16117 results about "BULK ACTIVE INGREDIENT" patented technology

The present invention covers spirocyclic compounds of general formula (I), in which R1, R2, X, Y, and Z are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant KRAS signaling, as a sole agent or in combination with other active ingredients.

The present invention covers imidazo pyrimidine compounds of general formula (I), in which R1, R2, R3, R4 and Z are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant KRAS signaling, as a sole agent or in combination with other active ingredients.

Provided is a medicine for treating or preventing cancer that contains a first active ingredient and that is used in combination with a second active ingredient, wherein: the first active ingredient is a compound represented by formula (1), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof; and the second active ingredient is GDC-6036 or a pharmaceutically acceptable salt thereof.

The invention relates to the technical field of drying process control, in particular to a medicinal material drying process control method and system for traditional Chinese medicinal material processing, and the method comprises the following steps: calling a temperature set value, a humidity discharge rate and heating power based on the operation condition of a drying chamber, and analyzing the difference value between the medicinal material moisture content and the target moisture content; combining the medicinal material density with the water content change rate, matching the coupling relationship between the humidity discharge rate and the heating power, and establishing an initial drying process control value; according to the method, through collaborative analysis of the temperature set value, the humidity discharge rate and the heating power, accurate matching of initial drying conditions and material characteristics is achieved, excessive drying is avoided, linkage of the air speed and the humidity discharge rate is optimized, humidity distribution uniformity and environmental stability are improved, the evaporation rate is dynamically matched, and the drying efficiency is improved. Drying uniformity and quality stability are improved, termination control parameters are optimized in real time, drying time is shortened, energy consumption is reduced, and active ingredients and physical characteristics of medicinal materials are reserved to the maximum extent.

The invention discloses a pharmaceutical composition containing melogabalin besylate and a preparation method of the pharmaceutical composition. Belongs to the technical field of pharmaceutical preparations. Comprising melogabalin besylate and pharmaceutically acceptable auxiliary materials, the pharmaceutically acceptable auxiliary materials comprise a filler, a disintegrating agent, an adhesive, an antioxidant and a lubricant, the antioxidant comprises vitamin E succinic acid polyethylene glycol ester, and the lubricant comprises vitamin E succinic acid polyethylene glycol ester. The melogabalin besylate as the active ingredient accounts for 2-15% by weight of the pharmaceutical composition, preferably 2-10% by weight of the pharmaceutical composition. According to the pharmaceutical composition, antioxidant particles are prepared by adopting a fluidized bed granulation process, raw material medicines, the antioxidant particles and other auxiliary materials are mixed, tableted and coated, an antioxidant comprises vitamin E succinic acid polyethylene glycol ester and tartaric acid, and the prepared tablet has good stability.

Provided is a compound useful as an active ingredient in a pharmaceutical composition for treating cancer.　The present inventors have examined a compound useful as an active ingredient in a pharmaceutical composition for cancer treatment, and have completed the present invention by finding that: a heterocyclic compound represented by formula (I) and formula (I-I) has excellent an action of inducing degradation of a mutant KRAS protein and a wild-type KRAS protein, and in particular, an action of inducing degradation of a KRAS protein having a G12C mutation, G12D mutation, G12V mutation, or G13D mutation; and said heterocyclic compound has mutant KRAS inhibition and the inhibitory activity of KRAS amplified by a wild-type KRAS gene, and in particular, inhibitory activity of KRAS having a G12C mutation, G12D mutation, G12V mutation, or G13D mutation. The heterocyclic compound according to the present invention or a salt thereof can be used as a therapeutic agent for cancer.

