JP2002523358A - Slow release tablets containing naproxen and pseudoephedrine - Google Patents

Abstract

  (57) [Summary] Pharmaceutical composition consisting of a substance comprising a non-steroidal anti-inflammatory analgesic naproxen and an anti-inflammatory pseudoephedrine in a sustained release tablet, and the sinuses, which are generally characterized by discomfort, pain, pain and dizziness Use thereof in the treatment of headaches associated with inflammation or cold.

Description

DETAILED DESCRIPTION OF THE INVENTION

BACKGROUND OF THE INVENTION The present invention relates generally to novel pharmaceutical compositions comprising a substance containing the nonsteroidal anti-inflammatory analgesic naproxen in combination with the anti-inflammatory agent pseudoephedrine and a suitable innocuous carrier, and And methods of using such compositions to treat headache associated with sinusitis or nasal cold, typical of discomfort, pain, distress, and dizziness.

Non-narcotic analgesics, commonly known as non-steroidal anti-inflammatory drugs such as naproxen, are widely administered orally in treatments to relieve acute pain. These agents have been shown to be useful in treating cough / cold symptoms in combination with certain antihistamines and anti-inflammatory agents. For example, U.S. Pat.No. 4,552,89
See No. 9.

[0003] Naproxen as a non-steroidal anti-inflammatory analgesic has significant advantages over other analgesics, acetaminophen, aspirin and ibuprofen. Naproxen has a longer duration or half-life, which leads to twice daily dosing. Reducing the number of doses is generally considered to be convenient for the patient and further improves compliance.

[0004] Originally, the combination of anti-inflammatory and antihistamine or anti-inflammatory drugs was combined without considering the very different duration or half-life of the drug. No attempt has been made to combine drugs with different half-lives in such a way as to provide a synergistic effect that makes them more efficiently available to the body at equal rates. This will result in an ineffective combination of anti-inflammatory and anti-inflammatory agents and will lead to some relapses.

[0005] The first An object of the present invention include pharmaceutically together acceptable excipients, a novel Xu methods agent comprising a material containing an analgesic effective amount of naproxen and effective amount of anti-inflammatory agents pseudoephedrine, Is to provide a composition.

[0006] A further object of the present invention is to administer a specific proportion of our composition to eliminate sinusitis, which causes headaches, distress, dizziness, and general malaise, To optimize the levels of both drugs to achieve the most effective drug levels in the body over time.

[0007] DETAILED DESCRIPTION Further details of the invention, we have a suitable base material in combination with (base salt), or without including them, sustained release combination formulation suitable for oral administration comprising naproxen and pseudoephedrine Was found. Through extensive research, we have found preferred dosage forms that result in immediate release of naproxen and pseudoephedrine, as well as a specific sustained release of pseudoephedrine.

[0008] Release of naproxen and pseudoephedrine occurs together for up to 12 hours, preferably up to 10 hours. One or two tablets, preferably two tablets, are orally administered. The active ingredient concentration range is 50-500mg / tablet for naproxen and 30-2 for pseudoephedrine.
40 mg / tablet. The concentration range is 7-30% for pseudoephedrine and 15-60% for naproxen, based on the weight of the coated tablet.

[0009] A preferred dosage form is a coated tablet, wherein naproxen and pseudoephedrine are present in the coating and are released immediately, while pseudoephedrine present in the core is prolonged, preferably during the half-life of naproxen, ie about 10%.
Released over time. The coating dissolves rapidly to release both naproxen and pseudoephedrine, and the inner core dissolves slowly, resulting in sustained release of pseudoephedrine via hydration and diffusion of the drug from the polymer.

[0010] The dosage range of naproxen ranges from 50-800 mg per day, depending on the requirements of the pain treatment.
It is. The dosage range of pseudoephedrine is between 30-240 mg per day, depending on the patient's blood pressure and overall health. The dosage of both drugs will vary depending on the age and weight of the patient, the severity of the symptoms and the incidence of side effects in humans.

The core portion is composed of a common hydrophilic expandable polymer such as 25 hydroxypropylmethylcellulose (HPMC) or hydroxypropylcellulose alone or in combination with each other. The hydrated polymer acts as a binder that swells and delays absorption when hydrated by gastric juice. The combination of macromolecules would represent about 15% of the weight of the tablet core. Tablet coating is HPMC and polyethylene
Contains plasticizers such as 30 glycol (PEG), both of which dissolve immediately in gastric juice. May contain suitable colorants and flavors.

