- Composition containing orlistat and GLP-1 receptor agonist, and use thereof
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The invention belongs to the technical field of medicines, and concretely relates to a composition containing orlistat and a GLP-1 receptor agonist, and a use thereof. The composition containing orlistat and the GLP-1 receptor agonist contains orlistat, and nano-particles comprising the GLP-1 receptor agonist and a copolymer. The composition containing orlistat and the GLP-1 receptor agonist has the advantages of realization of combined oral administration of orlistat and the GLP-1 receptor agonist, high bioavailability and good weight gain increase-inhibiting and weight-reducing effects.
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- Comprising orlistat nanosphere in use in the preparation of antineoplastic (by machine translation)
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The invention relates to the field of medical technology, in particular to a containing orlistat nanosphere in use in the preparation of antineoplastic. The nanosphere comprises orlistat and selected from vitamin A methyl acrylate - 2 - methacryloyl ethyl choline phosphate copolymer or vitamin E methyl acrylate - 2 - methacryloyl ethyl choline phosphate copolymer or vitamin D2 Methyl acrylate - 2 - methacryloyl ethyl choline phosphate copolymer in the copolymer. The in vitro test result display, the present invention provides nano-microsphere to human prostate cancer cells DU145, black pigment tumor cell A375 with human pancreatic cancer cell strain bxpc - 3 anti-tumor activity significantly higher than to the orlistat alone, and than to adopt the PMB30W as carrier preparation of contrasting the nanosphere and containing orlistat and polyethylene glycol - polycaprolactone nanosphere of better anti-tumor activity. (by machine translation)
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Paragraph 0111-0112; 0115
(2018/10/11)
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- Application of nanoparticle containing orlistat in preparing anti-hepatitis B virus medicine
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The invention relates to the technical field of medicines, in particular to application of a nanoparticle containing orlistat in preparing an anti-hepatitis B virus (HBV) medicine. The nanoparticle isprepared from the orlistat and a copolymer chosen from a vitamin A methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer or a vitamin E methacrylate-2-methacryloyloxyethyl phosphorylcholinecopolymer or a vitamin D2 methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer. The encapsulation efficiency of the nanoparticle is 82.67-93.83%; animal test shows that after oral administration of the nanoparticle, the blood drug concentration is higher, and the sustained-release effect is good; an in-vitro test result shows that the inhibition ratio of extracellular HBV DNA replication is used as an index, and the activity of the nanoparticle for resisting HBV infection is significantly higher than those of the orlistat and a contrast nanoparticle prepared by adopting PMB30W as acarrier.
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Paragraph 0084; 0085; 0088
(2018/10/11)
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- Orlistat nanosphere and application of same in preparation of obesity treatment drugs
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The invention relates to the technical field of medicine, in particular to an orlistat nanosphere and application of the same in preparation of obesity treatment drugs. The nanosphere comprises orlistat and a copolymer, wherein the copolymer is selected from one of a vitamin-A methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer, a vitamin-E methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer or a vitamin-D2 methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer. The encapsulation efficiency of the nanosphere is 82.67-93.83%. Animal experiments show that the vitamin absorption level of rats after the nanosphere is taken by the rats orally is obviously higher than the vitamin absorption level of rats after the orlistat and vitamins are taken by the rats orally at the same time (at the interval of two hours), and is similar to the vitamin absorption level of rats after the vitamins are taken by the rats individually and orally under fasting, so that deficiency of fat-soluble vitamin due to oral administration of the orlistat can be make up effectively, and safety weight loss can be realized.
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Paragraph 0082; 0083; 0086
(2018/10/11)
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- Synthetic method of artificial cytomembrane main ingredient 2-methacryloyloxy ethyl phosphorylcholine
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The invention provides a synthetic method of artificial cytomembrane main ingredient 2-methacryloyloxy ethyl phosphorylcholine. The synthetic method comprises the following steps: (1) dissolving phosphorus oxychloride in acetonitrile, adding triethylamine at 0 to 10 DEG C, dropwise adding 2,3-dibromo-2-hydroxyethyl methacrylate, reacting at -10 to 0 DEG C, adding triethylamine and choline chloride to facilitate the reaction at -10 to 0 DEG C, and obtaining bromophosphorylcholine after the reaction is ended; and (2) dissolving the bromophosphorylcholine obtained in the step (1) in ethanol, adding zinc powder, severely stirring, and obtaining 2-methacryloyloxyethyl phosphorylcholine. By adopting the synthetic method, a synthetic route of the original 2-methacryloyloxyethyl phosphorylcholine is simplified, no treatment is needed after the purification during the synthetic route, and the next operation can be directly carried out; severe conditions in the synthetic route are avoided, high-end equipment is not needed, uncontrollable factors during the synthetic route are reduced; raw materials are easy to obtain, the price is low, the cost is reduced, the use of solvents and raw materials with large toxicity is avoided, and the green synthesis is realized; and a foundation is set for the industrialization of the 2-methacryloyloxyethyl phosphorylcholine.
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Paragraph 0020; 0021; 0022; 0023; 0024; 0025
(2017/10/12)
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- POLYMER AND CONTRAST AGENT FOR PHOTOACOUSTIC IMAGING INCLUDING THE POLYMER
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To provide a polymer having a high ratio of the amount thereof present in a tumor to the amount thereof present in blood (hereinafter, sometimes abbreviated as a tumor/blood ratio). The polymer has phosphorylcholine (derivative) as a side chain and has a dye (near-infrared dye) having absorption in the near-infrared wavelength region bound to the polymer.
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Page/Page column 36
(2016/05/24)
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- ACRYLOYLOXYETHYLPHOSPHORYLCHOLINE CONTAINING POLYMER CONJUGATES AND THEIR PREPARATION
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The present invention relates to polymeric reagents and conjugates thereof, methods for synthesizing the polymeric reagents and conjugates, pharmaceutical compositions comprising the conjugates and methods of using the polymer conjugates including therapeutic methods where conjugates are administered to patients.
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Page/Page column 93; 94
(2010/11/28)
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- Preparation of phospholipid analogues using the phosphoramidite route
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The phosphoramidite route has been used to prepare phospholipid analogues possessing biocompatible properties and the monomer 2-(methacryloyIoxy)ethylphosphorylcholine, utilised in the preparation of biocompatible polymers. Modifications to established methodology include, as an alternative to the thermally unstable tetrazole, the use of 4,5-dichloroimidazole as an acid catalyst for preparing phosphite esters from the corresponding phosphoramidites, and the use of trimethylamine N-oxide as oxidant for the conversion of the phosphite esters into the corresponding phosphates. The Royal Society of Chemistry 2000.
- Browne, Judith E.,Driver, Michael J.,Russell, Jeremy C.,Sammes, Peter G.
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p. 653 - 657
(2007/10/03)
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