- Method for preparing difatty acyl phosphatidylcholine by solid-phase reaction
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The invention relates to a method for preparing difatty acyl phosphatidylcholine by a solid-phase reaction. Glycerol phosphatidylcholine is subjected to wet-process loading by using a high-activity solid adsorbent, and then a condensation reaction is carried out on the glycerol phosphatidylcholine with fatty acid to obtain the difatty acyl phosphatidylcholine. The method comprises the following steps: dissolving glyceryl phosphatidylcholine in an organic solvent, adding a high-activity solid adsorbent, carrying out adsorbing dispersion while stirring, removing the organic solvent by vacuum evaporation, and carrying out vacuum drying on the obtained solid-phase loaded mixed material; dissolving fatty acid in an organic solvent, adding a condensation coupling agent, carrying out heating reflux to prepare active ester of fatty acid, adding the solid-phase loaded glyceryl phosphatidylcholine, and continuing reflux to prepare a difatty acyl phosphatidylcholine crude product; and carrying out filtering to recover the high-activity solid adsorbent, desolventizing mother liquor, pulping a crude product by using an organic solvent, and carrying out recrystallizing to obtain the high-puritydifatty acyl phosphatidylcholine. According to the method, the reaction yield reaches 65% or above, the product purity reaches 99% or above, the process is simple, the production period is short, andindustrial production is easy to achieve.
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Paragraph 0023; 0024
(2019/12/25)
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- Process for the production of phospholipids
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A new enzymatic process for preparing 1,2-diacylated phospholipids using an enzyme preparation possessing phospholipase activity towards acylation at the sn-1 and sn-2 sites in a microaqueous reaction system. More particularly, the 1,2-diacyl-phospholipids produced according to the esterification/transesterification process are obtainable in high yield and purity and carry identical desired carboxylic acid, preferably fatty acid, acyl groups at the sn-1 and sn-2 positions. The process involves esterification/transesterification (acylation) of a glycerophospholipid, preferably glycerophosphoryl choline (GPC) with a desired carboxylic acid, preferably fatty acid, or their derivatives in the presence of the above mentioned appropriate enzyme preparation. The process of the invention further relates to a process for the production of 1-acyl-2-lyso-glycerophospholipid, preferably 2-lyso-PC by reacting glycerophospholipid, preferably glycerophosphoryl choline (GPC) with a desired carboxylic acid, preferably fatty acid, or their derivatives in the presence of a sn-1 specific phospholipase (PLA1 or PLA1,2) and a solvent, in a microaqueous medium.
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Page/Page column 17
(2008/06/13)
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- Allylamine-containing liposomes
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The invention concerns liposomal preparations comprising as the active agent a compound of formula I in free base form or in acid addition salt form. It also concerns a method of preparation of such liposomal preparations by encapsulating a compound of formula I with an appropriate liposome forming material, a corresponding pharmaceutical compositions, and methods of treatment of systemic, topical and pulmonal fungal infections.
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- FTIR studies of phospholipid membranes containing monoacetylenic acyl chains
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The conformational behaviour of phosphatidylcholine and phosphatidyl acid membranes derived from octadec-14-ynoic and octadec-9-ynoic acid is studied by FTIR spectroscopy comprising both the liquid crystalline and gel phases. In the vicinity of the transition from the gel to the liquid crystalline phase the conformational changes of the acyl chains are followed by the analysis of the CH2 stretching bands and CH2 wagging band progressions. In the liquid crystalline phase a quantitative determination of the amounts of gauche-trans-gauche, double gauche, and end gauche conformers is achieved by the analysis of the CH2 wagging band region. In this connection, several model compounds (hex-2-yne, and hex-3-yne, oct-4-yne) have been examined to assist the assignment of a special vibration band at 1328 cm-1 due to the CH2-C≡C unit. The results for the phospholipids studied here clearly demonstrate that the conformational properties critically depend on their actual lipid structure, sample composition and sample temperature. The derived data are discussed in conjunction with earlier investigations of more conventional lipid systems - mainly containing saturated acyl chains - to evaluate the specific influence of the incorporation of the C-C triple bond into the fatty acid chains.
- Wolfangel, Peter,Lehnert, Rene,Meyer, Hartmut H.,Mueller, Klaus
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p. 4833 - 4841
(2007/10/03)
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- Polymer-supported bases. XII. Regioselective synthesis of lysophospholipids using polymer-supported bicyclic amidines or guanidines
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1-Acylphosphatidylcholines were prepared in good yields by the regioselective monoacylation of L-α-glycerophosphorylcholine with acylimidazoles in the presence of polymer-supported bicyclic amidine of guanidine.
- Tamura,Fukuda,Tomoi,Tokuyama
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p. 2907 - 2914
(2007/10/02)
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- Composition and method for treatment of disseminated fungal infections in mammals
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A method is disclosed for treatment of disseminated fungal infection in a mammal comprising the administration of a fungicidally effective amount of Amphotericin B encapsulated in a substantially sterol-free liposome to the infected mammal. Also provided is an agent for treatment of disseminated fungal infection in a mammal comprising Amphotericin B encapsulated in a liposome which consists essentially of lipids other than sterols.
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- Acoustic shock wave targeting of drug delivery in patients
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Acoustic shock waves generated outside a patient's body are focused upon selected target zones within a patient's body to cause release of biologically active substances from liposomes administered to the patient. The procedures may serve to increase cell uptake of drugs and reduce systemic toxicity.
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- Viral liposome particle
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The outer membrane of influenza virus is attached to a liposome by two different techniques. In addition, one of the techniques allows the entrapment of intact virus, usually one virus per liposome. The techniques can be performed with either influenza virus A or B.
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