32results about How to "High drug loading" patented technology

The application discloses a sensitized ferroptosis lipid nano regulator and a preparation method and application thereof, and belongs to the technical field of new adjuvants and new dosage forms of drug preparation combined treatment. The lipid nano regulator is co-assembled by a GPX4 inhibitor and a FASN inhibitor through intermolecular forces, and is modified with an oxidation-reduction sensitive PEG modifier, a molar ratio of the GPX4 inhibitor and the FASN inhibitor is 10:1-1:10, a mass ratio of the sum of the GPX4 inhibitor and the FASN inhibitor to the PEG modifier is 10:90-90:10, and the intermolecular forces include pi-pi stacking force, hydrophobic force and hydrogen bond. The co-assembled nano preparation provides a new strategy and more choices for the development of drug delivery, and meets the urgent needs of high-efficiency and diverse ferroptosis treatment strategies in preparations in the clinic.

This invention discloses a Tibetan bath composition compound and its preparation method, relating to the field of daily chemical products technology. The Tibetan bath composition compound consists of a ternary complex of scutellaria baicalensis hydroxypropyl-β-cyclodextrin nanoshell powder, Bacillus subtilis, Tibetan medicine composition, starch, anhydrous citric acid, sodium bicarbonate, calcium citrate, crospovidone, and magnesium stearate. Bacillus subtilis is used to ferment the ternary complex of scutellaria baicalensis hydroxypropyl-β-cyclodextrin nanoshell powder to obtain a fermentation-modified porous carrier, which is then loaded with the Tibetan medicine composition to form a Tibetan medicine inclusion powder. This not only achieves efficient drug delivery through a triple mechanism of biomodification, metabolite synergy, and structural optimization, but also forms a quaternary system with Terminalia chebula. The effervescent effect also enhances the penetration of Tibetan medicine components, which is beneficial for better exerting the antibacterial and anti-inflammatory effects of active substances, and significantly improving fungal infections and eczema-related skin problems.

The utility model provides a spherical tablet, and belongs to the field of pharmaceutical preparations. The spherical tablet comprises an upper hemisphere, a lower hemisphere and a middle belt, and the middle belt is located in the middle of the spherical tablet and is in a belt shape with the same thickness. The upper hemisphere and the lower hemisphere are located on the two end faces of the middle belt, and the two hemispheres are the same in size and shape. The diameter of the middle zone is larger than the diameter of the hemisphere, the diameter of the hemisphere of an upper stamping die and the diameter of the hemisphere of a lower stamping die of a tablet pressing die adopted when the spherical tablet is pressed ranges from 6.5 mm to 10 mm, and the ratio of the arc depth to the diameter of the hemisphere is (0.2-0.4): 1. The spherical tablet is small in size, easy to swallow, high in drug loading capacity and less in taking quantity; and the tablet has the advantages of good compressibility, good hardness, strong shock resistance and wear resistance, small tablet weight difference, facilitation of later coating and other operations, and good uniformity and reproducibility.

The present invention relates to a bioactive conjugate, a preparation method therefor, and use thereof. In particular, the present invention relates to a novel type of bioactive molecular conjugates obtained by improving the coupling of a drug to a targeted moiety in ADC or SMDC, a preparation method therefor, and use thereof in the preparation of drugs for treating diseases associated with abnormal cellular activity.

The present application relates to the technical field of pesticides, and discloses a phase change eutectic carrier embedded with a photothermal agent as well as a preparation method and application thereof.The phase change eutectic carrier embedded with the photothermal agent mainly comprises a photothermal agent, a fatty acid, an organic solvent and water.The preparation process of the preparation is simple, the conditions are mild, a large number of additives are not needed, and the preparation can be quantitatively prepared.The dispersion and utilization rate of the bactericide can be improved through eutectic, and the effectiveness of the bactericide can be improved.The preparation is suitable for various application modes such as seed coating and soil treatment, can play various synergistic functions such as temperature response release, prolonging drug retention time, enhancing adhesion and permeability on the surface of pathogenic bacteria, and is a kind of green and efficient bactericide dosage form, which has a wide application prospect in green and intelligent agriculture.

