52 results about "Drug loading dose" patented technology

This invention discloses a meglumine-luteolin complex, its preparation method, and its applications, belonging to the interdisciplinary field of microbiome and drug delivery. Using luteolin as the main material, this invention employs a dual inclusion technique with hydroxypropyl-β-cyclodextrin and meglumine to synergistically prepare a meglumine-luteolin complex with colon-targeted delivery capabilities. This invention significantly improves the delivery efficiency and drug loading of luteolin in the colon through the dual inclusion technique. The preparation process is simple, and it exhibits excellent hypoglycemic effects and colon-targeted release characteristics in the treatment of diabetes and its complications.

The application provides an ambroxol oral dissolving film composition, a preparation method and application thereof. The ambroxol oral dissolving film composition comprises an active drug, a film forming material and a taste masking agent, and the active drug is 2-amino-3,5-dibromo-N-(trans-4-hydroxycyclohexyl) benzylamine and / or a pharmaceutically acceptable salt thereof, for example, ambroxol hydrochloride. The ambroxol oral dissolving film composition provided by the application has the advantages of thin thickness, good taste, stable properties, immediate dissolution in the oral cavity without drinking water, and fast oral absorption speed. Moreover, the ambroxol oral dissolving film composition has the advantages of simple process, high drug loading, good drug content uniformity, and good market prospect.

The application relates to an embolization microsphere and a preparation method and application thereof, and belongs to the technical field of embolization microspheres. The embolization microsphere has a double-network interlocking structure formed by mutual intertwining of a first network and a second network; wherein the first network is formed by cross-linking polymerization of ionized cyclodextrin and a first cross-linking agent, and the second network is formed by cross-linking polymerization of an ionic monomer and a second cross-linking agent. The embolization microsphere is formed by mutual intertwining of the first network and the second network through a non-chemical bonding interlocking structure, which not only maintains the compactness of the microsphere structure and high ion strength, but also maintains the rotation freedom and cavity openness of the polymer network structure, significantly improves the drug loading capacity and slow-release performance of the microsphere on the premise of maintaining good mechanical properties of the microsphere. Meanwhile, the embolization microsphere has excellent dry-rehydration performance, has wide-spectrum drug loading capacity, can efficiently load various drugs, realizes local delivery of the drugs, and is suitable for TACE treatment of various drugs.

This invention discloses a cinnamic acid-black phosphorus nanocomposite targeting Aβ, its preparation method, and its application. The composition uses 4-(dimethylamino)cinnamic acid as the Aβ-targeting group and consists of a drug-loaded host (BP, black phosphorus nanosheets), a modifying material C18-PEG-NH2 (amino polyethylene glycol stearic acid), a targeting material Tar (4-(dimethylamino)cinnamic acid), and a therapeutic material Cur (curcumin). The preparation method includes the following steps: (1) preparation of PEG-Tar, (2) preparation of PEG-Tar@Cur, and (3) preparation of the BP-PEG-Tar@Cur composition. This invention utilizes black phosphorus nanosheets to load Curcumin, whose excellent specific surface area significantly increases the drug loading capacity. Furthermore, by using 4-(dimethylamino)cinnamic acid as a group targeting Aβ, diffuse distribution of the drug in the brain is avoided, greatly improving the drug utilization rate of Curcumin. The synthesis process of this invention is simple, highly reproducible, and easy to scale up for industrial application, and it has a positive effect in the treatment of Alzheimer's disease.

This invention provides a method for preparing and applying a controlled-release agent of emamectin benzoate, belonging to the field of nanopesticide technology. This invention uses PFC-1, a hydrogen-bonded organic framework material with a porous structure, as a drug carrier. After loading emamectin benzoate through its porous structure, the loaded system is further modified by surface encapsulation with sodium lignosulfonate. The resulting nano-formulation with controlled-release function is called emamectin benzoate nano-controlled-release agent. The prepared drug-loaded system exhibits good insecticidal activity against diamondback moth. The preparation method includes a method for preparing emamectin benzoate-loaded agents. The prepared system has a high loading capacity of 19.6%. The drug-loaded system provided by this invention has good insecticidal effect against diamondback moth and exhibits pH-selective release effect in the midgut environment of the diamondback moth.

