515 results about "Drug loading dose" patented technology

Disclosed is an oral apparatus for injection administration in the digestive tract, comprising a housing, a trigger assembly, and an administration assembly. The housing comprises a top cover at the upper part thereof, a middle housing placed in the middle, and a base located at the bottom. The material density of the middle housing is less than the material density of the base, so that the apparatus is in the shape of a roly-poly toy. The trigger assembly comprises a soluble fixing member, an elastic member, and a transmission member. The administration assembly comprises a microneedle and a drug. The apparatus provided by the present invention, by means of an arranged liquid storage bag, greatly increases the drug loading capacity and can theoretically achieve a drug loading capacity of 50 mg, which is a significant improvement over the prior art.

The invention provides a preparation method and application of magnesium L-threonate, and belongs to the technical field of medicines. The preparation method comprises the following steps: dissolving L-ascorbic acid in water, adding magnesium hydroxide and alkaline magnesium carbonate, stirring, dropwise adding hydrogen peroxide, heating, stirring and reacting, filtering a product, purifying and concentrating by temperature-sensitive molecularly imprinted hydrogel while the product is hot, adding an ethanol water solution into a concentrated solution, standing, crystallizing, filtering, washing and drying to obtain the magnesium L-threonate. And cooling the temperature-sensitive molecularly imprinted hydrogel after adsorption to room temperature, washing and repeatedly using the temperature-sensitive molecularly imprinted hydrogel. The magnesium L-threonate is simple in preparation method, high in purity and high in yield, meanwhile, the slow-release magnesium L-threonate is prepared, and the magnesium L-threonate is low in toxicity, good in biocompatibility, large in drug loading capacity, low in economic cost and good in drug effect and has wide application prospects in preparation of anti-depression drugs.

The invention discloses a nano-film for relieving bone fracture pain and a preparation method thereof, and relates to the technical field of medical films, the nano-film comprises an inner layer, a middle layer and an outer layer, the three layers are prepared by mixing traditional Chinese medicine extracts and base materials, the nano-film is prepared through an electrostatic spinning technology, the components of all the layers are the same, but the proportions are different, and the inner layer and the middle layer are different. Wherein a polycaprolactone and polyvinyl alcohol blending system is selected as the base material; the inner layer has high drug-loading capacity to quickly relieve symptoms, the middle layer has continuous release, the outer layer has low drug-loading capacity to reduce initial stimulation and increase stability, the use frequency is reduced, the drug effect is prolonged, and adverse reactions are reduced; the functions of protection, slow release and quick release are realized only by adjusting the proportion of PCL / PVA, and the production process is simplified.

The invention provides a sustained-release microneedle for treating ill-conditioned pregnancy and a preparation method and application thereof, and relates to the technical field of biological medicines.The sustained-release microneedle for treating ill-conditioned pregnancy comprises a base and a needle tip on the base, the needle tip part of the gel microneedle is made of heparin medicine, and the needle tip part of the gel microneedle is made of gelatin. The heparin medicine comprises heparin, heparin sodium, low-molecular heparin, low-molecular heparin sodium or low-molecular heparin calcium; the needle point part comprises a heparin photo-crosslinking monomer, and the base comprises a biocompatible polymer matrix. The sustained-release microneedle for treating pathological pregnancy provided by the embodiment of the invention has good mechanical strength, skin permeability and anticoagulant activity, can reduce skin bruises caused by subcutaneous injection of heparin, improves abortion caused by infection and inflammation and abortion caused by APS (anti-phospholipid antibody syndrome), can realize sustained release of drugs and increase of drug loading capacity, and has good application prospects. Sustainable drug delivery is achieved, and frequent injection is avoided.

