46results about How to "Low burst rate" patented technology

The invention relates to a liraglutide sustained-release micro sphere preparation and a preparation method thereof. The liraglutide sustained-release microsphere preparation comprises 5mg to 100mg of liraglutide, 0.5mg to 10mg of a protective agent and 50mg to 1000mg of a polylactic acid-glycolic acid copolymer, wherein the protective agent is one or a mixture of a plurality of sucrose, mycose, gelatin, mannitol, glycine, lysine and human serum albumin; the molecular weight of the polylactic acid-glycolic acid copolymer is 5000-20000 Daltons, and the ratio of polylactic acid to glycolic acid in the polylactic acid-glycolic acid copolymer is 1:3 to 3:1. According to the liraglutide sustained-release microsphere preparation disclosed by the invention, regular microspheres and medicines uniformly distributed in the microspheres can be obtained by just emulsifying and volatizing an organic solvent; processing procedures are simple; operation is simple; good repeatability is realized in preparation; the prepared liraglutide sustained-release microsphere preparations in batches have no remarkable difference; the obtained microspheres are uniform in grain size, narrow in distribution, controllable in grain size, round and orderly in surfaces and low in burst release rate.

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 discloses a narcotic analgesic-loaded sustained-release microsphere and a preparation method thereof and application thereof. The narcotic analgesic-loaded sustained-release microspherecan be continuously released for 1 to 7 days, the burst release rate is less than 20% within 0.5 hour, and the drug embedding rate is higher than 80%, so that high drug embedding rate and low burst release rate and sustained release can be realized. The method has simple process, the obtained product has uniform particle size, batches of products have good repeatability, and the preparation methodis easy for industrial production.

The invention relates to a method that a functional drug is enveloped into a polymeric material with biodegradability to form a nano-micron microsphere system. The method comprises that the polymeric material and simvastatin are dissolved in an organic liquor to form uniform dispersion which is then added into an liquor containing emulsifier Tween 80 and biologically nontoxic electrolytic polyvinyl alcohol or sodium dodecyl benzene sulfonate (SDBS), and then the obtained liquor is stirred, evaporated at a reduced pressure, centrifugalized, washed and vacuum dried, finally the simvastatin-contained delayed-release microsphere system is obtained. The surface of the microsphere is smooth and round, the granule thereof is regular without conglutination, and the granule diameter, the drug-loading rate (1-10 percent) and the encapsulation rate (above 40 percent) are all controllable, and the delayed-release time exceeds 2 months. The prepared simvastatin-contained delayed-release microsphere system can be processed into various preparations used in bony tissue absorption or bony defect parts, the microsphere system is degraded at a proper speed, thus the simvastatin can be further released; the degradation of the polymer can provide bony tissue with subsequent recuperating space to complete the repair of the bony defect parts.

The invention discloses a method for preparing sustained-release microgranules. The method includes steps of 1), preparing solid dispersion of biodegradable and biocompatible water-insoluble polymer and water-soluble drug; 2), dissolving the prepared solid dispersion in an organic solvent C to form solid dispersion emulsion; 3), injecting the obtained solid dispersion emulsion into oil solution with surfactants to form uniform emulsion; 4), curing microgranules in the emulsion by means of solvent evaporation or solvent extraction, and collecting, washing and drying the microgranules to obtain the sustained-release microgranules. The invention further discloses the sustained-release microgranules prepared by the aid of the method and application of the sustained-release microgranules to implantable sustained-release pharmaceutical compositions. The method, the sustained-release microgranules and the application have the advantages that full procedures for preparing the sustained-release microgranules by the aid of the method are carried out at the normal temperature or the low temperatures, and accordingly the method is quite favorable for preparing polymer matrix compositions from high-temperature-sensitive drugs; excellent similarly zero-level sustained-release effects can be realized by the prepared sustained-release microgranules, and the drugs are stable in concentration in sustained-release period.

The invention provides a slow release microsphere agents, comprising thymosin Alpha 1 of 0.5% to 10% of the microsphere weight, degradable pharmaceutical macromolecular accessories with a molecular weight of 5,000 to 500,000 Dalton and of 70% to 99.5% of the macroshpere weight, and 0% to 10% of other pharmaceutically acceptable accessories. The invention also provides the preparation method of the slow release microsphere agents. The slow release microsphere agent of thymosin Alpha 1 for injection has the advantages that the poison and side effect of thymosin Alpha 1 is reduced; the bioavailability is enhanced; times for drug taking is reduced and the drug can be conveniently taken by patients.

The invention provides exenatide composite microspheres. The exenatide composite microspheres are characterized in that lecithin wraps exenatide and a protecting agent simultaneously, and after exenatide lipid nanoparticles are formed, a high-molecular polymer carrier encapsulates the exenatide lipid nanoparticles to prepare the exenatide composite microspheres; and the molecular weight of the high-molecular polymer carrier is 10000-90000, and the high-molecular polymer carrier is dissolved in a mixing organic solvent. The prepared composite microspheres are uniform in grain size, the encapsulation efficiency of the exenatide is high, the microspheres are spherical and have smooth surfaces, the mean grain size is between 1 mu m and 50 mu m, and by the characteristics of smooth surfaces, high encapsulation efficiency and uniform grain size, the releasing speed of the microspheres is stable, the microspheres can release for a long time, therefore, the drug-delivering frequency can be reduced, and the compliance of patients is good.