The application discloses a solid dispersion of olaparib and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The solid dispersion of olaparib adopts polyvinyl alcohol or polyvinyl alcohol and a plasticizer or polyvinyl alcohol and copolymerized povidone or polyvinyl alcohol, copolymerized povidone and an anti-sticking agent as a matrix polymer carrier, can effectively protect the olaparib raw material, reduce the degradation, and improve the drug loading of the solid dispersion. The solid dispersion of olaparib has small hygroscopicity, reduces the requirement of the environment humidity during the storage of the intermediate product of the olaparib preparation, reduces the energy consumption during the preparation process, and significantly improves the stability and effectiveness of the preparation.

The invention discloses a CaCO3-based validamycin controlled release preparation and a preparation method thereof, and the preparation method comprises the following steps: taking glucose, amino acid and water as raw materials, reacting under a microwave heating condition, and standing to obtain carbon dots; wherein the amino acid is one or a mixture of more of lysine, histidine and arginine; the preparation method comprises the following steps: mixing validamycin, water and calcium acetate, stirring, adding carbon dots, and stirring to obtain a validamycin / carbon dot mixed solution; and adding a sodium carbonate aqueous solution into the validamycin / carbon dot mixed solution, stirring, standing, and drying the obtained precipitate to obtain the CaCO3-based validamycin controlled release preparation. The controlled release preparation has the characteristics of high drug loading rate, controllable drug release, simple preparation process and the like, and provides a new strategy for developing CaCO3-based nano pesticides.

This invention relates to the field of biomedical technology, specifically to nanoparticles for treating retinal ischemia-reperfusion injury, their preparation method, pharmaceutical composition, and uses. The nanoparticles consist of a zeolite imidazole ester-8 core encapsulating baicalin and a polydopamine shell coating its surface, prepared via in-situ self-polymerization. The nanoparticles utilize the polydopamine shell to scavenge reactive oxygen species and prolong intraocular residence time, while their core responsively degrades in a weakly acidic pathological microenvironment, precisely releasing baicalin, thereby synergistically exerting antioxidant, anti-inflammatory, and anti-apoptotic effects. Experiments show that these nanoparticles can effectively reduce oxidative damage and inflammation in the model retina, significantly inhibit ganglion cell apoptosis, and restore electroretinogram function, providing a novel multi-target therapeutic strategy for retinal ischemic diseases.

The invention discloses dipeptide and curcumin molecule co-assembled nanoparticles as well as a preparation method and application thereof, and relates to the technical field of biological medicines and nano materials. The nano-particles are prepared by taking cationic diphenylalanine, genipin GNP and curcumin as raw materials through co-assembly by a'one-pot method '. Under an alkaline condition, amino of CDP and active dialdehyde formed by ring opening of GNP are subjected to a Schiff base reaction, a covalent cross-linked rigid skeleton is constructed, curcumin is efficiently entrapped through a hydrophobic effect and a pi-pi accumulation effect, and the entrapment efficiency can reach 90%. The obtained nanoparticles are regularly spherical and uniform in particle size, have positive charges on the surface, and have excellent anti-acid stability, pH response release characteristics and remarkable anti-tumor activity. The preparation method disclosed by the invention is simple, mild in condition and high in biological safety, and the obtained nanoparticles have a wide application prospect in an oral hydrophobic antitumor drug delivery system.

