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chitosan, xenical, orlistat

Chitosan versus Xenical

Is chitosan just another scam, or does it really block a significant amount of fat like Xenical? And if chitosan is a scam, why does Roche have a patent on it?

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Contents

Page 1
Chitosan versus Xenical.
Chitosan patents.
The synergistic effect of vitamin C.
Page 2
Sprague-Dawley rats and human rats.
Page 3
What they don't tell you about Xenical.
Page 4
My chitosan experiment and price comparison.

Page 5
Possible long-term side effects.
Possible long-term benefits.
Discussion.

Possible Long-Term Side Effects

The standard warning on chitosan says that you should not take it if you are allergic to any form of shellfish or if you are pregnant or nursing. In addition, chitosan will reduce the absorption of fat-soluble vitamins (A, D, E, and K) (11), minerals (11, 12), protein (13, 14), and possibly other nutrients (CoQ10, etc.), phytochemicals and some medications (contraceptives, estrogen, etc.). It would be wise to take these things a couple hours before your first dose of chitosan, or a good three or four hours after taking chitosan.

There are two schools of thought concerning vitamin supplementation and it is especially important that people taking fat blockers understand that the old school of thought is dead wrong. It seems rather schizophrenic to me, but the old school oscillates between saying vitamins do nothing except give you expensive urine, and treating supplements as if they were dangerous drugs that should only be given to treat disease (outright deficiency). Of course, to avoid 'toxic' side effects the lowest possible dose should be used. Despite the fact that this view of nutritional supplements is completely divorced from reality, there are still quite a few old school dinosaurs running around. This archaic attitude can be found in a number of Xenical studies:

"Fat-soluble vitamin levels generally remained within the reference range, and vitamin supplementation was required in only a few patients" (15).

"The results of this study will aid in the implementation of a vitamin supplementation strategy, should vitamin deficiency occur in patients undergoing orlistat [Xenical] therapy" (16).

On the other hand, the new school of thought acknowledges the fact that countless studies have shown significantly reduced risk of disease with supplementation at levels that far exceed the amount of nutrients that even the very best diet can provide.

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atoms_ani.gif (1980 bytes) Quality chitosan & vitamin C is available at very competitive prices at WebVitamins:

Natrol Chitosan: 360 capsules (500 mg).

Twinlab C-1000: 250 capsules (1000 mg).

The new school of thought is concerned with far more than avoiding outright deficiency. The new school of thought concerns itself with achieving optimum nutrition -- reducing the risk of disease as much as possible by consuming the optimal amount of each nutrient. With even the best diet, this is simply not possible without supplements. Thus, it would be absolutely moronic not to take supplements if you are going to take a fat blocker that reduces the amount of nutrients that you assimilate from food.

Don't be fooled by the human studies that showed little or no change in nutrient status. Those studies used pathetically low amounts of chitosan with no vitamin C. It's no wonder why they found no change in weight, cholesterol, or nutrient status -- with the tiny amounts of chitosan used in these studies there wasn't a snow balls chance of ANYTHING happening! This is why so many people mistakenly think chitosan is a scam.

But high doses of the chitosan/vitamin C combination are indeed quite powerful. The problem is, in addition to blocking a lot of fat, this combination can cause a "marked and rapid decrease in the serum vitamin E level" and even affect bone mineral content: "Chitosan feeding for 2 weeks caused a decrease in mineral absorption and bone mineral content, and it was necessary to administer twice the amount of Ca [Calcium] . . . to prevent such a decrease in the bone mineral content" (11).

Perhaps the best way to avoid a deficiency is to eat a small snack and wash your supplements down with a whey protein shake first thing in the morning -- at least a couple of hours before taking chitosan/vitamin C. And be sure to take plenty of calcium (12).