The invention relates to an optimized method for medicament preparation. A machine learning model of a deep neural network is adopted to perform screening and combinatorial optimization on active ingredients and auxiliary materials of the medicament, and a relation model among the ingredients, the drug effect and the stability is established; a dynamic blending module is adopted to adjust the component proportion and dosage in real time according to different medicament preparation conditions including temperature and pH value; constructing a self-adaptive reaction condition adjusting system, and monitoring reaction conditions including temperature, pressure, pH value and stirring speed in the preparation process in real time; a dynamic mixing system is introduced, and a microfluidic technology is adopted to control metering and mixing of pharmaceutical components; a medicament preparation process is decomposed into a plurality of key steps including primary reaction, purification and concentration, and each step is independently optimized; a real-time quality monitoring system is constructed, and the physical properties, including particle size distribution, solubility and purity, of the medicament are monitored in real time through a sensor and imaging equipment; and optimizing the integration platform in the whole process.

Disclosed is a pharmaceutically-acceptable composition in the form of a solid, amorphous, mono-particulate powder comprising a mixture of:a pharmacologically-effective dosage amount of an adrenergic receptor modulator, or a pharmaceutically-acceptable salt thereof; anda pharmaceutically-acceptable carrier material, which carrier material comprises a maltodextrin with a dextrose equivalent (DE) that is above 15.Compositions are suitable for transmucosal drug delivery, including nasal delivery, by which said compositions may be loaded into a single-use nasal applicator. Compositions are preferably made by way of spray drying and may further include a disaccharide, such as lactose or trehalose which, along with the active ingredient and maltodextrin, may be spray-dried together in combination. Compositions may further comprise one or more alkyl saccharides. Preferred alkyl saccharides include sucrose esters, such as sucrose monolaurate. Preferred adrenergic receptor modulators include epinephrine (adrenaline). The compositions are thus particularly useful in the treatment of allergic reactions, including anaphylaxis.

The present invention provides a pharmaceutical composition for treating IL-6-related diseases containing an IL-6 inhibitor as an active ingredient, wherein the pharmaceutical composition is routinely administered after a short-interval dosing period where the same dose as the routine dose is administered at a shorter interval than the routine dosing interval.

The invention discloses a traditional Chinese medicinal material quality evaluation method and system based on big data analysis, and relates to the field of traditional Chinese medicinal material detection, and the main scheme is as follows: obtaining soil parameter data of different medicinal material planting areas, and analyzing to obtain a soil fertility index and a planting suitability index; obtaining effective component contents of the traditional Chinese medicinal materials, and calculating effective component predicted values of the traditional Chinese medicinal materials; calculating a machining process stability index by analyzing the machining process parameters; calculating a mildew evaluation index according to the environmental mildew data and the medicinal material mildew data in the storage environment; a quality evaluation comprehensive index is obtained through comprehensive analysis; comparing the quality evaluation comprehensive index with a quality evaluation comprehensive index threshold value, judging whether the comprehensive quality evaluation of the traditional Chinese medicinal materials is qualified or not, and if the comprehensive quality evaluation is not qualified, judging a link causing a quality problem; the problems that a traditional Chinese medicinal material quality evaluation method in the prior art focuses on a single component and only focuses on the quality of traditional Chinese medicinal materials in a certain specific link are solved.

The present invention relates to a novel association or combination of active ingredients useful in the prevention and repair of neuronal damage, both centrally and peripherally. In greater detail, the present invention relates to an association or combination of i) an extract of Gastrodia elata and ii) at least one ingredient selected from the group comprising or, alternatively, consisting of citicoline, L-acetylcarnitine and, preferably, at least one vitamin of group D, and / or mixtures thereof, and / or at least one vitamin of group B, and / or mixtures thereof. Furthermore, the invention also relates to the pharmaceutical compositions and / or compositions for medical devices (Regulation (EU) 2017 / 745) and / or nutraceutical and / or food compositions comprising that association and to their use in therapy, in particular in the protection of the functionality of the nervous system and in the prevention and / or treatment of central and peripheral neuropathies.