The application provides an aggregated spider silk protein nanoparticle, a drug delivery system and a preparation method and application thereof, and belongs to the technical field of biological medicines.The application provides application of the aggregated spider silk protein in preparation of a drug delivery system.The application researches and finds that the aggregated spider silk protein nanoparticle prepared by using the amino acid sequence such as SEQ ID NO.1, SEQ ID NO.3 or SEQ ID NO.5 has good colloidal stability and good safety, and is a novel drug delivery system.The drug delivery system loaded with a tumor drug has high encapsulation efficiency and drug loading capacity for the tumor drug, the encapsulation efficiency is more than 60%, has a slow-release effect on the tumor drug, and is an excellent drug delivery system.The research finds that compared with the simple tumor drug, the drug delivery system loaded with the tumor drug has a significantly improved killing effect on tumor cells, and can effectively treat tumors.

This invention provides a peptide-human serum albumin (HSA) conjugate drug, its preparation method, and its application. The peptide-human serum albumin conjugate drug comprises a target tumor cell membrane protein peptide, human serum albumin, and a cytotoxin. This invention innovatively introduces an HSA and covalently conjugates the target tumor cell membrane protein peptide and cytotoxin to the HSA, resulting in a conjugate drug with good stability and minimal cytotoxin loss. This peptide-human serum albumin conjugate drug overcomes the technical shortcomings of large molecular weight and cumbersome preparation of ADCs and insufficient drug loading of traditional PDCs, achieving multiple technical advantages such as high drug loading, small molecular weight, and easy preparation, demonstrating significant advantages and promising application prospects. The preparation method provided by this invention is simple and easy to implement, requiring no complex antibody expression and purification processes, resulting in lower production costs.

This invention belongs to the fields of biomedicine, beauty, and personal care health technology, and specifically relates to an amorphous assembly of capryloylglycine and tranexamic acid, its preparation method, and its application. The method involves adding capryloylglycine and tranexamic acid to an alcoholic solution, rotary evaporating, and drying to obtain a co-amorphous compound; mixing a cyclodextrin compound solution with the co-amorphous compound, heating to react, and drying to obtain the product. This assembly achieves high drug loading, significantly improves apparent solubility and in vitro dissolution rate, and overcomes application bottlenecks without altering the structure and properties of the active ingredients. This invention achieves multi-pathway targeted oil control and whitening through the synergistic encapsulation of capryloylglycine and tranexamic acid, with effects superior to single components. The cyclodextrin inclusion imparts excellent stability to the system, inhibits recrystallization, and provides both solubilization and controlled release effects; the components are safe and mild, with a near-neutral pH and strong formulation compatibility; its preparation process is mild, simple to operate, has high yield, is environmentally friendly, and easily industrialized.

This invention relates to the field of animal feed processing technology, and discloses a biological anionic salt preparation and its preparation method, comprising: mixing a lignocellulose carrier with anionic salt particles; heating the mixture to plasticize the fiber skeleton and maintain the bound water in the tracheid lumen in a state of accumulation; applying pulse pressure with a specific pressurization rate, using the transient volume expansion of the bound water to drive radial strain at the tracheid lumen inlet; pressing the anionic salt particles into the tracheid lumen under the pressure peak; removing the pressure and cooling, using the solubility temperature change difference to accumulate and precipitate a crystal sealing layer at the tracheid lumen inlet. This invention utilizes the kinetic response of endogenous water in the carrier to open the natural pore inlet, achieving physical integration of anionic salts, resolving the contradiction between high drug loading and storage stability, and effectively enhancing the physical masking effect and moisture resistance of the preparation.

