The whole preparation process of the sustained-release microparticles is at normal or low temperature, which is highly advantageous for the preparation of a polymer-based composition from a high-temperature-sensitive drug, particularly a protein, nucleic acid and peptide drug, and the bioactivity of the active substance can be maintained to the greatest extent throughout the process compared to the disclosed technology; at the same time, the prepared sustained-release microparticles have an excellent sustained-release effect close to zero order, and the drug concentration is stabilized during the release, which overcomes the defects that the microparticles obtained by the conventional S/O/W process of pre-preparing the drug microparticles have no drug release in the earlier stage and a rapid release of the drug in the later stage; and in addition, the sustained-release microparticles have higher drug loading rate and drug encapsulation rate.
A tertiary amine pharmaceutical composition, comprising a medicine having a tertiary amine structure, a biocompatible polymeric material, and a quaternary ammonium salt impurity. The pharmaceutical composition is obtained by dissolving or dispersing the medicine in halogenated hydrocarbon or a mixed solvent mainly containing halogenated hydrocarbon or a solution containing halogenated hydrocarbon. The quaternary ammonium salt impurity is generated from reacting the medicine having the tertiary amine structure with halogenated hydrocarbon, characterized in that, the pharmaceutical composition comprises 40 to 80 wt% of the biocompatible polymeric material, 20 to 60 wt% of the medicine having the tertiary amine structure; the content of the quaternary ammonium salt impurity is less than 0.05 wt%; and the content of halogenated hydrocarbon in the composition is less than 1.5 wt%. Furthermore, the quaternary ammonium salt impurity does not increase or increase slowly during storage, complying with the requirements of pharmaceutical regulations.
A61K 31/519 - Pyrimidines; Pyrimidines hydrogénées, p.ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p.ex. rifampine, thiothixène
A61P 25/18 - Antipsychotiques, c. à. d. neuroleptiques; Médicaments pour le traitement de la manie ou de la schizophrénie
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
3.
Preparation method of sustained-release microparticles
In the present invention, the whole preparation process of the sustained-release microparticles is at normal or low temperature, which is highly advantageous for the preparation of a polymer-based composition from a high-temperature-sensitive drug, particularly a protein, nucleic acid and peptide drug, and the bioactivity of the active substance can be maintained to the greatest extent throughout the process compared to the disclosed technology; at the same time, the prepared sustained-release microparticles have an excellent sustained-release effect close to zero order, and the drug concentration is stabilized during the release, which overcomes the defects that the microparticles obtained by the conventional S/O/W process of pre-preparing the drug microparticles have no drug release in the earlier stage and a rapid release of the drug in the later stage; and in addition, the sustained-release microparticles have higher drug loading rate and drug encapsulation rate.
The present invention relates to a targeted hydrophobic anti-tumor drug nanoformulation, which comprises a hydrophobic anti-tumor drug and a carrier with a mass ratio of 1:4-32.5, wherein the carrier is composed of 37.5-95.3 wt % albumin and 4.7-62.5 wt % hyaluronic acid-albumin conjugate, and the hyaluronic acid-albumin conjugate is prepared by albumin and hyaluronic acid with a molar ratio of 1:1-20. A preparation method of the nanoformulation comprises: preparing hyaluronic acid-albumin conjugate; formulating carrier solution; formulating drug solution; and preparing nanoformulation. The nanoformulation has even particle size distribution and good dispersibility, is stable without aggregating. The particle size of the lyophilized nanoformulation after being redissolved substantially remains unchanged, the yield of the nanoformulation is high and the efficacy is good after being filtered by a millipore filter (0.22 μm).