The utility model discloses a medical dressing with medicine loading groove, medical dressing includes polyurethane film and antiseized layer, be equipped with a plurality of medicine loading groove on the polyurethane film, be equipped with hydrogel layer in the medicine loading groove, fill in the medicine of hydrogel layer, one side of the antiseized layer with polyurethane film is equipped with medicine loading groove and is close -fitted. The utility model discloses medical dressing is equipped with medicine loading groove on polyurethane film, fills hydrogel layer in medicine loading groove inner chamber, and the medicine is loaded in hydrogel, can promote the slow -release capacity of medical dressing. The medicine is distributed on the slow -release skeleton, and the slow -release skeleton is prepared through three -dimensional micro -nanometer printing, and the inner chamber is hollow, and the shape of slow -release skeleton is customized according to the shape of medicine loading groove, makes the quantity of slow -release skeleton in medicine loading groove maximization, forms medicine -skeleton load structure, can accommodate more medicine in medicine loading groove to good slow -release effect.

The present application relates to the technical field of nanomedicine, in particular to a β-cyclodextrin-carboxymethyl chitosan-deoxycholic acid nanoparticle carrying ginsenoside CK, a preparation method and application. A first esterification reaction is performed between a β-cyclodextrin solution and a carboxyl-activated carboxymethyl chitosan solution to obtain a β-cyclodextrin-carboxymethyl chitosan polymer; a second esterification or amidation reaction is performed by adding carboxyl-activated deoxycholic acid to the β-cyclodextrin-carboxymethyl chitosan polymer to obtain a β-cyclodextrin-carboxymethyl chitosan-deoxycholic acid polymer; an ethanol solution of ginsenoside CK is mixed with a water solution of the β-cyclodextrin-carboxymethyl chitosan-deoxycholic acid polymer to obtain a whole particle, and a freeze-drying protective agent is added for freeze-drying to obtain the β-cyclodextrin-carboxymethyl chitosan-deoxycholic acid nanoparticle carrying ginsenoside CK. The present application focuses on the design of an intelligent carrier, realizes the synergistic optimization of high drug loading and intelligent delivery, and overcomes the defects of the prior art.

The invention discloses a tulobuterol transdermal patch with a gradient drug release structure and a preparation method of the tulobuterol transdermal patch, belongs to the technical field of transdermal drug delivery systems, and aims at solving the problems that an existing single-layer tulobuterol patch takes effect slowly and is insufficient in later-stage drug release power. The transdermal patch sequentially comprises a backing layer, a gradient medicine-containing substrate layer and an anti-sticking release layer from top to bottom, the gradient drug-containing matrix layer comprises a high-concentration top long-acting drug release layer containing tulobuterol-mesoporous silica nanoparticles and a silicone adhesive, a middle-concentration middle stable drug release layer containing an SIS hot melt adhesive, and a low-concentration bottom quick-acting contact layer containing a specific penetration enhancer composition and an acrylate adhesive from top to bottom in sequence. Through the synergistic effect of bottom-layer penetration promoting driving, middle-layer stable transition and top-layer nanometer storage cavern relay, the traditional concentration barrier is broken through, and rapid effect taking within 1-2 hours and stable-state long-acting drug release within 24 hours or above are perfectly considered.

This invention belongs to the field of plant-derived pesticide technology, specifically relating to a method for preparing a juglone microemulsion and its insecticidal activity. The juglone microemulsion comprises juglone, an oil phase, an emulsifier, a co-emulsifier, and water, with the following mass percentage composition: juglone: ​​2.5–10%, oil phase: 5–25%, emulsifier: 5–15%, co-emulsifier: 5–35%, and the balance being water. The mass ratio of the emulsifier to the co-emulsifier is 1:0.5–1:3. The juglone microemulsion of this invention uses plant-derived juglone as the main active ingredient. The prepared juglone microemulsion is an O / W type microemulsion, a clear, stable brown liquid, which can be diluted and directly sprayed onto the leaves of crops to kill and repel insects.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to an indissolvable drug nano mixed micelle carrier system and a preparation method thereof. The carrier system has high drug loading capacity and high stability, and can avoid degradation of active ingredients caused by long-time placement; the targeting property is high, so that toxicity reduction and synergism are facilitated; meanwhile, the preparation method is simple, convenient and easy to operate, short in process time and high in stability, and continuous production of micelles can be realized.

