United States Patent:  6,030,642

Appl. No.:  884283

A method of providing a patient needing clonidine with an extended dosage of clonidine over a prolonged period of time. Such method involves administering to the patient an oral dosage unit comprising a homogenous mixture of a therapeutically effective amount of clonidine, about 30 to about 70 percent by weight of one or more cellulose ethers such as hydroxypropyl methylcellulose, and about 30 to about 70 percent by weight of an inert substance such as cornstarch. The oral dosage unit may be contained in a gelatin capsule or in the form of a tablet.

SUMMARY OF THE INVENTION

The present invention is directed to an extended release clonidine formulation which satisfies these needs. The present invention comprises an oral extended release dosage formulation comprising a homogenous mixture of a therapeutically effective amount of clonidine; from about 30 to about 70 percent by weight of one or more cellulose ethers, such as hydroxypropyl methylcellulose; and from about 30 to about 70 percent by weight of a therapeutically inert, pharmaceutically acceptable adjunct material such as cornstarch, as well as a method of administering an extended release formulation of clonidine to effect central alpha-adrenergic stimulation over a prolonged period of time for patients suffering from any condition which clonidine may benefit.

Clinical studies of an embodiment of the present invention yielded surprisingly effective and unanticipated results. The oral extended release dosage unit formulation of the present invention appeared to cause a sustained release of clonidine over a prolonged period of time. The side effects of transient sedation and rebound hyperarousal were overcome. Thus the present invention overcomes the "peak and trough" side effects of the traditional oral clonidine formulations to provide more stable therapeutic effects. Furthermore, the extended release clonidine formulation is more convenient to use than the transdermal patch thereby resulting in improved patient compliance.

Of particular importance is the ease with which the capsule can be manufactured. It does not require elaborate and expensive equipment and can be prepared quickly and inexpensively in a local pharmacy from ordinarily available materials by any pharmacist properly instructed in its preparation.

Claim 1 of 13 Claims

1. An oral pharmaceutical dosage unit formulation for the extended release of clonidine to effect central alpha-adrenergic stimulation over a prolonged period upon administration thereof, wherein the oral dosage unit is a gelatin capsule containing a homogeneous powder mixture, the homogenous mixture consisting essentially of:

a. from about 0.025 mg. to about 0.40 mg. clonidine for the treatment of attention deficit hyperactivity disorder;

b. from about 30 to about 70 percent by weight of a high molecular weight, high viscosity cellulose ether; and

c. a therapeutically inert, pharmaceutically acceptable adjunct material, wherein the release period is from about 8 to about 12 hours.

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