and patent medicine prospect. Besides, clinical test results show that the crystal form B of the compound as shown in the formula I has very good pharmacokinetic characteristics, low clinical toxicity, better safety and high oral bioavailability, and has a good treatment effect on various diseases.

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 a medicinal salt used as a tyrosine kinase inhibitor, a crystal, a preparation method and application thereof, in particular to a medicinal salt of (E)-4-(dimethylamino)-N-(7-(2-ethoxyethoxy ether)-4-((3-ethynyl phenyl) amino)-6-quinazoline)-2-buteneamide, a crystal form and a preparation method thereof. The invention also relates to a pharmaceutical composition containing a therapeutically effective amount of the crystal form and application of the crystal form in cancer treatment.

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 composition capable of improving oral bioavailability of drugs and a method thereof, and further discloses application of a delivery synergist in improving oral bioavailability of protein or polypeptide drugs. After the delivery synergist is added into the pharmaceutical composition provided by the invention, the delivery effect of a delivery agent can be exerted to the greatest extent under a certain proportion of the delivery synergist and the delivery agent, so that not only can the use amount of the delivery agent be reduced, but also the oral bioavailability of the medicine can be increased.

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.

Compounds based on biaryl amides and coumarins having modified sugar groups for use in the treatment of diseases associated with heat shock protein pathways are provided. The compounds have the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions of the compounds of Formulae (I), (II), (III), (IV) and (V). These biaryl amide and coumarin-based derivatives with modified sugar groups are useful for the treatment and prevention of diseases and disorders, including neurological disorders such as neurodegenerative diseases and neurological injury disorders, such as diabetic peripheral neuropathy. # imgabs0 #

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 application of the invention relates to an atorvastatin calcium derivative and a preparation method thereof, the developed novel atorvastatin derivative realizes multiple optimization through molecular design: fluorine atoms are introduced at para-positions of aromatic rings, and the metabolic stability is improved by utilizing high bond energy of C-F bonds and strong electronegativity of the fluorine atoms; a phosphate group is introduced, so that the oral bioavailability is improved by 30-40%. The synergistic effect of fluorine atoms and phosphate groups optimizes the combination with HMG-CoA reductase, and the combination energy is improved by about 15%. Through structural modification, the logP value is reduced from 5.7 to 4.5, and the water solubility is improved. The new derivative not only improves the enzyme inhibition activity by 20-30%, but also can bring additional treatment advantages through multi-target action, and provides a better treatment choice for patients with hyperlipidemia.

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 composition and a preparation process of a 20 (S)-protopanoxadiol (20 (S)-protopanoxadiol, 20 (S)-PPD) phospholipid / mesoporous silicon solid dispersion, and belongs to the technical field of medicines. The invention provides a 20 (S)-PPD phospholipid / mesoporous silicon solid dispersion preparation. The preparation consists of 20 (S)-PPD, phospholipid, ethanol, a crystal inhibitor and a dispersing agent. The preparation disclosed by the invention is prepared by adopting a solvent evaporation method; the prepared 20 (S)-PPD phospholipid / meso-porous silicon solid dispersion is good in stability; the drug loading capacity is high, and the content of 20 (S)-PPD in the preparation can reach 40% or above; and the absolute bioavailability of oral administration is high and can reach 23.95%. After the preparation is orally taken, the injury of podocyte for maintaining the integrity of a glomerular filtration barrier can be remarkably relieved, and adult chronic nephrotic syndromes such as membranous nephropathy (MN) can be treated.

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 invention discloses a valsartan solid self-microemulsion resin drug loading system and a preparation method and application thereof.The self-microemulsion is prepared through a solid carrier adsorption method, a solid carrier is ion exchange resin, and the drug loading system further comprises the following components for preparing the valsartan liquid self-microemulsion: valsartan, a liquid self-microemulsion oil phase, an emulsifier and a co-emulsifier; according to the invention, the macroporous ion exchange resin is adopted to cure the liquid self-microemulsion, and the solid carrier adsorption method is adopted to prepare the solid self-microemulsion, compared with other curing methods, the amount of the adsorbed liquid self-microemulsion can reach 70%, and the formed powder has good fluidity. And the liquid self-microemulsion is cured into spherical particles with uniform particle size and good morphology by a solid carrier adsorption method, so that the solubility of the medicine with poor water solubility is improved, quick release is realized, the oral bioavailability of the medicine is improved, and the problem of poor solubility of valsartan is solved.

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.