This invention relates to the field of self-assembled nanomaterials technology. This invention provides a mangosteenin self-assembled nanomaterial, its preparation method, and its application. The preparation method includes the following steps: (1) mixing a mangosteenin solution with a formaldehyde solution and stirring to obtain mixture 1; (2) adding glycine to the mixture and stirring to obtain mixture 2; (3) dialysis of mixture 2 to obtain the mangosteenin self-assembled nanomaterial. The mangosteenin self-assembled nanomaterial of this invention does not require exogenous carriers such as polymers or liposomes, but relies solely on the self-influence of drug molecules to complete assembly, solving the problems of carrier toxicity and insufficient drug loading in traditional formulations. Preparation requires no complex chemical reactions or expensive equipment; large-scale preparation can be achieved through simple steps such as ultrasound and incubation, reducing industrial costs. Relying on the anti-fibrotic activity of mangosteenin itself and the passive targeting advantage of nanoparticles, efficient enrichment of drugs at lesion sites is achieved.

The application discloses a drug sustained-release elastic embolism microsphere and a preparation method and application thereof, and belongs to the technical field of medical materials. The application is prepared by the following steps: taking an acetic acid aqueous solution in which chitosan is dissolved as a dispersed phase, mixing the dispersed phase and a continuous phase into a W / O monodisperse emulsion template through microfluidic technology, introducing the W / O monodisperse emulsion template into an acceptant phase containing genipin, a W / O surfactant and an organic oil, crosslinking under magnetic stirring for 4-24 hours, post-treating the obtained microspheres to obtain elastic embolism microspheres, and finally dispersing the elastic embolism microspheres in an impregnation liquid in which a hydrophilic antitumor drug is dissolved and performing oscillation treatment, so that the drug sustained-release elastic embolism microsphere is prepared. The application effectively optimizes the drug loading capacity and drug sustained-release performance of the formed microspheres by setting the single chitosan dispersed phase component and adopting the technical strategy of jointly regulating and controlling the microfluidic control emulsification and crosslinking time, so that the effect of simply preparing the drug sustained-release elastic embolism microsphere is achieved.

Provided are an oral dissolving film composition of rivaroxaban, a method for preparing same, and use thereof. The oral dissolving film composition comprises one or more of rivaroxaban and a pharmaceutically acceptable salt, hydrate, and solvate thereof as an active ingredient, and a film-forming material. Also, the present invention features a simple process, no sedimentation during the preparation of film solutions, qualified content uniformity, high drug loading capacity, and improved patient compliance, and is particularly suitable for patients with dysphagia.

The application belongs to the technical field of medicine, and particularly relates to a modularly constructed targeted-tumor-killing polypeptide-drug conjugate as well as a preparation method and application. The conjugate has a dendritic six-branch scaffold structure, and the scaffold can realize replaceable combination of a targeting polypeptide and a chemotherapeutic drug through chemical modification, so that precise drug delivery can be realized for different tumor types. Among them, a blood vessel binding peptide and an albumin binding peptide are selected as model polypeptides, and a common clinical drug doxorubicin is selected as a model drug. The polypeptide-drug conjugate has high drug loading and stability, can improve the pharmacokinetic characteristics of poorly soluble drugs, prolong in-vivo circulation, has small molecular weight and strong tissue permeability, can be precisely enriched in tumors, has good structural adjustability and functional expansion potential, and exhibits significant anti-tumor effect and safety.

The application provides a tumor inhibiting composition and a preparation method and application thereof, and belongs to the technical field of medicines. After mesoporous carbon nanotubes are oxidized and chlorinated, oleanolic acid dithiocarbamate conjugate and (2-hydroxypropyl)-beta-cyclodextrin are coupled, drugs are loaded, a protein liposome solution is added, ultrasonic treatment is carried out, centrifugal separation is carried out, unloaded drug-loaded carbon nanotubes are removed, supernatant is freeze-dried, and the tumor inhibiting composition is prepared. The tumor inhibiting composition greatly improves the drug loading capacity of the nanosystem, the synergistic effect of multiple drugs, the anti-tumor effect, realizes the effects of targeting, slow and controlled release of drugs, improves the drug utilization rate, reduces the intake amount of drugs, reduces side effects, and improves the compliance of patients.

