Drug – bio-affecting and body treating compositions – Designated organic nonactive ingredient containing other... – Carbohydrate or lignin – or derivative
Patent
1991-10-08
1993-09-14
Waddell, Frederick E.
Drug, bio-affecting and body treating compositions
Designated organic nonactive ingredient containing other...
Carbohydrate or lignin, or derivative
514785, 514786, 514943, A61K 4700
Patent
active
052449254
DESCRIPTION:
BRIEF SUMMARY
Fat emulsions which are intended, inter alia, for intravenous, nutrient supply and which exhibit insignificant secondary effects have been available since the beginning of the 1960's (Wretlind, A. Development of fat emulsions, JPEN 5: No. 3, 230.235, 1981). This development work has investigated the effect of emulsions which contain a number of mutually different fats (olive oil, cottonseed oil, soyabean oil, maize oil, safflower oil, coconut oil, etc.) and several mutually different emulsifiers (soyabean phospholipids, egg yolk phospholipids, cerebrosides, diglycerides etc.). One characteristic feature common to all of these emulsions is that the fats or oils used comprise triglycerides of fatty acids.
All of the fat emulsions earlier investigated and present day fat emulsions require preparation by homogenization under high pressure. One reason for this is because the fats used have high viscosities. Another drawback with present day fat emulsions is that the fats or oils used can only be cleansed with great difficulty, in a manner to free the glycerides completely from all other substances, such as sterols and unsaponifiable fractions. Several methods have been proposed for cleansing the oils used. One such method has been described by S. S. Chang (U.S. application Ser. No. 4, 101,673). The method to Chang involves removing a part of the polar, undesirable constituents with the aid of silica gel. Other attempts have been made with the aid of molecular distillation techniques. This latter method has not been found to have any practical value, however.
Consequently, there is a desire in this respect to find compounds other than triglycerides which will enable fatty acids to be administered in the form of emulsions, and optionally in the form of emulsions which are totally free from the so-called unsaponifiable residues present in fats of animal and vegetable origins. Another desire is one of discovering fatty acid compounds which have a lower viscosity than the lipids used hitherto and at present in the preparation of fat emulsions. A lower viscosity would also enable fat emulsions to be prepared in a somewhat simpler fashion, and would also enable emulsions to be prepared with smaller particle sizes of the colloidal suspension than those of conventionally prepared fat emulsions.
The present invention now makes it possible to prepare emulsions which will satisfy the aforesaid desiderata, with the use of alkyl esters, and then preferably ethyl esters of fatty acids deriving from synthetic, animal or vegetable origins. These alkyl esters can be obtained either by esterification of triglycerides with ethyl alcohol or other alcohols in the presence of a catalyst, such as sodium alcoholate and certain zinc compounds. Alternatively, fatty acids can be prepared by complete hydrolysis of triglycerides with sodium hydroxide or potassium hydroxide, whereafter the solution containing the salt compound of the fatty acids is extracted with hexane or some other organic solvent, so as to remove unsaponifiable residues. The free fatty acids are obtained subsequent to adding hydrochloric acid or some other acid. The free fatty acids can then be converted to ethyl esters or some other alkyl esters in some suitable way, by treating the fatty acids with ethyl alcohol or some other alkyl alcohol having one or two hydroxyl groups capable of esterification. Suitable esters can also be obtained by esterifying synthetic or otherwise produced fatty acids having an even or an odd number of carbon atoms.
The present invention thus relates to an emulsion intended for parenteral administration and including a hydrophobic phase emulsified in a water phase, this emulsion being characterized in that a substantial part of the hydrophobic phase comprises one or more alkyl esters of pharmacologically acceptable fatty acids. The alkyl esters will preferably comprise low-molecular alkyl esters having 2-4 carbon atoms in the alkyl groups, and then primarily ethyl esters.
The fatty acids are preferably of vegetable, animal or synthetic origins,
REFERENCES:
patent: 4252827 (1981-02-01), Yokoyama et al.
patent: 4284630 (1981-08-01), Yu et al.
patent: 4404182 (1983-09-01), Vermess et al.
patent: 4816247 (1989-03-01), Desai et al.
patent: 4840970 (1989-06-01), Ohasi et al.
The Merck Index 10th ed. (1983) cites 6706 (pp. 979-980) and 8308 (p. 1217).
Chemical Abstracts 97(20):168842c Morimoto et al. (1982).
Ajaxon Bengt M.
Wretlind Karl A. J.
Henley III Raymond J.
Kabi Pharmacia Aktiebolag
Waddell Frederick E.
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