The invention relates to the technical field of animal feed preparation, in particular to a functional feed additive for ruminants and a preparation method of the functional feed additive for the ruminants, and the functional feed additive for the ruminants is characterized by consisting of the following components in percentage by mass: probiotics which are saccharomycetes, bacillus subtilis and enterococcus faecalis; an enzyme preparation, xylanase and protease; prebiotics are added; a microcapsule coating material; a binder; the balance is a carrier; the probiotics and the enzyme preparation are wrapped in the chitosan / sodium alginate composite film through a microcapsule coating technology, adverse factors such as temperature, humidity and illumination in the production, transportation and storage process can be effectively isolated, meanwhile, in the rumen low-pH, strong-protease and complex-microorganism environment, the coating layer can slowly release and protect active ingredients, and the effect of preventing and treating the probiotics and the enzyme preparation is achieved. Effective content and activity during final feeding are ensured, consistent growth promotion can be kept in different varieties, weights and feeding stages, and production benefits and feeding stability are improved.

The invention relates to a preparation method of a chlorella exosome as well as a product and application of the chlorella exosome, the preparation method comprises the following steps: (1) mixing extremely micro chlorella with a separation buffer solution, and then carrying out wall breaking treatment to obtain a cell breaking solution; (2) centrifuging the cell disruption liquid, and reserving supernate; and (3) filtering the supernate to obtain the chlorella exosome. The preparation method of the chlorella exosome, provided by the invention, is simple in steps and easy to operate, the chlorella raw material and the specific separation buffer solution are subjected to wall breaking treatment, so that active ingredients in the prepared chlorella can be better extracted, the content of protein and polysaccharide in the obtained exosome is higher, and the purity of the exosome is improved. Meanwhile, gradient centrifugation, filter membrane filtration and the like are assisted in the preparation process, so that the prepared exosome is high in purity and less in impurities.

The invention provides a preparation method of lipidosome containing hair-growing active ingredients, and belongs to the technical field of hair-growing products. According to the invention, active substances are utilized to regulate hormone level, improve scalp blood circulation, stimulate anti-hair loss factors and promote hair growth in multiple directions, and lipidosome formed by lecithin and oil-soluble active ingredients as raw materials is utilized to integrally entrap the active substances, so that the anti-hair loss effect is improved. The defect of weak transdermal ability caused by large water solubility difference among the active substances is overcome, the stability and bioavailability of the active substances can be improved, and the hair growth and development effects of the prepared lipidosome containing the hair growth active components are remarkably improved.

The present invention belongs to the technical field of cosmetic raw materials, and specifically relates to a kind of oxidized hyaluronic acid-PDRN-peptide nanoemulsion and its preparation method. The nanoemulsion comprises oxidized hyaluronic acid, PDRN and polypeptide, and the nanoemulsion is formed by oxidized hyaluronic acid, PDRN and polypeptide through layer-by-layer self-assembly technology. Specifically: positively charged polypeptide is used to wrap negatively charged PDRN to form positively charged composite particles, or negatively charged PDRN is used to wrap positively charged polypeptide to form electrostatic composite particles, and then, the positively charged composite particles or the electrostatic composite particles are further wrapped with oxidized hyaluronic acid as a packaging material, and finally oxidized hyaluronic acid-PDRN-peptide nanoemulsion is formed. The nanoemulsion of the present invention can improve the stability of polypeptides, improve the problems that polypeptide molecules are difficult to penetrate the skin and have low bioavailability, and effectively improve the transdermal rate and stability of PDRN, give play to the tissue repair function of PDRN, further amplify the anti-inflammatory effects of the two, and improve the bioavailability of active ingredients.

The invention discloses a probiotic with the depression improving effect and a microecological preparation and application thereof, and is characterized in that the probiotic comprises lactobacillus mucus PC17 with the preservation number of CGMCC No.33866, the active ingredients of the lactobacillus microecological preparation comprise thalli of the lactobacillus mucus PC17, and a preparation method of the microecological preparation comprises the following steps: adding the lactobacillus mucus PC17 into the lactobacillus mucus PC17, uniformly mixing the lactobacillus mucus PC17, the lactobacillus mucus PC17, the lactobacillus mucus PC17, the lactobacillus mucus PC17, the lactobacillus mucus PC17, the lactobacillus mucus PC17 and the lactobacillus mucus PC17 The lactic acid bacteria are inoculated into a fermentation culture medium according to a volume ratio of 1-5% to prepare the lactic acid bacteria microecological preparation, can be used for preparing antidepressant drugs, and has the advantages of being capable of promoting RIN14B cells to secrete 5-hydroxytryptamine and 5-hydroxytryptophan, reducing the levels of interleukin-1beta, interleukin-6, tumor necrosis factor-alpha, corticosterone and corticotropin in serum, and improving the antidepressant activity of the antidepressant drugs. The levels of aminobutyric acid and brain-derived neurotrophic factors in serum are improved, and the depression-like behaviors of CUMS depression model mice are obviously improved.

