13 results about "Cladribine" patented technology

The present invention discloses a transmucosal delivery composition in the form of a sublingual intraoral dispersible film containing cladribine as an active ingredient.

The application belongs to the technical field of non-antibiotic compounds as bacteriostatic agents, and discloses an application of a known non-antibiotic compound, cladrabine, in inhibiting the growth of multi-drug resistant Klebsiella pneumoniae. The application finds that cladrabine can inhibit the growth of multi-drug resistant Klebsiella pneumoniae, and the minimum bacteriostatic concentration reaches 64 mg / L. Further exploration of the bacteriostatic mechanism finds that after exposure to cladrabine, the permeability of the bacterial cell membrane is enhanced, and the macromolecular substances (nucleic acids and proteins) in the cell are excreted, causing the integrity of the bacterial cell membrane to be destroyed, and further causing the death of Klebsiella pneumoniae. The application proposes that cladrabine can destroy the cell membrane of bacteria, change the permeability of the cell membrane, has a good inhibitory effect on multi-drug resistant Klebsiella pneumoniae, and can be further applied to the preparation of related drugs.

The invention discloses a transmucosal delivery composition in form of a sublingual orally dispersible film comprising cladribine as active ingredient.

The present invention relates to compounds for the treatment of Myasthenia Gravis and related methods and dosing regimen. Specifically, the invention pertains to the field of treatment scheme of oral formulation of cladribine and relevant for the treatment of Myasthenia Gravis, more specifically generalized Myasthenia Gravis.

The present invention relates to the use of multiple doses of Cladribine combined with beta interferon for the treatment of multiple sclerosis in patients who are refractory to at least one conventional therapy.

The present invention relates to the use of 2-chloro-2′-deoxyadenosine, hereinafter referred to as cladribine, or a pharmaceutically acceptable salt thereof, for treating or ameliorating an autoimmune, neuromuscular disorder, e.g. the autoimmune neuromuscular disorder myasthenia gravis (MG).

A transmucosal delivery composition in form of a sublingual orally dispersible film comprising cladribine as active ingredient and comprising at least two hydrophilic polymers, wherein the at least two hydrophilic polymers represent at least 20% (w / w) of the total composition, wherein cladribine is contained in the composition as a cladribine-cyclodextrin complex. Said composition for use in the treatment of multiple sclerosis (MS), myasthenia gravis (MG), neuromyelitis optica spectrum disorders (NMOSD). A method for producing a transmucosal delivery composition in form of a sublingual orally dispersible film, wherein cladribine or cladribine-cyclodextrin complex is mixed with film-forming polymers by stirring with at least 100 rpm for at least 10 min at a temperature of at least 30° C.

The invention relates to a method of producing cladribine with a purity greater than 99.9 wt.% from 2-deoxyuridine and 2-chloroadenine by using the catalytic action of high concentrations (at least 20.000 U / L) of freely dissolved transglycosidases UP (uridine phosphorylase) and PNP (purine nucleoside phosphorylase) in an enzymatic synthesis in an aqueous environment without the presence of any organic solvent.

Specific oral dosings, specific oral dosage forms, and / or specific oral dose regimens including Cladribine can be effective for the treatment of progressive forms of Multiple Sclerosis, especially Primary Progressive Multiple Sclerosis and / or Secondary Progressive Multiple Sclerosis. Methods of treatment can be based on specific oral dosings, specific oral dosage forms, and / or specific oral dose regimens including Cladribine.

The present invention relates to the use of multiple doses of Cladribine combined with beta interferon for the treatment of multiple sclerosis in patients who are refractory to at least one conventional therapy.

The application discloses a mucous membrane-adhesive polymeric microcarrier loaded with disodium cladribine tetrasodium and a preparation method and application thereof. Sodium alginate is modified by phenylboronic acid to obtain a PBA-Alg polymer; disodium cladribine tetrasodium is mixed with the polymer to obtain a precursor solution; microdroplets are formed by a microfluidic electrospray technology and sprayed into a calcium ion crosslinking solution to be solidified to obtain the microcarrier. In the microcarrier, the phenylboronic acid groups form reversible borate ester bonds with cis-diol groups in the disodium cladribine tetrasodium molecules, so that stable anchoring and continuous release of the drug are realized. The phenylboronic acid groups on the surface of the microcarrier can form dynamic covalent bonds with sialic acid residues in ocular surface mucin, so that long-acting adhesion on the ocular surface is realized; meanwhile, the borate ester bonds are oxidatively cleaved in the presence of excess active oxygen on the ocular surface, so that the active oxygen is consumed and inflammation is inhibited. The microcarrier has a highly uniform size and shear thinning characteristics, and can be safely, comfortably, efficiently and low-frequency used for the treatment of ocular surface diseases such as dry eye.