This invention relates to a brain-targeting nanomedicine formulation for glioblastoma and its preparation method, belonging to the field of pharmaceutical technology. The formulation comprises an active pharmaceutical ingredient, an amphiphilic block copolymer carrier, a covalently bonded brain-targeting ligand, and a stabilizer. The preparation method includes: chemically coupling the targeting ligand to the carrier material; self-assembling the drug, modified carrier, and stabilizer into nanoparticles using a nanoprecipitation method; and obtaining the final product through membrane extrusion granulation, purification, and lyophilization. The resulting nanoparticles have uniform particle size, high drug loading, and good stability, and can simultaneously achieve efficient crossing of the blood-brain barrier and specific targeting of glioma cells. In vitro and in vivo experiments show that this formulation can significantly improve drug accumulation at brain tumor sites, inhibit tumor growth, and prolong the survival of model animals. Furthermore, the preparation process is controllable and easily scaled up.

A retinoic acid prodrug to which a boron functional group having a structure represented by chemical formula 1 is bound is described. The retinoic acid prodrug self-assembles to form nanoparticles. Therefore, an anticancer drug composition comprises the same as an active ingredient. According to the retinoic acid prodrug, targeted therapy of tumor cells is possible through the synergistic anticancer effect of retinoic acid and the boron functional group and the surface modification of particles. In particular, the retinoic acid prodrug enables a drug loading of 100 wt %, and thus can provide an effective anticancer drug.

The application discloses a pH-sensitive asiaticoside drug-loaded micelle as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The drug-loaded micelle takes mPEG-PLGA-PHis triblock copolymer as a carrier, realizes high drug loading, high encapsulation efficiency and pH 5.5 precise response drug release by limiting the molar ratio of lactic acid and glycolic acid to 70:30-80:20, the specific molecular weight interval of each block and the mass ratio, the micelle particle size is 30-120 nm, the structure is stable in a neutral environment, and the drug is quickly released by depolymerization in an inflammatory micro-acid environment. The preparation adopts a film dispersion-dialysis process, has low organic solvent residue, uniform particle size, good batch repeatability and is suitable for industrial production. The drug-loaded micelle can be made into gel, cream and other external preparations, is used for skin inflammation repair, wound healing, scar lightening and post-medical beauty repair and has good clinical application and industrial value.

This invention belongs to the field of pharmaceutical formulation technology, specifically relating to a supersaturated SN38 lipid delivery system. The lipid delivery system comprises: SN38, injectable oil, lipids, a precipitation inhibitor, and an optional porous carrier material. The supersaturated SN38 lipid delivery system designed in this invention achieves a drug concentration exceeding its equilibrium solubility in aqueous solution, resulting in high drug loading. The system stability is increased by introducing a precipitation inhibitor and solidifying the liquid lipid delivery system, solving the problems of low drug loading and poor stability in existing formulations. The supersaturation state of the SN38 lipid delivery system of this invention is induced by an organic solvent method, effectively avoiding degradation of the drug and excipients. Furthermore, the preparation process is simple, controllable, and easy to industrialize. This supersaturated SN38 lipid delivery system protects the active lactone ring structure of the drug from damage and can utilize the EPR effect of nano-formulations to target tumor tissue, improving efficacy and reducing toxicity.

The application belongs to the field of drug delivery nanotechnology, and provides a method for preparing cubic lipid nanoparticles encapsulating small interfering ribonucleic acid and application thereof. The application adopts a trinity design of ion complex pre-assembly of succinylated glycerol monooleate and cationic lipids, space stabilization of poloxamer 407, and rapid particle formation by microfluidics, realizes stable construction of internal nanostructure of inverse bicontinuous cubic phase, encapsulation of small interfering ribonucleic acid in water channel network with high drug loading, long-term stability of colloids under physiological ion strength conditions, and excellent batch consistency, solves the technical contradictions of existing lipid nanometer delivery systems, such as difficulty in giving consideration to low polydispersion and batch consistency, mutual restraint of cationic complex strength and colloidal stability, and difficulty in synergistic optimization of high drug loading and stability of cubic phase structure under high solid content microfluidic conditions, and has wide application value in gene therapy and nucleic acid drug delivery.

