Pharmaceutical composition of topiramate

Abstract

The invention is directed to a pharmaceutical composition of topiramate, an anticonvulsant which is useful for treating epilepsy. More specifically, the present invention provides a solid dosage formulation of topiramate intended primarily for use by pediatric patients, or for patients who have difficulty swallowing tablets. Processes for preparing the pharmaceutical composition are also described.

Description

CROSS-REFERENCE TO RELATED APPLICATION [0001] This application claims priority from U.S. provisional application Ser. No. 60 / 076,770, filed Mar. 4, 1998, the contents of which are hereby incorporated by reference.FIELD OF THE INVENTION [0002] The present invention provides a solid dosage formulation of topiramate and process for producing the solid dosage formulation. More particularly, the solid dosage formulation comprises core particles which are coated with a taste mask coating to provide coated particles which can be sprinkled onto food to ease administration to patients who have difficulty swallowing tablets or capsules, e.g., pediatric patients. BACKGROUND OF THE INVENTION [0003] The pharmaceutical industry employs a variety of dosage formulations for orally administering medicinal agents to patients. Typical formulations for oral administration include liquid solutions, emulsions, or suspensions, as well as solid forms such as capsules or tablets (as used herein, the term “t...

AI Technical Summary

Benefits of technology

"The present invention is about a process for making a pharmaceutical composition of topiramate. The process involves preparing core particles of topiramate, drying them, coating them with a taste masking mixture, and drying them again. The resulting pharmaceutical composition has a taste masking mixture ranging from about 7% to about 15% by weight. The invention also includes pharmaceutical compositions made using this process, as well as methods of treating various conditions using these compositions. The technical effect of the invention is to provide a pharmaceutical composition with improved taste masking, which can be used to treat various conditions such as convulsions, epilepsy, neuropathic pain, amyotrophic lateral schlerosis, acute ischemia, obesity, diabetes, psoriasis, and bipolar disorder."

Problems solved by technology

Since these conventional solid dosage formulations are usually intended for adults who can easily swallow large tablets whole, the often disagreeable taste of the active ingredient need not be taken into account in formulating the medicine, except for the provision of means to prevent the taste from being apparent during the short time that the medicine is in the mouth.

A major requirement of any such solid form is that it must be palatable, since an unpalatable formulation greatly increases the risk of a patient neglecting to take a medication.

In cases where the active ingredient is particularly unpalatable and somewhat unstable, it may be difficult, if not impossible, to identify a solid form that fulfills both of these requirements (i.e., palatable and bioavailable).

Difficulty in identifying a chewable solid form of topiramate has ensued due to the extremely bitter taste of topiramate and problems associated with stability of the active agent, especially upon exposure to moisture and heat which are known to cause degradation of topiramate.