Method for lowering high blood cholesterol levels in hyperlipidemic animals and confections as the ingestion medium

A process for lowering the blood cholesterol of hyperlipidemic patients by oral ingestion of pyruvate and a confection (cereal bar, fruit bar, candy) containing pyruvate as the ingestion medium.

BACKGROUND OF THE INVENTION 
1. Field of the Invention 
The present invention provides a method for lowering high blood cholesterol 
levels in hyperlipidemic animals, and more particularly, feeding such 
hyperlipidemic animals a therapeutically effective amount of pyruvate to 
accomplish the objective. The invention also concerns confections 
containing pyruvate as media for ingesting the pyruvate. 
In human patients, blood cholesterol levels range from 120 to 330, measured 
as milligrams of cholesterol in a deciliter of blood (mg/dl). High blood 
cholesterol is a subjective determination. High levels of blood 
cholesterol are a risk factor for developing heart disease when 
accompanied by high blood pressure, obesity, organic heart disease or a 
family history of organic heart disease, diabetes, smoking (tobacco), and 
in patients who have recently survived heart attacks. The age, medical 
history and condition of each patient must be reviewed before determining 
what constitutes a "high" level of blood cholesterol for that patient. For 
example, in a healthy patient, less than 30 years old with no significant 
medical history, a blood cholesterol level above 200 mg/dl might be 
considered "high" and a patient is a candidate for treatment. In a healthy 
patient 20 to 40 years old with no significant medical history, a blood 
cholesterol level above 220 mg/dl might be considered "high". In a healthy 
patient 40 to 50 years old, with no significant medical history, a blood 
cholesterol level above 250 mg/dl might be considered "high". In any 
patient, blood cholesterol levels above 250 mg/dl are usually considered 
to be "high" and appropriate for treatment. 
2. Description of the Prior Art 
Hyperlipidemic patients exhibit high blood cholesterol levels and are 
considered to be in jeopardy of various circulatory diseases, diabetes and 
heart attacks. 
Pyruvate and mixtures of pyruvate with dihydroxyacetone have been described 
for a number of beneficial results: 
U.S. Pat. No. 4,158,057 describes oral administration of pyruvate and 
dihydroxyacetone to prevent excessive accumulation of fatty deposits in a 
mammal liver due to ethanol ingestion. 
U.S. Pat. No. 4,351,835 describes oral administration of pyruvate and 
dihydroxyacetone to reduce an expected weight gain from a given diet or to 
induce a weight loss in a mammal. The patent also describes oral 
administration of pyruvate and dihydroxyacetone to athletes prior to 
strenuous athletic events to increase endurance and/or performance. 
U.S. Pat. No. 4,415,575 describes oral administration of pyruvate and 
dihydroxyacetone to increase the body protein concentration in a mammal. 
U.S. Pat. No. 4,458,937 describes oral administration of pyruvate to a 
mammal to induce a weight loss or reduce an expected weight gain from a 
given diet. 
U.S. Pat. No. 4,645,764 describes oral administration to a living being of 
pyruvate and dihydroxyacetone to induce a weight loss or to reduce an 
expected weight gain from a given diet and for inhibiting body fat while 
increasing body protein concentration. 
U.S. Pat. No. 4,812,478 describes oral administration of dihydroxyacetone 
to an animal to induce a weight loss or to reduce an expected weight gain 
from a given diet. 
Copending patent application Ser. No. 232,118, filed Aug. 15, 1988, 
describes the use of pyruvate and dihydroxyacetone for increasing the 
glucose uptake in the muscles of an animal. Application Ser. No. 232,118 
has been abandoned and replaced with continuation application Ser. No. 
546,680, filed Jul. 5, 1990. 
These described results of oral administration of pyruvate and pyruvate 
with dihydroxyacetone are of great interest for medical patients who 
ingest ethanol; medical patients having fatty liver deposits or tendencies 
toward fatty liver deposits; medical patients who are obese or have a 
tendency toward obesity; normal subjects desiring to lose body weight or 
to retard body weight increase; normal patients, particularly athletes, 
who desire to increase endurance; and medical patients having diabetic 
tendencies.

