Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1991-04-22
1992-10-06
Dees, Jose G
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514 90, 514249, 514274, 514283, 514654, 514772, 514946, 568567, 568675, 568680, A61K 3170
Patent
active
051531798
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
The invention concerns a medicament which makes possible an improved penetration of the active material through the tissue membrane or barrier of the object organ.
A known problem in the case of the administration of medicaments consists in that the actual active material frequently can only poorly pass the cell membrane so that either the per se possible actions of the medicament cannot in practice be achieved or the active material must be overdosed to such an extent that the undesired side actions, especially in organs other than the object organ, are increased.
Especially problematical in this regard is the co-called blood-brain barrier. The normal blood brain barrier is a highly selective permeability barrier which prevents the blood/brain transfer of many compounds. This especially marked barrier has its anatomical basis in the capillary vessels which display special structural characteristics. The ability of an active material in free solution (i.e. not bound to protein) in the blood plasma to penetrate the blood-brain barrier is substantially determined by the ability of the active material itself to separate out of the plasma and to penetrate into the lipid of the endothelial cell plasma membranes. If no specific mechanism is here present, the lipid solubility is the important factor which causes the penetration of the active material through the blood-brain barrier so long as the molecular weight of the active material is not greater than about 500. Higher molecular active materials are then also not able to penetrate the blood-brain barrier even when the lipid solubility is good.
Therefore, it has already been suggested chemically to modify medicaments by adding a radical with high lipid solubility which makes the penetration into the barrier easier. In the case of suitable choice of this group, it would then again be split off by the metabolism, whereby the active material is liberated in its active form.
A disadvantage of this concept consists in that a modification, which under certain circumstances is difficult to carry out, of the actual active material is necessary and, in the case of the known sensitivity of the effectiveness of medicament active materials to changes in the molecule, activity impairments or new undesired side effects are to be feared.
Similar difficulties as in the case of the blood-brain barrier are also present in the case of other organs, for example in the case of the liver, skin etc.
Therefore, the problem forming the basis of the invention is to solve this problem in a simple way and without change of the actual active material.
According to the invention, this succeeds with a medicament which is characterised in that it consists of an active material in combination with a compound of the general formula ##STR2## in which one of the residues R.sub.1 and R.sub.2 signifies an alkyl, alkenyl, alkynyl or alkoxy group with, in each case, 3 to 7 C-atoms and the other residue signifies an H-atom and conventional pharmaceutical additive and dilution agents.
The compound of the general formula is a glycerol derivative which is substituted in position 1 or in position 2 with one of the above-mentioned short-chained groups. The substituents can be straight-chained or branched and possibly also cyclic and contain up to two double or triple bonds. Typical examples of the compounds according to the invention are 1-n-propylglycerol, 1-n-isopropylglycerol, 1-n-butylglycerol, 1-isobutylglycerol, 1-tert. butylglycerol, 1-n-pentylglycerol, 1-n-hexylglycerol, 1-cyclohexylglycerol and 1-n-heptylglycerol, as well as their isomers 1-methylbutylglycerol, 1-allylglycerol, 1-butynglycerol, the corresponding 2-glycerol compounds, as well as proprionic acid, butyric acid, valeric acid, valeric acid, oenanthic acid, acrylic acid, crotonic acid, angelic acid or tiglic acid, hexenoic acid, heptenoic acid, propionic acid and tetrolic acid esters in position 1 or 2 of the glycerol.
The compounds of the general formula in which R=H are new and, as such, form a subject of the invention.
REFERENCES:
patent: 4393073 (1983-07-01), Boguth et al.
patent: 4562075 (1985-12-01), Rajadhyaksha
Dyer, H. M., An Index of Tumor Chemotherapy, Mar., 1949, pp. 10-12, 149, and 155.
Dees Jose G
Max-Planck-Gesellschaft zur Foerderung der Wissenschaft e.V.
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