JP2003532671A - Standardization of packaging for pseudoephedrine hydrochloride and fexofenadine hydrochloride - Google Patents

Abstract

SUMMARY A package for dispensing two or more pharmaceutically active compounds is disclosed and claimed. In one embodiment of the invention, the packaging is predominantly comprised of (a) a container (1) dispensing a therapeutically effective amount of fexofenadine or an agent (A) having a pharmaceutically acceptable addition salt thereof; Dispense a container (2) that dispenses an effective amount of a combination of fexofenadine and pseudoephedrine or a drug (B) containing a pharmaceutically acceptable addition salt thereof. This embodiment also provides an indication to distinguish between drugs (A and B) in containers (1 and 2). Various preferred embodiments of the package of the present invention are also described and claimed.

Description

Detailed Description of the Invention

[0001]

【Technical field】

The present invention relates to a manner of packaging two separate medications in two separate dosage units. This has proven useful for convenience. More specifically, the present application relates to packaging of two drugs containing fexofenadine hydrochloride and sudoephedrine hydrochloride. Dosage units containing Pseudoephedrine Hydrochloride are administered during the daytime, and dosage units lacking Pseudoephedrine Hydrochloride are administered during the night.

[0002]

[Background technology]

The manner in which two separate agents are packaged together as a daytime and nighttime packaging scheme is well established in the art. To give a few examples, E. Knudsen is a US patent.
4,295,567 describes standardization of packaging in the form of plastic packaging which dispenses two separate dosage units for treating respiratory disorders. Weinstein et al. In International Application WO99 / 21556 published on May 6, 1999 set forth a packaging standard containing two different dosage units of medicines for treating rhinitis introduced in bottles, plastic packaging or sachets. Disclosure.

However, there is no single packaging standard in the state of the art that specifically includes fexofenadine hydrochloride and pseudoephedrine hydrochloride. Furthermore, there is no prior art technique for specifically dispensing and providing two separate medications as a container or bottle in a small convenient unipackage such as a box. Further, the present invention contains both fexofenadine hydrochloride and pseudoephedrine hydrochloride in two separate dosage units, so that one presentation of the prescription card and one copayment Provide the benefits of. At the current state of the art, two payments are required to receive these two therapeutic agents. More importantly, the prescribing physician is unable to write a single prescription that covers both of these types of drugs.

Accordingly, it is an object of the present invention to provide a single package such as a box containing two separate medications. More particularly, the invention provides a single package as a box containing i) drug A consisting of fexofenadine hydrochloride and ii) drug B consisting of fexofenadine hydrochloride and sudoephedrine hydrochloride. With the goal. Beyond the current state of the art, the object of the present invention is for convenience that the consumer presents a prescription card once to receive both fexofenadine hydrochloride and pseudoephedrine hydrochloride for the treatment of their condition. Just provide good features. This feature facilitates the ability to co-distribute these two drugs together in one lump sum payment rather than two payments.

[0005]

DISCLOSURE OF THE INVENTION

The present invention combines a box of therapeutically effective amounts of both fexofenadine hydrochloride and pseudoephedrine hydrochloride in a single package with the advantage of one payment by the consumer and one presentation of a prescription card. To be integrated.

The present invention comprises (a) a container 1 in which a drug A having a therapeutically effective amount of fexofenadine or a pharmaceutically acceptable addition salt thereof is dispensed, and (b) a therapeutically effective amount of fexofenadine and sudo. Provided is a package containing 2 or more pharmaceutically active compounds containing a container 2 containing drug B having ephedrine or a pharmaceutically acceptable addition salt thereof. In this case, drugs A and B and container 1
Provide an indication that distinguishes between and.

DESCRIPTION OF THE FIGURES FIG. 1 is a front view of a single package as a box, broken to show how the containers are placed inside the package. Figure 2 is a view of a single package as a box with flaps, with the flaps open to show the position where the container is inserted into the box. FIG. 3 is a view showing a container as an open bottle in which the screw top cap is located right above the opening.

[0008]

Detailed description of the invention

It has now been found that consumers can receive two separate medications by presenting a prescription card once and making a single payment.

