DE19608137A1 - Improved diatetics or transport media for actives incorporated in liposomes - Google Patents

Abstract

Use of vegetable phospholipids, as well as special oils or fatty acids, as phospholipid-based diatetics and/or transport media for active materials incorporated in liposomes is new.

Description

The invention relates to the application of both vegetable phospholipids as well as special oils or Fatty acids as a dietary based on phospholipids and / or as a transport medium for those incorporated into liposomes Active ingredients.

Phospholipids and lecithins have been used for dietary purposes for decades administered. The therapeutic benefits have been particularly in the past 15 years Has been the subject of various clinical investigations. Priorities of the Research is in the fields

• Lipid, especially cholesterol metabolism,
• - liver dysfunction,
• - neurological diseases,
• - memory performance
• - Brain development (especially in infants).

The German pharmaceutical authorities have a large number of positive clinical results prompted two monographs on the therapeutic benefits of soy To adopt phospholipids:

1988; Deoiled soy lecithin for fat metabolism disorders
1994: Soybean phosphatidylcholine against lipid disorders and liver diseases.

Over the past few years, the industrial manufacture of phospholipids for dietary purposes almost completely focused on the raw material soy. Soy- Phospholipids have the typical fatty acid composition for soy (approx. 60% linoleic acid, approx. 7% linolenic acid).

Now it can be assumed that for the therapeutic effectiveness of Phospholipids also determine their fatty acid composition Meaning is. Raw materials that phospholipids with long-chain highly unsaturated Contain fatty acids (arachidonic acid, eicosapentaenoic acid, docosahexaenoic acid - so-called PUFA’s) are almost without exception of animal origin (e.g. brain, Fries) are, however, for reasons of health risk for the Consumers (BSE, oxidation problems) not used.  

Consequently, there is no lack of work on the synthesis of phospholipids targeted fatty acid composition. The so obtained Phospholipids are not only complex and expensive to manufacture, they are also often contaminated with a multitude of traces of chemicals by the synthetic route!

The idea of this invention is now through a suitable combination of vegetable (Soybean) phospholipids with special oils or fatty acids a physiological to offer an equivalent alternative.

The basic idea is that both in the human and animal organism Phospholipids and triglycerides only after enzymatic hydrolysis by the Digestive enzymes are absorbed. Before the transition of the resorbed Substances in the bloodstream, however, undergo a reacylation in which the body accesses the fatty acid pool in the intestinal mucosa cell and largely reactivated according to availability.

Are plant phospholipids together with z. B. a PUFA-rich oil administered, simultaneous hydrolysis of phospholipid and triglyceride takes place, then, however, resynthesis from a purely statistical point of view.

As a result, phospholipids appear in the bloodstream that have at least a portion of them PUFA's included. The principle described can of course also be used apply free fatty acids.

A special embodiment of the invention is the combination of the above PUFA's in free or bound form with either phospholipids Emulsion form or in liposomal form.

The particular embodiment is based on the idea, these fat-soluble ones Substances with the aid of vegetable or animal phospholipids in water to emulsify or solubilize. The process of emulsion formation of fats and oils using lecithin and / or phospholipids is sufficient described and used industrially.

Under certain conditions, phospholipids form so-called liposomes. Liposomes consist of one or more phospholipid bilayers (Membrane-like), the spherical or onion-like an aqueous interior enclose. Liposomes are characterized by their inclusion capacity for both water-soluble substances (inside the aqueous compartments), as well as for fat-soluble ingredients. The latter are in a dissolved form inside the Phospholipid double layer before. Because liposomal preparations are stable dispersions represent in water, both water-soluble substances and also especially fat-soluble substances stable and permanent in water be incorporated.  

Suitable liposomes - also on an industrial scale - are available Methods available.

Combine dietary drinks in emulsion but especially in liposome form various advantages for the manufacturer and also for the consumer:

• - Solubilization of fat-soluble substances (here PUFA's in free or triglyceride form),
• -Improved absorption of fat-soluble substances,
• - protection of sensitive substances,
• - "Additional dietary benefit" due to the use of phospholipids in the Manufacture,
• - completely natural ingredients,
• - easy manufacture,
• - "High Tech" marketing image of liposomes.

