18 results about "Initial burst" patented technology

This invention relates to the field of medical device technology and provides a method for preparing a drug sustained-release coating and a medical device containing the same. The method includes forming a drug sustained-release coating on the surface of the medical device using a drug sustained-release polymer and a drug. The drug sustained-release polymer is a multi-component polymer containing functional groups for anti-protein adsorption, drug sustained-release, and chemical cross-linking. While ensuring the anticoagulant properties and adhesion to the surface of the medical device, the drug sustained-release coating, through the synergistic effect of butyl methacrylate and trimethoxysilyl propyl methacrylate, achieves an initial burst release of less than 20% of the total drug amount and slows down drug release to ensure a drug release cycle in vivo of no less than 21 days. This drug sustained-release coating can release a stable amount of drug to the tissue wall it contacts over a long period, aiming to achieve a long-term therapeutic or preventative effect on diseases such as luminal stenosis.

The present invention relates to a pharmaceutical composition which does not undergo rapid initial burst release of a drug by comprising sustained release microspheres consisting of texipatide or a pharmaceutically acceptable salt thereof, an initial burst release inhibitor, and a biodegradable polymer, has a high drug content with respect to particle size, and has high bioavailability, thus, the composition can minimize patient pain and inflammatory response that may occur when administered to a human body, and thus can be effectively used in the prevention or treatment of diabetes, beta cell dysfunction, hypertension, hyperlipidemia, obesity, and non-alcoholic steatohepatitis.

The present invention relates to a pharmaceutical composition useful for prevention or treatment of diabetes, beta-cell function preservation, high blood pressure, hyperlipidemia, obesity, non-alcoholic steatohepatitis or neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease, as it comprises a sustained-release microsphere comprising semaglutide, a pharmaceutically acceptable salt, hydrate or solvate thereof, and thereby, it can effectively inhibit fatal side-effects by preventing initial burst of a drug and comprise a high content of drug compared to a particle size, and therefore, it can minimize the patient's pain and inflammatory reaction that may occur during administration.

The present invention relates to a pharmaceutical composition which does not undergo rapid initial burst release of a drug by comprising sustained release microspheres consisting of canagliflozin or a pharmaceutically acceptable salt thereof, an initial burst release inhibitor, and a biodegradable polymer, has a high drug content with respect to particle size, and has high bioavailability, thus, it is possible to minimize patient pain and inflammatory response that may occur when administered to a human body, and thus it is effective for preventing or treating diabetes, beta cell dysfunction, hypertension, hyperlipidemia, obesity, non-alcoholic steatohepatitis, or Alzheimer's disease.

The invention relates to a method for altering the release characteristics of a long acting drug delivery device containing at least two drugs in different segments, wherein the segments are arranged to a specific sequence.The invention furthermore relates to a drug delivery device with reduced initial burst containing two different drugs in different segments.The invention further relates to a delivery device manufactured according to the a.m. method and its use in contraception and gynecological therapies.

The invention provides a full-groove drug-loading coating stent, a clamp and a preparation method of the stent, and belongs to the technical field of medical instruments. The support comprises a support base body, matrix grooves are formed in the support base body, and the matrix grooves are evenly distributed in the surface of the support base body in the circumferential direction of the support base body. A plurality of matrix grooves are formed in the support base body in the axis direction of the support base body. The medicine carrying coating comprises an active medicine, nano particles and a degradable polymer, the degradable polymer is arranged on the bottom layer of the matrix groove, and the active medicine and the nano particles are arranged on the top of the degradable polymer. The stent can avoid explosive release at the initial stage of the medicine, realizes stable, lasting and uniform release of the medicine, can reduce toxic stimulation to vascular endothelium, and ensures a long-term treatment effect.

The invention relates to the technical field of biomedical materials, and particularly discloses temperature and pH dual response type hydrogel and a preparation method and application thereof, and the temperature and pH dual response type hydrogel is prepared from the following raw materials through polymerization reaction: a temperature response component N-isopropylacrylamide, a pH response component, a performance adjusting component and a structure enhancing component. According to the invention, beta-(acryloyloxy) propionic acid (beta-CEA) is introduced as a pH response monomer, N-vinyl pyrrolidone (NVP) is introduced as a function enhancing monomer and sodium alginate (SA) to construct a semi-interpenetrating network structure, so that the drug loading capacity of the material is remarkably improved synergistically; the long-acting stable release of the medicine is realized, and the initial burst release phenomenon is effectively avoided; in different pH environments, the compound shows obvious release difference and shows good targeted release potential; meanwhile, the hydrogel has excellent temperature and pH dual responsiveness, reversibility and biocompatibility. The hydrogel is simple and convenient in preparation process and mild in condition, and a reliable material basis is provided for developing a high-performance intelligent drug delivery system.

