14 results about "Cabazitaxel" patented technology

The invention discloses folate receptor mediated manganese ion coordination type cabazitaxel-loaded albumin nanoparticles as well as a preparation method and application thereof. Human serum albumin is covalently linked with folic acid through an amide condensation reaction to obtain a folic acid-albumin modifier with folic acid targeting; further combining with manganese ions through metal coordination to form a folic acid-albumin-manganese ion modifier with a targeting function; finally, efficient loading of cabazitaxel is achieved through a simple heating polymerization method, and the folate receptor mediated cabazitaxel-loaded albumin nanoparticles are formed. According to the nanoparticles provided by the invention, the particle size is about 140 nm, the stability is good, and the drug loading capacity and the encapsulation efficiency of cabazitaxel are high; the compound has a slow release effect, is good in in-vitro release behavior, and has important application value in the aspect of targeted delivery of drugs to tumors. Compared with other traditional nanoparticles, the nanoparticles show a remarkable anti-tumor effect.

The invention relates to a hybrid nano assembly for dual synergistic chemotherapy as well as a preparation method and application of the hybrid nano assembly, and belongs to the technical field of pharmaceutical preparations. The invention relates to a hybrid nano assembly for dual synergistic chemotherapy, which is formed by co-assembling a cabazitaxel prodrug and gossypol under hydrophobic action and hydrogen bond driving, and is modified by adopting a PEG (Polyethylene Glycol) modifier, the molar ratio of the cabazitaxel prodrug to the gossypol is 1: (1-7), and the ratio of the total mass of the cabazitaxel prodrug and the gossypol to the mass of the PEG modifier is 4: 1. A cabazitaxel prodrug and a sensitizer gossypol are co-assembled to obtain a hybrid nano assembly, the hybrid nano assembly is oxygenated to obtain the oxygen-carrying preparation, the nano assembly and the oxygen-carrying preparation are simple and convenient to prepare and high in drug loading efficiency, and efficient co-loading of drugs can be achieved; meanwhile, the curative effect of chemotherapy can be enhanced through dual mechanisms of relieving tumor hypoxia and promoting tumor apoptosis, and the pharmaceutical composition has a good clinical application prospect.

The present invention relates to a solution pharmaceutical preparation of cabazitaxel which is an ethanol-free direct infusion dilution of cabazitaxel and has excellent storage stability. Specifically, the present invention relates to a solution pharmaceutical preparation containing cabazitaxel as an active ingredient that contains a glycol solvent selected from polysorbate, polyethylene glycol, and / or propylene glycol and an organic acid. The pH of the solution pharmaceutical preparation diluted by water to a cabazitaxel concentration of 0.1 mg / mL is from higher than 3.5 to 5.5.

A taxane supramolecular nanocomposite. The supramolecular nanocomposite comprises a taxane active substance, including but not limited to paclitaxel, docetaxel, and cabazitaxel, as well as a self-assembling carrier, a high molecular polymer, and a dissolution promoter. The dissolution promoter may comprise one or more of alcohols, polybasic organic acids, and amino acids. Also disclosed are a preparation method and use of the supramolecular nanocomposite. The supramolecular nanocomposite is suitable for oral administration and topical application, providing effects such as increased local drug exposure concentration and efficacy, reduced systemic side effects, etc.

The invention discloses an elemene cabazitaxel engineered bionic liposome, a preparation method and an application, belongs to the technical field of bionic liposomes, and solves the limitation that an existing single treatment means is used, for example, chemotherapy is only used for eliminating evil, and an immune checkpoint inhibitor is poor in penetrability through double-way synergistic interaction of'direct killing of tumor cells' and'repairing of anti-tumor immunity '. The BBB penetration and glioma homing characteristics of the MSCs membrane are combined with the specific combination of PD-1 / PD-L1, so that the enrichment of the drug at the tumor site is remarkably improved, the off-target effect is reduced, and the MSCs membrane coated particles are superior to the traditional liposome and unmodified MSCs membrane coated particles; an autologous MSCs membrane is adopted for coating, so that the immunogenicity is reduced; in-vivo and in-vitro experiments do not show toxicity of liver, kidney and hematopoietic systems, and the problem of toxic and side effects of free drugs and part of nano-carriers is solved; and the capsule has the advantages of uniform particle size, stable storage, no obvious change in 15 days, and high drug encapsulation efficiency, and provides a basis for subsequent clinical transformation.

This disclosure is directed to a pharmaceutical composition comprising sodium bicarbonate and a polymer-drug nanoaggregate having a polymer and a taxane. The polymer is water soluble and comprises at least one first terminal group modified with a hydrophobic moiety and a second terminal group modified with a hydrophilic moiety and can be a modified symmetrically or asymmetrically branched polymers. The taxane can include paclitaxel, docetaxel, cabazitaxel, larotaxel, milataxel, ortataxel, tesetaxel, derivatives therefrom or a combination thereof, which are water insoluble or poorly water soluble. Such polymer-drug nanoaggregates can improve drug solubility, stability, in vivo availability and efficacy, and reduce side effects such as renal toxicity. This invention is also directed to a process for producing the pharmaceutical composition comprising the polymer-drug nanoaggregate. This invention is further directed to a method for treating a disease including cancer using the pharmaceutical composition disclosed herein.