This invention provides a cariprazine orally disintegrating film composition, its preparation method, and its application. The orally disintegrating film composition comprises an active ingredient, a film-forming material, and a plasticizer, wherein the active ingredient is selected from one or more mixtures of cariprazine, pharmaceutically acceptable salts of cariprazine, and their inclusion compounds. The orally disintegrating film composition of this invention has the advantages of thin thickness, good taste, stable properties, immediate dissolution in the oral cavity without water, and rapid oral absorption. It also features a simple process, high drug loading capacity, and good drug content uniformity. The orally disintegrating film composition of this invention helps improve medication compliance, medication retention, and vomiting in patients with schizophrenia, and is particularly suitable for patients with swallowing difficulties, showing promising market prospects.

The application belongs to the technical field of pharmaceutical preparations, and particularly relates to a rivaroxaban tablet, a preparation method and use. The rivaroxaban tablet comprises a rivaroxaban inclusion compound, lactose, starch, low-substitution hydroxypropyl cellulose and magnesium stearate. The rivaroxaban is packaged by using trimethylamine modified methyl cellulose as a packaging material, and the preparation process is optimized. The problem of low drug loading and low encapsulation efficiency of the rivaroxaban inclusion compound in the prior art is solved. The rivaroxaban tablet with a rivaroxaban inclusion compound with high drug loading and high encapsulation efficiency is provided, and the delivery efficiency of the rivaroxaban inclusion compound is improved. Through verification, the rivaroxaban tablet provided by the application has high dissolution rate, few impurities and stability.

The application discloses a painkilling preparation containing radix scophulariae and radix aconiti and a preparation method thereof, and belongs to the technical field of traditional Chinese medicine. The preparation is a transdermal patch, which is composed of a backing layer, a drug depot layer and an anti-sticking layer. The drug depot layer contains traditional Chinese medicine active ingredients and patch auxiliaries such as pressure-sensitive adhesive and transdermal absorption accelerators. The traditional Chinese medicine active ingredients take radix scophulariae and radix aconiti as the core drug pair, and are supplemented with one or more of the following drugs: qi-regulating analgesic drugs, blood-removing qi-regulating drugs, blood-activating analgesic drugs, blood-stasis-removing analgesic drugs, warm-qi-activating cold-dispelling drugs, wind-dispelling cold-dispelling drugs and external analgesic drugs. The application is a modern traditional Chinese medicine external preparation prepared by a patch technology, and the drug can penetrate the skin and directly reach the lesion, thereby playing a therapeutic role on inflammatory pain, cancer pain and idiopathic pain. The preparation has the characteristics of large drug loading, good transdermal absorption, fast analgesic effect, long-acting effect and avoidance of oral toxicity risk.

This invention relates to a transnasal brain-targeting nanosphere loaded with miR-195, its preparation method, and its applications, belonging to the field of biomedical technology. To address the limitations of existing drug delivery carriers in simultaneously achieving efficient nasal delivery to the brain, precise targeting of Aβ lesions, and stable loading of nucleic acid drugs such as miR-195, this invention provides a transnasal brain-targeting nanosphere loaded with miR-195. From the inside out, it comprises a drug-loaded core, a biomimetic cell membrane shell, and a dual-ligand functionalized surface canopy. The miR-195 loading in the nanosphere is 0.2–0.8% w / w. This invention's nanospheres deliver directly to the lesion via the nose. The cationic GO-Cl4 and neutral polymer synergistically protect miR-195 from degradation. Dual-ligand modification enables naso-brain barrier penetration and Aβ targeting, improving treatment precision and providing an effective treatment option for Alzheimer's disease, with broad clinical application prospects.

The application belongs to the technical field of medicine, and discloses a kind of methylbenzimidazole amorphous composition with polylysine or polyglutamic acid as carrier and its preparation method and application.The methylbenzimidazole amorphous composition is obtained by mixing methylbenzimidazole and carrier material (polylysine or polyglutamic acid) according to three proportions (1:3-3:1) and fully ball milling.The preparation method has the advantages of simple operation, high yield, no solvent residue, etc.Compared with traditional solid dispersion and co-amorphous system, the drug loading of the composition is 25%-75%, and the composition has ideal physical stability.Compared with crystalline methylbenzimidazole, the amorphous composition significantly improves the dissolution rate and solubility of methylbenzimidazole, providing a good intermediate for oral preparation of methylbenzimidazole.

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.