Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form
Patent
1995-01-30
1998-12-01
MacMillan, Keith D.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
252312, 252314, 514340, 514365, 514372, 514938, 514974, A61K 31255
Patent
active
058434658
DESCRIPTION:
BRIEF SUMMARY
FIELD OF INVENTION
This invention relates to a novel pharmaceutical formulation comprising an emulsion-stabilizing surface active drug which may be administered parenterally or orally; and to the use of and a process for preparing said formulation.
BACKGROUND OF THE INVENTION
The present commercially available parenterally administered formulation of 5-(2-chloroethyl)-4-methylthiazole, hereafter abbreviated as CMZ, is a 0.8 w/v % solution of the edisilate salt of CMZ in 4 w/v % aqueous glucose. The product is not available in a more concentrated form because the incidence of hemolysis and venous thrombophlebitis is then unacceptably high. The solubility of the active ingredient is also too low at physiological pH. The low concentration of CMZ may require a large fluid load if the product is used for a prolonged period of time. This is a problem especially in patients with renal failure and those with fluid and electrolyte problems. Hence, the above mentioned problems have limited the product's usefulness in the clinic. Moreover, the presence of glucose is contraindicated in the treatment and/or prevention of neurodegeneration. Other undesirable properties of the commercially available product are the poor stability of the CMZ-edisilate at room temperature (the product must be stored at +4.degree.-8.degree. C.) and the substantial sorption of CMZ by intravenous infusion giving sets. This sorption to plastics results in a safety problem in the clinic, especially when treating disorders requiring very accurate dosing. Finally, the oral liquid dosage form, a 5 w/v % syrup of CMZ-edisilate, also has a number of disadvantages such as poor stability at room temperature and a low level of patient acceptance due to the acidity and bitter taste of the product. There is accordingly a great need for an improved product both from a pharmaceutical and clinical point of view.
DESCRIPTION OF THE INVENTION
The problems mentioned above have surprisingly been solved by a novel formulation. Thus, the object of the invention is to provide a novel, clinically and pharmaceutically acceptable and useful formulation which is an oil-in-water emulsion for parenteral and oral use which comprises
The present invention is preferably related to emulsion-stabilizing surface active drugs having an anti-convulsant or sedative-hypnotic effect or drugs for preventing and/or treating neurodegeneration caused by acute and chronic neuropsychiatric disorders characterised by progressive processes that sooner or later lead to neuronal cell death and dysfunction. Such disorders include stroke; cerebral ischaemia; dysfunctions resulting from brain and/or spinal trauma; hypoxia and anoxia, such as from drowning, and including perinatal and neonatal hypoxic asphyxial brain damage; multi-infarct dementia; AIDS dementia; neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's chorea, epilepsy, multiple sclerosis and amytrophic lateral sclerosis; brain dysfunction in connection with surgery involving extracorporeal circulation or in connection with brain surgery, including endarterectomy of the carotid arteries; and CNS dysfunctions as a result of exposure to neurotoxins or radiation. This utility is manifested, for example, by the ability of the claimed formulation to inhibit delayed neuronal death in the gerbil bilateral occlusion model of ischaemia.
Preferred emulsion-stabilizing surface active drugs are the CMZ-base which is an oil at room temperature, and/or some analogues thereof which are oils at room temperature, namely 5-(2-chloroethyl)-4-methyloxazole, 5-(2-chloroethyl)-2,4-dimethyloxazole, 5-(2-chloroethyl)-2,4-dimethylthiazole or 5-(2-chloro-l-hydroxyethyl)-4-methylthiazole or its optical isomers, the surface active drug functioning, besides having a pharmacological effect, as a stabilizing surfactant or co-surfactant at the large interface in an oil in water emulsion system or in another aspect of the invention, functioning as the actual oil phase in an emulsion system.
The use of this invention is,
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Astra Aktiebolag
MacMillan Keith D.
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