Possible Long-Term Benefits

In addition to all the health benefits associated with weight loss, chitosan can probably reduce the risk of heart disease due to its beneficial effects on cholesterol metabolism. Chitosan was found to lower serum LDL (the "bad" cholesterol) in a study involving obese women "who had not changed their eating habits" (3). A study involving apolipoprotein E-deficient mice also produced impressive results:

" highly significant inhibition of atherogenesis, in both the whole aorta and the aortic arch, was observed in the chitosan fed animals--42 and 50%, respectively . . . [This study] suggests that the agent [chitosan] could be used to inhibit the development of atherosclerosis in individuals with hypercholesterolaemia" (17).

It is important to note that these benefits are probably not limited to people eating high fat diets and genetically-doomed knockout mice. Rats fed a cholesterol-free diet also experienced an improvement in the ratio of high-density lipoproteins (HDL) to very low-density lipoproteins (VLDL) and increased fecal excretion of cholesterol (8). In addition, chitosan has been found to increase excretion of fecal bile acid (18) and triglyceride (14). Indeed, the research suggests that chitosan has a number of beneficial effects on cholesterol metabolism (9, 14, 19).

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"America's abundance was not created by public sacrifices to "the common good," but by the productive genius of free men who pursued their own personal interests and the making of their own private fortunes . . . the good of the country was made possible precisely by the fact that it was not forced on anyone as a moral goal or duty; it was merely an effect; the cause was a man's right to pursue his own good. It is this right -- not its consequences -- that represents the moral justification of capitalism."  -- Ayn Rand
Capitalism: The Unknown Ideal

* Check out Dr. Mary Ruwart's thoughtful commentary on research incentives in a Libertarian society and the negative influence of excessive regulations.

Written
Sep 2001
Last Update
Sep 2001

Chitosan has also been found to improve glycemic control and prevent the progression of low dose streptozotocin-induced non-insulin-dependent diabetes mellitus (NIDDM) (20). But one study found that chitosan did not help obese type NIDDM (21). There are few things that annoy me more than the use of the phrase "more research is needed" as a mindless mantra to avoid the risk of drawing conclusions from data. But I've got to say it: more research is needed. However, although a number of details are still open to debate, I think it is clear that chitosan is definitely the best fiber supplement (9, 10, 18, 22) -- especially for obese people.

Discussion

Frankly, when I started gathering research for this post, I assumed the conclusion would be "it might work, but you would have to eat a pound of it." But the High Dose Chitosan/Vitamin C combination is only seven capsules taken before meals. I realize people who hate swallowing pills will probably think that's ridiculous, but it costs half as much as Xenical and it seems to have none of the nasty side effects. In addition, it may actually be more effective than Xenical. I use the word "may" because we definitely need some well-designed human research.

The tiny doses recommended by the supplement companies are probably a waste of money. Interestingly, the Hoffmann-La Roche patent (# 6,030,953) on chitosan/Xenical zeros right in on the effective dose range:

"the dosage amount is from 10 to 120 mg of orlistat and from 2 to 6 g of chitosan, particularly about 60 mg of orlistat and about 2.5 g of chitosan per fat containing meal consumed by the patient. Preferably, the composition is orally administered to the patient at breakfast, lunch and dinner."

After reading this patent, I tried the 6 gram megadose and experienced no side effects except an inability to eat more than two meals a day. Specifically, the dose I used was 6 grams of chitosan and 2 grams of vitamin C taken 30 minutes before each meal. I've got news for Hoffmann-La Roche: a person would have to have one heck of an appetite to eat three times a day while taking 6 grams of chitosan before each meal.

I'm glad I took the time to personally experiment with the chitosan/vitamin C combination. I'm not big on anecdotes because they don't prove anything, but during the experiment, I lost 18 pounds. This is a good bit more than I would have lost with my normal routine. Reducing fat absorption and appetite while simultaneously taking ECA seems to be a very powerful combination. The ECA stack normalizes the respiratory quotient and prevents your metabolism from slowing down in response to the reduced food intake. For more information on the respiratory quotient, see my post on Green Tea And Thermogenesis.

