4 results about "Ziconotide" patented technology

The invention provides a ziconotide nasal-brain delivery preparation which is high in brain targeting, safe and noninvasive and directly enters the brain through nasal administration. The nasal-brain delivery preparation comprises an active component ziconotide and an absorption enhancer, wherein the absorption enhancer is selected from one or more of dodecyl-beta-D-maltoside (DDM), menthol, hydroxypropyl-beta-cyclodextrin (HP-beta-CD), sodium glycocholate (SGC) and related derivatives thereof. The absorption enhancer with a specific type and content and the ziconotide cooperate and act together, so that the ziconotide bypasses a blood brain barrier, enters the brain through a nasal olfactory mucous membrane, forms a medicine storage bank in an olfactory bulb, is slowly released to the brain and keeps a long-term medicine effect, and therefore, a traditional ziconotide intrathecal administration mode is abandoned; the ziconotide nasal-brain administration mode is created, and the ziconotide nasal-brain administration method is a new-generation therapy for pain diseases related to the central nervous system.

The invention discloses a ziconotide-loaded PLGA (poly (lactic-co-glycolic acid)) sustained-release microsphere as well as a preparation method and application thereof. The PLGA microspheres are mainly prepared from a polylactic acid-glycolic acid copolymer (PLGA), ziconotide and trehalose; the PLGA microspheres are prepared from the following components in percentage by mass: 85.2 to 95.6 percent of PLGA, 4.4 to 8.2 percent of ziconotide and 0 to 7.4 percent of trehalose, ziconotide medicine is uniformly dispersed in PLGA, microspheres are prepared by adopting a double-emulsification method, and stable medicine carrying microspheres are formed. The PLGA microspheres prepared by the invention can realize long-time slow release of ziconotide, significantly prolong the drug effect maintenance time, and show relatively low toxic and side effects in vivo; by means of controllable degradation of the PLGA material, ziconotide can be continuously released in vivo, the bioavailability of the medicine is improved, the compliance burden of a patient is reduced, the defects of an existing ziconotide administration mode are overcome, and an efficient, safe and sustainable slow-release treatment scheme is provided.

The present invention relates to an inhibitor of FXYD2 wherein the inhibitor reduces the expression and / or activity of FXYD2 in a subject in need thereof and targets at least a region comprising or consisting of nucleotides 219-229 of SEQ ID NO: 3. The inventors have demonstrated that targeted FXYD2 regions can be used to inhibit and / or reduce the expression and / or activity of FXYD2. The antisense oligonucleotide (SEQ ID NO: 4) targeting the FXYD2 genes of the rat and the human is designed and synthesized by the FXYD2 genes of the rat and the human. They have been subjected to an intrathecal injection of FXYD2 optimized ASO in two modes of rat pain (neuropathic pain and inflammatory pain). It has been proved that FXYD2 ASO can effectively reduce the expression of FXYD2 ASO in rat dorsal root ganglion (DRG). It has been proved that the FXYD2 ASO can significantly reduce the neuropathic pain in a spinal nerve ligation (SNL) rat model, and the analgesic effect of the FXYD2 ASO on the neuropathic pain is better than that of the leading Zconotide in the current market. The FXYD2 ASO also shows that the FXYD2 ASO can obviously reduce the inflammatory pain in a rat model induced by a complete Freund's adjuvant (CFA).

The invention relates to a Ziconotide temperature-sensitive nasal spray, which comprises a solvent, and Ziconotide, a first matrix, a second matrix, an absorption enhancer, a pH buffer system and a polypeptide stabilizer dispersed in the solvent, the first matrix is poloxamer 407, and the second matrix is poloxamer 188; the temperature-sensitive nasal spray comprises the following components in percentage by mass: 5%-20% of the first substrate, 0-5% of the second substrate, 0.01%-10% of the absorption enhancer, and the balance of the temperature-sensitive nasal spray, the pH buffer system is an acetic acid-acetate system or a lactic acid-lactate system. The ziconotide temperature-sensitive nasal spray can form a good spray form through a nasal spray device, the viscosity has a temperature-sensitive characteristic, and the ziconotide temperature-sensitive nasal spray is not easy to lose and has good stability.