45 results about "Trimetazidine hydrochloride" patented technology

The invention discloses a trimetazidine hydrochloride sustained release tablet prepared from the following ingredients in percentage by weight: 10-25% of trimetazidine hydrochloride, 20-60% of hydrophilic gel skeleton material, 1-20% of a hydrophobic blocker, 15-55% of filler, 1-10% of a lubricant, 0 or 1-10% of a coating material and a proper dosage of adhesive. A wet granulation method is adopted in the preparation process. After the trimetazidine hydrochloride sustained release tablet disclosed by the invention touches water, the hydrophilic gel skeleton material can expand rapidly to form a gel layer with a plurality of pores, a drug can be slowly released through the pores, and the hydrophobic blocker can partially block the pores to avoid the burst release of the drug. Proper mass and proper proportion of hydrophilic gel skeleton material and hydrophobic blocker are added to realize slow and uniform release of the drug under the cooperation of the two ingredients and well avoid the burst release phenomenon so as to beneficially ensure the safety and effectiveness of drug therapy.

The invention discloses a long-acting sustained-release pellet and a preparation method thereof. The long-acting trimetazidine hydrochloride sustained-release pellet comprises a drug-containing core and a sustained-release coating layer from inside to outside sequentially, wherein an optional isolation coating layer is arranged between the drug-containing core and the sustained-release coating layer; the isolation coating layer accounts for 0-15 percent of the mass of the drug-containing core, and the sustained-release coating layer accounts for 5-30 percent of the mass of the drug-containing core; a gastrointestinal adhesive is contained in the sustained-release coating layer. According to the trimetazidine hydrochloride sustained-release pellet, the prescription is meticulously designed, the drug-containing core is uniformly coated by utilizing the sustained-release coating material, so that slow and uniform drug release of the drug-containing core can be maintained, the active component releasing speed can be reduced, the time for reaching the peak can be postponed, the pellet can be constantly and stably released in 24 hours, the blood concentration stability can be maintained, and the phenomenon of insufficient blood concentration in morning ischemia can be avoided. The administration frequency can be reduced to once a day, and the compliance of patients can be improved.

The invention belongs to the field of sustained release medicament preparations, and particularly relates to a trimetazidine hydrochloride sustained release tablet and a preparation method thereof. The trimetazidine hydrochloride sustained release tablet is prepared from 40 to 45 parts of trimetazidine hydrochloride, 100 to 200 parts of polyoxyethylene, 100 to 200 parts of dextrin, 60 to 100 parts of 3-10 percent ethyl cellulose solution and 3 to 5 parts of magnesium stearate through material mixing, soft material preparing, drying, tabletting and other steps. In the trimetazidine hydrochloride sustained release tablet, the polyoxyethylene serves as an auxiliary material, and the sustained release tablet is prepared from the medicaments by a method of direct tabletting or tabletting aftergranulating. The drug dissolution of the trimetazidine hydrochloride sustained release tablet reaches about 90 percent 6 hours later, so the sustained release tablet is only required to be taken twice a day; therefore, the sustained release tablet has the advantages of releasing drug slowly and uniformly to reduce release rate and postpone peak time, reducing the number of administration times per day, improving the compliance of patients to the medicament and the like. Furthermore, the preparation method of the invention is simple and easy to operate.

The invention provides a high-stability sustained-release tablet prepared by using hydroxy propyl cellulose. The sustained-release tablet comprises the following components in parts by weight: 5-40 parts of trimetazidine hydrochloride and 10-85 parts of hydroxy propyl cellulose. A preparation method for the high-stability sustained-release tablet is a common wet granulation tableting process or a powder direct tableting process. According to the trimetazidine hydrochloride sustained-release tablet prepared by using the hydroxy propyl cellulose as a sustained-release material, the problem of low stability of a commercially available trimetazidine hydrochloride sustained-release tablet prepared by using the hydroxy propyl cellulose as a sustained-release material is solved.

The invention provides a novel synthesis path of trimetazidine hydrochloride. The novel synthesis path comprises the steps of: reacting 1,2,3-phenol (II) react with Boc piperazine to generate a compound III, reacting the compound III react with dimethyl sulfate to generate a compound IV, and carrying out deprotection and salifying on the compound IV to obtain trimetazidine hydrochloride. The novel synthesis path has the advantages of simple process, high yield and low cost and is easy for industrial production.

The invention discloses a trimetazidine hydrochloride osmotic pump controlled-release tablet and a preparation method thereof, which is a single-chamber osmotic pump controlled-release preparation, comprising a single-layer tablet core, an insoluble semipermeable film coat and small holes for drug release. The present invention can effectively improve drug hysteresis and drug release terminal residues by screening and optimizing the combination of fillers, adjust drug release rate and controlled release time, and reach a certain blood drug concentration in a relatively short period of time, forming a stable and constant rate release, and realizing rapid drug release. The purpose of drug controlled release design is to achieve effective, stable drug release and reduce side effects.

