33results about How to "Reduce burst phenomenon" patented technology

The invention relates to a method for preparing a small molecule hydrophilic drug-embedded sustained-release capsule. The method comprises the following steps: filtering a prepared'internal aqueous phase/oil phase/external aqueous phase' pre-multi-emulsion solution through a microporous membrane; and then removing a solvent, washing and drying to obtain the small molecule hydrophilic drug-embedded sustained-release capsule, wherein the internal aqueous phase comprises a small molecule hydrophilic drug and a thickening agent. The small molecule hydrophilic drug-embedded sustained-release capsule provided by the invention has the advantages of uniform grain diameter, high embedding rate, low burst-release rate, stable drug release and long action.

The invention relates to a drug-loaded liposome and preparation method thereof. The liposome contains hydrogenated lecithin or synthetic phospholipid composition and hydroxyethyl starch assuring stable structure of the liposome. The liposome is used to encapsulate and load drugs, so as to control flocculation, agglomeration, precipitation and the like of the liposome, reduce leakage of the encapsulated and loaded drugs, prolong the release of drugs, improve stability of liposome preparation in liquid and solid states; therefore, it is convenient for the storage and the transportation of the preparation. The liposome is suitable for encapsulating various drugs, and is especially suitable for insoluble drugs, heat-reactive drugs and biomacromolecule drugs, and the fitting range is wide.

The invention relates to a phospholipid protein particle composite microsphere and a preparation method thereof. The preparation method comprises the following steps: stirring and mixing protein or polypeptide water-soluble drugs, an aqueous solution of a freeze-drying protective additive and an alcoholic solution of phospholipid to obtain a lipid vesicle suspension of phospholipid protein; freeze-drying for removing the solvent to obtain phospholipid protein particles; uniformly dispersing the phospholipid protein particles into an organic solution of a polymer carrier material, then adding an aqueous solution containing an emulsifying agent, and shearing at a high speed to prepare emulsion of S/O/W; and carrying out the processes of solvent volatilization, microsphere curing and the like to form the phospholipid protein particle composite microsphere. The phospholipid protein particle composite microsphere prepared by the method provided by the invention has a high drug envelopment rate and a low sudden release rate, wherein the release rate at the first day is 9-15%; the release rate is stable and lasting, the slow release period of the preparation can reach 20-60 days, and the bioactivity of the drugs in the microsphere is high; and therefore, the phospholipid protein particle composite microsphere has practical values in clinical application.

The invention provides a colon-targeted gel microsphere with a controllable core-shell ratio, and preparation and application of the colon-targeted gel microsphere. The gel microsphere comprises a core layer, an inner shell layer and an outer shell layer from inside to outside in sequence, wherein the core layer comprises cereal prolamin and an active matter; the inner shell layer comprises gel polysaccharide; the outer shell layer comprises chitosan, a cross-linking agent and a suspending aid. The inner shell layer and the core layer form core-shell structure fog drops through a coaxial electrostatic spraying technology, in an outer shell layer solution, the inner shell layer gel polysaccharide of the core-shell structure fog drops is cross-linked with the cross-linking agent and is subjected to electrostatic layer-by-layer adsorption with chitosan, and therefore, the colon-targeted gel microsphere is prepared. The particle size of the gel microsphere is 100-600 [mu] m, the core-shell ratio is 0.5-0.9, the encapsulation efficiency of a water-soluble active matter is as high as 60%, the encapsulation efficiency of an alcohol-soluble active matter is as high as 90%, the release amounts in a stomach simulation liquid and a small intestine simulation liquid within 1 h and 3 h can be as low as 10% and 25%, and the gel microsphere can be efficiently delivered and targeted to the colon.

The invention relates to the field of medicines, and provides an antibacterial and wound healing promoting composition and a medical hydrocolloid oil yarn thereof. The composition capable of resistingbacteria and promoting wound healing comprises chitosan quaternary ammonium salt, polyethylene glycol and sodium hyaluronate with a mass ratio of 1:(0.1-0.6):(0.2-0.4). The antibacterial and wound healing promoting composition is embedded by using gelatin to form microspheres, and the microspheres are added into a hydrocolloid oil yarn to form the medical hydrocolloid oil yarn which has the effects of inhibiting gram-negative bacteria and gram-positive bacteria and also has the remarkable effects of diminishing inflammation, promoting wound healing and repairing. Compared with the prior art,remarkable progress is achieved.

The invention provides a microsphere for double protection of antibody drug and intravitreal injection, and a preparation method thereof. Particles of a monoclonal antibody drug are prepared by adopting a method of water phase-water phase emulsification, polylactic acid-glycolic acid copolymer and polyketal are utilized as carrier materials, and a sustained release microsphere that wraps and carries the particles of a dextran-monoclonal antibody drug is prepared by employing an emulsion solvent volatilization method of water phase-oil phase-solid phase. Denaturation and aggregation of antibodies are caused by an acidic microenvironment of polylactic acid-glycolic acid in an organic phase/aqueous phase interface and a degradation process, the drug loading capacity of the microsphere is increased and a burst release phenomenon during a releasing process of the microsphere is reduced, and double protection on the monoclonal antibody drug of the microsphere is achieved; the polyketal enables the drug loading capacity of the microsphere to be increased, enables the stimulation of an acidic degradation product of the polylactic acid and glycolic acid on eye environment to be reduce, andenables side effects such as endophthalmitis to be reduced; and the microsphere can release the monoclonal antibody for not less than 28 days in the in vitro environment and for not less than 2 monthsin the eye, and so, the frequency of administration can be reduced, pain of patients and economic burden are reduced, and the compliance of patients is improved.