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p.ex. fungichromine ayant des cycles à quatre chaînons, p.ex. taxol
A61K 31/436 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à six chaînons ayant l'oxygène comme hétéro-atome du cycle, p.ex. rapamycine
A61K 31/4745 - Quinoléines; Isoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. phénanthrolines
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 31/704 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p.ex. phloridzine liés à un système carbocyclique condensé, p.ex. sennosides, thiocolchicosides, escine, daunorubicine, digitoxine
Disclosed in the present invention are a lenalidomide gastro-retentive sustained-release tablet and a preparation method therefor. The sustained-release tablet comprises 3 to 14 wt% of lenalidomide, 14 to 68 wt% of a release enhancer having low bulk density, 23 to 70 wt% of a sustained-release material having a low bulk density, and the balance of other pharmaceutically acceptable excipients. The release enhancer has a bulk density of 0.24 to 0.52 g/cm3. The bulk density of the sustained-release material is 0.29 to 0.51 g/cm3. The sustained-release tablet of the present invention is in a floating state in the gastric environment, and is not directly discharged from the stomach due to gastric emptying, has the effect of gastric retention, and is not easily discharged with the gastric contents, and has high drug bioavailability and small side effects.
A61K 31/454 - Pipéridines non condensées, p.ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p.ex. pimozide, dompéridone
A61K 9/22 - Pilules, pastilles ou comprimés du type à libération prolongée ou discontinue
Disclosed is a long-acting slow-release pharmaceutical preparation. The pharmaceutical preparation contains 25%-60% of a water-insoluble or sparingly-soluble drug and 40%-75% of a high-molecular polymer. After the pharmaceutical preparation is subjected to one time of intramuscular injection administration, the ratio of a maximum plasma concentration to a minimum plasma concentration in a main release period is less than 5; the slope of a linear trend line of a cumulative release curve is less than 8 under an in-vitro simulated release condition; the daily release amount is less than 8.5%; and the simulated release condition is a buffer solution with the temperature of 37±0.5°C and the pH of 6.5-8.4. The prepared long-acting slow-release pharmaceutical preparation in the present invention has the beneficial effects that an obvious release delay period or a burst release phenomenon are avoided after administration, a steady state plasma concentration can be quickly achieved, the plasma concentration with a relatively small fluctuation range can be maintained in several weeks or longer after single administration, and the pharmaceutical preparation can take effect quickly and has good compliance with a patient.
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
A61K 45/00 - Préparations médicinales contenant des ingrédients actifs non prévus dans les groupes
A61K 31/519 - Pyrimidines; Pyrimidines hydrogénées, p.ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p.ex. rifampine, thiothixène
A61P 25/18 - Antipsychotiques, c. à. d. neuroleptiques; Médicaments pour le traitement de la manie ou de la schizophrénie
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p.ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
A long-acting sustained-release preparation of a drug for treating Parkinson's disease and a preparation method thereof. The long-acting sustained-release preparation is microspheres comprising rasagiline or a pharmaceutically acceptable salt thereof and a biodegradable and biocompatible high molecular weight polymer. The microspheres comprise microspheres with an average particle size of 0.5-5 mm and microspheres with an average particle size of 20-150 mm.
Disclosed is a poorly water-soluble/slightly water-soluble sustained release pharmaceutical composition, comprising more than two poorly water-soluble/slightly water-soluble sustained release pharmaceutical microspheres with different release behaviours. A sustained release polymer is at least one of polylactide, lactide-glycolide copolymer, and the copolymers thereof with polyethylene glycol.
Disclosed are a sustained release composition of aripiprazole and a derivative thereof and a preparation method therefor. The non-solvent preparation raw materials of the sustained release composition comprise aripiprazole and a sparingly water-soluble polymer. The sustained-release composition has a good release performance, has no obvious release delay period or burst release phenomenon, and can maintain a stable blood drug concentration for several weeks or more, and has a relatively good stability.
A61K 9/54 - Préparations en capsules, p.ex. de gélatine, de chocolat du type à libération prolongée ou discontinue contenant des particules distinctes avec des revêtements de différentes épaisseurs ou de différents matériaux
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p.ex. rifampine, thiothixène
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
A61P 25/18 - Antipsychotiques, c. à. d. neuroleptiques; Médicaments pour le traitement de la manie ou de la schizophrénie
10.
