- Synthesis of phosphatidylcholine with conjugated linoleic acid and studies on its cytotoxic activity
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Phospholipids with conjugated linoleic acid (CLA), which are potential lipid prodrugs, were synthesised. CLA was obtained by the alkali-isomerisation of linoleic acid and was subsequently used in the synthesis of 1,2-di(conjugated)linoleoyl-sn-glycero-3-phosphocholine in good (82%) yield. 1-Palmitoyl-2-(conjugated)linoleoyl-sn-glycero-3-phosphocholine was obtained by a two-step synthesis in 87% yield. All the compounds were tested in an in vitro cytotoxicity assay against two human cancer cell lines, HL-60 and MCF-7, and a mouse fibroblast cell line, Balb/3T3. The free form of CLA exhibited the highest activity against all cancer cell lines. Results obtained for the Balb/3T3 line proved that phosphatidylcholine derivatives decreased the cytotoxic effect of CLA against healthy cell lines.
- Niezgoda, Natalia,Mitula, Pawel,Kempinska, Katarzyna,Wietrzyk, Joanna,Wawrzenczyk, Czeslaw
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p. 354 - 361
(2013/05/22)
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- NOVEL FORMULATION OF DEHYDRATED LIPID VESICLES FOR CONTROLLED RELEASE OF ACTIVE PHARMACEUTICAL INGREDIENT VIA INHALATION
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A new formulation of dehydrated lipid vesicles employs a vesicle preserver and permits the control of release and delivery of active pharmaceutical ingredients into the respiratory system for treatment in particular of asthma. The typical formulation provides controlled release of the active pharmaceutical ingredient from 0% to 100% from 0 to 72 hours after inhalation, changes the systemic administration to topical administration, allows prolonged therapeutic period for one administration, increased stability, with reduced dose, reduced systemic side effects, reduced toxicity.
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- Total synthesis of 2-(5,6-epoxyisoprostane A2)phosphorylcholine and elucidation of the relative configuration of the isoprostane moiety
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(Chemical Equation Presented) The two possible diastereomers of 5,6-epoxyisoprostane A2 were synthesized efficiently through aldol condensations of a substituted cyclopentenone and the corresponding epoxyaldehydes (see picture). The relative configurations of the products were assigned by comparing their 1H NMR spectra with literature data. Condensation of the epoxyisoprostane A2 with lysophosphorylcholine (lyso-PC) then furnished the title lipid.
- Acharya, Hukum P.,Kobayashi, Yuichi
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p. 3481 - 3484
(2007/10/03)
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- A rapid condensation between lysophosphorylcholine and fatty acids with an easily separable amine base
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With 2,6-Cl2C6H3COCl and 1-methylimidazole, the title condensation completed at room temperature within 12 hours, which is shorter time than that with the standard DCC/DMAP system. Use of easily separable 1-methylimidazole from the crude product by chromatography is an additional advantage of the present reagent system. Georg Thieme Verlag Stuttgart.
- Acharya, Hukum P.,Kobayashi, Yuichi
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p. 2015 - 2018
(2007/10/03)
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- Novel pharmaceutical composition of ceftiofur
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The present invention relates to a pharmaceutical oily suspension comprising cephalosporin antibiotic or its pharmaceutically acceptable salt, at least a biocompatible oil, a wetting agent, a dispersing agent and a resuspendibility enhancer, said suspension has improved properties, such as resuspendibility and chemical stability and process thereof.
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- Deuterated cyclosporine analogs and their use as immunomodulating agents
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Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.
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- 2-methyl-thieno-benzodiazepine formulation
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The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.
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- Synthesis of a small library of mixed-acid phospholipids from D-mannitol as a homochiral starting material
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Synthesis of a series of mixed-acid phospholipids containing a polyunsaturated fatty acid using a newly protecting strategy are described. Thus, benzyl and methyl α-(2,4-dinitrophenyl)acetic acid which were respectively removed by BCl3 and 354 nm light are used as protecting groups.
- Xia, Jie,Hui, Yong-Zheng
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p. 1659 - 1663
(2007/10/03)
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- Process for the preparation of L-α-glycerylphosphoryl-choline and of L-α-glycerylphosphorylethanolamine
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A process for the purification of glycerylphosphorylcholine (GPC) and glycerylphosphorylethanolamine (GPE) from crude mixtures by eluting the latter on a cationic resin in acid form equilibrated in an anhydrous solvent, washing the resin with alcohol or a hydrated mixture thereof followed by washing with water, and then eluting on a strong basic resin in OH form to separate purified GPC and GPE.
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- Modified biologically active proteins
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A modified biologically active protein consisting essentially of a biologically active protein bonded to lecithin via a covalent linking group and a pharmaceutical composition comprising the modified biologically active protein in a pharmaceutically-acceptable carrier. The biologically active proteins include antibodies, superoxide dismutase, insulin, and callidinogenase. Lecithin derivatives are also disclosed.
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- Fluoroaliphatic-group-substituted esters and method of making the same
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Fluorine-containing compounds comprising fluoroaliphatic-group-substituted esters derived from (A) ethylenically unsaturated ester comprising a residue of an aliphatic polyol compound substituted with at least one acyl group derived from an ethylenically unsaturated fatty acid, said acyl group having at least one non-terminal carbon-carbon double bond, and (B) fluoroaliphaticsulfonyl chloride or bromide compound.
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- Composition and method for introducing heme, hemoproteins, and/or heme-hemoprotein complexes into the body
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A liquid coacervate composition and a method of introducing heme, hemoproteins and/or heme-hemoprotein complexes into the body. The liquid composition, comprising an oxygen-carrying molecule containing iron and a two-phase aqueous coacervate system, can be administered orally or intraveneously. The liquid composition is utilized to augment the oxygen transport capability of the body, to treat for several of the anemias and/or to act as an oxygen-carrying plasma volume extender.
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- Solid galenical form for oral administration, and the process for its preparation
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New solid galenical form for oral administration, consisting of a mixture of one or more active products and two or more excipients which can be liquefied at a temperature compatible with the active product or products, and which are solid at ambient temperature.
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- Complexes of saponins with phospholipids and pharmaceutical and cosmetic compositions containing them
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Complexes of saponins with natural or synthetic phospholipids have high lipophilia and improved bio-availability and are suitable for use as the active principle in pharmaceutical, dermatologic and cosmetic compositions.
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- Oil-in-water emulsion for parenteral administration
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An emulsifier adapted for use in a nutritive oil-in-water emulsion suitable for parenteral administration is produced by extracting vegetable lecithin with alkyl alcohols having from 1 to 3 carbon atoms, or mixtures thereof, followed by fractional precipitation at specific temperatures and concentrations effective to cause the removal of toxic materials. The alcohol soluble phospholipid fraction produced by the process contains an increased level of phosphatidyl choline and reduced levels of phosphatidyl ethanolamine, inositol phospholipids, phosphatidic acid and glycolipids.
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- Potentiated sulfonamide injectable preparation
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Potentiated sulfonamide compositions useful for intramuscular injection are disclosed which comprise mixtures of alkali metal sulfonamides with microcrystalline potentiators wherein the microcrystals have been coated with mixtures of phospholipids and non-ionic surfactants. The compositions are advantageous in that they can be used extemporaneously by addition of sterile water for injection, the resulting aqueous preparation is stable for long periods of time and upon use the compositions are characterized by syringeability and lack of irritation at the injection site.
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