One argument against chitosan that I've seen many times is that it is easier and cheaper to just eat less fat. But based on my experience and some of the animal research, high doses of chitosan can significantly reduce appetite. If this effect occurs in most people and persists, the chitosan/vitamin C combination will prove to be a uniquely useful weight loss tool, since most appetite suppressants quickly lose their effectiveness. In addition, bodybuilders that are on extremely strict diets might want to take it once in a while -- an occasional chitosan and pizza night might make it easier to stick to the diet the rest of the time.

I am going to continue my experiments with the chitosan/vitamin C combination, but one thing that is certain is the need for more research. There are a LOT of studies that need to be done, but there is little incentive to do them. Understandably, the pharmaceutical companies are interested in doing research related to drug development. And there is little motivation for supplement companies to fund this kind of research. But I don't see this as a reason to throw more money in the black hole of government. Since obese people have the most to gain (so to speaksmiley.gif (125 bytes)), we should form an organization and directly fund this kind of neglected research -- research that can yield almost immediate benefits. He who pays the piper calls the tune and if we rely on government bureaucrats or "business as usual," the tune will be our swan song, but if we rely on ourselves, it can be a victory march.

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References

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1.) Guerciolini R; Radu-Radulescu L; Boldrin M; Dallas J, and Moore R. "Comparative evaluation of fecal fat excretion induced by orlistat and chitosan." Obes Res, 2001 Jun; Vol: 9; Number: 6; Page: 364-7; PMID: 11399783.

2.) Pittler MH; Abbot NC; Harkness EF, and Ernst E. "Randomized, double-blind trial of chitosan for body weight reduction." Eur J Clin Nutr, 1999 May; Vol: 53; Number: 5; Page: 379-81; PMID: 0010369493.

3.) Wuolijoki E; Hirvela T, and Ylitalo P. "Decrease in serum LDL cholesterol with microcrystalline chitosan." Methods Find Exp Clin Pharmacol, 1999 Jun; Vol: 21; Number: 5; Page: 357-61; PMID: 0010420392.

4-NA.) Kanauchi O; Deuchi K; Imasato Y; and Kobayashi E. "Increasing effect of a chitosan and ascorbic acid mixture on fecal dietary fat excretion." Biosci Biotechnol Biochem, 1994; Vol: 58; Page: 1617-20.

5.) Kanauchi O; Deuchi K; Imasato Y; Shizukuishi M, and Kobayashi E. "Mechanism for the inhibition of fat digestion by chitosan and for the synergistic effect of ascorbate." Biosci Biotechnol Biochem, 1995 May; Vol: 59; Number: 5; Page: 786-90; PMID: 0007787293.

6.) Deuchi K; Kanauchi O; Imasato Y, and Kobayashi E. "Effect of the viscosity or deacetylation degree of chitosan on fecal fat excreted from rats fed on a high-fat diet." Biosci Biotechnol Biochem, 1995 May; Vol: 59; Number: 5; Page: 781-5; PMID: 0007787292.

7-BK.) Fox, Arnold and Adderly, Brenda. "The Fat Blocker Diet." New York: St. Martin's Press; 1997; ISBN: 0-312-17102-1.

8.) Sugano M; Fujikawa T; Hiratsuji Y; Nakashima K; Fukuda N, and Hasegawa Y. "A novel use of chitosan as a hypocholesterolemic agent in rats." Am J Clin Nutr, 1980 Apr; Vol: 33; Number: 4; Page: 787-93; PMID: 0007361697.

9.) Razdan A; Pettersson D, and Pettersson J. "Broiler chicken body weights, feed intakes, plasma lipid and small- intestinal bile acid concentrations in response to feeding of chitosan and pectin." Br J Nutr, 1997 Aug; Vol: 78; Number: 2; Page: 283-91; PMID: 0009301417.

10.) Kondo H and Osada A. "Influence of dietary fiber on the bioavailability of zinc in rats." Biomed Environ Sci, 1996 Sep; Vol: 9; Number: 2-3; Page: 204-8; PMID: 0008886332.

