36 results about "Cetrorelix" patented technology

In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over several weeks by complexation with suitable biophilic carriers. The acidic polyamino acids polyglutamic acid and polyaspartic acid were selected for complexation with cetrorelix. The cetrorelix polyamino acid complexes are prepared from aqueous solutions by combination of the solutions and precipitation of the complexes, which are subsequently centrifuged off and dried over P2O5 in vacuo. If complexes having a defined composition are to be obtained, lyophilization proves to be a suitable method. The cetrorelix-carboxylic acid complexes were also prepared from the aqueous solutions. In the random liberation system, the acidic polyamino acids poly-Glu and poly-Asp showed good release-delaying properties as a function of the hydrophobicity and the molecular mass of the polyamino acid. In animal experiments, it was possible to confirm the activity of the cetrorelix-polyamino acid complexes as a depot system in principle. It is thus possible by complexation of cetrorelix with polyamino acids to achieve testosterone suppression in male rats over 600 hours. The release of active compound here can be controlled by the nature and the molecular mass of the polymers.

A lyophilizate, method of preparation, and use of the lyophilizate for gonad protection is described. The lyophilizate comprises cetrorelix dissolved in 30% (v / v) acetic acid, transferred to water, and freeze-dried.

A method for realizing the solid phase synthesis of cetrorelix comprises the following steps that: Fmoc-Linker-MBHA-Resin is used as a starting raw material and is connected in turn with amino acid with Fmoc-protecting groups according to a solid phase synthesis method, so as to obtain protective decapeptide resin; meanwhile, the Fmoc-protecting groups are divested in turn; one sort of HBTU / HOBT or DIC / HOBT is used as condensing agent to carry out synthesized peptide, thereby obtaining protective decapeptide resin; acetylation reaction is carried out, and then protecting group side chain divesting and peptide cutting are carried out synchronously to obtain cetrorelix acetate which is separated and purified through C18 or C8 chromatographic column; finally, cetrorelix acetate acetate or trifluoroacetate is obtained after freeze drying.

The invention relates to a stable cetrorelix medicinal composition and a preparation method thereof. The medicinal composition is obtained through the preparation method which comprises the following steps: 1, preparing a solution of mannitol and cetrorelix acetate, and filtering the solution; 2, packaging the solution obtained in step 1 to a container, and cooling step by step according to a case which comprises the following stages: a, cooling a plate layer to -25--40DEG C according to a cooling rate of not greater than 3DEG C / min and keeping the temperature for not less than 1h, and b, continuously cooling to -40DEG C or below and keeping the temperature of not less than 1h; and 3, drying to obtain the lyophilized medicinal composition. The stability of the medicinal composition obtained through the preparation method is good, so the medicinal composition still has definite curative effects when the medicinal composition is preserved for a long time.

The invention relates to the field of medicine synthesis and discloses a method for synthesizing cetrorelix. The present invention adopts a brand-new amino resin as a carrier, and adopts protected D-Orn as the precursor of D-Cit, then removes the side chain protecting group and reacts with tert-butyl isocyanate to generate D-Cit (tBu), through the unique containing Hydrogen bromide trifluoroacetic acid solution to acid hydrolyze the cetrorelix peptide resin, and simultaneously remove the side chain protecting group tBu of the generated D-Cit(tBu) to the greatest extent, and the finally obtained cetrorelix has a higher The purity and total yield avoid the generation of toxic impurity [D-Cit(Ac)]-cetrorelix, the whole method is simple and easy to operate, the conditions are mild, and the product quality is high.

The invention discloses a method for purifying cetrorelix and belongs to the technical field of separation and purification. The method disclosed by the invention mainly comprises the following steps:dissolving, stirring and filtering crude cetrorelix peptides; loading the filtered solution into a reverse phase silica gel column filled with polyoctadecane for performing chromatography; eluting the target product by taking a mixed solution of sodium sulfate and trifluoroacetic acid as a mobile phase A and taking an organic solvent as a mobile phase B; collecting the elution solution accordingto a target peak order, analyzing and detecting various collected solutions, gathering all the collected solutions meeting requirements, and inspecting. According to the method for efficiently and rapidly separating and purifying cetrorelix disclosed by the invention, [D-Arg8]-cetrorelix and [beta-Ala-D-Cit6]-cetrorelix can be effectively separated, the single purity content can be less than 0.1%by virtue of one-step purification, the total purity is 99.9% or higher, and the purification yield reaches 80%. The production process is simple and can be applied to enlarged and large-scale production, and the production cost of enterprises is reduced.

The present invention relates to a stable formulation of Cetrorelix or its pharmaceutically acceptable salt in the form of ready-to-use solution. The stable ready-to-use solution of Cetrorelix prevents gel formation and provides better patient compliance. Further, the invention relates to a process for preparation of the stable ready-to-use solution of Cetrorelix.

The invention relates to application of Cetrorelix to preparation of medicine for treating AIDs. The invention provides a compound of Cetrorelix and a pharmaceutically acceptable salt and application thereof to preparation of medicine for treating AIDs. The human T lymphoid cell series C8166 and HIV-1 experiment strain HIV-1<NL4-3> are used for performing in-vitro cytotoxicity and anti-HIV activity detection; the cytotoxicity is detected by an MTT colorimetric method; the anti-HIV activity is detected by two methods including a synplasm inhibition experiment method and an HIV-1p24 antigen quantitative method. The result proves that the cytotoxicity of the Cetrorelix is very low; CC<50> is higher than 200 muM; when the concentration is EC<5>0(1.788 muM), the Cetrorelix completely has no toxicity on the cell C8166. Therefore the Cetrorelix can be used as the anti-HIV medicine.