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

a technology of compositions and topiramate, applied in the direction of drug compositions, antibacterial agents, metabolic disorders, etc., can solve the problems of obesity, shortness of breath, and substantial increase in the risk of morbidity from hypertension, so as to reduce the side effects of bupropion and reduce the exposure

Inactive Publication Date: 2009-12-10
VIVUS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0034]In certain aspects of the invention, the topiramate reduces bu

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

Method used

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

Examples

Experimental program
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Effect test

example 1

[0151]The controlled release topiramate beads were made using an extrusion spheronization process to produce a matrix core comprised of topiramate: 40.0% w / w; microcrystalline cellulose, Avicel® PH102: 56.5% w / w; and Methocel™ A15 LV: 3.5% w / w. The topiramate cores were then coated with ethyl cellulose: 5.47% w / w and Povidone K30: 2.39% w / w.

[0152]The final coated beads % w / w were as follows:

Ingredient% w / wtopiramate36.85microcrystalline cellulose,52.05Avicel ® PH102Methocel ™ A15 LV3.22ethyl cellulose5.47Povidone K302.39

[0153]The phentermine beads were straight immediate release drug coated onto sugar spheres. Both sets of beads were then encapsulated into one capsule.

example 2

[0154]In a study comparing controlled-release formulation of topiramate according to the present invention versus immediate release topiramate (Topamax®) in combination with phentermine, the controlled release formulation of the instant invention of topiramate had a 10-15% lower effect on phentermine exposure (FIG. 2).

[0155]The mean and statistical comparisons for plasma phentermine PK parameters at steady state in multiple dose administrations are summarized in Table 2.

TABLE 2Arithmetic Mean (SD) and Statistical Comparison of Pharmacokinetic Parameters forPlasma PhentermineMean ± SDTreatment 2 Versus Treatment 4PharmacokineticTreatment 2Treatment 490% ConfidenceParameters(N = 13)(N = 12)Intervals% Mean RatioAUC0-tau (ng * hr / mL)2250 ± 563 2530 ± 644 (75.6, 105.3)89.2AUC0-96 (ng * hr / mL)4640 ± 15705550 ± 1960(67.1, 105.0)84.0AUC0-t (ng * hr / mL)4640 ± 15705550 ± 1960(67.1, 105.0)84.0Cmax,96 (ng / mL) 114 ± 23.6 127 ± 27.6(78.8, 104.5)90.7Cmin,68 (ng / mL)9.84 ± 7.2414.6 ± 11.3(42.5, 109....

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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...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61P3/10A61K9/48A61K9/52A61P3/04
CPCA61K31/137A61K47/38A61K31/357A61K31/35A61K9/1629A61K9/167A61K9/1676A61K9/4866A61K9/5026A61K31/7048A61K31/135A61K31/00A61K9/5084A61K9/5073A61K9/5047A61K2300/00A61K9/5042A61P1/08A61P11/00A61P11/06A61P15/00A61P19/02A61P19/06A61P21/00A61P25/00A61P25/02A61P25/06A61P25/20A61P3/04A61P31/04A61P35/00A61P3/06A61P43/00A61P9/10A61P9/12A61P3/10A61K9/20A61K9/1623
Inventor NAJARIAN, THOMASTAM, PETER Y.WILSON, LELAND F.
Owner VIVUS
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