The invention relates to an application of a stable silicic acid aqueous solution in preparation of a product for treating acne, and the mass concentration of the stable silicic acid aqueous solution is 0.5-2%. The product taking the stable silicic acid aqueous solution as an active ingredient can be used for treating acne or preventing and / or treating sebaceous gland homeostasis imbalance, can fade the color of sebaceous gland spots at the mass concentration of 0.5-2%, and has an anti-acne effect, and meanwhile, the stable silicic acid aqueous solution is low in raw material cost, environment-friendly, safe and suitable for industrial production. The tretinoin can be used as a traditional tretinoin substitute medicine with a good curative effect.

The present invention relates to a solution for assessing alterations in biological tissue in a non-invasive manner based on computer-implemented analysis of hyper and / or multispectral images of the biological tissue of interest. Alterations can be related to stresses, aging, pests, diseases, changes related to concentration of an active ingredient, and / or resistances against active ingredient, or the like as well as combination thereof. In a particular embodiment such alterations can be assigned to an alteration type and / or the degree of alteration can be quantified over time.

The invention belongs to the technical field of biological medicines, and particularly discloses an epidermal growth factor-linker polypeptide-collagen, and the linker polypeptide has an amino acid sequence as shown in SEQ ID No.1. The linker polypeptide capable of connecting the EGF and the collagen is designed and synthesized, the N end of the linker polypeptide simulates an EGF receptor structure and can be combined with the EGF, and the linker polypeptide is connected with the EGF through non-covalent Van der Waals force, so that the structure of the EGF cannot be damaged; the C terminal of the linker polypeptide is rich in lysine residues, and can be covalently crosslinked to collagen through glutamine transaminase to form EGF-linker polypeptide-collagen. The protein solution taking EGF-linker polypeptide-collagen as active ingredients is low in cytotoxicity and high in biological safety, and meanwhile, the action time of the epidermal growth factor can be remarkably prolonged. In addition, a stable repairing microenvironment can be formed on the surface of the endometrium, and the endometrium injury repairing effect is remarkably improved.

The invention provides a nano transdermal delivery system based on superoxide dismutase, the nano transdermal delivery system is of a capsule composite structure of a small molecule active component-superoxide dismutase-polymer shell layer, the small molecule active component is loaded in superoxide dismutase, the surface of the superoxide dismutase is coated by the polymer shell layer, and the superoxide dismutase is loaded in the capsule composite structure. The diameter of the superoxide dismutase-based active ingredient transdermal delivery system is 20-100 nm, and the thickness of the polymer shell layer is 7.5-52.5 nm. In the delivery system, the polymer shell layer provides a protection effect for the superoxide dismutase and the micromolecular functional substances with the anti-oxidation effect, the capsule composite structure is in a nanogel form, and the nanogel not only promotes the penetration depth of the capsule, but also reduces the irritation effect of the capsule on the skin. The raw materials are biologically friendly, the preparation method is simple, the yield is high, and industrial large-scale production can be realized.