The invention discloses a high-utilization-rate ginseng active ingredient medicinal preparation and a preparation method thereof, and relates to the technical field of medicines. The high-utilization-rate ginseng active ingredient pharmaceutical preparation is prepared from chitosan coated drug-loaded porous silicon dioxide composite nanoparticles and a drug-loaded MIL-101 metal organic framework matrix material, chitosan-coated drug-loading porous silicon dioxide composite nanoparticles are loaded on the surface of a drug-loading MIL-101 metal organic framework base material, and sodium alginate and a chitosan gel material are subjected to cross-linking connection, so that independent coating is formed, the framework base material and the composite nanoparticles are connected into a whole, the encapsulation performance and the drug loading capacity are improved, and the drug-loading capacity of the drug-loading MIL-101 metal organic framework composite nanoparticles is improved. Furthermore, the loading and the loading stability of the ginsenoside are improved, the adverse effects of gastric juice and gastrointestinal peristalsis on the activity of the ginsenoside are effectively reduced, the release and the absorption of the ginsenoside in intestinal tracts are remarkably enhanced, and the bioavailability is relatively high.

The invention discloses an antibiotic slow-release system based on hierarchical porous silicon dioxide and a preparation method of the antibiotic slow-release system, and belongs to the technical field of biological medicines. The antibiotic slow-release system comprises a spherical hierarchical-pore silicon dioxide microsphere carrier, amino functional groups covalently bonded to the outer surface and the inner surface of a pore channel of the spherical hierarchical-pore silicon dioxide microsphere carrier, antibiotic molecules loaded in the pore channel of the spherical hierarchical-pore silicon dioxide microsphere carrier, and a pH-responsive chitosan gating layer. The preparation method comprises the following steps: (1) preparing a hierarchical pore silicon dioxide microsphere carrier; (2) aminating the surface of the carrier; (3) loading antibiotics; and (4) constructing the pH responsive chitosan gating layer. According to the invention, the silicon dioxide carrier with a macroporous-mesoporous hierarchical structure is constructed to realize high drug loading capacity, and the pH-responsive chitosan gating layer is covalently bonded at the orifice of the silicon dioxide carrier to realize intelligent controlled release, so that the problem that high drug loading capacity, low burst release rate and biological safety are difficult to achieve at the same time in the prior art is solved.

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses a cyclophosphamide ternary nano-micelle and a preparation method thereof.The cyclophosphamide ternary nano-micelle prepared through the method can be used for treating malignant lymphoma, multiple myeloma, leukemia, breast cancer, ovarian cancer, cervical cancer, prostatic cancer, colon cancer, bronchial cancer, lung cancer and the like. Reasonable preparation steps and a preparation formula are adopted, the use of an organic reagent is reduced, the irritation of cyclophosphamide is reduced and the stability of the micelle is improved by adjusting a freeze-drying technology, and the cyclophosphamide micelle adopts amphiphilic macromolecules as a carrier material, so that the drug loading capacity and the stability of the micelle are obviously improved, and the bioavailability of the micelle is improved. The ternary nano-micelle system has the advantages that the solubility of cyclophosphamide is improved, the in-vivo bioavailability is increased, the preparation method is simple, the micelle performance is stable, and large-scale industrial production is facilitated.

The invention relates to the technical field of pharmaceutical preparations, in particular to a docetaxel oral self-microemulsion composition and a preparation process thereof. The docetaxel oral self-microemulsion composition is prepared from docetaxel, an oil phase, a surfactant, a cosurfactant, a stabilizer and an antioxidant, the oil phase is caprylic / capric acid mono / diglyceride, medium chain triglyceride, caprylic acid propylene glycol ester or lauric acid propylene glycol ester. The docetaxel oral self-microemulsion composition provided by the invention has relatively high drug loading capacity, good physical and chemical stability and relatively high bioavailability, and is more suitable for clinical medication.