11.) Deuchi K; Kanauchi O; Shizukuishi M, and Kobayashi E. "Continuous and massive intake of chitosan affects mineral and fat- soluble vitamin status in rats fed on a high-fat diet." Biosci Biotechnol Biochem, 1995 Jul; Vol: 59; Number: 7; Page: 1211-6; PMID: 0007670180.

12.) Wada M; Nishimura Y; Watanabe Y; Takita T, and Innami S. "Accelerating effect of chitosan intake on urinary calcium excretion by rats." Biosci Biotechnol Biochem, 1997 Jul; Vol: 61; Number: 7; Page: 1206-8; PMID: 0009255987.

13.) Razdan A and Pettersson D. "Hypolipidaemic, gastrointestinal and related responses of broiler chickens to chitosans of different viscosity." Br J Nutr, 1996 Sep; Vol: 76; Number: 3; Page: 387-97; PMID: 0008881711.

14.) Zacour AC; Silva ME; Cecon PR; Bambirra EA, and Vieira EC. "Effect of dietary chitin on cholesterol absorption and metabolism in rats." J Nutr Sci Vitaminol (Tokyo), 1992 Dec; Vol: 38; Number: 6; Page: 609-13; PMID: 0001304604.

15.) Hollander PA; Elbein SC; Hirsch IB; Kelley D; McGill J; Taylor T; Weiss SR; Crockett SE; Kaplan RA; Comstock J; Lucas CP; Lodewick PA; Canovatchel W; Chung J, and Hauptman J. "Role of orlistat in the treatment of obese patients with type 2 diabetes. A 1-year randomized double-blind study." Diabetes Care, 1998 Aug; Vol: 21; Number: 8; Page: 1288-94; PMID: 0009702435.

16.) Melia AT; Koss-Twardy SG, and Zhi J. "The effect of orlistat, an inhibitor of dietary fat absorption, on the absorption of vitamins A and E in healthy volunteers." J Clin Pharmacol, 1996 Jul; Vol: 36; Number: 7; Page: 647-53; PMID: 0008844448.

17.) Ormrod DJ; Holmes CC, and Miller TE. "Dietary chitosan inhibits hypercholesterolaemia and atherogenesis in the apolipoprotein E-deficient mouse model of atherosclerosis." Atherosclerosis, 1998 Jun; Vol: 138; Number: 2; Page: 329-34; PMID: 0009690916.

18.) Gallaher CM; Munion J; Hesslink R Jr; Wise J, and Gallaher DD. "Cholesterol reduction by glucomannan and chitosan is mediated by changes in cholesterol absorption and bile acid and fat excretion in rats." J Nutr, 2000 Nov; Vol: 130; Number: 11; Page: 2753-9; PMID: 11053517.

19.) LeHoux JG and Grondin F. "Some effects of chitosan on liver function in the rat." Endocrinology, 1993 Mar; Vol: 132; Number: 3; Page: 1078-84; PMID: 0007679967.

20.) Kondo Y; Nakatani A; Hayashi K, and Ito M. "Low molecular weight chitosan prevents the progression of low dose streptozotocin-induced slowly progressive diabetes mellitus in mice." Biol Pharm Bull, 2000 Dec; Vol: 23; Number: 12; Page: 1458-64; PMID: 11145178.

21.) Miura T; Usami M; Tsuura Y; Ishida H, and Seino Y. "Hypoglycemic and hypolipidemic effect of chitosan in normal and neonatal streptozotocin-induced diabetic mice." Biol Pharm Bull, 1995 Nov; Vol: 18; Number: 11; Page: 1623-5; PMID: 0008593495.

22.) Jennings CD; Boleyn K; Bridges SR; Wood PJ, and Anderson JW. "A comparison of the lipid-lowering and intestinal morphological effects of cholestyramine, chitosan, and oat gum in rats." Proc Soc Exp Biol Med, 1988 Oct; Vol: 189; Number: 1; Page: 13-20; PMID: 0003186761.

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