11 results about "Rifapentine" patented technology

This application relates to a rifapentine-containing pharmaceutical composition and its preparation method. The rifapentine-containing granules are prepared by dry granulation, which reduces the content of impurities present in existing pharmaceutical compositions, especially the content of the genotoxic impurity 1-cyclopentan-4-nitrosopiperazine, thereby improving the safety and efficacy of the drug.

The invention relates to the technical field of nano-micelles, in particular to rifapentine-loaded bone targeting nano-micelles as well as a preparation method and application thereof.The rifapentine-loaded bone targeting nano-micelles are prepared by accurately controlling a synthesis process (shading, catalyst ratio, temperature and feed ratio) of a bone targeting nano-micelle carrier (ALN-PLGA-mPEG) modified by alendronate sodium (ALN). The bone targeting ability of alendronate sodium (ALN) is combined with the drug loading and long circulation advantages of polymer mPEG-PLGA micelles to construct a bone targeting nano-micelle carrier (ALN-PLGA-mPEG), so that the obtained rifapentine-loaded bone targeting nano-micelle (ALN-PLGA-mPEG (at) RPT) can significantly improve the bone targeting and slow release performance, and provides a new strategy with high efficiency and low toxicity for precise treatment of bone tuberculosis.

The invention discloses a rifapentine isoniazide tablet and a preparation method thereof, the rifapentine isoniazide tablet is a core-coated tablet, and comprises an inner-layer tablet core containing rifapentine and an outer-layer tablet layer containing isoniazide; the inner-layer tablet core comprises rifapentine, edetate disodium, sodium ascorbate and lauryl sodium sulfate, the rifapentine accounts for 53-63% of the total mass of the inner-layer tablet core, and the rifapentine tablet further comprises a filler, a stabilizer, a disintegrating agent, an adhesive, a surfactant, a lubricant and a coating layer; the coating layer coats the inner-layer tablet core; the outer sheet layer comprises isoniazide, a filling agent, a disintegrating agent, an adhesive, a lubricant and an adhesive; and the mass of the isoniazide accounts for 75-95% of the total mass of the outer sheet layer. According to the rifapentine isoniazide tablet disclosed by the invention, the compliance of a patient is enhanced. And meanwhile, the potential safety hazard problem of impurity increase caused by incompatibility of rifapentine and isoniazide is solved.

The invention provides a preparation method of a lung inhalation microsphere carrying rifapentine, which comprises the following steps: weighing a biodegradable high-molecular polymer and rifapentine, and dissolving the biodegradable high-molecular polymer and the rifapentine in a low-boiling-point organic solvent to form an oil phase; weighing a stabilizer, and dissolving the stabilizer in pure water to form a water phase; slowly dropwise adding the oil phase into the water phase, and stirring and emulsifying at a high speed for 1-30 minutes to form an emulsion; lowering the stirring speed, and continuously stirring for 1-24 hours at a uniform speed until the organic solvent is completely volatilized; carrying out low-speed centrifugation on the residual solution for 1-10 minutes, collecting sustained-release microspheres prepared at the bottom of the solution, then washing the centrifugal microspheres with purified water, and repeating for three times; and freeze-drying a solid product obtained by centrifugation to obtain the microspheres. The production process is simple, the prepared drug-loaded microspheres can accurately deliver drugs to the lung, the drugs can be concentrated at a target site and slowly released after being administered, the maintenance time of the effective concentration of the drugs in local tissues is prolonged, and the compliance of patients is improved.

The invention discloses a rifapentine capsule type dry powder inhaler and a preparation method thereof, the capsule type dry powder inhaler comprises a capsule shell and a capsule content, and the capsule content comprises the following components in parts by weight: 1 part of rifapentine, 1-30 parts of a carrier and 0.01-1 part of a flow aid. According to the invention, micronized drug bulk drugs and appropriate excipients are in the form of capsules, and atomized drugs are actively inhaled into the lungs by a patient through a specially-made dry powder inhalation device. The delivery efficiency of the preparation is high, and the lung deposition rate is high; the particle size of the preparation and the stability of the preparation are high, and the compatibility between raw materials and auxiliary materials is good. The rifapentine capsule type dry powder inhaler disclosed by the invention has no gastrointestinal tract degradation effect and no liver first-pass effect, the medicine can directly act on the lung, the absorption is quick, and the effect is quick after administration; meanwhile, local administration is realized, the dosage is obviously reduced, and toxic and side effects are small. The preparation method disclosed by the invention is simple and easy to implement, has no too high requirements on technical equipment, and is suitable for domestic industrial production.