The invention provides a platelet membrane bionic nano-drug delivery system as well as a preparation method and application thereof, and relates to the technical field of medicines. According to the invention, through membrane engineering modification, a wrapping material obtained through hybridization of a platelet membrane and an NK cell exosome is used for loading ginsenoside Rg3 for the first time, a ginsenoside Rg3 delivery system with high encapsulation efficiency and high drug loading capacity is obtained, and the system has excellent stability and can be stored for a long time in normal-temperature and high-temperature environments; the ginsenoside Rg3-loaded platelet membrane bionic nano-drug delivery system is simple in preparation method and suitable for wide popularization and application; according to the ginsenoside Rg3-loaded platelet membrane bionic nano-drug delivery system, the lung cancer treatment effect of ginsenoside Rg3 can be effectively improved, a novel drug is provided for lung cancer treatment, and the drug is high in safety, high in biocompatibility, free of adverse reaction in the treatment process and obvious in anti-inflammatory effect.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to an oral instant film with high drug loading capacity. The oral instant film agent comprises the following components: an active component, a film-forming material, a plasticizer, a coloring agent and a flavoring agent. The film-forming material is preferably combined with hydroxypropyl methylcellulose E15 and xanthan gum, so that the high drug loading capacity of the oral cavity instant film agent is ensured. Film-forming materials including hydroxypropyl methylcellulose E15 and xanthan gum are combined and compounded with a plasticizer polyethylene glycol 400, and sucralose is adopted as a flavoring agent, so that the stability of the oral instant film agent is ensured. The oral cavity instant film is good in appearance property, moderate in flexibility, good in taste, high in drug loading capacity, good in stability, low in cost, easy to operate, free of heating and suitable for industrial production.

The invention provides a semeglutide long-acting sustained release microsphere and a preparation method of the semeglutide long-acting sustained release microsphere. According to the method, the semeglutide long-acting sustained-release microspheres are prepared based on a water-in-oil-in-oil (W / O / O) phase separation method. According to the method, the problems of low drug loading capacity and high burst release of a water-in-oil-in-water (W1 / O / W2 type) multiple emulsion method are solved; meanwhile, the particle size of the long-acting and sustained-release microspheres of the semeglutide is between 10 microns and 300 microns, the particle size distribution Span value is between 0.5 and 1.5, and compared with a control drug, the long-acting and sustained-release microspheres of the semeglutide have no burst release effect and no drug release lagging stage after being administrated, have the same onset time as the control drug in an animal body, can be slowly released for one month and have a remarkable blood glucose reducing effect.

The invention provides donepezil sustained-release microspheres and a preparation method, a pharmaceutical preparation and application thereof. The preparation method comprises the following steps: forming a water phase (containing a surfactant, an osmotic pressure regulator and water, and regulating the pH value with a pH regulator); forming an oil phase (comprising donepezil, a carrier material and an organic solvent); and adding the oil phase into the water phase, dispersing to form a pre-emulsion, performing membrane emulsification on the pre-emulsion to form an emulsion, and finally curing, washing and freeze-drying the emulsion to obtain the donepezil sustained-release microspheres. The preparation process is stable and controllable, the batch-to-batch repeatability is good, the surface of the microsphere is smooth and complete, the particle size distribution is uniform, the size is controllable, the microsphere has high drug loading capacity, long-term stable release can be realized, the injectability is excellent, the administration frequency can be reduced, and the adverse reaction of gastrointestinal tracts can be reduced.

The invention relates to an exosome fusion liver targeting liposome drug delivery system as well as a preparation method and application thereof, and belongs to the field of high polymer material science and pharmaceutical preparations. The invention discloses an exosome-fused liver-targeted liposome drug delivery system, which combines high-concentration PEG8000 and Nycodenz in a breakthrough manner, synergistically improves the fusion efficiency of exosome and liposome, and forms bionic vesicles with uniform size and high drug loading capacity. The exosome not only can exert the anti-inflammatory and anti-oxidation characteristics, but also plays a role in resisting a severe gastrointestinal environment and crossing a biological barrier. In addition, liposome is modified by cholic acid derivatives through EDC / NHS mediated amidation reaction, precise targeting of the liver is achieved, and the liposome is fully accumulated in the liver. The effects synergistically realize the treatment of type II diabetes and non-alcoholic steatohepatitis.

The invention is applicable to the technical field of biomedicine, and provides dipeptide-photosensitizer molecule co-assembled nanoparticles as well as a preparation method and application thereof. According to the invention, cationic diphenylalanine (CDP) and a biological cross-linking agent genipin are self-assembled to form a dipeptide carrier, and then the dipeptide carrier and a photosensitizer molecule chlorin e6 (Ce6) are co-assembled, so that nanoparticles with controllable size, controllable drug loading capacity and good biocompatibility are successfully prepared. The preparation method is simple and easy to implement, effectively solves the key problems that the traditional photosensitizer molecule Ce6 is poor in biocompatibility and easy to gather, not only can efficiently deliver Ce6, but also obviously improves the application safety and biocompatibility of Ce6. The Ce6 is almost free of dark toxicity under a dark condition, can play a strong photodynamic killing role under illumination, and greatly improves the possibility and application potential of the Ce6 in tumor photodynamic therapy by virtue of the flexible regulation and control advantages of the size and the drug loading capacity.