The tablet core also contains everything needed for a standard tablet, such as excipients such as macromolecules, fillers, binders, lubricants, and anti-blocking agents. The binder is present at a concentration of 5% and is generally starch, gelatin, a natural or artificial viscous substance. Bulking agents are present at a concentration of about 10 to 20% of the tablet core weight and can include starch or cellulose. Antiblocking agents used to prevent sticking to tablet presses generally include silica and talc and are present at 0-6% of the tablet core weight. Common lubricants are magnesium stearate, boric acid, or sodium benzoate, present at a concentration of about 2.5% to 5% of the tablet core weight. Additional binders used in granulating the drug polymer mixture include povidone and corn starch. Such a binder is present at a concentration of about 5% to 3% of the tablet core weight.

[0013] Means for preparing the compositions of the present invention, such as tableting, compression, and coating are well known to those skilled in the art.

Example 1 mg / Tablet A. Tablet Core Pseudoephedrine Sulfate 30 Microcrystalline Cellulose 140 Povidone 15 HPMC / PEG 40 Magnesium Stearate 10 B. Coated naproxen 100 pseudoephedrine sulfate 30 HPMC / PEG 10

Manufacturing Method A. Coating 1. Dissolve HPMC / PEG in alcohol mixture 2. Disperse naproxen and pseudoephedrine in HPMC / PEG solution Coating the following internal tablets with the solution using standard methods B. Internal core 1. Mix pseudoephedrine sulfate, microcrystalline cellulose, and HPMC. 2. Dissolve the povidone in the alcohol mixture and use it to crystallize the powder mixture. 3. Dry the pseudoephedrine sulfate crystal mixture. Compression into tablets

Although the present invention has been described and described with reference to certain preferred embodiments, those skilled in the art will recognize that various changes or modifications may be made without departing from the spirit of the invention. For example, an effective amount of the active ingredient outside the preferred range described above may be used. It is intended that the invention be limited only by the following claims.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61P 11/02 A61P 11/02 (81) Designated country EP (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE), OA (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG), AP (GH, GM, KE, LS, MW, SD, SZ, UG, ZW), EA (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM ), AL, AM, AT, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, H U, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL , PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TR, TT, UA, UG, UZ, VNF terms (reference) 4C076 AA38 AA44 BB01 CC05 DD41 EE16 EE23 EE32M FF06 FF21 FF31 FF33 GG11 GG16 4C206 AA01 DA22 FA08 KA01 KA04 MA03 MA05 MA28 MA29 MA55 MA72 NA05 NA12 ZA34 ZB11 ZC13

Claims (6)

 [Claims] 1. A pharmaceutical composition for treating sinusitis in a mammal, comprising substantially naproxen, pseudoephedrine, and an inert ingredient. 2. A pharmaceutical composition in the form of a sustained release coated tablet, wherein the tablet comprises a combination of an anti-inflammatory agent naproxen and an anti-inflammatory agent pseudoephedrine with an inner core in a sustained release form comprising pseudoephedrine. A pharmaceutical composition, comprising a coating consisting of: 3. A pharmaceutical composition according to claim 2, comprising substantially from 7% to 30% of pseudoephedrine by weight of the coated tablet, and from about 15% to 60% of naproxen by weight of the coated tablet. 4. The pharmaceutical composition according to claim 2, further comprising hydroxypropylmethylcellulose, and hydroxypropylcellulose. 5. The method of claim 1, wherein the inner core further comprises about 10% to 20% of a total tablet core weight by weight of a filler, zero to 6% of an anti-blocking agent, and 0.25% to 3% of a binder. 3. The pharmaceutical composition according to claim 2. 6. A pharmaceutical composition, comprising: mixing a pseudoephedrine sulfate, microcrystalline cellulose, and hydroxypropylmethylcellulose into a powder mixture to form a tablet inner core; a crystallized powder mixture. Drying; compressing the dried crystalline powder mixture into tablets; preparing a coating solution for tablets by dissolving hydroxypropyl methylcellulose and polyethylene 30 glycol in an alcohol mixture; Coating the crystallized tablet: A pharmaceutical composition characterized by being prepared by: