Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1996-08-19
1998-06-16
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
A61K 3800
Patent
active
057670668
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/GB95/00352, filed Feb. 21, 1995.
The present invention relates to the use of the mixture of enzymes known as bromelain in the treatment of conditions requiring a reduction or other modification in the bile acid pool. In particular, the invention relates to the treatment and prophylaxis of hyperlipidaemia, especially hypercholesterolaemia.
Coronary heart disease is one of the leading causes of death in the Western World and results from the accumulation of atherosclerotic plaques within the major arteries supplying the heart with oxygen and nutrients. Atherosclerosis progresses for decades without clinical effect gradually constricting the arterial lumen. Coronary Artery Disease is defined as less than 75% occlusion of the arterial lumen, Coronary Heart Disease is defined as greater than 75% occlusion. Symptoms occur when a vessel becomes completely blocked; angina (sharp chest pain) or myocardial infarction (heart attack), or sometimes sudden death. A number of major risk factors have been identified for Coronary Artery and Coronary Heart Disease: age, male sex, hypertension, cigarette smoking, lack of exercise, stress, diet, diabetes, lifestyle and elevated serum cholesterol (hypercholesterolaemia; particularly where the cholesterol is carried as LDL-cholesterol).
Cholesterol is an important component of cell membranes, steroid hormones and bile acids. Approximately two thirds of the daily cholesterol requirement is met by endogenous synthesis by the liver, the remainder being supplied by the diet. Cholesterol is an insoluble lipophilic material which requires encapsulation in lipoproteins before it can be transported in the blood. The main types of lipoproteins are chylomicrons, very low density lipoprotein (VLDL), intermediate-density lipoprotein (IDL), low density lipoprotein (LDL) and high density lipoprotein (HDL). The liver secretes cholesterol into the blood as VLDL that is converted into IDL, which is in turn converted into LDL. LDL makes up about two thirds of the cholesterol carried in the blood where it is transported back to the liver with the help of HDL. Many cells exhibit LDL receptors on their surface enabling the uptake and extraction of LDL cholesterol for synthesis of cellular components. It is the liver, however, which is responsible for the extraction of most LDL-cholesterol, where it may be secreted into the blood or alternatively into bile (either as bile acids or free cholesterol). Chylomicrons are made by gastrointestinal cells from lipids, including cholesterol, absorbed from the diet, secreted into the lymph and subsequently enter the systemic blood supply where peripheral tissues break down and utilise the lipid components. The resulting chylomicron remnants are returned to the liver.
Elevated blood LDL levels may be reduced in a number of ways with a concomitant decrease in the risk of developing disorders associated with atherosclerosis. Normal serum cholesterol levels are defined as below 200 mg/dl, mild hypercholesterolaemia requiring modification to the diet as 200-220 mg/dl, moderate hypercholesterolaemia as 220-260 mg/dl and severe hypercholesterolaemia, requiring drug and dietary intervention, as more than 260 mg/dl. T. Gordon, W P Castelli, M C Hjortland, W B Kannel and T R Dawber (1984), Predicting Coronary Heart Disease in Middle-Aged and Older Persons. The Framingham Study: Journal of the American Medical Association (1977); 238, 497. National Institute of Health Consensus Development Conference Statement on Lowering Blood Cholesterol, Dec. 10-12th (1984).
When hypercholesterolaemia is detected, a series of possible treatments may be considered:
For mild and moderate hypercholesterolaemia the initial recommended therapy is not drugs but diet. Dietary modification includes a reduced consumption of foods rich in cholesterol and saturated fat such as eggs, dairy products and red meat.
In patients with severe hypercholesterolaemia or moderate hypercholesterolaemia which is resistant to changes in diet then drug treatment may be considere
REFERENCES:
patent: 4440749 (1984-04-01), Fugisaki et al.
patent: 5460812 (1995-10-01), Sipos
Cortecs Limited
Jordan Kimberly
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