The invention provides a trimetazidine hydrochloride bi-layer osmotic pump controlled release tablet and a preparation method thereof. The osmotic pump controlled release tablet is formed by a drug-containing layer, a booster layer and a coating film, wherein the drug-containing layer comprises the following components in percentage by weight: 10-50% of trimetazidine hydrochloride, 30-80% of suspension agent and the balance of other auxiliary materials; the booster layer comprises the following components in percentage by weight: 20-90% of swelling agent, 5-70% of osmotic active substance and 0.5-5% of lubricating agent; the semipermeable coating film comprises 10-20g of semipermeable high polymer material and 1-5g of water-soluble pore-forming agent every 100 tablets. The trimetazidine hydrochloride bi-layer osmotic pump controlled release tablet can realizes constant release of drug in the body of a patient without being affected by pH value of a medium environment, enzyme, gastrointestinal motility and food, and is capable of maintaining the stability of plasma concentration of drug, reducing toxic and side effects of drug, decreasing dosing frequency and improving compliance of the patient.

The invention relates to a method for preparing trimetazidine hydrochloride. In the method, 2,3,4-trimethoxybenzaldehyde and piperazine are used as raw materials, palladium carbon is used as a catalyst for catalytic hydrogenation so as to salify to generate the trimetazidine hydrochloride, and a solvent used in the hydrogenation is mixed solution of water and ethanol. The solution ensures the complete reaction, cannot cause partial excess of the 2,3,4-trimethoxybenzaldehyde and can reduce impurities.

The invention provides a high-stability sustained-release tablet prepared by using hydroxy propyl cellulose. The sustained-release tablet comprises the following components in parts by weight: 5-40 parts of trimetazidine hydrochloride and 10-85 parts of hydroxy propyl cellulose. A preparation method for the high-stability sustained-release tablet is a common wet granulation tableting process or a powder direct tableting process. According to the trimetazidine hydrochloride sustained-release tablet prepared by using the hydroxy propyl cellulose as a sustained-release material, the problem of low stability of a commercially available trimetazidine hydrochloride sustained-release tablet prepared by using the hydroxy propyl cellulose as a sustained-release material is solved.

The invention relates to a trimetazidine hydrochloride sustained-release pharmaceutical composition and a preparation method thereof. The composition consists of an effective amount of trimetazidine hydrochloride and pharmaceutical auxiliary materials, the ratio of the main drug is 10%-20%, the slow-release material hypromellose is 10%-45%, and the slow-release material carbomer is 22%. ~40%, Sustained-release material Eudragit 0.2%~10%, diluent calcium hydrogen phosphate dihydrate 10%~48%, glidant colloidal silicon dioxide 0.3%~1.5%, magnesium stearate 0.5%~ 1.5%. The invention also provides a preparation method of the trimetazidine hydrochloride composition, that is, granulating through direct mixing process or fluidized bed, tableting and coating. The invention overcomes the defect of trimetazidine hydrochloride in the prior art that multiple administrations are required due to its short relative half-life, and can avoid side effects caused by excessive initial concentration of administration; the preparation process is simple and is suitable for large-scale industrial production.

The invention relates to a trimetazidine hydrochloride tablet preparation, in particular to a sublingual tablet containing trimetazidine hydrochloride medicine, which contains trimetazidine hydrochloride, at least one diluent, at least two flavoring agents, at least one taste masking agent, at least one disintegrating agent and at least one lubricant, and the preparation contains 2mg of trimetazidine hydrochloride. The trimetazidine hydrochloride sublingual tablet in a specific proportion meets the requirements of a sublingual tablet preparation in quality, and has high disintegration and dissolution rates. Other advantages of the pharmaceutical preparation include simple process preparation. The invention further relates to a preparation method of the trimetazidine hydrochloride tablet, a sample prepared by the method is good in reproducibility, and the quality of the sample conforms to relevant regulations of sublingual tablets.

The invention provides a kind of trimetazidine oxalate, its molecular formula is C 16 h 24 N 2 o 7 , the trimetazidine oxalate is obtained by reacting trimetazidine and oxalic acid at a molar ratio of 1:1. The angle of repose of the trimetazidine oxalate is smaller than that of trimetazidine hydrochloride, and its surface morphology is flaky, which improves the fluidity and moisture absorption of the drug compared with the prismatic crystals of the trimetazidine hydrochloride bulk drug At the same time, the tensile strength of the trimetazidine oxalate reaches a maximum value of 3.99MPa at 150MPa, which is significantly higher than that of trimetazidine hydrochloride under the same pressure, which improves the tableting performance of the medicine.

The invention provides a trimetazidine hydrochloride sustained-release preparation and a preparation method thereof. The trimetazidine hydrochloride sustained-release preparation is composed of sustained-release microtablets and capsule shells, and each sustained-release capsule is composed of a Sustained release microtablets are filled. The microtablet is mainly composed of trimetazidine hydrochloride, a binder, a diluent, a sustained-release material and a lubricant. The trimetazidine hydrochloride sustained-release preparation comprises the following components in percentage by weight: trimetazidine hydrochloride 50-80%, diluent 1-20%, binder 1-20%, sustained-release material 10-40% %, lubricant 0.1 to 5%. The invention also discloses a preparation method of the trimetazidine hydrochloride sustained-release preparation: each material is granulated and then pressed into microtablets, and then filled into hollow capsules according to a certain amount. The preparation process has good stability, simple process and high production efficiency, and is suitable for industrialized mass production.