MXPA01001969A

MXPA01001969A - Timed release tablet comprising naproxen and pseudoephedrine.

Info

Publication number: MXPA01001969A
Application number: MXPA01001969A
Authority: MX
Inventors: Chris E Platt
Original assignee: Platt Chris
Priority date: 1998-08-25
Filing date: 1998-08-25
Publication date: 2002-04-24
Also published as: AU8919898A; EP1107740A4; AU758880B2; CA2341485A1; EP1107740A1; JP2002523358A

Abstract

Pharmaceutical compositions and methods of using same comprising non-steroidal anti-inflammatory analgesic naproxen and the decongestant pseudoephedrine in a time release tablet form in the therapy or cure of sinusitis, or sinus headaches, generally exemplified by discomfort, pain, pressure, and dizziness.

Description

TIMED RELEASE TABLET COMPRISING NAPROXEN AND PSEUDOEPHEDRINE BACKGROUND OF THE INVENTION The present invention relates generally to novel pharmaceutical compositions of matter comprising the non-steroidal anti-inflammatory analgesic naproxen in combination with the decongestant pseudoephedrine and appropriate non-toxic vehicles and methods for using said compositions in the therapy or cure of sinusitis. , or breast problems, usually exemplified by discomfort, pain, pressure and vertigo. Non-narcotic analgesics, commonly known as nonsteroidal anti-inflammatory drugs, such as naproxen, are widely administered orally in the treatment of mild to severe pain. These medications have been described as being useful for treating cough / cold symptoms in combination with certain antihistamines and decongestants. See, for example, U.S. Patent No. 4,552,899 to Sunshine. The naproxen as a non-steroidal anti-inflammatory pain relief device has greater advantage than other pain relief devices of acetaminophen, aspirin and ibuprofen. Naproxen has a significantly longer duration or a half-life that leads to twice a daily dose. It is generally accepted that reduced dosing leads to patient convenience and better compliance. Originally, the combinations of anti-inflammatories, antihistamines or decongestants were combined without consideration to the half-lives or duration of the drug quite different. These drugs with different half-lives were not combined in a synergistic way that led the body to use them effectively in equal amounts. This would lead to ineffective combinations of anti-inflammatories and decongestants and the return of partial symptoms.

BRIEF DESCRIPTION OF THE INVENTION It is a principal object of the present invention to provide a new timed release pharmaceutical composition of matter comprising an analgesically effective amount of naproxen and an effective amount of decongestant pseudoephedrine with pharmaceutically acceptable excipients. It is a further object of the present invention that the administration of our specific proportion of composition optimizes the most effective drug level of both drugs in the body during the time for the release of nasal sinus congestion that causes the headache, pressure, vertigo and malaise.

DETAILED DESCRIPTION OF THE INVENTION More specifically, the Applicant herein has found that a timed release combination product suitable for oral administration comprising naproxen and pseudoephedrine combined with or without an appropriate base salt. Through extensive study the applicant found the preferred dosage form that provides the immediate release of naproxen and pseudoephedrine, and the specific timed release of pseudoephedrine. The release of naproxen and pseudoephedrine takes place up to 12 hours, preferably 10 hours. One to two tablets are administered orally, preferably two. The concentration ranges for the active ingredients are naproxen, 50-500 mg per tablet, pseudoephedrine, 30-240 mg per tablet. The concentration ranges represent 7-30% by weight of tablet coated with pseudoephedrine and 15-60% naproxen. The preferred dosage form is a coated tablet, wherein the naproxen and pseudoephedrine are in the outer coating, thus being released immediately, while the pseudoephedrine in the core is released over time, preferably for the duration of the half-life of naproxen, approximately 10 hours. The outer coating dissolves rapidly to release both naproxen and pseudoephedrine and the inner core dissolves slowly to release pseudoephedrine timed through the hydration and diffusion of the drug from the core polymer. The dose range for naproxen is from 50-500 mg per day depending on the pain management requirements. The range of pseudoephedrine is between 30-240 mg per day, depending on the blood pressure values and the general health of the patient. Both medications will vary depending on the age and weight of the patient, the severity of the symptoms and the incidence of side effects for humans.