The invention provides emamectin benzoate-sodium alginate composite microspheres and a preparation method thereof, and belongs to the technical field of pesticide preparations. The composite microspheres disclosed by the invention are prepared from the following raw materials: 0.5 to 1 part of emamectin benzoate, 0.2 to 1 part of a modifier, 0.1 to 0.5 part of isopropyl phenyl triphosphate, 0.5 to 5 parts of sodium bentonite and 1 to 8 parts of sodium alginate. The emamectin benzoate-sodium alginate composite microsphere photolysis-resistant slow-release pesticide is prepared by taking sodium alginate and modified organobentonite as carriers to load active ingredients of emamectin benzoate. The emamectin benzoate-sodium alginate composite microspheres prepared by the invention have the advantages that the drug loading capacity is obviously improved, the drug release time is obviously prolonged, and the slow release effect is better. According to the invention, sodium alginate and organic bentonite are utilized to load emamectin benzoate to form a'date cake model 'structure, so that direct irradiation of ultraviolet rays can be effectively shielded, the light degradation rate of emamectin benzoate is slowed down, and meanwhile, the effective utilization rate of emamectin benzoate is improved.

The invention discloses a pharmaceutical composition and application thereof. The invention specifically discloses a pharmaceutical composition containing progesterone, grease, phospholipid and a solvent. The pharmaceutical composition has one or more of the following advantages: good safety, high drug loading capacity, convenience in administration, slow release performance, good stability and suitability for industrial production.

The invention relates to a water-in-oil nanoemulsion with high drug loading capacity as well as a preparation method and application of the water-in-oil nanoemulsion. The water-in-oil nanoemulsion is prepared by dropwise adding a water-phase solution containing tocoxolam into an oil-phase solution, the water-phase solution is prepared from tocopherol, a cosurfactant, a hydrophilic active matter, a preservative and water; the oil phase solution is composed of liquid grease and a surfactant; the water-in-oil nanoemulsion is prepared from the following components in percentage by mass: 50 to 64 percent of liquid grease, 10 to 17 percent of surfactant, 5 to 8 percent of tocoxolam, 5 to 12 percent of surfactant, 0.1 to 6 percent of hydrophilic active matter, 0.2 to 0.6 percent of preservative and 8 to 15 percent of water. The water-in-oil nanoemulsion has the advantages of high drug loading capacity, good skin permeability, high retention volume in skin cells, high bioavailability, good stability, high safety and the like, and can be used in pure oil cosmetics.

The invention discloses a colchicine external preparation with high intradermal residual quantity and percutaneous transmittance as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The invention provides a colchicine external preparation with high intradermal residue and transdermal transmittance. The colchicine external preparation comprises: a) colchicine or a pharmaceutically acceptable salt thereof; b) a penetration enhancer; c) pharmaceutically acceptable excipients and / or excipients; the penetration enhancer is at least one of polyglycerol oleate or isosorbide dimethyl ether. The drug loading capacity and the percutaneous transmittance of the colchicine external preparation disclosed by the invention are remarkably improved. When polyglycerol oleate is selected as a penetration enhancer to prepare colchicine gel, the intradermal retention volume can reach 358.08 micrograms within 20 hours. When isosorbide monomethyl ether is selected as a penetration enhancer to prepare ethosome gel, the accumulated penetration amount can reach 106.87 mu g / cm < 2 >, and the intradermal residual amount can reach 90.58 mu g or above.

