827 results about "Drug loading dose" patented technology

The invention discloses a hollow mesoporous silica microsphere with hollow core and adjustable mesopore and penetrating through a shell, preparation method and application thereof. The hollow mesoporous silica microsphere is obtained by the following steps: under the condition of acid or alkaline solution, taking hexadecyl trimethyl ammonium bromide or PEO-PPO-PEO triblock copolymer as template, adding non-polar solvent, stirring at a certain temperature, emulsifying, then adding silica source, after hydrolysis and condensation, filtering, drying, and roasting to remove the template. The preparation method has simple technique and short time, easy operation and low cost, the prepared microsphere comprises both macropore and mesopore structures, the mesopore penetrates through the shell, the aperture thereof is larger than 5nm and is adjustable within the range of 5-20nm, and by relatively large mesopore channel, internal and external transmissions of large guest molecules can be realized. The microsphere can be used as drug carrier, the drug loading amount can exceed 50% (mass percentage), and the drug release can be controlled by adjusting aperture of the mesopore and dissolutionrate of indissolvable drug can be improved.

A transdermal drug delivery system with microprojections for disrupting a body surface to an individual. At least some of the microprojections arise from a first microprojection layer and at least some of the microprojections arise from a second microprojection layer. The first and second microprojection layers are stacked together.

The invention provides an in-vivo degradable and absorbable artificial medical tissue repairing film and a preparation method thereof. The biodegradable repairing film is composed of a porous layer and a reinforcing layer and is a sponge-like substance which is of a two-layer, three-layer or multi-layer overlapped structure, wherein the layers are closely combined. The porous layer has a certain thickness so that the biodegradable repairing film has a certain shape and a certain drug loading capacity so as to meet the needs of tissue repair; the reinforcing layer is compact and has reinforcing and anti-tearing effects; each layer of structure can be prepared from different raw materials at different ratios and loaded with different drugs according to treatment requirements; the degradation speed and drug release can be controlled by controlling the quantity and size of holes. The porous layer is higher than the reinforcing layer in degradation speed, so that the repairing film keeps a certain mechanical strength within a certain time and the drug is released slowly and directionally. The repairing film is excellent in operability and suturing property, nontoxic, degradable and absorbable in vivo, good in biocompatibility, free of injuries to tissues, applicable to various surgical repair operations and suitable for popularization and implementation.

The present invention provides organic nanoparticles that include a molecule having a Log P value of about 3 or above, an amphiphilic diblock copolymer or a surfactant, and a pharmaceutically-acceptable hydrophilic polymer. The present invention also provides methods of making these nanoparticles, e.g., by flash nanoprecipitation, with control over particle size and surface properties. The methods of the present invention provide a means for co-precipitating a water-insoluble compound with an amphiphilic stabilizer within a few milliseconds. The nanoparticles of the present invention exhibit high drug loading, e.g., 50% w/w, and can be produced with a mean particle size less than 200 nm and with a narrow particle size distribution.

The invention designs and synthesizes a series of paclitaxel-oleic acid small-molecular prodrugs; with the application of a chemical connecting arm which is sensitive to an oxidation-deoxidation environment, the rapid release of the drugs in tumor cells is promoted. On the basis, small-molecular prodrug self-assembled nano-drug delivery systems are prepared. The small-molecular prodrug self-assembled nano-drug delivery systems have the advantages that by virtue of a one-step nano-precipitation method, nano-drug self-assembled nanoparticles are simple in preparation process and easy for industrialization; the nano-drug self-assembled nanoparticles are small and uniform in grain size (to 100nm), and the nano-drug self-assembled nanoparticles are enriched in a tumor part by virtue of an EPR (enhanced permeability and retention) effect; an ultrahigh drug-loading capacity is guaranteed, which is beneficial for reducing adverse reactions caused by auxiliary materials and biological materials; surface modification is easy to implement, and the intake of a reticuloendothelial system can be effectively avoided and the intake of the tumor cells to the nanoparticles can be improved by virtue of PEG (polyethylene glycol) and active targeting modification; and on the basis of the sensitivity of the chemical connecting arm to the oxidation-deoxidation microenvironment of the tumor cells, the specific drug release of paclitaxel in the tumor part is achieved, a curative effect is improved and toxic and side effects are reduced.