The invention relates to cubic liquid crystal in-situ gel injection of local anesthetic, and a preparation method of the injection. The injection is prepared from the local anesthetic, a liquid crystal material and an organic solvent and/or a release regulator; the local anesthetic is amide local anesthetic and the mass concentration of the local anesthetic is 0.1 to 8 w/w%; the organic solvent is an organic solvent which is mutually soluble with water, the liquid crystal material is mono-oleic acid glycerolipid, and the mass ratio of the liquid crystal material to the organic solvent is (1-9):1; and the release regulator is selected from at least one of medium chain triglyceride, oleic acid, tocopherol and tocopheryl acetate, and the mass concentration of the release regulator is 0 to 30 w/w%. The cubic liquid crystal in-situ gel injection of the local anesthetic has very good long-acting sustained release effect, low sudden release raten high compliance and small adverse effect, can reduce administration times and can avoid the peak valley phenomenon.

The invention relates to a preparation method of an exenatide microsphere preparation. The method comprises the steps of: (1) weighing 5-50wt% of exenatide and 95-50wt% of polyester, which is one of or a mixture of PLGA and PLA at an ester group terminal or carboxyl terminal, with the molecular weight of PLGA being 3.0*10<3>-7*10<4> Dalton and the molecular weight of PLA being 4.0*10<3>-7*10<4> Dalton; (2) dissolving the polyester material in an organic solvent completely to obtain a clear solution, then putting exenatide into the clear solution, and conducting mixing and stirring evenly to obtain a homogeneous oil solution; and (3) supplying the homogeneous oil solution into a high speed rotating disc of an ultra-particle preparation system's (UPPS) droplet generation device by a peristaltic pump to form droplets, and curing the droplets to obtain the microsphere preparation. The microsphere preparation prepared by the method has excellent sustained release performance, a drug loading rate of 35%, an encapsulation rate of above 95%, low burst release rate, a sustained release period of more than 2 weeks, and no release lag period.

The invention provides low-sudden-release-rate semaglutide microspheres and a preparation method thereof. The preparation is a long-acting injection prepared from the active ingredient semaglutide with the weight being 1-20% of the weight of the microspheres, a biocompatible polymer substrate with the weight being 60-99% of the weight of the microspheres, and other pharmaceutically acceptable auxiliary materials with the weight being 0-20% of the weight of the microspheres. The semaglutide microspheres prepared by using the method are high in encapsulation efficiency, low in sudden release rate and capable of being slowly continuously released, the slow-release effect can last for 20-60 days, the effect on reducing blood sugar can last for at least 2-4 weeks, it only takes two weeks to onemonth or longer to conduct injection administration one time, the bioavailability of the polypeptide drug semaglutide is obviously improved, the metabolic half-life of the semaglutide is prolonged, the semaglutide administration frequency is further reduced, and the drug application compliance of a patient is further improved; because there are few drugs on the surface and the superficial layer of the preparation, the preparation is little released in the incipient administration stage, and therefore, the adverse drug sudden release effect is avoided.

The invention relates to a low-bursting-rate pure titanium seamless pipe for a metal corrugated pipe and a production process of the low-bursting-rate pure titanium seamless pipe The seamless pipe ischaracterized in that the seamless pipe has the grain size of 6-7 levels, the tensile strength Rm is larger than or equal to 300 MPa and smaller than or equal to 400 MPa, the yield strength Rp0.2 is larger than or equal to 180 MPa and smaller than or equal to 310 MPa, the ductility is larger than or equal to 50%, the wall thickness is uniform and is +/-5%t, the limit flaring rate is larger than orequal to 60%, and the bursting rate is smaller than or equal to 3%. According to the pure titanium seamless pipe prepared through the method, the grain size reaches the 6-7 levels, the room-temperature ductility reaches 50% or above, the wall thickness deviation is controlled to be +/-5%t, the limit flaring rate reaches 60% or above, and the bursting rate in subsequent corrugated pipe preparationcan be 3% or below.

The invention relates to huperzine A slow-release orally disintegrating tablets and a preparation method thereof. The huperzine A slow-release orally disintegrating tablets are prepared from huperzineA slow-release microspheres and acceptable auxiliary materials in orally disintegrating tablets. The huperzine A slow-release microspheres are prepared from huperzine A and raw materials of a framework material, the mass ratio of the huperzine A to the framework material is (0.1-0.6):100, and the framework material comprises ethyl cellulose and poloxamer in the mass ratio being (10-50):1. The huperzine A slow-release orally disintegrating tablets have more ideal slow-release effect, lower sudden release rate, can stably release in 24 h, can realize the release effect of basically complete release in 24 h, have the accumulated release quantity in 24 h up to 90% or above and are expected to be prepared into an oral slow-release preparation taken once a day, the medicine taking times of patients are reduced, and the compliance of patients is improved.

The invention discloses injectable in-situ gel capable of replacing a surgical catgut for acupuncture and moxibustion embedding. The injectable in-situ gel is mainly prepared from PLGA, HMPC, PEG400, NMP and alpha-asarin or ephedrine. The injectable in-situ gel is good in fluidity, curing forming performance and release degree and high in bioavailability. Meanwhile, the injectable in-situ gel has a good anti-asthma treatment effect, can be used for acupoint injection treatment on asthma and can replace surgical catgut for acupuncture and moxibustion embedding in treatment.