The invention provides a silibinin mixed micelle injection as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The cholate / lecithin mixed micelle system constructed by adopting specific cholic acid and phospholipid has good stability, can be well compatible with the silibinin so as to well encapsulate the silibinin, can obviously improve the solubility of the silibinin, has higher safety under the condition of ensuring the stability of the silibinin, and can be used for preparing a medicine for treating the silibinin. Therefore, the bioavailability of the silibinin is greatly improved. According to the invention, a shearing dispersion method is adopted to prepare the mixed micelles, and the mixed micelles with high drug loading capacity, clarification and good stability for silibinin are formed by destroying and shearing the raw and auxiliary materials in a molecular level, so that the mixed micelles have better physical and chemical stability, the drug quality is easier to control, the process is more simplified, the clinical medication is safer and the cost is lower; and the accessibility of the medicine is improved.

The invention discloses oral brain-targeted nanoemulsion as well as a preparation method and application thereof, and belongs to the field of biological medicine preparations. Drug molecules and a stabilizer are dispersed in oil phase molecules, and then a surfactant and water are added to prepare the nano-emulsion. Drug molecules are dispersed in oil-phase molecules and then form an oil-in-water nanoemulsion with water, so that the problems of poor stability and poor water solubility of current drug molecules are solved, the oral bioavailability of the drug is improved, fusion of different drug molecules of multiple targets is realized, the drug loading capacity of the drug molecules can be effectively ensured, and the bioavailability of the drug is improved. In addition, the drug can pass through an intestinal barrier and a blood brain barrier to be successfully delivered to a brain region to realize multi-target treatment, so that efficient treatment of multi-target brain diseases such as neurodegenerative diseases and central nervous system tumors is realized.

The invention relates to an ROS response type persulfide biomacromolecule nano prodrug, a nano preparation and a preparation method and application of the ROS response type persulfide biomacromolecule nano prodrug and the nano preparation, and belongs to the technical field of nano preparations. According to the invention, the hydrogen persulfide is protected by utilizing ROS to respond to a small molecule group, so that the defect that the existing hydrogen persulfide is unstable is overcome; meanwhile, biomacromolecules are used as a carrier of the hydrogen persulfide, so that the liver targeting property, the water solubility and the biological safety of the hydrogen persulfide are improved, and multi-site modification and adjustability of the drug loading capacity are realized; in addition, the nano preparation is simple in reaction process, mild in condition and beneficial to clinical transformation.

The invention provides a preparation method and application of cystamine modified hyaluronic acid hydrogel. The preparation method comprises the step of synthesizing hydrogel with a three-dimensional network structure by taking hyaluronic acid as a carrier and cystamine as a cross-linking agent. The insoluble drug is entrapped by the hydrogel, so that the solubility of the insoluble drug is effectively improved. The preparation method disclosed by the invention is simple in process, the prepared hydrogel has excellent performance and has the characteristics of uniform pores, good hydrophilicity, high drug loading capacity and high encapsulation efficiency, and the prepared drug-loaded hydrogel can slowly and continuously release drugs and has good antioxidant and antibacterial properties.

The invention discloses an oil-soluble composition containing recombinant collagen. The composition comprises recombinant collagen, a polyhydroxy compound, grease, an emulsifier and water. The invention also provides a preparation method of the composition. The composition disclosed by the invention has the characteristics of good transparency, high drug loading capacity, good adaptability and good stability.

The invention relates to a plaster with large drug loading capacity and strong permeability and a preparation method thereof, belongs to the technical field of pharmaceutical preparations, and solves the problems of low drug loading capacity and poor drug transdermal efficiency of the traditional plaster. The plaster comprises the following components in parts by weight: 10-20 parts of gelatin, 5-15 parts of sodium polyacrylate, 1-3 parts of carbomer 9401 and 150-260 parts of glycerol. 0.1 to 0.5 part of a volatile oil compound and 0.2 to 0.4 part of azone; 5 to 15 parts of silicon dioxide, 0.1 to 0.5 part of ethylparaben and 3 to 5 parts of deionized water. The plaster provided by the invention is high in drug loading capacity, the drug loading capacity reaches 80% or above, the permeability is strong, and the preparation process of the plaster is stable.

The invention relates to an application of a CAR exosome drug carrier in tumor treatment. The application of the CAR exosome loaded medicine in tumor treatment is based on the strategy of CAR exosome coupling medicine, so that the completeness of the exosome and the controllability of the medicine loading capacity are greatly protected, the purpose of accurately delivering the medicine to tumors in a targeted manner is achieved, and a new direction is provided for tumor treatment.

