Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Reexamination Certificate
2001-12-14
2003-05-06
Meller, Michael V. (Department: 1651)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
Reexamination Certificate
active
06558690
ABSTRACT:
The present invention relates to a nutritional composition that is taken with a lipase inhibitor prior to the consumption of a meal which enhances the efficacy of the lipase inhibitor by increasing CCK levels and enhancing and extending post meal satiety.
BACKGROUND OF THE INVENTION
Lipase inhibitors are being prescribed for weight reduction in obese patients. A lipase inhibitor functions by inhibiting gastric and pancreatic lipases, thereby rendering them temporarily unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglycerides. The undigested triglycerides are excreted without being metabolized. As the undigested triglycerides are not absorbed, the resulting caloric deficit may have a positive effect on weight control.
Clinical studies have shown that lipase inhibitors, taken prior to consuming a meal containing a moderate amount of fat, significantly increase the excretion of fat. In this fashion, a lipase inhibitor produces weight loss by blocking a percentage of fat that would normally be absorbed. Indeed, it has been shown that lipase inhibitors, such as the prescription drug tetrahydrolipstatin, generically known as Orlistat, are effective in obesity management. Cholecystokinin (CCK) is a peptide released following the consumption of food which is a major satiety signal in humans. Studies have shown that individuals receiving CCK demonstrate a reduction in caloric intake of from about 16-22%. Although the full mechanism whereby CCK exerts its effect on satiety is not known, there appear to be two components, a central component involving CCK receptors in the brain and a peripheral component involving the stomach and small intestine. When food is consumed, CCK releasing protein (CCKRP) is released in the small intestine. CCKRP stimulates CCK release from intestinal cells.
The release of CCK slows gastric emptying and generates the behavioral symptoms associated with satiety. At the same time CCK activates a number of negative feedback mechanisms that effectively shut down the CCK response. There are two primary negative feedback mechanisms, one involving proteases secreted by the pancreas and the second bile salts released from the gallbladder. CCK stimulates the pancreas to secrete a number of proteases, specifically trypsin and chymotrypsin, which inactivate CCKRP thereby effectively reducing its own release. CCK also stimulates gallbladder contraction causing bile salts to be released into the intestinal lumen. Bile salts are powerful regulators of CCK, inhibiting its release.
It is known that fat is a powerful stimulus for the release of CCK in the body. Hence, it might be expected that a lipase inhibitor, by reducing the metabolism of triglycerides, would decrease the release of CCK in the body. In fact, Borovicka et al.
Gut,
2000:46:774-781 report studies showing that a lipase inhibitor, such as Orlistat, accelerated gastric emptying of both the solid and fat phases of a mixed meal and decreased CCK release. These additional actions of lipase inhibitors can profoundly affect normal appetite control mechanisms controlled by CCK. By this is meant that, by decreasing CCK levels, lipase inhibitors interfere with normal appetite control mechanisms. This has important implications for individuals attempting to lose weight using a lipase inhibitor. On one hand, a lipase inhibitor increases the amount of fat excreted. While a lipase inhibitor exerts a positive effect in promoting the excretion of malabsorpted fat. However, by doing so, lipase inhibitors negatively impact the normal physiological mechanism that turns off appetite. Thus, over time, individuals taking a lipase inhibitor would feel more hungry and, as a result, may consume more calories.
It is the logical conclusion, therefore, that the effect of a lipase inhibitor on CCK may, in part, negate its action on fat excretion since weight loss is a function of caloric intake, caloric utilization and excretion. This has been substantiated by Feinle et al. Gastroenterology 2001: 120: 1100-1107 who describe the interrelation between lipase inhibitors and CCK and state that, although the malabsorption of fat is maintained by the lipase inhibitor tested during long-term administration, the mean weight loss is less than would be predicted by the degree of fat malabsorption.
Compositions that stimulate satiety are known. U.S. Pat. No. 4,833,128 discloses the oral administration of phenylalanine in conjunction with protein, carbohydrate and fat to stimulate satiety. It is stated that consumption of a dietary supplement containing phenylalanine fifteen minutes prior to a meal generates a feeling of satiety resulting in reduced food consumption. The presence of phenylalanine in the disclosed preparations limits their use in patients with phenylketonuria. Finally, the patent makes the statement, alluding to a literature citation, that the appetite suppression of CCK may be merely temporary resulting in a limited satiety effect, possibly followed by a “rebound” of weight gain.
U.S. Pat. No. 4,491,578 discloses the oral administration of a trypsin inhibitor to enhance satiety by stimulating the release of CCK. This patent teaches that the release of trypsin from the pancreas provides a negative feedback signal for cholecystokinin secretion. The administration of a therapeutically effective quantity of trypsin inhibitor, therefore, blocks the trypsin released from the pancreas, thereby interfering with the negative feedback mechanism from reducing the release of CCK.
U.S. Pat. No. 5,932,561 teaches that dietary supplements that bind lipids can aid in weight loss and reduce cholesterol. The patent discloses a dietary supplement composition that combines chitosan and saponins from aloe and states that the latter increases the capacity of chitosan to bind fat. The saponins also act as a laxative to off set the constipating effects of chitosan. This patent does not teach that either chitosan or saponins can be used to stimulate cholecystokinin. The weight management characteristics of the disclosed compositions are to primarily the result of its capacity to combine with fat and cholesterol and remove them from the body.
U.S. Pat. No. 5,703,052 teaches that saponins are useful in controlling hypercholesterolemia. However, pure saponins must be utilized in massive amounts to exert a significant effect on the absorption of cholesterol unless they are combined with another moiety, such as certain steroidal glycosides. There is neither teaching nor disclosure of the possible use of saponins as a stimulator of CCK
There is no indication in any of the patents described above that the compositions described therein, or for that matter any composition, would be useful in conjunction with a lipase inhibitor for weight control. There is no recognition in the art that any nutritional or intervention composition would possess such capacity. There is a definite need in the art for a safe and effective nutritional composition that can be taken in conjunction with a lipase inhibitor which would stimulate CCK release, thereby enhancing the effectiveness of a lipase inhibitor. Such compositions are provided in accordance with the present invention.
SUMMARY OF THE INVENTION
In accordance with the present invention, there is provided a method of enhancing the efficacy of a lipase inhibitor utilized in a weight reduction program by administering in conjunction therewith an intervention composition comprising a glycomacropeptide, one or more long chain fatty acids and at least one of soluble and insoluble fibers. The subject nutritional intervention compositions, which may additionally contain other proteins, a source of calcium and conventional flavoring agents and artificial sweeteners, may be administered in combination with certain solid or liquid foods, including water.
DETAILED DESCRIPTION OF THE INVENTION
In accordance with the present invention, it has been found that a nutritional intervention composition, given in conjunction with a lipase inhibitor, significantly enhances the efficacy t
Gibbons, Del Deo, Dolan Griffinger and Vecchione
Meller Michael V.
Pacific Health Laboratories, Inc.
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