The invention discloses preparation and application of an insoluble drug-entrapped poloxamer/amphiphilic polysaccharide mixed micelle. The insoluble drug-entrapped poloxamer/amphiphilic polysaccharide mixed micelle is prepared through a dialysis method or a solvent evaporation method. The mixed micelle is low in critical micelle concentration, is high in drug-loading rate, is capable of obviously prolonging the stabilization time and has the long-circulation function of a nanomicelle and has dual functions of restraining the metabolism of P-glycoprotein and cytochrome P450 enzyme and is capable of increasing the bioavailability of oral administration. The mixed micelle is simple in preparation method, is mature in process and is high in yield and can be prepared into preparations for the oral administration, such as tablets, capsules, pills and syrups.

The invention relates to a paclitaxel-loaded sustained release nano-fibre material which comprises the components of bio-degradable polymer material and pure paclitaxel, the mol ratio of which is 1.33 to 10. The diameter of the nano-fibre is 90nm to 1.44micrometer, and the drug-loading rate can be regulated within the range of 0 percent to 100 percent. The preparation of the nano-fibre comprises the steps as follows: (1) the bio-degradable polymer material is solved in organic solvent and stirred to be solved completely to obtain lamella spinning solution A; (2) the white pure paclitaxel powder is solved in trifluoroethanol and stirred to be solved completely to obtain core spinning solution B; (3) clear transparent solutions A and B are respectively added into two injectors; the speed of a microinjection pump, the voltage of a static generator and the receiving distance between a grounded aluminum foil and a spinning needle are adjusted, and unordered drug-loaded nano-fibre is obtained by a coaxial electrostatic spinning technology. A nanometer control release system composed by the drug-loaded nano-fibre effectively controls the sustained release of the drug and is applied to the preparation of the drug for remedying malignant tumor.

The invention discloses an oral disintegrating tablet and a preparation method thereof, and especially discloses an oral disintegrating tablet containing a bicomponent as a binder, and a preparation method thereof. The oral disintegrating tablet of the invention is prepared through adopting a lyophilizing process, and components of the tablet comprise effective doses of drug active components, a skeleton supporting agent, the binder, and a suspending aid, wherein the binder comprises pullulan and an auxiliary binder. The preparation method which utilizes the compound use of pullulan and the auxiliary binder in a specific application amount range solves problems of slow disintegration and incomplete dissolving-out when the lyophilized oral disintegrating tablet loads a large dose of the drug. Compared with lyophilized oral disintegrating tablets which are prepared with the prior art and have large drug loading doses, the lyophilized oral disintegrating tablet prepared in the invention, which has the advantages of rapid disintegration and complete dissolving-out, has a very good application value.

The invention relates to aripiprazole sustained-release microspheres and a preparation method thereof. The sustained-release microspheres include aripiprazole and a bio-degradable pharmaceutical high-molecular material PLGA, wherein the ratio of lactic acid to hydroxyacetic acid in the PLGA is 75:50-25:50. The PLGA is 25000-35000 Dolton in molecular weight. The addition weight ratio of the aripiprazole to the PLGA is 1:1-20. The aripiprazole accounts for 3.01-21.09% of total weight of the microsphere. The aripiprazole sustained-release microspheres have high drug embedding rate, is high in drug loading capacity, is smooth and round in surface and can release more than 90% of the drug in 30 days.

Disclosed are methods of preventing adverse clinical events in a patient undergoing a percutaneous coronary intervention procedure or a peripheral percutaneous interventional procedure comprising administering a therapeutically effective amount of a thrombin receptor antagonist, such as SCH 530348, to the patient. Administration of a loading dose of about 40 mg of SCH 530348 in as little as one hour prior to the procedure can result in therapeutically effective levels of platelet aggregation.

