Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
2000-09-22
2001-10-30
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
Reexamination Certificate
active
06310100
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention is directed to methods of treating diseases such as hypertension using ferulic acid compounds. It also relates to compositions, such as fat compositions, comprising a ferulic acid compound and a diglyceride.
2. Description of the Background Art
Hypertension is correlated with cardiac diseases such as angina pectoris, myocardial infarction and heart failure. It also is associated with cerebrovascular diseases such as cerebral infarction, cerebral hemorrhage and subarachnoid hemorrhage. Cardiac diseases and cerebrovascular diseases are the second and third causes of death in Japan, respectively. Such diseases cause substantial mortality and morbidity in many other countries as well, particularly in the more developed parts of the world. In the year 1998, sixty four patients per thousand in Japan visited the hospital regularly for hypertension according to research by the Ministry of Health and Welfare and hypertension is a primary cause of death.
As a countermeasure against the hypertension, a number of therapies have been developed, for instance development and use antihypertensive drugs such as diuretics, sympatholytic depressants, vasodilators and angiotensin converting enzyme inhibitors. These drugs are usually administered to patients diagnosed with a serious degree of hypertension.
On the other hand, treatments which generally improve health or contribute to a healthy lifestyle are indicated for patients with slight or serious hypertension. Such lifestyle changes or therapies include, dietary improvements or supplementation, stress reduction, therapeutic exercise and restriction of smoking and drinking. Improvement in dietary habits is of particular importance, as some foods may induce or contribute to hypertension. On the other hand selection of foods that provide hypotensive or anti-hypertensive effects may provide a positive overall benefit. Certain antihypertensive compounds or compositions have been identified and isolated from various food products.
While pharmaceutical medications and drugs generally act faster and exert a satisfactory anti-hypotensive effect than lifestyle or dietary changes, they often burden a patient with undesirable side-effects. On the other hand, while traditional food and nutritional products providing anti-hypertensive benefits are generally safe and free from substantial side-effects, the anti-hypertensive effects provided by these products may not always be satisfactory strong or efficacious, particularly in moderate or severe cases of hypertension, or the beneficial effects of such products may require a long time to develop.
Ferulic acid (3-(4-Hydroxy-3-methoxyphenyl)-2-propenoic acid (C
10
H
10
O
4
) is widely distributed in small amounts in plants. It may be isolated according to the method of Batesmith, Chem. & Ind. (London) 1954, 1457 or Klosterman, Muggli, J. Am. Chem. Soc. 81, 2188 (1959). It may also be prepared by chemical synthesis, for example, a process by a condensation reaction of vanillin and malonic acid, Journal of American Chemical Society, 74, 5346, (1952). Ferulic acid has the following chemical structure:
SUMMARY OF THE INVENTION
It is an object of the present invention to provide a drug, quasi-drug, pharmaceutical composition, or food or nutritional product which exerts a significantly high hypotensive effect, but which is safe, convenient to administer, and easily assimilated. The present inventors have discovered that ferulic acid and its derivatives, such as salts and esters of this compound exert a remarkable anti-hypertensive or hypotensive effect.
Additionally, it has been found that an even higher hypotensive effect can be achieved by a combining a ferulic acid derivative with a diglyceride. For instance by combining a diglyceride with a ferulic acid compound selected from the group consisting of ferulic acid, a salt of ferulic acid and a ferulic ester. Ferulic acid products either alone or in combination with diglycerides are advantageously incorporated into pharmaceutical, nutraceutical or other nutritional products, such as foods for treatment of diseases such as those associated with hypertension.
According to the present invention, there is thus provided a method of treating hypertension, which comprises administering ferulic acid or a salt thereof. The present invention also provides a method of treating hypertension, which comprises administering a composition containing:
(a) at least one ferulic acid compound, for instance selected from the group consisting of ferulic acid, a salt of ferulic acid and a ferulic ester and
(b) a diglyceride.
An inventive fat composition is provided comprising:
(a) at least one ferulic acid compound selected from the group consisting of ferulic acid, a salt of ferulic acid and a ferulic ester and
(b) a glyceride composition containing at least 15% by weight of a diglyceride.
According to the present invention, a ferulic acid compound may be taken by itself as the only active antihypertensive ingredient in a pharmaceutical composition or food, or alternatively in a composition containing a diglyceride. Either alone or in combination, such compositions suppress elevated blood pressure and reduce the effects of hypertension, thus improving the prognosis of diseases associated with hypertension. Additionally, ferulic acid compounds may be combined with other conventional medications for hypertension, or other hypotensive agents. Therefore, the products according to the present invention are useful as drugs and food for preventing and treating hypertension.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
Ferulic acid, and its derivatives, such as its salts and esters used in the present invention may be extracted from natural substances, particularly plants, containing them or industrially manufactured by chemical synthesis. Ferulic acid derivatives also encompass chemical compounds which are biotransformed or converted into ferulic acid when administered to a subject. Such derivatives also include biologically active hypotensive or anti-hypertensive compounds derived from a ferulic acid, its salts or esters when administered to a subject. Incidentally, stereoisomers exist in ferulic acid and its derivatives. However, all the isomers may be used, and mixtures of different isomers may also be used.
Ferulic acid may be extracted from plants such as coffee, onion, Japanese radish, lemon,
Cnidium ooficinale
Makino,
Angelica acutiloba
, pine,
Captis japonica
Makino, asafetida, sweet potato, corn, barley and rice, with rice being particularly preferred. The term “rice” in the present specification includes green or dried products of grain such as
Oryza sative
LINNE.
For the preparation of a ferulic ester, a rice bran oil is first prepared from rice bran, and then partitioned with hydrous ethanol and heat at room temperature under weakly alkaline conditions, thereby obtaining the ferulic ester in a hydrous ethanol fraction. Ferulic acid can be obtained by hydrolyzing the ferulic ester obtained by the above-described process with sulfuric acid with heating under pressure and purifying the resultant hydrolyzate or by culturing Pseudomonas in a medium containing clove oil from buds and leaves of
Syzygium aromaticum
MERRILL et PERRY by steam distillation, or eugenol obtained by purifying clove oil and subjecting the medium to isolation and purification.
The solubility of ferulic acid in water can be improved by providing it in the form of a salt, and its physiological effectiveness thus enhanced. No particular limitation is imposed on the salt of ferulic acid so far as it is a pharmaceutically acceptable salt. Examples of a basic substance used for forming such a salt include alkali metal hydroxides such as lithium hydroxide, sodium hydroxide and potassium hydroxide; alkaline earth metal hydroxides such as magnesium hydroxide and calcium hydroxide; inorganic bases such as ammonium hydroxide; basic amino acids such as arginine, lysine, histidine and ornithine; and organic bases such as monoethanolamin
Ochiai Ryuji
Suzuki Atsushi
Tokimitsu Ichiro
Henley III Raymond
Kao Corporation
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