The invention discloses a preparation process of rifapentine, and relates to the technical field of medicine preparation. According to the method, after rifoxazine is prepared through cyclization reaction, a distillation process is adopted to replace traditional centrifugal separation, cyclization reaction liquid is directly transferred into ring-opening reaction, the post-treatment procedure of an intermediate product rifoxazine is reduced, and rifoxazine is continuously generated in the distillation process, so that the yield of the product is ensured, and the method is suitable for industrial production. And other components in a cyclization reaction system do not have negative effects in subsequent ring opening, condensation and post-treatment processes of a final product, but have higher purity, so that the problems of man-hour plants, more wastes and insufficient purity and yield in the prior art are solved.

The present invention relates to a solid composition comprising nanoparticles of rifamycin, such as rifapentine, dispersed in a matrix comprising a first excipient and a second excipient. The invention also relates to microneedle arrays, implantable rods, aqueous dispersions and pharmaceutical compositions obtained from said solid compositions as well as their uses.

The invention discloses a capsule type pharmaceutical composition and a preparation method thereof, the capsule type pharmaceutical composition is prepared by pouring rifapentine micro-tablets and isoniazide micro-tablets into a capsule shell, the weight difference of the rifapentine micro-tablets is controlled to be + / -5.0%, the average hardness range is 20-40N, and the diameter of the micro-tablets is 3mm; the weight difference of the isoniazide microchip is controlled to be + / -5.0%, the average hardness range is 20-40N, and the diameter of the microchip is 2mm. The two medicines are prepared into micro-tablets and then are filled into capsules, so that doctors can adjust the dosage according to the conditions of patients, and the patients can take the capsules conveniently.

The invention discloses a rifapentine tablet preparation method, which comprises: S1, mixing materials of an inner layer tablet core, carrying out dry granulation, and tabletting to prepare the inner layer tablet core containing rifapentine; the inner-layer tablet core is prepared from the following materials: rifapentine, edetate disodium, sodium ascorbate, a filler, a stabilizer, a disintegrating agent, an adhesive, a surfactant and a lubricant; the mass of the rifapentine accounts for 50%-70% of the total mass of the inner-layer tablet core; s2, preparing mixed powder from a coating material, adding the mixed powder into a fluidized bed, and granulating to prepare an outer sheet layer; and S3, wrapping the inner-layer tablet core with the outer-layer tablet layer, and pressing to obtain the rifapentine tablet. The rifapentine, edetate disodium and sodium ascorbate are prepared into the tablet-coated tablet, so that the problem of impurity increase caused by high temperature in the rifapentine tablet coating process is solved, the stability of rifapentine is further improved, the product quality is ensured, and the stability and safety of the product are improved.

This invention relates to the field of pharmaceutical technology and proposes a rifapentine microsphere thermosensitive gel and its preparation method. The rifapentine microsphere thermosensitive gel includes rifapentine microspheres and a thermosensitive gel matrix. The rifapentine microspheres comprise a continuous aqueous phase and an oil phase dispersed in the aqueous phase. The oil phase includes rifapentine, an emulsifier, and vegetable oil. The aqueous phase includes glycerol and water. The emulsifier consists of poloxamer and lecithin in a mass ratio of 5:4~6. The rifapentine microsphere thermosensitive gel provided by this invention has good encapsulation efficiency and drug loading, solving the problems of insufficient encapsulation efficiency and drug loading in existing rifapentine microsphere thermosensitive gels.

Safe and effective methods for treating a subject suffering from cortisol excess of and in need of concomitant administration of mifepristone along with a CYP3A4 inducer are disclosed herein. The CYP3A4 inducer may be, for example, mitotane, rifampin (also known as rifampicin), rifabutin, rifapentin, phenobarbital, phenytoin, carbamazepine, or St. John's wort. In embodiments, the CYP3A4 inducer is a strong CYP3A4 inducer. In embodiments, the CYP3A4 inducer is a moderate CYP3A4 inducer. In embodiments, the CYP3A4 inducer may be any CYP3A4 inducer. Mifepristone may be orally administered. Mifepristone may be administered with food.