Lipid-soluble thiamine derivatives in the treatment of autism

Details Lipid-soluble thiamine derivatives in the treatment of autism Lipid-soluble thiamine derivatives in the treatment of autism

2002-03-13

2003-07-01

Azpuru, Carlos A. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

C424S433000, C424S436000, C424S443000, C424S449000, C424S451000, C424S464000

Reexamination Certificate

active

06585996

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates to pharmaceuticals and, more specifically, using pharmaceuticals to treat autism.
BACKGROUND OF THE INVENTION
Autism is a disabling neurological disorder that affects thousands of Americans and includes a number of subtypes, with various assumed causes and few documented ameliorative treatments. Autism is characterized by behavioral syndrome often recognized between two and three years of age. There is no clear-cut biological marker for autism. Diagnosis of the disorder is made by considering the degree to which the child matches the behavioral syndrome, which is characterized by poor communicative abilities, peculiarities in social and cognitive capacities, and maladaptive behavioral patterns.
There currently is no known medical treatment for autism. A number of different therapies have been attempted in an effort to cure autism or at least lessen its symptoms, including drug therapies as well as psychiatric care and attempted counseling. In general, results of such treatments have been disappointing, and autism remains very difficult to effectively treat, particularly in severe cases.
In 1951, scientists in Japan discovered that garlic bulbs contained a disulfide derivative of thiamine that was, biologically, a very active form. Scientists noted that this disulfide passes through the lipid barrier in cell membranes, hence, it is referenced to as fat soluble. This lipid soluble form of thiamine was shown to be more readily absorbed from the intestine to produce higher levels of thiamine in the blood, cerebrospinal fluid, and urine, and to induce less thiamine fecal loss than the water-soluble forms of thiamine.
A variety of lipid-soluble thiamine compounds, known as thiamine alkyl disulfides or allithiamines, have been synthesized and are commercially available in Japan, parts of Europe, and elsewhere. The lipid-soluble thiamines most commonly used on humans include thiamine tetrahydrofurfuryl disulfide (TTFD), thiamine propyl disulfide (TPD), and O-benzoylthiamine disulfide.
The lipophilic character of the lipid-soluble thiamines allows these compounds to pass through the membranes of cells, thus allowing a greater amount of thiamine to be introduced into the cell versus the water-soluble form of thiamine. The water soluble forms of thiamine require an enzymatic system to transport it through cell membranes, thus, making the water soluble form less efficient than the lipid soluble form.
Lipid-soluble thiamines have been used on humans on an experimental basis to investigate the short-term treatment of disorders of thiamine deficiency and thiamine metabolism.
There remains a need in the art for a pharmaceutical treatment offering clinical improvement in the autistic patient.
DISCLOSURE OF THE INVENTION
The present invention features a method of treating autism in a patient. The method comprises the step of administering to a person in need of such treatment a therapeutically effective amount of a lipid-soluble thiamine derivative. In one embodiment, the lipid-soluble thiamine derivative is tetrahydrofurfuryl disulfide.
According to one method, the lipid-soluble thiamine derivative is administered rectally in the form of a suppository. In an alternative method, the lipid-soluble thiamine derivative is administered parenterally. Parenteral administration allows for the thiamine derivative to enter the blood stream without being processed through the digestive tract. Parenteral administration can be accomplished by administering the lipid-soluble thiamine derivative transdermally by applying a transdermal carrier substance to the skin and rubbing the composition into the skin. The transdermal composition can be in the form of a gel, lotion, cream or any other transdermal composition as known to those skilled in the art. In yet another alternative method, parenteral administration can be accomplished by administering the lipid-soluble thiamine derivative sublingually.
Other methods of administering lipid-soluble thiamine derivatives, include but are not limited to, administering the lipid-soluble thiamine derivatives orally in the form of a tablet or capsule and administering intravenously. The present invention also contemplates other physiologically acceptable carriers or excipients for carrying an effective amount of the lipid-soluble thiamine derivative into the patient's body.
In a preferred aspect of the instant invention, the method of treating autism comprises administering a lipid-soluble thiamine derivative, in particular, tetrahydrofurfuryl disulfide, to a child in need of such treatment. In yet another embodiment, the lipid-soluble thiamine derivative is administered to a child in need of such treatment in the form of a suppository.


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