(-) HCA is also proven to lower blood triglyceride levels.

Xenical® (orlistat) is the new FDA approved drug (lipase inhibitor), developed by Roche Pharmaceuticals, to treat obesity. Xenical® has the following properties compared to CitrinÒ:

FORMULATIONS:

• Citrin®- All natural, non-drug alternative
  
  
• Xenical®- A new class of non-systemically acting drugs known as lipase inhibitors
  

MODE OF ACTION:

Citrin®- acts through its involvement in the Citric Acid Cycle or Kreb’s Cycle in the body as shown in Figure 1.

Figure. 1 : Role of(-) Hydroxycitric Acid in Fat metabolism

Lipid biosynthesis occurs in the cytoplasm (or extramitochondrial part of the cell). Acetyl Coenzyme A is the source of all carbon atoms in the synthesis of fatty acids. Although there are many sources of this enzyme within the cell (both inside and outside of the mitochondria), most acetyl Coenzyme A production occurs in the mitochondria. Coenzyme A in the form of citrate diffuses across the mitochondrial membrane into the cytoplasm. Citrate lyase (also known as the citrate cleavage enzyme), located in the cytoplasm, catalyzes the degradation of citrate into acetyl Coenzyme A and oxaloacetate.

Fatty acids, the building blocks of lipid or fat, are synthesized from acetyl Coenzyme A. However, Citrin® competes with citrate for the enzymatic activity of citrate lyase. Thus, in the presence of Citrin®, less acetyl Coenzyme A is formed. Consequently, a reduced amount of fat is synthesized. This chain of events illustrates one of the mechanisms through which Citrin® helps to block the accumulation of unwanted fat in the body. In addition, Citrin® inhibits the production of malonyl Coenzyme A. The lowered levels of malonyl Coenzyme A block fatty acid biosynthesis and activate the oxidation of fat in the liver and adipose tissues. Through this process, Citrin® helps to accelerate the burning of excess fat in the body.

A third mechanism of Citrin®, related to the first, is that (-) HCA’s inhibition of citrate lyase causes less dietary glucose to be utilized for the synthesis of fatty acids. Thus, dietary glucose is instead converted into its storage form, glycogen which sends a metabolic message to the brain that the body has consumed enough food, and this results in an appetite suppressant effect. In addition, the stored glycogen is available for energy requirements during exercise.

Xenical®- Blocks a pancreatic enzyme that breaks down fat in the intestine, preventing about 30% of it from being absorbed.

DEVELOPMENT:

Citrin®- The trademarked name of Sabinsa Corporation for an unique calcium salt of (-) HCA (hydroxycitric acid, a weight loss phytonutrient.

• 1991- Sabinsa Corporation was the first to standardize (-)HCA.
  
  
• 1991- Dr. Anthony A. Conte conducted the first double-blind clinical study in Hilton Head, SC.
  
  
• 1993- Consumer study in Allendale, SC
  
  
• 1994- Consumer study in Hilton Head, SC

Xenical®- Developed and researched by Hoffmann-La Roche.

• 1970s- Animal experiments
  
  
• 1993- Introduced as a drug

SIDE EFFECTS:

• Citrin®- NO SIDE EFFECTS have been observed in over 250 volunteers in the three clinical studies and in thousands of patients in private practice in the USA and Europe since 1991.
  
  
• Xenical®- Gastrointestinal symptoms such as flatulence, diarrhea, fatty or oily stool, and "anal leakage" occur.
  

RECOMMENDED USE:

• Citrin®- All degrees of obesity for prevention treatment, maintenance and stabilization phases
  
  
• Xenical®- Recommended for obese patients who are at least 30% above their ideal weight. Its use is contraindicated in patients with chronic malabsorption syndrome or cholestasis (disease of the liver preventing bile flow).

RESULTS:

• Citrin®- In clinical studies, patients have lost on average 10 lbs in eight weeks on the Citrin® regimen calculated as 750 mg of pure (-) HCA per day. All subjects followed the Smart Choice Diet: three meals of "ordinary" food in moderation and balanced for fat, carbohydrate, and protein.
  
  
• Xenical®- People lost ± 7.5 more pounds in a year than those who were on a strict diet alone.
  

LOSS OF FAT-SOLUBLE VITAMINS:

• Citrin®- No such effects have been observed. CitrinÒ is often administered with vitamin supplements.
  
  
• Xenical®- The absorption of fat-soluble vitamins A, D, E, and K as well as beta-carotene are reduced. Thus, patients are advised to take a daily supplement that contains fat-soluble vitamins and beta-carotene two hours before or after taking orlistat.
  

DOSAGE:

• Citrin®- INDIVIDUALIZED: 1-3 capsules per day
  
  
• Xenical®- One capsule three times a day with meals
  

COST:

• Citrin® - On average the cost of Citrin® range from $35.00-$45.00/84 capsules for a 4 week supply.
  
  
• Xenical®- The cost is $1.10 per capsule wholesale, which may add up to $1200 per year or more considering the retail price, $2.00-$3.00 per capsule.
  
  

POTENTIAL MISUSE:

• Citrin® - For the last 8-9 years, (-) HCA (Garcinia cambogia) has been used judiciously and selectively with phentermine, phendimetrazine, phenylpropanolamine and Tenuate, safely and effectively.
  
  
• Xenical®- Since only 5-10% loss of a person’s original weight occurs in a year, patients and doctors may have to use other appetite suppressants (phentermine for instance) along with orlistat. According to the FDA, no studies have been conducted for such a therapy.
  

STUDIES:

Citrin®-

1. Katts, G.R., Pullin, D., Parker, L.K., Keith, P.L., and Keith, S. Abstract/Poster: Merida, Yucatan, Mexico, March 4, 1995.
   
   
2. Thom, E. Abstract/Poster: 7th European Congress on Obesity in Barcelone, May 14-17, May 1996.
   
   
3. Conte, A.A. The Bariatrician, Summer 1993: 17-19.
   
   
4. Conte, A.A. Alternative and Complementary Therapies, June/July 1995: 212-215.
   
   
5. Badmaev, V. and Majeed, M. Sabinsa Study.

Xenical®- done by Hoffmann-La-Roche