The invention relates to a cabazitaxel self-emulsifying oral preparation and a preparation method thereof. The cabazitaxel self-emulsifying oral preparation is prepared from the following raw materials: a cabazitaxel active matter, grease, a surfactant and a cosurfactant, the cabazitaxel active matter is cabazitaxel or pharmaceutically acceptable salt, ester and solvate of cabazitaxel. After the cabazitaxel self-emulsifying oral preparation developed by the invention is in contact with an aqueous medium, nano-emulsion with small particle size (below 450 nm) can be spontaneously formed, drugs can be quickly released, and the first-pass effect of the liver can be bypassed through lymphatic transport, so that relatively high oral bioavailability is realized; the invention provides a comprehensive technical scheme capable of simultaneously solving the three problems of dissolution, permeation and metabolism, and a brand-new feasible path is opened up for oral administration of the cabazitaxel active matter.

The invention discloses a co-crystal of cabazitaxel and plant essential oil active ingredients as well as a preparation method and application of the co-crystal. The co-crystal provided by the invention is a co-crystal formed by self-assembling raw materials including cabazitaxel and plant essential oil active ingredients. Mixing cabazitaxel and plant essential oil to form a material to be crystallized; and performing crystallization treatment to obtain the eutectic crystal of cabazitaxel and plant essential oil active ingredients. According to the cabazitaxel-plant essential oil active component eutectic, the problems that a solvent is easily removed from a cabazitaxel solvate in the heating or long-term storage process to cause component change or crystal form conversion and cabazitaxel in a solvent-free form easily absorbs moisture in the long-term storage process are solved, and the stability of cabazitaxel is improved. Meanwhile, the inhibition effect of the co-crystal on tumor cells is remarkably improved, and the anti-tumor activity of cabazitaxel can be further improved. In conclusion, the eutectic crystal of cabazitaxel and plant essential oil active ingredients has good stability, does not have solvent toxicity, is relatively high in safety, and can better meet the patent medicine requirements in the aspects of production, quality control, clinical application and the like.

The invention relates to a cabazitaxel composition and application of the cabazitaxel composition. Embodiments provide a composition comprising cabazitaxel and at least one lipid and / or cougsterol, and / or a cougsterol derivative, and / or sodium cholesterol sulfate, in the form of a tablet or capsule, and administering the composition to a subject.

The invention relates to a cabazitaxel composition and application of the cabazitaxel composition. Embodiments provide a composition comprising cabazitaxel and at least one lipid and / or cougsterol, and / or a cougsterol derivative, and / or sodium cholesterol sulfate, in the form of a tablet or capsule, and administering the composition to a subject.

This invention belongs to the field of novel excipients and dosage forms for pharmaceutical preparations, and relates to the construction of four cabazitaxel prodrugs and their self-assembled nanoparticles. Specifically, it involves the synthesis of four different cabazitaxel prodrugs using three different disulfide bonds as connecting bonds and 9-fluorenylmethanol or cyclopentylmethanol as side chains, further preparing self-assembled nanoparticles, and exploring their application in drug delivery systems. The prodrugs are prepared by forming anhydrides from dithiodiacetic acid, 3,3'-dithiodipropionic acid, or 4,4'-dithiodibutyric acid, followed by esterification with 9-fluorenylmethanol or cyclopentylmethanol to obtain intermediate products. These intermediate products then undergo esterification with cabazitaxel to obtain the cabazitaxel prodrugs. Self-assembled nanoparticles of the cabazitaxel prodrugs are obtained through a one-step nanoprecipitation method. The prepared prodrug self-assembled nanoparticles can rapidly release the parent drug at the tumor site, exerting their tumor-killing effect and demonstrating excellent anti-tumor efficacy.

Disclosed are a cabazitaxel micelle and a preparation method therefor. The cabazitaxel micelle of the present invention comprises cabazitaxel and a polyethylene glycol-derived phospholipid. The polyethylene glycol-derived phospholipid comprises a polyethylene glycol moiety and a phospholipid moiety, and the phospholipid moiety thereof is di(C12-C24 fatty acyl)phosphatidylethanolamine. The polydispersity index of the micelle is not greater than 0.09. The cabazitaxel micelle of the present invention has one or more of the following advantages: uniform product particle size, good stability, low impurity content, high release degree, short reconstitution time, and convenient clinical administration.

The application belongs to the technical field of medicine, and particularly relates to a cell membrane coated prodrug self-assembled nanoparticle and a preparation method and application thereof. The nanoparticle is a prodrug self-assembled nanoparticle for which a four-sulfur bond bridged cabazitaxel dimer prodrug (gamma-4S-2CTX) and a polyethylene glycol (PEG) modifier are co-assembled to prepare a tumor cell membrane coated with the prodrug self-assembled nanoparticle as a core. The gamma-4S-2CTX is shown in structural formula (I). The biomimetic cell membrane coated nanoparticle (CM-pDPNAs) prepared by the application exhibits significant tumor specific recognition ability and low toxic side effects, greatly improves the selectivity and treatment effect of the drug in the body, and shows good safety and anti-tumor effect in the in-vivo anti-tumor experiment. The application provides an efficient and low-toxic anti-tumor drug delivery system, and has good application prospect.

The invention discloses a cabazitaxel micelle and a preparation method thereof. The cabazitaxel micelle disclosed by the invention is prepared from cabazitaxel and polyethylene glycol derivatized phospholipid, the polyethylene glycol derivatized phospholipid comprises a polyethylene glycol part and a phospholipid part, and the phospholipid part is di (C12-C24 fatty acyl) phosphatidyl ethanolamine; the polydispersity coefficient of the micelle is not higher than 0.09. The cabazitaxel micelle provided by the invention has one or more of the following advantages: the product has uniform particle size, good stability, low impurity content, high release rate, short redissolution time and good clinical medication convenience.