The invention discloses a colon-targeted sinomenine hydrochloride slow-release nanofiber membrane and a preparation method and application thereof. The nanofiber membrane comprises a shell layer and acore layer coated in the shell layer, wherein the shell layer comprises the following components: Eudragit S100 or Eudragit RS100; the core layer comprises the following components: any one or more than two of Eudragit S100, Eudragit RS100, polycaprolactone and polyvinylpyrrolidone, and sinomenine hydrochloride. The drug loading capacity of sinomenine hydrochloride in the nanofiber membrane is 10%-30%. According to the sinomenine hydrochloride slow-release nanofiber membrane with the shell-core structure, slow release and targeting of the drug are realized and the membrane has good biocompatibility.

The invention relates to the field of medical technology and discloses a long-acting preparation of lactic-glycolic acid copolymer (PLGA) for the recombination of endostatin of vein and the application to preparing a drug for treating tumor. The invention uses four methods of implanting a pump in vivo, implanting a microsphere in vivo, a W/O/W solvent volatilization method and a W/O/O solvent volatilization method to prepare the long-acting preparation. The sustained-release time of the long-acting preparation prepared is 7 to 28 days in accordance with the needs.

The invention discloses a polycystic liposome gel capable of overcoming burst release and maintaining antibody activity, and belongs to the field of eye sustained and controlled release preparations of biological macromolecular drugs. A monoclonal antibody clone antibody drug is wrapped in the polycystic liposome with good biocompatibility and biodegradability, and then the polycysticliposome is dispersed in sol formed by a temperature-sensitive polymer material, and after the sol is injected through a vitreous cavity, the sol is solidified into semi-solid gel at the body temperature to form apolycysticliposome-temperature-sensitive hydrogel composite preparation, so that release of the antibody drug is controlled. By the adoption of the polycystic liposome gel capable of overcoming burstrelease and maintaining antibody activity, the advantages of the polycystic liposome and the hydrogel preparation are utilized, in-vitro release of the antibody drug can be kept for about 60 days, the burst release problem of a general dosage form of the antibody drug is reduced, the activity of the antibody drug is greatly maintained, retention time of the antibody drug in eyes after vitreous injection is prolonged to a greater extent, injection frequency is reduced, and compliance of patients is improved.

The invention provides a konjac glucomannan and sodium alginate composite drug-loaded microsphere and a preparation method and application thereof.The preparation method of the composite drug-loaded microsphere comprises the following steps that a konjac glucomannan solution and a sodium alginate solution are mixed, attapulgite is added and stirred, fluorouracil is added and stirred, and the konjac glucomannan and sodium alginate composite drug-loaded microsphere is obtained. And injecting the solution into a CaCl2 solution by using an injector to form microspheres, transferring the microspheres into a glutaraldehyde solution, reacting, washing and drying. The inorganic mineral attapulgite is added into a natural high polymer material to increase the encapsulation and controlled release of the natural high polymer material to drugs, the composite material is prepared by a simple gel method, the encapsulation efficiency of fluorouracil is high, and the burst release phenomenon of 5-FU in a simulated solution can be obviously reduced; the preparation method disclosed by the invention is simple, the raw materials are rich, the thermal stability is good, the biocompatibility is good, the drug encapsulation efficiency is high, and the prepared composite drug-loaded microspheres are obvious in slow-release effect.

The invention discloses a topical pharmaceutical composition containing a water-insoluble analgesic and a preparation method and application thereof. The topical composition includes a water-insolubleanalgesic drug and ozone. The water-insoluble analgesic drug is flurbiprofen axetil or propofol. The weight ratio of the water-insoluble analgesic drug to ozone is (10-100): (6-15). The drug encapsulation rate is improved and can reach 90% and above, which effectively reduces burst release of the drug. The drug release rate is stable and durable, and the sustained release period can reach 2 to 3days. The pharmaceutical composition is easy to apply and convenient to carry, and patient compliance is improved. The preparation method is simple, the conditions are mild, the preparation process issimple, parameters are controllable, reproducibility is good, production efficiency is high, and continuous large-scale production can be achieved. The pharmaceutical composition has low requirementson storage conditions and is easy to package, transport and store.

The invention discloses an injectable long-acting semi-solid gel preparation which comprises a mixture containing ricinoleic acid triglyceride and a gelling agent and an active ingredient, and the active ingredient comprises loteprednol, latanoprost, celecoxib, triamcinolone acetonide or betamethasone. The pharmaceutical composition provided by the invention is a biologically erodible semisolid carrier gel preparation, has the advantage of sustained release of drugs, and does not have an obvious burst release phenomenon.

The invention relates to the technical field of pharmaceutical preparations, in particular to a rebamipide sustained release tablet and a preparation method thereof. The rebamipide sustained release tablet is prepared from rebamipide, a framework material and a microcrystalline cellulose-carboxymethyl cellulose sodium compound. The preparation method comprises the following steps: firstly, mixing the rebamipide with the framework material and the microcrystalline cellulose-carboxymethylcellulose sodium compound, and granulating; and mixing the granulated particles with a lubricant, tabletting, and coating. The rebamipide sustained release tablet provided by the invention not only can improve the bioavailability of the rebamipide tablet, but also can improve the common burst release phenomenon of a sustained release preparation, not only has important clinical significance, but also can reduce the production cost.