Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1988-11-30
1990-04-17
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
514 77, 514 78, A61K 31685
Patent
active
049180622
DESCRIPTION:
BRIEF SUMMARY
The invention refers to pharmaceutical compositions containing as the active principle L-.alpha.-glycerylphosphorylcolamine for the treatment of cerebral psycho-organic syndromes.
The L-.alpha.-glycerylphosphorylcolamine or L-.alpha.-glycerylphosphorylethanolamine (GPE) (J. Am. Chem. Soc. 75, 4510-14, 1953), physiological metabolite in the lipids metabolism, is a deacylated precursor of cephalins, particularly abundant phospholipids in the central nervous system.
The L-.alpha.-glycerylphosphorylcolamine is also a precursor of glycerylphosphorylcholine and of phosphatidylcholine.
According to what is presently known on the cerebral metabolism and biochemistry it is however impossible to devise any therapeutic use for GPE.
It has now been surprisingly found that GPE, administered to laboratory animals is able to significantly improve the response to the learning and memory tests, whereas, when administered to man, it has shown the ability to influence in a likewise significant way the neurophysiological parameters, the psychometric tests and the used neurologic scales.
Said pharmacological actions are probably due on one side to the activation of the phospholipids biosynthesis in the microsomes of the Central Nervous System (CNS) and on the other to the stimulation of the biosynthesis of the neurotransmitter acetylcholine, through the metabolic intermediates glycerylphosphorylcholine and phosphatidylcholine.
It is well known in fact that the frequent memory disturbances constantly found in aging are related with a decrease of the central cholinergic transmission: it has been shown in fact that a functional and anatomic impairment of cholinergic circuits constantly accompanies the alteration of the mnemonic functions (Drachman D. A., Sahakiam B. J.: Effects of cholinergic agents on human learning and memory, in: Nutrition and brain, 5, Barbeau A. et al. J. eds. 351-361, Raven Press Pubs, New York, 1979).
The validity of the invention is not in any way connected to the verification of the above stated mechanisms of action. The results obtained with GPE in pharmacological and clinical tests are reported hereinafter.
TOXICITY
It is meaningless to speak of subacute or chronic toxicity for GPE, which is physiological metabolite normally present in the human body.
As far as acute toxicity is concerned, the following data are obtained: both in mice and rats and in rabbits. mg/kg.
PHARMACOLOGICAL TESTS
The GPE administered i.p. to 20 male mice at the dose of 100 mg/kg subjected to the electroshock test as described by Esseman in Pharmacol. Res. comm. 5, 295-302, 1973, and at the same dose and for the same route to 20 male rats subjected to the pole-climbing test as described by Cook and Weindley (Ann. N.Y. Acad. Sci. 66, 740-752, 1957) has significantly shown the ability to activate learning and memory in comparison to the untreated animals.
CLINICAL TESTS
The above described pharmacological activity has been confirmed in clinical tests in the treatment of senile cerebral alteration, of both involutive and cerebro-vascular insufficiency origin, and of the related symptomatology, such as slowing of psychic activity, memory and alertness decrease, mood alteration, emotional weakness, irascibility, anxiety, etc.
20 patients (10 male and 10 female) 59 to 76 years old were treated; the overall clinical evaluation, taking into account the improvement of the neurophysiological and neurological exams carried out, of the psychometric tests and of the used neurological scale (De Renzi E., Nichelli P.: Verbal and non-verbal short-term memory impairment following hemispheric damage, Cortex, 11, 341-354, 1975; Bisiach E. et. al.: Neurologia Clinica, Ricerche di psicologia, Ed. F. Angeli, Milano, 1977; Cafarra P. et al.: Neuropsychological testing during a transient global amnesia episode and its follow-up, Acta Neurol. Scand. 63, 44-50, 1981; Kobs S. C.: Intelligence measurement, Mc Milan Pubs, New York, 1923), has shown a significantly positive therapeutic effect in 19 cases, whilst only one treatment was considered to
Friedman Stanley J.
Riace Establishment
Schneider Walter H.
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