Egg phospholipids naturally contain approx. 70-75% phosphatidylcholine with 3-4% Docosahexaen acid, as well as 5-6% arachidonic acid (through targeted feeding the DHA content can be increased to over 6%).

Phosphatidylcholine has been shown to increase blood choline levels after oral intake Level and thus the synthesis rate of the neurotransmitter acetylcholine.

Extensive work on the positive correlation of elevated blood choline Spiegel mitigating the symptoms of certain neurological diseases and moderate memory improvement are known. This effect is both described about egg as well as soy phosphatidylcholine.

Docosahexaenoic acid (DHA) is also associated with one Increase in brain function in the direction of memory improvement in adult people, or with the development of brain performance and Eyesight in the infant / growing animal.

The great advantage of egg phospholipid-containing preparations is that they are synergistic combination of proven neurologically active components included, both for adult humans, and for the infant and the toddler improves brain development / performance to have. The literature suggests that the administration of egg phospholipids also strengthens the immune system.

The substances mentioned are also of extraordinary importance the breeding of land animals as well as fish and crustacean larvae. The breeding and Breeding success is significantly improved and the failure rates drastically reduced.

Egg phospholipids can be administered orally for the purposes mentioned (dietetics, capsules, tablets,...), as well as the feed in any form be added. Administration in is also suitable in humans disperse form (possibly with the help of known dispersing aids) possible intravenously.  

A special embodiment in turn consists of a liposomal Preparation of egg phospholipids, which can not only be administered as a drink, but is also suitable for injection purposes and at the same time to improve Resorption leads. In addition, egg phospholipid liposomes have both water-soluble active ingredients can be loaded, which in the sense of described effects have a reinforcing effect, as well as with lipophilic substances - such as PUFA’s - in free or bound form.

Examples

• 1. 100 g of fish oil (e.g. Tuna Orbital 011) are mixed with 50 g soy lecithin (e.g. Epikuron 135 F from LUCAS MEYER). The homogeneous, transparent solution is suitable for direct encapsulation in soft gelatin 1 capsule of 500 mg content contains:
  150 mg phospholipids
  53 mg phosphatidylcholine
  50 mg docosahexaenoic acid (DHA)
  10 mg eicosapentaenoic acid (EPA).
• 2. 6 g of egg lecithin (eg Ovothin 170 from LUCAS MEYER) are dispersed in 969 ml of water and the dispersion takes about 30 minutes. left to allow the phospholipids to swell sufficiently. Then 25 g of fish oil (e.g. Tuna Orbital Oil) are worked in with vigorous stirring. The coarse emulsion is then homogenized 4 × at 350 bar and then at 123 ° C. for 30 minutes. long sterilized. The fish oil emulsion is stable and can be flavored as desired. Contain 50 ml (a daily dose) of this emulsion
  approx. 300 mg DHA
  approx. 60 mg EPA
  4.2 g phosphatidylcholine corresponding to 655 mg choline.
• 3. 40 g of egg phospholipids (e.g. Ovothin 170 from LUCAS MEYER) are added in 10 g of abs. Ethanol and 40 g glycerol dissolved. This pro-liposome form according to EP 0158441 is then homogeneously mixed with 8 g of fish oil (e.g. tuna orbital oil). The slow addition of 942 ml of water with continuous stirring forms a liposomal preparation in which the fish oil is enclosed in the liposome membrane. The preparation can then be sterilized. 50 ml of this preparation contain:
  1400 mg PC corresponds to 220 mg choline
  100 mg DHA
  20 mg EPA.
• 4. As example 3, but without the conversion of the pro-liposome into the final liposome dispersion.
  This preparation does not require sterilization and can either be taken in capsule form by the user or converted into a liposomal preparation by stirring into a liquid (milk, juice, water).

Claims (1)

Use of both vegetable phospholipids as well special oils or fatty acids as one on phospholipids based dietary and / or as a transport medium for in Active ingredients incorporated into liposomes.