The invention discloses a progesterone long-acting slow-release injection as well as a preparation method and medical application thereof. The progesterone long-acting slow-release injection comprises a therapeutically effective amount of progesterone, a pharmaceutically acceptable ester organic solvent; the solvent is selected from the combination of glyceryl triacetate and benzyl benzoate. The progesterone long-acting slow-release injection provided by the invention can form a drug reservoir in situ after injection, realizes long-term slow release of progesterone, remarkably reduces the initial burst release effect, and can be used for treating or preventing luteal insufficiency or luteal support in assisted reproduction. In addition, the progesterone long-acting slow-release injection is simple in preparation process, all the components can be dissolved and mixed at the room temperature, and large-scale production is easy to achieve.

The present invention relates to a depot composition comprising a lipid component inside microspheres. The depot composition is capable of controlling the excessive initial burst of an active ingredient from a formulation containing a biodegradable polymer and an active ingredient and has excellent suspensibility, and thus, even when using same as an injection, a layperson can obtain the effect of the active ingredient uniformly and continuously.

This invention discloses a method for preparing collagen-containing bioactive glass; this invention belongs to the field of biomedical materials technology. This invention is the first to construct a quaternary innovative system of "modified HAPNTs-Eucomycin-VEGF microspheres-ε-polylysine," which addresses degradation regulation, tissue-directed induction, long-term promotion of angiogenesis, and broad-spectrum antibacterial effects, covering the core needs of multi-tissue repair. Simultaneously, it employs an "ultrasound-stirring synergistic dispersion + nitrogen-protected collagen" process to solve the problems of inorganic particle aggregation and collagen denaturation, improving the uniformity of particle dispersion within the material by more than 40%. The VEGF sustained-release microsphere re-emulsification-freeze-drying process increases the growth factor encapsulation rate to over 85%, avoiding initial burst release. By adjusting the amount of modified HAPNTs added, this invention can precisely control the material degradation cycle to 1-6 months, adapting to the regeneration rates of soft tissue, bone tissue, and nerve tissue. Furthermore, the differentiated molding process allows for adjustable mechanical properties of the material, meeting the mechanical requirements of different tissues.

The invention relates to the technical field of composite material preparation, in particular to a preparation method and drug release application of multi-mode magnetic field control permanent magnetic aerogel. Firstly, a vertical orientation magnetic field is applied, so that the permanent magnetic neodymium iron boron aerogel is stably kept in a vertical posture in gastric juice, the contact area between the drug release surface of the aerogel and the gastric juice is minimum, and the non-specific leakage and the initial burst release effect of the drug can be effectively inhibited; secondly, under the condition of no magnetic field, the aerogel is kept in a horizontal floating state in gastric juice, the drug release surface is in complete contact with the gastric juice, and the drug is freely and slowly released from aerogel pore channels, so that low-content release is realized; finally, by applying a dynamic horizontal rotating magnetic field, the aerogel in a lying state is driven to stably rotate, high-content release of the medicine is actively and efficiently triggered, the problems that a traditional oral preparation is poor in stomach targeting, uncontrollable in release, short in residence time and the like are solved, and an innovative solution is provided for intelligent and accurate medicine delivery.

The invention relates to the technical field of controlled release coatings, and discloses a drug-loaded PLGA core-coated PVDF-HFP shell nanoparticle and application thereof. The particle size of the drug-loaded PLGA core-coated PVDF-HFP shell nanoparticles prepared by the invention can be controlled to be 100-500nm, and the nanoparticles have good core-shell structure integrity, can effectively reduce initial burst release of an anti-restenosis drug and realize sustained release of the drug, and have stability in a physiological environment. By regulating and controlling the shell thickness of the PVDF-HFP, the purposes of degrading the PLGA and regulating and controlling the drug release rate by the PVDF-HFP can be achieved. The drug-loaded PLGA core-coated PVDF-HFP shell nanoparticles with different shell layer thicknesses are mixed and sprayed on the surface of the stent as a coating, and drug sequential release can be realized through different particle sizes of the drug-loaded nanoparticles, so that effective release of drugs in the early stage, the middle stage and the later stage after the stent is implanted is realized, and the requirements of different stages of vascular repair on the drugs are further met.

The application belongs to the technical field of biomedical materials, and particularly relates to a hydrogel based on a magnesium oxide-based nanoscale enzyme loaded with polydopamine-manganese dioxide as well as a preparation method and application thereof. The magnesium oxide-based nanoscale enzyme of polydopamine-manganese dioxide is integrated in a double-crosslinked three-dimensional network hydrogel which can be cured in situ and has a self-healing property, fundamentally overcoming the problems of coalescence inactivation and initial burst release of the nanoscale enzyme under a complex physiological microenvironment, and realizing long-acting, stable and on-demand supply of active components (Mg 2+ , Mn 2+ ) in a lesion area. Moreover, due to the self-healing and in-situ light curing properties of the hydrogel, the system can perfectly fit and anchor in an irregular periodontal pocket after injection, thereby constructing a local, persistent and intelligently responsive drug delivery and microenvironment regulation platform, and providing sustained biochemical and mechanical support for periodontal tissue regeneration.