This invention provides a pH / ROS dual-responsive nanomedicine carrier, the structure of which is cyclodextrin modified with cinnamaldehyde and 4-hydroxyphenylboronic acid pinacol ester. Lecithin, phospholipid-polyethylene glycol (DSPE-PEG), and phospholipid-polyethylene glycol-RGD peptide are used as the shell of the nanomedicine, and the core consists of glucocorticoids and the prepared pH / ROS dual-responsive drug carrier to form a nanoformulation. This invention designs a pH / ROS dual-responsive drug carrier based on the microenvironment of the disease site. Compared with single pH-responsive or single ROS-responsive drug carriers, this carrier has better microenvironment responsiveness and can more effectively degrade and release therapeutic molecules according to the microenvironment of the lesion site.

The invention belongs to the technical field of skin photoaging, and particularly relates to a preparation method of a frozen microneedle patch for preventing skin photoaging, and the preparation method comprises the following steps: S1, placing venous blood in a blood collection tube for centrifugation; s2, centrifuging, and then taking out platelet-rich fibrin gel on the middle layer; s3, injecting the platelet-rich fibrin gel into a microneedle mold, filling a needle cavity with the platelet-rich fibrin gel, and standing; s4, after the microneedle mold is precooled, freezing forming is conducted, demolding is conducted after forming, and the frozen microneedle patch is obtained.The fibrin rich in platelets is combined with the frozen microneedle technology, the action mechanism of the skin photoaging phenotype is improved, efficient loading and long-acting release of growth factors are achieved, and a new direction is provided for regenerative medicine of photoaging.

The invention relates to the technical field of medicines, in particular to a flurbiprofen organic silicon pressure-sensitive adhesive patch and a preparation process thereof. The patch is composed of a backing layer, a medicine storage layer and a protective layer, and the medicine storage layer takes an organic silicon pressure-sensitive adhesive as a matrix and comprises the following components in percentage by weight: 1-15% of flurbiprofen, 85-99% of the organic silicon pressure-sensitive adhesive and 0.5-5% of a composite penetration enhancer. The organic silicon pressure-sensitive adhesive is prepared from vinyl silicone oil, hydrogen-containing silicone oil, MQ silicon resin, a catalyst, an inhibitor and a solvent through hydrosilylation. The preparation method comprises the following steps: dissolving flurbiprofen in a composite penetration enhancer in advance, then mixing with an organic silicon pressure-sensitive adhesive system, coating and curing to prepare the patch. The patch disclosed by the invention has the advantages of high solubility of medicines in a matrix, uniform dispersion, controllable release behavior, moderate adhesion performance and good skin compatibility, can realize stable transdermal release of flurbiprofen, and is suitable for analgesic and anti-inflammatory external treatment.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a hippophae rhamnoides flavone solid dispersion and a preparation method thereof.The hippophae rhamnoides flavone solid dispersion comprises hippophae rhamnoides flavone and a carrier material, the mass ratio of the hippophae rhamnoides flavone to the hydrophilic carrier material is 1: 4-1: 7, and the carrier material is povidone. The solubility of the solid dispersion is remarkably improved, the dosage of auxiliary materials is relatively small, the preparation process is simple and controllable, and the technical bottleneck of low solubility of the seabuckthorn flavone is effectively solved.

The invention relates to the technical field of biological medicine manufacturing, and provides a water-soluble microcapsule and a preparation method thereof.The preparation method comprises the following steps that an emulsifying agent, a thickening agent and a water-soluble monomer are dissolved in water, and an emulsion continuous phase is obtained; the content of the emulsifier in the water is 0.5%-5%; the content of the thickening agent in the water is 0.5%-5%; the ratio of the water-soluble monomer to the water is (1: 100)-(20: 100); the water-soluble monomer is introduced to increase the viscosity of a water phase and participate in construction of a shell layer, so that diffusion of a core material to the water phase is effectively inhibited, and high encapsulation efficiency and high drug loading capacity are realized; the process parameters such as the emulsifying rotating speed and the monomer proportion are easy to adjust, microcapsules with the particle size ranging from 1 micrometer to 800 micrometers can be prepared in a controlled mode, the packaging requirements of different water-soluble active substances such as vitamins and enzyme preparations are met, and the product adaptability is good.