RISPERIDONE SUSTAINED RELEASE COMPOSITION AND PREPARATION METHOD THEREFOR
Disclosed are a sustained release composition and a preparation method therefor. The non-solvent preparation raw materials comprise risperidone, a sparingly water-soluble polymer and a release regulator. The release regulator comprises an organic lipophilic substance. The preparation method comprises the following steps: (1) dissolving the non-solvent preparation raw materials in an organic solvent to form an internal oil phase; (2) dissolving a surfactant in an aqueous medium to form an external aqueous phase; and (3) adding the internal oil phase obtained in step (1) to the external aqueous phase to prepare an emulsion, and then hardening microparticles in the solution by means of solvent evaporation or solvent extraction, collecting the microparticles, and washing and drying same.
A61K 9/52 - Préparations en capsules, p.ex. de gélatine, de chocolat du type à libération prolongée ou discontinue
A61K 31/519 - Pyrimidines; Pyrimidines hydrogénées, p.ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 47/12 - Acides carboxyliques; Leurs sels ou anhydrides
A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes ; Huiles, graisses ou cires naturelles ou naturelles modifiées, p.ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
A61P 25/18 - Antipsychotiques, c. à. d. neuroleptiques; Médicaments pour le traitement de la manie ou de la schizophrénie
11.
RISPERIDONE SUSTAINED RELEASE COMPOSITION AND PREPARATION METHOD THEREFOR
Disclosed are a risperidone sustained release composition and a preparation method therefor. The non-solvent preparation raw materials of the composition comprise risperidone, a sparingly water-soluble polymer and a release regulator. The release regulator comprises an organic lipophilic substance and an organic hydrophilic substance.
A61K 9/52 - Préparations en capsules, p.ex. de gélatine, de chocolat du type à libération prolongée ou discontinue
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
A61K 47/12 - Acides carboxyliques; Leurs sels ou anhydrides
A61K 47/10 - Alcools; Phénols; Leurs sels, p.ex. glycérol; Polyéthylène glycols [PEG]; Poloxamères; Alkyléthers de PEG/POE
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. carbomères
A61K 31/519 - Pyrimidines; Pyrimidines hydrogénées, p.ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61P 25/18 - Antipsychotiques, c. à. d. neuroleptiques; Médicaments pour le traitement de la manie ou de la schizophrénie
Disclosed are an implant and a preparation method therefor. The raw materials of the implant comprise the following components in parts by weight: 25-65 parts of a sparingly water-soluble/slightly water-soluble drug, 35-75 parts of a sparingly water-soluble polymer, and 0-10 parts of a release regulator. The preparation method comprises: (1) dissolving the sparingly water-soluble/slightly water-soluble drug and the release regulator in an organic solvent to obtain a sparingly water-soluble/slightly water-soluble drug solution; (2) mixing the sparingly water-soluble polymer and the drug solution obtained in step (1), and removing the organic solvent to obtain a solid mixture; and (3) placing the solid mixture obtained in step (2) into a hot melt extruder for extrusion and cutting, or subjecting the solid mixture obtained in step (2) to press forming so as to obtain the implant. The preparation method effectively avoids or reduces the phenomena of the crystallization or agglomeration of the drug and the degradation of the polymer, and is beneficial for the long-term release of the drug.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 45/00 - Préparations médicinales contenant des ingrédients actifs non prévus dans les groupes
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
13.
SUSTAINED RELEASE COMPOSITION OF PALIPERIDONE AND DERIVATIVE THEREOF AND PREPARATION METHOD FOR SAME
Disclosed are a sustained release composition of paliperidone and a derivative thereof and a preparation method therefor. The raw materials comprise paliperidone or a paliperidone derivative and a sparingly water-soluble polymer. The sustained release composition has a good sustained release performance and stability.
Provided are a sparingly water-soluble/slightly water-soluble drug sustained release composition, wherein the non-solvent preparation raw materials of the sparingly water-soluble/slightly water-soluble drug sustained release composition comprise a release regulator. The release regulator is added to the preparation raw materials of the sparingly water-soluble/slightly water-soluble drug sustained release composition, and the release regulator is capable of effectively regulating the release rate of the sparingly water-soluble/slightly water-soluble drug in the sustained release composition, such that the sparingly water-soluble/slightly water-soluble drug sustained release composition has no obvious release delay period or burst release phenomenon after administration, has a good sustained release performance, can maintain a therapeutic blood drug concentration for several weeks or longer, has a relatively good stability, and can still preserve the release behaviour thereof after long-term storage. Also provided is a method for preparing the sparingly water-soluble/slightly water-soluble drug sustained release composition.