The core consists of common hydrophilic expandable polymers such as hydroxypropylmethylcellulose (HPMC) or hydroxypropylcellulose either by themselves or in combination with each other. Hydrated polymers act as a binder that expands when hydrated by gastric media and delays absorption. The polymer combination will represent approximately 15% of the tablet core weight. The outer coating of the tablet comprises HPMC and a plasticizer such as polyethylene glycol (PEG), both of which dissolve immediately in gastric fluids. Suitable flavoring and coloring agents can be included. The tablet core also comprises excipients such as polymers, fillers, binders, lubricants and antiblocks, all required for the manufacture of the standard tablet. The binders are presented in a concentration of 5% and are typically starch, gelatin, natural or artificial gums. The fillers are presented in a concentration of about 10 to 20% by weight of the tablet core and can include starches or cellulose. The anti-adherents used to prevent the tablets from sticking to tablet pressure, typically include silicas and talcum, present from 0 to 6% of the weight of the tablet core. Typical lubricants are magnesium stearate, boric acid, or sodium benzoate in a concentration of about 2.5% to 5% of the weight of the tablet core. Additional binders used in the granulation of the medicament polymer mixture include povidin and corn starch. Such binders are present in a concentration of about 5% to 3% of the weight of the tablet core. The means for preparing the compositions of the present invention, for example, tablet mixing, compaction and coating, are well known to those skilled in the art. EXAMPLE I Mg / Tablet A. Tablet Core Pseudoephedrine Sulfate 30 Microcrystalline Cellulose 140 Povidone 1 5 HPMC / PEG 40 Magnesium Stearate 1 0 B. Exterior Coating Naproxen 100 Pseudoephedrine Sulfate 30 HPMC / PEG 10 Manufacturing Method A. Exterior Coating 1. Dissolve HPMC / PEG in a mixture of alcohol. 2. Disperse Naproxen and Pseudoephedrine in the HPMC / PEG solution. 3. Coat the inner tablets underneath with the solution, using standard procedures. B. Interior Core 1. Mix the pseudoephedrine sulfate, microcrystalline cellulose and HPMC 2. Dissolve povidone in an alcoholic mixture and use it to crystallize the powder mixture. 3. Dry the crystallized pseudoephedrine sulfate mixture. 4. Compress in tablets. Although the invention is described and illustrated with reference to certain preferred embodiments thereof, those skilled in the art will appreciate that various changes or modifications may be made therein without departing from the spirit and scope of the invention. For example, effective doses of the active ingredients other than the preferred ranges set forth herein may be used. It is proposed that the invention be limited only by the scope of the following claims.

Claims

CLAIMS 1. A pharmaceutical composition consisting essentially of naproxen, pseudoephedrine, and inert ingredients for treating sinusitis in mammals.
2. A pharmaceutical composition in the form of a sustained release coated tablet, wherein the tablet has an outer coating consisting essentially of a combination of anti-inflammatory naproxen and a decongestant pseudoephedrine, with an inner core of pseudoephedrine in a form of timed release.
The pharmaceutical composition according to claim 2, characterized in that the naproxen and the pseudoephedrine consist essentially of pseudoephedrine in between about 7% and 30% of the weight of the coated tablet and naproxen in about 15% to 60% of the weight of the tablet coated.
4. The pharmaceutical composition according to claim 2, characterized in that it further includes a hydroxypropylmethylcellulose and hydroxypropylcellulose.
5. The pharmaceutical composition according to claim 2, characterized in that the inner core includes about 10 to 20% filler, zero to 6% non-stick, 0.25% to 3% binder, of the total weight of the tablet core.
6. A pharmaceutical composition prepared by the process of: preparing an inner tablet core by mixing pseudoephedrine sulfate, microcrystalline cellulose and hydroxypropylmethylcellulose in a powder mixture; drying the crystallized powder mixture, compressing the dry crystallized powder mixture into tablets; prepare an outer coating solution for the tablets by dissolving hydroxypropylmethylcellulose and polyethylene glycol in a mixture of alcohol; and coating the crystallized, dry, interior tablets with the outer coating solution.