This invention discloses a solid dispersion, a pharmaceutical composition, a method for preparing the same, and its application. The solid dispersion of this invention comprises: (1) a compound of formula () or a pharmaceutically acceptable salt thereof; and (2) a polymer carrier, wherein the polymer carrier comprises one or more of copovidone, povidone, and hydroxypropyl methylcellulose; formula ().

The present invention relates to a bioactive conjugate, a preparation method therefor, and use thereof. In particular, the present invention relates to a novel type of bioactive molecular conjugates obtained by improving the coupling of a drug to a targeted moiety in ADC or SMDC, a preparation method therefor, and use thereof in the preparation of drugs for treating diseases associated with abnormal cellular activity.

The application discloses a kind of bionic microneedle, and provides its preparation method and application.The bionic microneedle of the application is based on protein and high molecular polysaccharide composite film microneedle, specifically, the shell of the bionic microneedle is prepared by the composite film formed by protein and high molecular polysaccharide, and the hollow cavity in the middle can be used to load functional active substance.The microneedle shell formed by the composite film of the protein and high molecular polysaccharide of the application can significantly improve the mechanical strength of polymer microneedle;The hollow cavity of microneedle can be used to load functional active substance, and the loading capacity of microneedle can be significantly improved, so as to effectively improve the conversion potential of microneedle.

The invention belongs to the technical field of biological medicines, and particularly relates to vitexin-probucol self-assembled nanoparticles as well as a preparation method and application thereof. The nanoparticle is formed by self-assembly of vitexin and probucol, and the mass ratio of vitexin to probucol is 2: (1-5). The nano particles are prepared by adopting a nano precipitation method, and the method specifically comprises the following steps: mixing vitexin and probucol, and dissolving and dispersing in a good solvent to obtain a mixed solution; and adding the obtained mixed solution into a poor solvent, and promoting the vitexin and probucol to be self-assembled to form the nanoparticles by utilizing a solvent replacement effect. The nanoparticles have the advantages of high drug loading capacity, synergistic anti-inflammation and anti-oxidation, long-acting circulation and the like, and can effectively treat atherosclerosis, reduce side effects and improve the treatment effect and safety.

The application discloses a doxorubicin-quadruple platinum drug-norcantharidin three-drug combination nano drug and a preparation method and application thereof, and belongs to the technical field of medical materials. 2+ The application constructs a novel nano drug through coordination of doxorubicin and a quadruple platinum drug modified by norcantharidin, and then polymerizes polydopamine with a mild photothermal effect to prepare a nano drug for the three-drug combination of doxorubicin, the quadruple platinum drug and norcantharidin. The nano drug has the ability of controlled release of drugs under acidity and reduction, can realize photothermal conversion to generate a mild photothermal effect under laser irradiation, has a better tumor cell killing effect, has the ability of consumption of glutathione and generation of hydroxyl radicals, can enter cancer cells through an endocytosis mode and release DOX, and provides a new idea for multi-drug combination, chemotherapy-chemical kinetics treatment-photothermal treatment multi-mode combined treatment.

This invention relates to the field of biomedical materials technology. It discloses a metal-organic hydrogel-mediated soluble microneedle patch, its preparation method, and its applications. The microneedle patch comprises a matrix and needles, wherein the matrix and needles contain a metal-organic hydrogel, polydimethylsiloxane, and a poorly soluble target drug. This application innovatively applies a metal-organic hydrogel to the preparation of a soluble microneedle patch, constructing an amphiphilic matrix with polydimethylsiloxane. This enables the preparation of soluble microneedle formulations containing uniformly distributed poorly soluble drugs, expanding the application scenarios for poorly soluble drugs and improving resource utilization. It has significant value in the formulation preparation of poorly soluble drugs.

