Human chorionic gonadotropin (hcg) formulations for facilitating weight loss and body contouring

This application is a divisional of application Ser. No. 11/496,554 filed on Jul. 31, 2006, which claims priority to and benefits from U.S. Provisional Patent Application No. 60/704,014, filed Jul. 29, 2005.

1. Field of the Invention

This invention relates generally to formulations incorporating human chorionic gonadotropin for administration to mammals to facilitate weight loss and body contouring.

2. Description of the Related Art

hCG (human chorionic gonadotrophin) is a hormone that is naturally produced during pregnancy. hCG is a glycoprotein hormone normally secreted by trophoblastic cells of the placenta during pregnancy. It consists of two chains, called the alpha and beta subunits. It is believed that one of the functions of hCG in pregnancy is to provide a constant supply of fat to the fetus regardless of what or when the mother eats. And, in particular, hCG works to supply both mother and fetus with a steady source of nutrition and fuel in the event of some kind of starvation state. For example, if the mother is ill and cannot keep food down, then hCG will break down stored fat and the baby will be born weighing approximately a normal weight (i.e. 6 or 7 lbs).

It has been postulated that there are two types of fat in the body: structural fat and excess fat. Structural fat is used by the body to provide support and fuel to vital organs. Excess fat is fat that goes directly into storage in the body. It has been found that hCG administered through injections in very small amounts in combination with a modified diet has the capability of targeting excess fat storage for use in providing support to the vital organs. Thus, hCG injections together with a modified diet result in weight loss in the areas where there is the most excess fat storage.

The beneficial effects of hCG administered by injection have been known in the medical and weight-loss industries for many years. Studies have shown that administering hCG by daily injection in small doses, e.g., 125 I.U., facilitates weight loss and redistribution of fat in human patients. See The Action of Chorionic Gonadotrophin in the Obese, A. T. W. Simeons (The Lancet, Nov. 6, 1954). Daily hCG injections administered over a period of ten days without concomitantly subjecting patients to a modified diet result in lower measurements around the hips and waists of the patients but no significant weight loss. These injections also lead to partial appetite suppression and eliminate sudden compulsive hunger experienced by some patients soon after consuming heavy meals. When combined with a modified diet, such as a very low calorie diet, the hCG injections result in significant weight loss in addition to “body contouring” (loss of excess fat in storage areas). Studies also show that this regime of hCG injections coupled with a 500 calorie/day diet does not lead to vitamin or protein deficiencies. Multiple other benefits have been observed in association with this regime. Patients that are overweight due to diabetes lose weight in response to the regime without developing acetonemia, and in cases of mild diabetes patients maintain normal blood sugar levels while weight loss is maintained; weight gain following this regime accompanied by higher sugar levels can be counteracted by another course of the regime. Following this regime, patients with gout have reduced or normal blood-uric acid levels; these patients remain well following treatment while they maintain their weight loss. Similarly, abnormally high blood-cholesterol levels decrease in patients following the regime with free cholesterol increasing and the esterified fraction decreasing, mirroring values seen in pregnancy. Treatment according to this regime also increases libido and decreases or eliminates oligomenorrhea, hyperestrogenic dysmenorrhea, fluor albus simplex, abnormal hair loss, peptic ulcer symptoms, and various dermatoses. Following the regime has also been found to cause brittle finger-nails and improve the quality of singers\' voices.

However, administration of hCG by injection has created many problems for both patients and practitioners.

For patients, the process is painful and inconvenient. The injection must be given daily so patients either have to visit a clinic every day or be trained to inject themselves. Even for trained patients administering the injections can be inconvenient because the hCG solution must be refrigerated. Proper disposal of the needles and syringes is also problematic for patients and a major concern for physicians. Another potential difficulty is that in order for the injections to be effective they must be administered subcutaneously in a very specific way.

For medical practitioners, it may be hard to get consistent results depending on whether patients visit clinics daily for the injections or inject themselves properly. Another major concern is that many patients are very needle-phobic and cannot participate in an hCG program that requires the hCG to be administered by injection.

For a long period of time, medical practitioners have dealt with the drawbacks of using hCG injections because it was believed that changing the route of administration of hCG would change its biological activity such that it would not be effective for the treatment of obesity. This belief was challenged in 2003 when Dr. Daniel Belluscio of Buenos Aires, Argentina published a study on the internet suggesting that oral formulations of hCG could also be effective in promoting weight loss. See Utility of an Oral Presentation of hCG for the Management of Obesity: A Double Blind Study, Dr. Daniel Belluscio, Dr. Leonor Ripamonte, and Dr. Marcelo Wolansky (http://drbelluscio.tripod.com/hcg.htm).

There remains an unmet need in the art for oral hCG formulations and methods of administering such formulations for facilitating weight loss and body contouring as effectively as hCG injections.

Embodiments of this invention disclose sublingual formulations for promoting weight loss and/or body contouring, comprising reconstituted hCG, having a pH in the range of about 6.0 to about 8.0, one or more buffer(s), one or more absorption-enhancing compound(s), and one or more taste-enhancing agent(s). In preferred embodiments, the pH of the reconstituted hCG is about 7.0.

The buffers can be selected from the group comprising carbonates, and sodium bicarbonate is a preferred buffer. The absorption-enhancing compounds are preferably alcohols, and a highly preferred alcohol is ethanol. The one or more taste-enhancing agent(s) can be any one of the following: glycerine, monosaccharides, disaccharides, oligosaccharides, glycerol monostearate, sorbitol, mannitol, glycerol, xylitol, fructose, high fructose corn syrup, dextrose, lactose, maltose, trehalose, galactose, and artificial sweeteners. Glycerine is one preferred taste-enhancing agent. One example of an artificial sweetener to be used in some embodiments is aspartame. The sublingual hCG formulations can also comprise absorption rate enhancing compounds such as mineral oil or corn oil. In some embodiments, the formulations also comprise one or more flavored syrup(s). Different forms of the hCG formulations include a liquid, tablet, lozenge, capsule, or spray.

Embodiments of this invention also disclose methods of reducing body weight and/or contouring the body of a patient comprising administering hCG formulations to patients sublingually. The formulations can, for example, be administered twice daily, in doses of 0.125 ml per administration. In some embodiments, the formulations can be held sublingually by patients for between about 30 seconds and about 45 seconds. The hCG formulations can also be administered in combination with modified diets. For example, patients can be put on a low calorie diet, sometimes comprising between about 500 and about 700 calories per day. The diet may also include pharmacological support such as appetite suppressants and potassium supplements. In some embodiments, the hCG patients are further subjected to an exercise regime.

The rate of absorption of sublingual hCG formulations can be determined by administering embodiments of the formulations comprising flavored syrup(s).

Embodiments of this invention also disclose transdermal formulations for promoting weight loss and/or body contouring, comprising reconstituted hCG and one or more absorption-enhancing agent(s). The absorption-enhancing agent(s) can comprise liposomes, dermal penetration enhancers, and lipophilic solvents and formulations. The transdermal formulations can be in the form of a cream, lotion, spray, solution, or skin patch. The transdermal formulations can also comprise ointment bases such as hydrophilic ointments or a petrolatum bases.

Embodiments of this invention also disclose methods of reducing body weight and/or contouring the body of a patient comprising administering hCG formulations as described above transdermally. Furthermore, hCG formulations can be administered transdermally in combination with subjecting patients to ultrasound.