The invention discloses a cosmetic composition and a preparation method thereof, and belongs to the technical field of cosmetics. The invention discloses a chamomile essential oil toner which is mainly prepared from the following raw material components in parts by mass: 10 to 20 parts of modified toner, 50 to 60 parts of water, 4 to 6 parts of glycerol, 2 to 4 parts of propylene glycol, 0.8 to 1.2 parts of sodium chloride, 6.5625 to 7.875 parts of chamomile essential oil polymer micelle, 2.1875 to 2.625 parts of adhesive, 10.5 to 11.5 parts of capric triglyceride and 0.8 to 1.2 parts of cetyl polyethylene glycol. Through the synergistic effect of the modified toner and chamomile essential oil polymer micelles in a specific ratio, the dispersion stability of the toner is improved, meanwhile, the slow release effect of active ingredients is enhanced, and the chamomile essential oil toner has the advantages that the makeup holding property, the storage stability and the mildness are improved, meanwhile, the toner dispersity is improved, and the sensitive skin stimulation risk is reduced.

The invention provides a traditional Chinese medicine composition and an application thereof in preparing a product for preventing, alleviating or treating acute hepatopancreatic necrosis of shrimp, belonging to the field of veterinary medicine. The active ingredients of the traditional Chinese medicine composition include isatis root, artificial bezoar, liquorice, borneol, pig gall powder and xuanming powder. The traditional Chinese medicine composition has a good therapeutic effect on preventing, alleviating or treating acute hepatopancreatic necrosis of shrimp, with a cure rate of more than 70%, has antibacterial and liver-protecting effects, can effectively improve the degree of liver damage, improve the survival rate of shrimp and reduce losses.

The invention relates to the technical field of health care products, and discloses kidney function health wine based on traditional Chinese medicine fermentation and a preparation method of the kidney function health wine. 6-10 parts of cistanche deserticola; 9-30 parts of radix astragali and 6-12 parts of fructus lycii; the fermentation strain comprises lactobacillus acidophilus, lactobacillus plantarum, bifidobacterium longum subsp. Longum, saccharomyces cerevisiae and bacillus subtilis, and the fermentation strain comprises the following strains: lactobacillus acidophilus JYLC-374, lactobacillus plantarum JYLC-482, bifidobacterium longum subsp. Longum JYBB-163, saccharomyces cerevisiae JYSC-710 and bacillus subtilis JYBS-312. By adopting the technical scheme that a traditional Chinese medicine compound formula is combined with specific probiotic fermentation, the technical effects of enhancing the bioavailability of active ingredients and promoting kidney function regulation are achieved, and the dissolution rate and the biotransformation rate of herbal medicine active substances are improved.

The present invention provides methods, compositions (e.g., eyedrop or spongarion composition), and uses for alleviating and preventing age-associated vitreous degeneration in a mammal, comprising administrating to the mammal in need thereof a therapeutically effective amount of L-ergothioneine, an analog or derivative thereof, or a pharmaceutically acceptable salt, acid, ester, polymer, analog or derivative thereof, as an active ingredient. In particular, L-ergothioneine is capable of scavenging chronic reactive oxygen species directly and radically to mitigate and prevent HA depolymerization and HA decreasing-viscosity in the mammal's vitreous body; and / or improving vitreous liquefaction in the mammal.

The invention discloses a vitamin K2 composite micro-capsule system with stomach protection and intestine slow release functions and a preparation method and application thereof, the vitamin K2 composite micro-capsule system with stomach protection and intestine slow release functions comprises three layers, namely a core layer, a middle layer and an outer layer from inside to outside in sequence; the core layer is formed by coating vitamin K2 with a zein-lac hydrophobic core, the middle layer is a pea protein-pectin electrostatic compound, and the outer layer is sodium alginate and chitosan double-network gel. The micro-capsule system provided by the invention can be tightly combined in a gastric acid environment after being orally taken, the release of active ingredients in the stomach is reduced, and then the micro-capsule system stays at intestinal mucosa for a long time and slowly releases contents, so that the functions of the micro-capsule system are slowly presented outside, the half-life period is prolonged, and the action effect is improved. Vitamin K2 directly or indirectly participates in and regulates various physiological processes related to health, and plays an important role in the aspects of maintaining bone health, preventing cardiovascular diseases, protecting nerves, improving metabolism and the like.