This invention relates to the field of microneedle drug delivery technology, specifically to a soluble microneedle and its preparation method. The soluble microneedle includes a needle hub and at least one needle body located on the needle hub. The needle body includes a first intermediate segment, a second intermediate segment, and a needle tip. The first intermediate segment is located on the needle hub, and the second intermediate segment is located between the first intermediate segment and the needle tip. The density of the second intermediate segment is greater than that of the first intermediate segment. The needle tip contains a drug active ingredient. The soluble microneedle provided by this invention has the drug active ingredient concentrated in the needle tip. Furthermore, the second intermediate segment, which is in contact with the needle tip, is a high-density segment, which can prevent the drug active ingredient in the needle tip from diffusing into the second intermediate segment and the first intermediate segment. Therefore, the soluble microneedle of this invention can significantly increase the local drug delivery concentration, achieving precise, targeted, and quantitative drug delivery.

The invention discloses sinomenine hydrochloride solid lipid nanoparticles, gel, a preparation method and application, by exploring the preparation method of the sinomenine hydrochloride solid lipid nanoparticles HA-SH-SLNs, when the mass ratio of sinomenine hydrochloride to soya bean lecithin to hyaluronic acid modified targeting molecule DSPE-PEG-HA to poloxamer Pluronic F-68 is (0.3-0.7): (1-4): (0.0125-0.1): (1-4), the gel can be used for preparing the sinomenine hydrochloride solid lipid nanoparticles HA-SH-SLNs. The sinomenine hydrochloride solid lipid nanoparticles which are uniform in particle size, high in encapsulation efficiency, high in drug loading capacity and stable in quality are obtained, and the preparation method of the sinomenine hydrochloride solid lipid nanoparticle gel is further researched. The obtained sinomenine hydrochloride solid lipid nanoparticle gel HA-SH-SLNs-Gel is good in stability and small in hemolysis rate, the in-vivo residence time is longer than that of sinomenine hydrochloride solid lipid nanoparticles, the drug release period is delayed, and better articular cavity injection administration is facilitated.

A drug conjugate of an Eribulin derivative. Specifically, provided are an HER2 antibody conjugate that is formed by binding the Eribulin derivative to structural domain II of HER2, a preparation method therefor, and a pharmaceutical application thereof. The present invention further relates to a method for treating a cancer by means of administration of an antibody-drug conjugate, and a composition.

The application belongs to the technical field of pharmaceutical preparations, and particularly relates to a polypeptide nanocrystal stabilizer, a preparation method thereof and application thereof. The polypeptide nanocrystal stabilizer is connected by an active drug and an amphiphilic peptide segment through a degradable covalent bond. The active drug is a non-steroidal anti-inflammatory drug. The degradable covalent bond is one or more of an amide bond, an ester bond, a disulfide bond, a hydrazone bond or an imine bond. The amphiphilic peptide segment is one or more of a surface active peptide, an alternating hydrophilic and hydrophobic polypeptide and an aromatic short peptide. The polypeptide nanocrystal stabilizer provided by the application has both prodrug characteristics and interface stabilization functions, can significantly improve the drug loading capacity, colloidal stability and biocompatibility of nanocrystals, and has a simple, controllable, green and environmentally-friendly preparation method, and is suitable for the development of nanocrystal preparations of poorly soluble drugs.

This invention relates to a tofenamic acid liposome, its preparation method, and its application. The raw materials for preparing the tofenamic acid liposome include phospholipids, cholesterol, and tofenamic acid. The tofenamic acid is encapsulated in a lipid bilayer. The tofenamic acid liposome of this invention improves the solubility of tofenamic acid and has a high encapsulation efficiency and drug loading capacity.