- Application of Monodisperse PEGs in Pharmaceutics: Monodisperse Polidocanols
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Polydisperse PEGs are ubiquitously used in pharmaceutical industry and biomedical research. However, the monodispersity in PEGs may play a role in the development of safe and effective PEGylated small molecular drugs. Here, to avoid the polydispersity in polidocanol, the active ingredient in a clinically used drug, a macrocyclic sulfate-based strategy for the efficient and scalable synthesis of monodisperse polidocanols, their sulfates, and their methylated derivatives, was developed. TLC and HPLC analysis indicated a complex mixture in regular polidocanol and high purities in monodisperse polidocanols and their derivatives. Assay on HUVEC, L929, and HePG2 cells showed that monodisperse polidocanols have much higher cytotoxicity and safety than that of regular polidocanol. It was found that the monodispersity of PEGs in polidocanols is crucial for achieving the optimal therapeutic results. Therefore, based on this case study, it would be beneficial to optimize PEGylated small molecular drugs with monodisperse PEGs in pharmaceutical research and development.
- Yu, Zeqiong,Bo, Shaowei,Wang, Huiyuan,Li, Yu,Yang, Zhigang,Huang, Yongzhuo,Jiang, Zhong-Xing
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- Drug carrier based on sulfonium lipidosome structure and preparation method and application of drug carrier
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The invention relates to the technical field of medicine, in particular to a sulfonium compound shown as a general formula (A), and discloses a preparation method of the compound. The compound is poly-condensed with genes to form a nanometer compound with the particle size of 100-300 nm and Zeta potential of +20-+40. The gene loading capability of the sulfonium compound enables the sulfonium compound to have potential application in gene transfer.
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Paragraph 0049; 0061-0063
(2019/08/14)
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- Polyoxyethylene ether carboxylic acid dimeric surfactant type drag reducer as well as preparation method and application thereof
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The invention discloses a polyoxyethylene ether carboxylic acid dimeric surfactant type drag reducer as well as a preparation method and application thereof. The polyoxyethylene ether carboxylic aciddimeric surfactant type drag reducer has a structure formula m=2, 3, 4, and n=1, 2, 3. The drag reducer disclosed by the invention is a dimeric surfactant type drag reducer which has a head group of carboxylic acid, and the head group has the advantages of being very good in temperature resistance, salt resistance, environment protection and the like, and is capable of overcoming influence of a high-salt environment upon drag reduction performance, so that the drag reducer disclosed by the invention is high in drag reduction efficiency, good in shearing resistance, long-lasting and stable in drag reduction rate and good in salt resistance; and polyoxyethylene ether carboxylic acid dimeric surfactants of different mass concentrations are dissolved into water, a drag reduction solution whichis high in drag reduction efficiency, good in shearing resistance, long-lasting and stable in drag reduction rate and good in salt resistance can be prepared without any other compounded chemical reagent, solution blending steps are simple, the drag reducer is very convenient to use, and meanwhile, the salt resistance is greatly improved.
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Paragraph 0096-0098; 0123-0125; 0150-0152
(2019/09/13)
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- Preparation method and application of monodisperse nonapolyethylene glycol dodecyl alcohol monoether and sulphate thereof
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The invention discloses a preparation method and application of monodisperse nonapolyethylene glycol dodecyl alcohol monoether and sulphate thereof and belongs to the field of pharmaceutical and chemical industry. Starting from dodecyl alcohol, firstly ring-opening reaction is carried out with nonapolyethylene glycol cyclic sulphate once or with multiple oligomeric ethylene glycol cyclic sulphate containing nine ethylene glycol units in total for multiple times in presence of alkali, so that sulphate of nonapolyethylene glycol dodecyl alcohol monoether is obtained; and then hydrolysis is carried out in presence of sulphuric acid, so that the nonapolyethylene glycol dodecyl alcohol monoether is obtained. The preparation method can be applied to preparation of long-chain alkyl monoether of monodisperse polyethylene glycol and sulphate thereof. The preparation method disclosed by the invention has the advantages that single molecular weight polyethylene glycol cyclic sulphate is taken as a raw material, efficient synthesis of more than hexameric alkyl alcohol monoether of ethylene glycol is realized, no protecting group is used during synthesis, steps are simple and convenient, the preparation method is applicable to industrial production, and the obtained product has obvious advantages compared with existing prepared lauromacrogol.
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- Synthesis and surface properties of N,N-dimethyl-N-dodecyl polyoxyethylene amine-based surfactants: Amine oxide, betaine and sulfobetaine
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Nonionic-zwitterionic hybrid surfactants, namely N,N-dimethyl-N-dodecyl polyoxyethylene (3) amine oxide, and the corresponding betaine and/or sulfobetaine, have been synthesized. Their molecule structures were characterized by means of electrospray ionization mass spectrometry and 1H nuclear magnetic resonance. Compared to the structurally related conventional amine oxide, betaine and sulfobetaine, the critical micelle concentrations of the three hybrid surfactants are one order of magnitude smaller than those of traditional ones. The polyoxyethylene segment between the hydrophilic head group and the hydrophobic tail makes the surface activities of the hybrid surfactants superior to their structure-related counterparts.
- Hou, Liya,Zhang, Huinian,Chen, Hui,Xia, Qibo,Huang, Dongyang,Meng, Li,Liu, Xuefeng
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p. 403 - 408
(2014/05/20)
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- PHOSPHOLIPID-DETERGENT CONJUGATES AND USES THEREOF
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The invention relates to novel compounds, in particular novel O-substituted phospholipids that are useful for the in vitro and in vivo delivery of drugs as well as nucleic acids into cells. The invention also relates to pharmaceutical compositions and supramolecular complexes comprising said compounds and the use of these compounds in therapeutic treatment, in particular in gene therapy.
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Page/Page column 79; 80
(2013/03/26)
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- Combinatorial synthesis of PEG oligomer libraries
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A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.
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Page/Page column 9
(2010/02/15)
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- Omega-hydrofluoroalkyl ethers, precursor carboxylic acids and derivatives thereof, and their preparation and application
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Normally liquid, omega-hydrofluoroalkyl ether compounds (and selected mixtures thereof) have a saturated perfluoroaliphatic chain of carbon atoms interrupted by one or more ether oxygen atoms. The compounds can be prepare, e.g. by decarboxylation of the corresponding fluoroalkyl ether carboxylic acids and are useful, e.g., in cleaning and drying applications.
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