A61K 47/10 - Alcools; Phénols; Leurs sels, p.ex. glycérol; Polyéthylène glycols [PEG]; Poloxamères; Alkyléthers de PEG/POE
A61K 47/12 - Acides carboxyliques; Leurs sels ou anhydrides
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
15.
PREPARATION METHOD OF SUSTAINED RELEASE MICROPARTICULATES, SUSTAINED RELEASE MICROPARTICULATES THEREBY AND USE THEREOF
A preparation method of sustained release microparticulates, comprising the following steps: 1) preparing a solid dispersion of water-soluble drug and biodegradable and biocompatible water-insoluble polymer; 2) dissolving the prepared solid dispersion in an organic solvent to obtain a solid dispersing emulsion; 3) injecting the obtained solid dispersing emulsion into an oil solution which contains surfactant to form a uniform emulsion; and 4) solidifying microparticulates in the emulsion by means of solvent volatilization or solvent extraction, collecting and washing the solidified microparticulates, and drying the microparticulates to obtain the sustained release microparticulates. The sustained release microparticulates prepared by the preparation method and use thereof in an implanted sustained release pharmaceutical composition. The whole process of the preparation method of the sustained release microparticulates is carried out at normal temperature or low temperature; the prepared sustained release microparticulates have a sustained-released effect close to zero order; the drug concentration is stable in the sustained release period.
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
A61K 31/7088 - Composés ayant au moins trois nucléosides ou nucléotides
A61K 38/16 - Peptides ayant plus de 20 amino-acides; Gastrines; Somatostatines; Mélanotropines; Leurs dérivés
Sustained-release microgranules and a method for preparing same. The method comprises the following steps: 1) preparing a solid dispersion of a water-soluble drug and a biodegradable and biocompatible water-insoluble polymer; 2) dissolving the prepared solid dispersion in an organic solvent to form a solid dispersion emulsion; 3) injecting the obtained solid dispersion emulsion into a surfactant-containing aqueous solution to form a uniform emulsion; and 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 method for preparing sustained-release microgranules is carried out at normal temperature or low temperature in the whole process, the prepared sustained-release microgranules have an approximate zero-level sustained-release effect, and the drug has a stable concentration in a sustained-release period.
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
A61K 31/7125 - Acides nucléiques ou oligonucléotides ayant des liaisons internucléosides modifiées, c. à d. autres que des liaisons 3'-5' phosphodiester
17.
SOLID DISPERSION, PREPARATION METHOD FOR SAME, AND APPLICATIONS THEREOF
A solid dispersion and a preparation method therefor. The solid dispersion comprises a water-soluble medicament and a water-soluble polymer, the mass ratio of the two being 1 : (1-25), and the mass percent of the water-soluble medicament in the solid dispersion being 3.8-50%. The solid dispersion is applicable in preparing a solid implant, an in situ gel implant, and a sustained release particle.
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
18.
METHOD FOR PREPARING SUSTAINED RELEASE MICROPARTICLES, PREPARED SUSTAINED RELEASE MICROPARTICLES AND APPLICATION THEREOF
A method for preparing sustained release microparticles, comprising the following steps: 1) preparing a solid dispersion of a water-soluble drug and a biodegradable and biocompatible water-insoluble polymer; 2) dissolving the prepared solid dispersion in an organic solvent to form a solid dispersion emulsion; 3) injecting the obtained solid dispersion emulsion into an oil solution with surfactants to form an uniform emulsion; and 4) curing microparticles in the emulsion by means of solvent evaporation or solvent extraction, and collecting, washing, and drying the microparticles to obtain the sustained release microparticles. Sustained release microparticles prepared by means of the method for preparing sustained release microparticles as well as application of the sustained release microparticles in an implantable sustained release pharmaceutical composition. The method for preparing sustained release microparticles is carried out at the normal temperature or a low temperature in full procedures. The prepared sustained release microparticles have an approximate zero-level sustained release effect, and the drug is stable in concentration in the sustained release period.