The invention relates to the technical field of medicines, and particularly provides an active oxygen responsive paclitaxel prodrug which has a structure as shown in a formula I or a formula II. Aiming at the problem of hydrophobic aggregation of paclitaxel, the paclitaxel drug is modified, the water solubility of the modified paclitaxel drug is greatly enhanced, the self-assembly performance is obtained, the modified paclitaxel drug can be self-assembled in an aqueous solution to obtain the nano particles, and the nano particles have ultrahigh drug loading capacity and drug loading efficiency. The paclitaxel nano-preparation prepared by the method can be used for preparing the paclitaxel nano-preparation, can specifically respond to high-concentration active oxygen in a tumor microenvironment, not only can improve the insufficiency of drug loading capacity of a traditional paclitaxel nano-preparation, but also can respond to release paclitaxel at a tumor position, is beneficial to reduction of drug dosage and reduction of toxic and side effects, and has important significance on improvement of patient prognosis and prolonging of patient lifetime.

The invention relates to the field of medical materials, in particular to a process for realizing a controllable slow-release antibacterial biological patch with high drug loading capacity. Different from a conventional coating type structure, the effective antibacterial components of the antibacterial patch are distributed at all positions of a patch structure network, but not only distributed at a certain layer. The prepared patch has good mechanical properties and a structure which is not easy to loosen when encountering water, the process stability is enhanced, the drug loading capacity, the drug loading speed and the like can be quantitatively and controllably adjusted according to actual requirements, and the patch can be applied to various surgical scenes such as an abdominal cavity open operation and the like and has wide application prospects. The biological patch is especially suitable for being applied to instant antibiosis after a surgical operation, not only is beneficial to infection resistance, but also can guide tissue regeneration, and is degraded along with tissue repair.

The invention discloses folate receptor mediated manganese ion coordination type cabazitaxel-loaded albumin nanoparticles as well as a preparation method and application thereof. Human serum albumin is covalently linked with folic acid through an amide condensation reaction to obtain a folic acid-albumin modifier with folic acid targeting; further combining with manganese ions through metal coordination to form a folic acid-albumin-manganese ion modifier with a targeting function; finally, efficient loading of cabazitaxel is achieved through a simple heating polymerization method, and the folate receptor mediated cabazitaxel-loaded albumin nanoparticles are formed. According to the nanoparticles provided by the invention, the particle size is about 140 nm, the stability is good, and the drug loading capacity and the encapsulation efficiency of cabazitaxel are high; the compound has a slow release effect, is good in in-vitro release behavior, and has important application value in the aspect of targeted delivery of drugs to tumors. Compared with other traditional nanoparticles, the nanoparticles show a remarkable anti-tumor effect.

The present invention discloses a semaglutide oral patch and a preparation method and application thereof, belonging to the field of pharmaceutical preparations. The oral patch comprises the following ingredients: 0.3-0.8 parts of semaglutide, 0.3-0.8 parts of an absorption enhancer, 1-2 parts of a film former and 0.2-0.5 parts of a plasticizer; wherein the film former is composed of hydroxypropyl cellulose, hydroxyethyl cellulose and carboxymethyl cellulose. The oral patch of the present invention has the advantages of high drug loading, high bioavailability, excellent demoulding, mechanical properties, taste and no drug precipitation, and is used to treat type 2 diabetes.

This invention discloses a protein-polysaccharide ternary nanoparticle loaded with cordycepin, its preparation method, and its applications. The invention employs a layer-by-layer self-assembly method to modify the surface of zein nanoparticles. Since zein has a positive surface charge, the first layer modification uses the anionic polysaccharide sodium alginate for electrostatic bonding, and the second layer modification uses the cationic polysaccharide chitosan, constructing positively charged ternary composite nanoparticles. These nanoparticles have small particle size, high encapsulation efficiency, high drug loading capacity, and a sustained-release effect, significantly reducing cytotoxicity and significantly improving the therapeutic effect on osteoarthritis. This invention develops a novel cordycepin formulation, overcoming the limitations of cordycepin's clinical use.