The invention generally relates to a dose packaging system for the administration of a liquid formulation to a patient requiring load-dose titration therapy of a pharmaceutically active drug, such as steroid therapy. More particularly, the invention relates to a dose packaging system for administering titration therapy of liquid formulations to a patient which eliminates the disadvantages that are associated with cups, dosing spoons, calibrated oral syringes and bottles.

The invention relates to a preparation method of a difunctional naonparticle preparation entrapping vincristine sulphate, which belongs to the technical field of medicine. The difunctional naonparticle preparation is prepared by entrapping the vincristine sulphate in a PLGA-PEG polymer carrier modified by folic acid/cell-penetrating peptide through a multiple emulsion method. The difunctional naonparticle preparation shows favorable pharmacokinetic behaviors in vitro and vivo. The diameter of the prepared PLGA-PEG difunctional naonparticle modified by folic acid/cell-penetrating peptide is 287.2+/-0.8nm, and the difunctional naonparticle preparation has high drug loading rate, high entrapment rate and good stability.

The invention discloses a preparation method and use of a traditional Chinese medicine asiaticoside carrying core/shell structure nanometer fiber film. The traditional Chinese medicine asiaticoside carrying core/shell structure nanometer fiber film is prepared from a lactic acid/glycollic acid copolymer (PLGA) as a shell and polycaprolactone (PCL) as an inner core through a coaxial electrospinning method. The preparation method has the advantages of use of easily available raw materials, operation easiness, good controllability and large scale industrial production easiness. The traditional Chinese medicine asiaticoside carrying core/shell structure nanometer fiber film can be used for wound dressing and has the advantages of controllable drug loading amount, high drug utilization rate and excellent wound healing promoting effect.

The invention provides a paclitaxel lipid compound and a micellar compound used in the injection of the paclitaxel lipid compound. The paclitaxel liposome compound is composed of paclitaxel with a therapeutic dose, phospholipid, cholesterol sulfate or/and similar cholesterol derivative, additive and injection water. By means of the lipidization of the paclitaxel, the problem about organic menstruum of an injection and the problem of hypersusceptibility of a surface active agent are solved. A paclitaxel lipid compound injection provided by the invention has the advantages of small side effect, low blood vessel simulation, high drug-loading rate, narrow particle size distribution, capability of filtering and degerming, good pharmaceutical stability, etc.

The invention belongs to the technical field of a microneedle, and concretely relates to a drug-loaded soluble microneedle patch and a preparation method thereof. The microneedle patch of the presentinvention comprises a needle and a base patch, and the needle and the base patch are prepared by centrifuging, freezing and thawing a polyvinyl alcohol-glucan solution with different mass fractions, the drug powder is placed between the needle and the base patch to form the drug-loaded soluble microneedle patch. The microneedle patch has high safety, good solubility, good mechanical properties andlarge drug loading; the invention also provides the preparation method of the microneedle patch, the method is simple and easy, does not require special equipment and preparation processes, and is suitable for popularization. In the microneedle patch of the invention, a sandwich layer between the tip of the needle and a substrate can be loaded with a large amount of solid powder medicine, which greatly increases the drug loading amount of the microneedle patch, and achieves the purpose of transdermal sustained release of the drug or vaccine.

The invention relates to the medical technical field, in particular to a paeonol micro-emulsion preparation and a preparation method thereof. The paeonol micro-emulsion preparation consists of components with the weight percentage as follows: 0.1 percent to 2 percent of paeonol, 10 percent to 25 percent of surfactant, 5 percent to 30 percent of cosurfactant, 5 percent to 15 percent of oil phase and 40 percent to 70 percent of deionized water. The mouse percutaneous experiment in vitro shows that the paeonol micro-emulsion prepared by the invention has obviously higher capacity of penetrating through the horny layer than the saturated aqueous solution of paeonol (p is less than 0.05), and the paeonol micro-emulsion can penetrate into the skin deeply to take curative effect within a short time and also has certain sustained and controlled release function. At the same time, the paeonol micro-emulsion improves the solubility of the paeonol obviously, increases the drug loading quantity of the preparation and reduces the drug administration times and the dosage. The paeonol micro-emulsion preparation has simple preparation method and uniform grain diameter of the preparation, has the advantages of being safe, stable and efficient and, can be used for preparing dermal medication preparation or cosmetic.