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
A61K 38/16 - Peptides ayant plus de 20 amino-acides; Gastrines; Somatostatines; Mélanotropines; Leurs dérivés
A method for preparing sustained release microparticles, comprising the following steps of: 1) preparing a solid dispersion of a water-soluble drug and a biodegradable and biocompatible water-insoluble polymer; 2) dissolving the prepared solid dispersion into an organic solvent to form an emulsion of the solid dispersion; 3) injecting the obtained emulsion of the solid dispersion into an aqueous solution containing a surfactant to form a uniform emulsion; 4) curing microparticles in the emulsion by means of solvent volatilization or solvent extraction, collecting the microparticles, washing and drying same to obtain the sustained release microparticles. The whole method for preparing the sustained release microparticles is carried out at a normal temperature or a low temperature, the prepared sustained release microparticles have a near-zero order sustained release effect, and the concentration of the drug remains stable during the sustained release period.
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
Disclosed is a targeted hydrophobic anti-tumour medicine nanometre preparation, comprising a hydrophobic anti-tumour medicine and a carrier with a mass ratio of 1:4-32.5, wherein the carrier is composed of 37.5-95.3 wt% of albumin and 4.7-62.5 wt% of hyaluronic acid-albumin conjugate, and the hyaluronic acid-albumin conjugate is prepared by albumin and hyaluronic acid with a molar ratio of 1:1-20. The method for preparing the nanometre preparation comprises: preparing the hyaluronic acid-albumin conjugate; formulating the carrier solution; formulating the medicine solution; and preparing the nanometre preparation. The particle diameter distribution of the nanometre preparation is relatively even, and the dispersibility is good, stable without aggregating. The particle diameter of the nanometre preparation redissolved after being freeze-dried substantially remains unchanged, and the recovery rate of the nanometre preparation is high and the efficacy is good after filtering (0.22 ìm) with a millipore filter.
A61K 9/19 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres lyophilisées
A61K 47/42 - Protéines; Polypeptides; Leurs produits de dégradation; Leurs dérivés p.ex. albumine, gélatine ou zéine
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p.ex. fungichromine ayant des cycles à quatre chaînons, p.ex. taxol
A61K 31/4745 - Quinoléines; Isoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. phénanthrolines
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p.ex. phosphate de pyridoxal
A61K 31/704 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p.ex. phloridzine liés à un système carbocyclique condensé, p.ex. sennosides, thiocolchicosides, escine, daunorubicine, digitoxine
A61K 38/14 - Peptides contenant des radicaux saccharide; Leurs dérivés
A trimetazidine hydrochloride long-lasting, sustained-release micropellet comprises, from the inside outward, a drug-containing pellet core, a sustained-release coating layer, and, optionally, an isolation coating layer provided between the core and the sustained-release coating. The mass weight of the isolation coating layer is 0-15% of that of the core, the mass weight of the sustained-release coating layer is 5-30% of that of the core, and the sustained-release coating layer contains a gastrointestinal tract adhesive. The release rate of the active components in the trimetazidine hydrochloride long-lasting, sustained-release micropellet is reduced, delaying the peak time, such that release occurs steadily and continuously over 24 hours and plasma concentration stability is maintained, thereby reducing the dosage rate to once per day.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p.ex. pipérazine
A polypeptide-medicine-slow-releasing microsphere preparation. The preparation method for the preparation comprises the steps: dissolving a polylactic acid-glycolic acid polymer or a polylactic acid together with a protective agent and polypeptide medicine in an organic solvent to form a uniform mixed solution; adding the mixed solution to an oil phase to form an emulsion; removing the organic solvent, centrifuging, washing, and freezing and drying to obtain the polypeptide-medicine-slow-releasing microspheres. By using the 0/0 method, outward diffusion of the medicine into water phase is eliminated, and the medicine embedding rate is raised to 60% to 95%. The release time for a bioactive polypeptide medicine can last several weeks to several months, and in vitro release approximately matches zero-order release.
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol o
A61K 38/00 - Préparations médicinales contenant des peptides
brevets