The application discloses a composite drug sustained-release system based on a biomimetic glycocalyx coating and a medical catheter. The sustained-release system comprises, in sequence, an adhesion layer, a drug storage layer and a biomimetic glycocalyx coating arranged on the surface of a base. The adhesion layer is formed by in-situ polymerization of polyphenols. The drug storage layer embeds active drugs through hydrophobic or amphiphilic polymers. The biomimetic glycocalyx coating simulates the structure of vascular endothelium and is formed by cross-linking of modified polyethylene glycol and biological macromolecules through polyphenols and metal ions. The application can realize self-repairing of damage by using the double cross-linking network of the biomimetic glycocalyx coating, and can synergistically regulate drug release kinetics through a high hydration physical barrier and the storage layer, thereby significantly reducing the friction coefficient of intervention, and also endowing the medical catheter with properties such as antithrombosis and drug sustained release, effectively inhibiting initial burst release of drugs and prolonging the release period, and significantly improving the mechanical resistance, biocompatibility and safety of the medical catheter.

The application relates to the technical field of high polymer composite materials, and provides a composite microsphere, which comprises a core body and a coating layer covering the core body, the core body comprises doped hydroxyapatite doped with zinc ions and cerium ions, the coating layer comprises polylactic acid and beta-cyclodextrin, and graphene oxide is distributed between the core body and the coating layer; the composite microsphere has a porous structure, and beta-cyclodextrin is filled in at least part of the porous structure. The composite microsphere provided by the application can significantly improve the drug encapsulation performance of the composite microsphere by utilizing the synergistic effect among the Ce / Zn co-doped doped hydroxyapatite, polylactic acid, graphene oxide and beta-cyclodextrin, can effectively inhibit and reduce the initial burst release phenomenon of the drug, and can construct a stable, long-acting and controllable drug sustained-release system.

Disclosed are pharmaceutical compositions containing micronized antibodies encapsulated and / or dispersed in polymeric particles for antibody delivery. The judicious identification of (i) a subset of polymers, (ii) polymers with certain average molecular weights, (iii) a subset of antibody loadings, and / or (iv) pre-loading antibody processing, leads to formation of polymeric particles that possess minimal to no initial burst release of micronized antibody at zero time point. The pharmaceutical compositions are formulated for oral, subcutaneous, or percutaneous administration, and are particularly suited for treatment regimens that involve antibody-based therapy.

The invention belongs to the technical field of drug sustained-release preparations, and discloses a method for improving the effectiveness of a PQQ sustained-release preparation. According to the method, PQQ and basic amino acid form ion pairs, the ion pairs are loaded on an ion cross-linked polysaccharide gel core, a thioacetal cross-linked reactive oxygen species (ROS) response shell layer is constructed on the surface of the core, the outer layer is coated with an adhesion quick-release polysaccharide layer containing a catechol or dopamine structure, and the outer layer PQQ accounts for 10%-20% of the total amount of the preparation PQQ. The obtained multi-layer particles are prepared into an oral preparation, first-dose quick release can be generated in a small intestine environment, particle adhesion is maintained, more than 90% of slow release can be realized within 8 hours, and when oxidative stress is enhanced, the ROS responds to a shell layer to improve the release rate in the middle and later periods, so that initial burst release is effectively avoided, the action time of PQQ in intestinal tracts is prolonged, and the curative effect of PQQ on intestinal tracts is improved. The in-vivo bioavailability and the utilization efficiency of the oral PQQ are obviously improved.

This invention relates to a stimulus-responsive drug delivery core-shell structure microsphere with an asymmetric partially coated shell, its preparation method, and its applications. The microsphere comprises a stimulus-responsive core layer and an asymmetric shell. The stimulus-responsive core layer is composed of a stimulus-responsive carrier material and loaded with an active ingredient. The asymmetric shell partially coats the outer surface of the stimulus-responsive core layer, exposing a portion of the uncoated area of ​​the core layer, thereby forming an outlet channel for the release of the active ingredient. The asymmetric partially coated structure of this invention effectively resolves the contradiction between severe initial burst release and delayed response in traditional stimulus-responsive carriers. It significantly inhibits initial burst release in a non-stimulated state, while achieving sensitive pulsed release through a release window upon stimulation. This on-demand drug delivery characteristic has broad application prospects in the field of intelligent drug delivery.