Novel topiramate compositions and an escalating dosing strategy for treating obesity and related disorders

Abstract

The present invention is drawn to novel topiramate compositions as well as methods for treating obesity and related conditions, including conditions associated with and / or caused by obesity per se. The present invention also features a pharmaceutical composition that includes, e.g., topiramate alone or in combination with a sympathomimetic agent and a novel escalating dosing strategy for administering such compositions.

Description

BACKGROUND[0001]The prevalence of obesity in both children and adults is on the rise in first world countries, especially in the United States, as well as in many developing countries such as China and India. Many aspects of a person's life are affected by obesity, from physical problems such as knee and ankle joint deterioration, to emotional problems resulting from self-esteem issues and society's attitude towards heavy people. The medical problems caused by obesity can be serious and often life-threatening and include diabetes, shortness of breath and other respiratory problems, gallbladder disease, hypertension, dyslipidemia (for example, high cholesterol or high levels of triglycerides), cancer, osteoarthritis, other orthopedic problems, reflux esophagitis (heartburn), snoring, sleep apnea, menstrual irregularities, infertility, gout, problems associated with pregnancy, heart trouble, muscular dystrophy and metabolic disorders, including hypoalphalipoproteinemia, familial combi...

AI Technical Summary

Benefits of technology

[0028]In certain aspects of the invention, the topiramate reduces phentermine exposure and reduces side effects associated with phentermine.

[0034]In certain aspects of the invention, the topiramate reduces bupropion exposure and reduces side effects associated with bupropion.

Problems solved by technology

The medical problems caused by obesity can be serious and often life-threatening and include diabetes, shortness of breath and other respiratory problems, gallbladder disease, hypertension, dyslipidemia (for example, high cholesterol or high levels of triglycerides), cancer, osteoarthritis, other orthopedic problems, reflux esophagitis (heartburn), snoring, sleep apnea, menstrual irregularities, infertility, gout, problems associated with pregnancy, heart trouble, muscular dystrophy and metabolic disorders, including hypoalphalipoproteinemia, familial combined hyperlipidemia, insulin resistant syndrome X or multiple metabolic disorder, coronary artery disease, and dyslipidemic hypertension.

Moreover, obesity substantially increases the risk of morbidity from hypertension, dyslipidemia, type 2 diabetes, coronary heart disease, stroke, gallbladder disease, osteoarthritis and endometrial, breast, prostate, and colon cancers.

Higher body weights are also associated with increases in all-cause mortality.

Accordingly, while society has seen tremendous advances in the field of pharmaceuticals, there are, of course, drawbacks to the administration of any given pharmaceutical agent.

Sometimes, the disadvantages, characterized as “side effects,” are so severe as to preclude administration of a particular agent at a therapeutically effective dose.

For example, these drugs may be effective only in a subset of patients and their long term use is limited by side effects, some of which are severe.

Many agents in the same therapeutic class, however, display similar side effect profiles, meaning that patients either have to forego therapy or suffer from unpleasant side effects associated with a particular medication.

By “indirectly” reducing side effects is meant that a first pharmaceutical agent allows the second agent to be administered at a lower dose without compromising therapeutic efficacy, thus resulting dose-dependent unwanted effects.

However there have been adverse effects associated with the use of topiramate in humans, such as diarrhea and anal leakage, which can discourage many obese patients from taking this drug.

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