The invention belongs to the technical field of composite medicine materials as well as a preparation method and application thereof, more particularly discloses a nanoparticle for embedding medicinal Adriamycin. The nanoparticle has a core-shell type structure with an inner core embedded by an outer shell, wherein the inner core is embedded medicinal adriamycin, and the material for the outer shell is silicon dioxide; and the preparation method of the nanoparticle comprises the following steps of: evenly mixing cyclohexane, a surfactant and n-hexylalcohol, adding a sodium fluoride solution into the mixed solution after being evenly mixed to form a reverse-phase microemulsion; adding adriamycin and tetraethoxysilane into the reverse-phase microemulsion, and reacting to obtain a nanoparticle microemulsion system for embedding the adriamycin; adding a silylanization reagent containing functional groups into the microemulsion system, stirring for reacting, adding ethanol and demulsifying, centrifuging and then preparing the nanoparticle for embedding the medicinal adriamycin and modifying the functional groups. The nanoparticle embedding for the adriamycin has good stability, good biocompatibility, long slow-release time, large drug-loading rate, high medicine packaging rate, and the like, and has application prospect in the fields of tumor imaging and treatment.

The invention provides an ultrathin calcium silicate nanosheet with an ultrahigh specific surface area and a preparation method thereof. According to the ultrathin calcium silicate nanosheet with the ultrahigh specific surface area, the mole ratio of calcium to silicon is 0.4-1.5, the BET specific surface area is 200-550m<2>/g, and the thickness of the nanosheet is 1-10nm. The ultrathin calcium silicate hydrate nanosheet and an ultrathin non-crystal water calcium silicate nanosheet prepared by the method are uniform in shape and size and ultrathin in thickness, and the specific surface areas of the ultrathin calcium silicate hydrate nanosheet and the ultrathin non-crystal water calcium silicate nanosheet are larger than those of other calcium silicate nanosheets. Compared with the other methods in the prior art, the method provided by the invention has the advantages that the prepared ultrathin calcium silicate hydrate nanosheet and the prepared ultrathin non-crystal water calcium silicate nanosheet are very large in specific surface area, can be used as drug carriers, have extremely high drug loading capacity and good drug slow release performance on drugs difficult to dissolve in water, have the extremely strong capability of absorbing protein and heavy metal ions, and have a good application prospect in the fields of biological medicine and water treatment.

The invention relates to a method for preparing rapamycin/magnetic carboxymethyl chitosan nano drug-loaded microspheres. According to the method, synthesized Fe3O4 nanoparticles are added to liquid paraffin oil, the liquid paraffin oil is then mixed with carboxymethyl chitosan liquid, a crosslinking agent is added, nanospheres are collected through magnetic separation, and magnetic carboxymethyl chitosan nanospheres are obtained through washing and drying; aqueous dispersion liquid is prepared by using the obtained magnetic carboxymethyl chitosan nanospheres, rapamycin is dissolved in acetonitrile, and stirring is carried out so as to mix the rapamycin and the acetonitrile; and magnetic separation is carried out, a lower layer of precipitate is washed by using ultrapure water, and the rapamycin/magnetic carboxymethyl chitosan nano drug-loaded microspheres are obtained through freeze-drying and crushing. The nano drug-loaded microspheres prepared by the method have the characteristics of strong targeting, high drug loading capacity, good slow release performance, small particle size, low drug toxic and side effect and the like, and the tumor cell killing rate of rapamycin drugs can be remarkably increased; and the method is simple in process, mild in preparation conditions and easy in scale production.