9 results about "Rotigotine" patented technology

The invention belongs to the technical field of biology and medicinal chemistry, and discloses a transaminase mutant, a method and application of the transaminase mutant in preparation of a key chiral intermediate of rotigotine, and the preparation method of the key chiral intermediate of rotigotine is a biological conversion method using the transaminase mutant as a main enzyme. The amino acid sequence of the transaminase mutant is an amino acid sequence obtained by mutating the amino acid sequence of wild type transaminase as shown in SEQ ID NO.1, the amino acid sequence of the transaminase mutant has a mutation site in the mutated amino acid sequence, and the amino acid sequence of the transaminase mutant has more than 90% of homology with the mutated amino acid sequence. When 5-methoxy-2-tetralone (a compound shown in a formula III) is catalyzed by an enzymatic reaction method to prepare a key chiral intermediate (S)-5-methoxy-1, 2, 3, 4-tetrahydronaphthalene-2-amine (a compound shown in a formula II) of rotigotine, the product is chiral purity gt, and the purity gt of the key chiral intermediate (S)-5-methoxy-1, 2, 3, 4-tetrahydronaphthalene-2-amine is gt. The yield of the biological catalysis step is gt; 95%.

This rotigotine-containing adhesive patch comprises a support layer and an adhesive layer, wherein the adhesive layer contains: at least one selected from the group consisting of rotigotine and pharmaceutically acceptable salts of rotigotine; a rubber-based adhesive base; and an antioxidant. The antioxidant includes propyl gallate, ascorbyl palmitate, and sodium pyrosulfite.

The present invention relates to a transdermal therapeutic system (TTS) for administering rotigotine as an active ingredient, comprising a matrix layer containing rotigotine, the matrix layer further comprising one or more non-amine-resistant silicone adhesives in an amount of more than 50% by weight, based on the total weight of the pressure-sensitive adhesives contained in the matrix layer, and paraffin, and to a method for preparing the same. The transdermal therapeutic system of the present invention is particularly suitable for the treatment of Parkinson's disease.

The application belongs to the technical field of biology and pharmaceutical chemistry, and discloses a transaminase mutant, a method and application of the transaminase mutant in preparation of a key chiral intermediate of rotigotine, and a preparation method of the key intermediate of rotigotine is a biological conversion method with the transaminase mutant as a main enzyme, an amino acid sequence of the transaminase mutant is an amino acid sequence mutated from an amino acid sequence of a wild-type transaminase shown in SEQ ID NO. 1, the amino acid sequence of the transaminase mutant has a mutation site in the mutated amino acid sequence, and has more than 90% homology with the mutated amino acid sequence. When 5-methoxy-2-naphtalone (a compound of formula III) is catalyzed to prepare a key chiral intermediate (S)-5-methoxy-1,2,3,4-tetrahydronaphthalen-2-amine (a compound of formula II) of rotigotine through an enzymatic reaction method, the chiral purity of the product is greater than 99.9%, and the yield of the biological catalysis step is greater than 95%.

A rotigotine-containing patch comprising a support layer and an adhesive layer, wherein the adhesive layer contains at least one selected from the group consisting of rotigotine and pharmaceutically acceptable salts of rotigotine, a rubber-based adhesive base, and an antioxidant, wherein the antioxidant comprises propyl gallate, ascorbyl palmitate, and sodium pyrosulfite.

This invention relates to a transdermal therapeutic system (TTS) for the administration of the active ingredient rotigotine and its preparation method. The transdermal therapeutic system (TTS) comprises a matrix layer containing: rotigotine; one or more non-amine-resistant silicone adhesives in an amount greater than 50% by weight, based on the total weight of the pressure-sensitive adhesives in the matrix layer; and paraffin. The transdermal therapeutic system according to the invention is particularly suitable for the treatment of Parkinson's disease.

The invention discloses a rotigotine lyotropic liquid crystal precursor solution as well as a preparation method and application thereof, and belongs to the field of pharmaceutical preparations, the rotigotine lyotropic liquid crystal precursor solution comprises the following components: phospholipid, grease, a release regulator, an organic solvent and rotigotine or pharmaceutically acceptable salt thereof, the organic solvent accounts for 10-40% of the mass of the precursor, and the rotigotine or pharmaceutically acceptable salt thereof accounts for 1-30% of the mass of the precursor. The rotigotine lyotropic liquid crystal precursor solution is low in viscosity and easy to inject, lyotropic liquid crystal gel can be formed when the rotigotine lyotropic liquid crystal precursor solution encounters body fluid after injection, and the gel wraps a medicine to be slowly released, so that the rotigotine lyotropic liquid crystal precursor solution has a good slow-release effect, the medication frequency can be reduced, and the compliance of a patient is improved; the auxiliary materials are good in biocompatibility, and do not easily cause inflammatory response of the organism; the production cost is low, and the preparation method is simple and easy to industrialize. The invention can be used for auxiliary treatment of early primary Parkinson's disease and late primary Parkinson's disease.

The present application provides the anti-multiple myeloma activity and application of rotigotine. Experimental results show that rotigotine is relocated to the Tudor domain of the polycomb-like protein family PHF19 protein, and PHF19 is a significant marker of multiple myeloma. Rotigotine has good selectivity to non-polycomb-like proteins, effectively inhibits the viability of multiple myeloma cells MM1.S, and inhibits tumor growth in tumor-bearing mice, showing that rotigotine can become an anti-multiple myeloma drug.

The preparation method comprises the following steps: (1) mixing citric acid-L-carnitine ionic liquid, acrylic acid, methacrylic acid N, N-dimethylaminoethyl ester and a photoinitiator to obtain a pre-polymerized mixed solution, and then adding rotigotine medicine powder to obtain a medicine-carrying ionic gel pre-polymerized solution; and (2) injecting the drug-loaded ionic gel prepolymerization liquid into a microneedle mold, covering the surface of the drug-loaded ionic gel prepolymerization liquid with a PDMS friction layer subjected to oxygen plasma treatment, and performing curing demolding to obtain a PDMS upper layer and a rotigotine-loaded ionic gel microneedle lower layer, thereby obtaining the rotigotine-loaded triboelectric microneedle patch. The patch prepared by the preparation method disclosed by the invention has good flexible fitting property and biological safety, self-powered driving can be realized by virtue of self tremor of a Parkinson's disease patient, controllable transdermal delivery of rotigotine is promoted, and the treatment effect of the Parkinson's disease is improved.