The preparation method comprises the following steps: mixing saccharomycetes, lactic acid bacteria and bacillus subtilis according to a ratio of 1: 1: 1 to obtain mixed bacteria; 0.25 g of mixed bacteria is taken and dissolved in 5 mL of sterile water for standby application; slicing and crushing the dried rhizoma polygonati, and sieving with a 10-mesh sieve to obtain rhizoma polygonati powder; the preparation method comprises the following steps: mixing water and rhizoma polygonati powder according to a liquid-material ratio of 10mL: 1g, sterilizing at 121 DEG C for 30min, cooling, adding mixed bacteria according to an inoculum size of 3% of the mass of rhizoma polygonati, culturing in a constant-temperature shaking table incubator at 120r. Min <-1 > for 72h at the culture temperature of 035 DEG C, sterilizing at 100 DEG C for 30min after fermentation, cooling and centrifuging to obtain rhizoma polygonati fermentation liquor, and storing at 4 DEG C. The prepared polygonatum sibiricum fermentation liquor is high in active ingredient content, has good cell safety, anti-oxidation, anti-inflammatory and whitening effects, and has the potential of being used for developing functional raw materials of traditional Chinese medicine cosmetics.

The invention discloses a centella asiatica plant extraction repairing agent and application thereof in cosmetics. The centella asiatica plant extraction repairing agent comprises the following components: an olive leaf extract, a centella asiatica root extract and an oat kernel extract. According to the preparation process of the centella asiatica plant extraction repairing agent, plant water-soluble active ingredients are obtained by adopting enzymolysis and alcohol extraction modes, plant oil-soluble active ingredients are obtained by adopting critical CO2 extraction, and then a novel preparation is prepared by adopting an ultrasonic emulsification technology, so that the repairing agent can permeate into skin cuticles more easily, the effect of active matters can be brought into full play, and the repairing agent has a good application prospect. When the composition is applied to cosmetics, a good repairing effect can be realized.

The invention discloses a method for simultaneously detecting ergothioneine, ergosterol, ergosterol peroxide and lentinine in lentinus edodes, and belongs to the technical field of measurement of active ingredients of the lentinus edodes. The method comprises the following steps: detecting a shiitake mushroom extracting solution by adopting an ultra-high performance liquid chromatography-tandem mass spectrometry mode, wherein a chromatographic column is an HILIC or C18 chromatographic column; the mobile phase A and the mobile phase B are an aqueous solution containing formic acid and a methanol or acetonitrile solution containing formic acid respectively; the mass spectrum conditions comprise an electrospray ionization source; a positive ion multiple reaction monitoring mode; the ion spraying temperature is 315-325 DEG C; the temperature of the ion transmission tube is 320-330 DEG C; and the ion spraying voltage is 3500 V to 3700 V. The method has the characteristics of high sensitivity, high selectivity and high accuracy, and is suitable for quantitative detection of ergothioneine, lentinine, ergosterol peroxide and ergosterol compounds in shiitake mushrooms.

The present invention relates to novel (3,3-dimethyl-2-oxo-butoxy)phenyl derivatives and (2- aryl-2-oxo-ethoxy]phenyl derivatives and to their application in a process for the preparation of (3,3,3-trifluoro-2-oxo-propoxy)phenyl derivatives and their further transformation into [(2- trifluoromethyl-1,3-dioxolan-2-yl)methoxy]phenyl derivatives and (2-ethoxy-3,3,3-trifluoro- prop-1-enoxy)phenyl derivatives suitable for use, e.g., as active ingredients, which have microbiocidal activity, in particular, fungicidal activity.

The invention provides an intelligent response type medical liquid application and a preparation method thereof, and relates to the technical field of medical dressings. The liquid application is composed of a basic repairing component, a natural antibacterial component, a plant active component, an intelligent carrier system and auxiliary materials. Accurate release of active ingredients is realized by adopting a pH / temperature double-response intelligent delivery system, and the transdermal absorption rate is remarkably improved; wound healing is accelerated through the synergistic effect of the compound protein and the plant extract; active ingredients are effectively reserved through a multi-mode sterilization process. The liquid application disclosed by the invention has the characteristics of strong antibacterial property, good environmental adaptability, excellent healing effect and the like.