STATEMENT OF THE PRESENT INVENTION 
According to this invention I have discovered that high blood cholesterol 
levels of hyperlipidemic patients can be lowered when the patients receive 
oral administration of pyruvate. 
The pyruvate portion of the patient's diet will be from 2 to 15 percent of 
the total calories in the diet. The treatment is most effective when the 
hyperlipidemic patient is on a low fat, weight maintenance diet for 
sub-weight maintenance (reducing) diet. The pyruvate may be mixed as an 
additive with other foods and preferably is included in all or most of the 
patient's meals. Alternatively the pyruvate may be incorporated in candy 
such as hard-coated chocolate or mint pellets, cereal bars (e.g. molded 
granola with fruits) etc. Typically the calorie content of the pyruvate 
will comprise 2 to 15 percent of the total calories in the patient's diet. 
A convenient medium for administering the pyruvate is a confection 
containing 2 to 20 weight percent pyruvate. Such confections may be candy, 
cereal bars, fruit bars and similar food products which are customarily 
consumed between scheduled or planned meals. The confection should be one 
in which the pyruvate is not heated above 180.degree. F. Candy such as 
chocolate bon-bons, hard-candy coated chocolate, nut-filled chocolates, 
fruit or mint jellies or fruits or hard candies are preferred. Snack bars 
comprising coated raw or partially cooked cereal grains and/or fruits 
and/or nuts also are useful as an ingestion medium. 
DESCRIPTION OF THE PREFERRED EMBODIMENTS 
A group of 39 human subjects was assembled for outpatient treatment over an 
observation period of six weeks. All of the subjects were hyperlipidemic 
patients having high blood cholesterol levels, both plasma cholesterol 
(greater than 240 mg/dl) and LDL cholesterol (greater than 150 mg/dl). The 
subjects were divided into a placebo group (20 subjects) and a treatment 
group (19 subjects). Both groups received a weight maintenance diet 
throughout the evaluation period containing 35-40 percent of the calories 
in the form of normal fat and containing normal cholesterol of 400-500 
milligrams/day. A weight maintenance diet contains 28 to 30 calories per 
kilogram of weight. 
The Placebo Group--The 20 subjects of the placebo group included 16 female 
patients and 4 male patients having an average weight 76.3.+-.3.9 
kilograms and an average age of 54.8.+-.2.8 years. The placebo group 
received 7% of the carbohydrate calories in the form of Polycose.TM., 
which is a solution of glucose, i.e., 19 to 32 grams daily. 
Treatment Group--The 19 subjects of the treatment group included 15 female 
patients and 4 male patients having an average weight of 80.4.+-.5.2 
kilograms and an average age of 56.3.+-.2.5 years. The treatment group 
received 7% of the carbohydrate calories in the form of pyruvate, i.e., 26 
to 44 grams daily. 
A statistically significant reduction in the total blood cholesterol was 
observed after six weeks in the treatment group whereas zero change was 
observed in the placebo group. The results are summarized in the following 
TABLE 1. 
TABLE 1 
______________________________________ 
RESULTS OF SIX WEEKS EVALUATION OF SUBJECTS 
HAVING HIGH BLOOD CHOLESTEROL LEVELS 
PLACEBO TREATMENT 
GROUP GROUP 
______________________________________ 
Total Subjects 20 19 
Males 4 4 
Females 16 15 
Average Weight (kilograms) 
76.3 .+-. 3.9 
80.4 .+-. 5.2 
Average Age (years) 
54.8 .+-. 2.8 
56.3 .+-. 2.5 
Total Cholesterol 
In Plasma (start) mg/dl 
265 .+-. 7 
275 .+-. 7 
LDL Cholesterol (start) mg/dl 
175 .+-. 7 
186 .+-. 7 
Total Cholesterol 
In Plasma (ater 6 weeks) mg/dl 
265 .+-. 7 
264 .+-. 7 
LDL Cholesterol (after 6 weeks) 
175 .+-. 7 
176 .+-. 7 
mg/dl 
Change in Cholesterol 
In Plasma mg/dl 0 -11 
LDL Cholesterol mg/dl 
0 -10 
Percentage Change in Cholesterol 
In Cholesterol 0 -4%* 
LDL Cholesterol 0 -5.4%* 
______________________________________ 
*Standard deviation &lt;0.05 compared to placebo values. 
The standard deviation (p=&lt;0.05) indicates that the reported results are 
statistically significant. 
For hyperlipidemic patients weighing from 110 to 250 pounds, an effective 
dosage of pyruvate is from about 10 to about 50 grams per day as a 
substitute for other carbohydrate nutrients in the patient's diet. 
Preferably the calorie content of the pyruvate comprises 2 to 15 percent of 
the total calories in the diet.