The term packaging as used herein means any means by which a drug can be dispensed in a single unit. For example, packaging types include, but are not limited to, boxes of different geometric configurations. Examples of such geometric configurations include rectangular, circular, square or cylindrical boxes on the bottom. The preferred packaging method for the present invention is a rectangular box. More preferably, the present invention is in the form of a convenient, single package or unipackage.
Convenient term means to present a one-time payment and / or one-time prescription card for the consumer after receiving the prescription or after dosing at the counter.

The term container as used herein includes containers suitable for containing the agents A and B. The container in the present invention is, but is not limited to, a medical bottle. Other examples include cans, plastic containers, tubes,
Or individual packets are included. Medical term means any drug treatment or administration in the form of capsules, caplets, tablets or liquid formulations. Drug treatment is administered either by prescription or overcounter drug administration.

A therapeutically effective amount of a compound means an amount sufficient to achieve the desired effect. A therapeutically effective amount of a compound of the invention can be administered to a subject in any acceptable manner. For example, this includes oral administration of capsules, caplets, tablets or liquid formulations. The term "therapeutically effective amount" does not necessarily mean total cure of the condition. Many factors are considered in determining a therapeutically effective amount. Illustrative examples of some of these factors include, but are not limited to, the particular condition involved, the degree of intensity of the condition, the response by the individual subject, and which compound is administered. , The mode of administration, and the species of the animal, its weight, age and general health in general.

The term “subject” as used herein is meant to refer to any warm-blooded animal. More particularly, it means an animal having a condition treatable by various dosage units containing fexofenadine hydrochloride and pseudoephedrine hydrochloride. Further examples of such animals include, but are not limited to, guinea pigs, dogs, cats, rats, mice, horses, cows, sheep and most preferably humans.

[0013] The label here means an identifiable feature of two containers in a package. Such examples include markings that indicate size, color, shape, or which container contains drug A and which container contains drug B. The preferred indication of the present invention is size.

The present invention relates to (a) a container 1 containing a drug A having a therapeutically effective amount of fexofenadine or a pharmaceutically acceptable addition salt thereof, and (b) a therapeutically effective amount of fexofenadine and sudo. Drug A in a convenient single package or unitary package in the form of a box containing 2 or more pharmaceutically active compounds containing a container 2 with ephedrine or a pharmaceutically acceptable addition salt thereof. And B and the labels identifying Containers 1 and 2 are applied so that they can be purchased by the consumer. The term pharmaceutically active compound, as used herein, refers to agents that have potential utility in the prevention, diagnosis and treatment of human disease (Goodman &Gilman's,
^{The Pharmacological Basis of Therapeutics, 9 th} Edition, page 1, line 8-9
, McGraw Hill, 1996).

In one aspect of the invention, the packaging according to the invention includes size and color as indicia. In a more preferred embodiment, the packaging of the present invention has the size of a container as an indicator. More specifically, Drug A is contained in the smaller bottle,
Drug B is contained in the larger bottle and both are contained in a convenient unipackage such as a box. In one aspect of the invention, the packaging according to the invention is containers 1 and 2 in the form of medical bottles. Containers as referred to herein are made in many different ways. Representative examples include, but are not limited to, U.S. Pat.
And the description provided in US Pat. No. 5,850,940. These descriptions are incorporated herein by reference. Drug A is displayed for night use,
Drug B is indicated for daytime use, both of which consist of pharmaceutical carriers and formulation aids.

The forms of drugs A and B include capsules, caplets, tablets and liquid formulations. In a preferred embodiment of the invention, the drugs A and B in the package are in the form of capsules and tablets, respectively. Acceptable formulations of Drugs A and B are shown in the table below.

[0017]

[Table 1]

Drug A contains about 14.4% by weight of fexofenadine hydrochloride, 5 mg to 180 mg,
It has a particle surface area of 1.0 m ² / g or more. In one aspect of the present invention, the particle surface area in the range of 2m ² / g~10m ² / g. In a further preferred embodiment, the particle surface area is 2m ² / g~6m ² / g. And in another preferred embodiment, the particle surface area in the range of 2m ² / g to about 4m ² / g. Drug A contains further ingredients, at least one of which is an inactive ingredient. Acceptable inactive ingredients can be selected from the group consisting of croscarmellose sodium, lactose, microcrystalline cellulose, pregelatinized starch, gelatin, calcium carbonate, magnesium stearate and sodium starch glycolate.

In one aspect of the invention, the packaging containing Agent A according to the invention contains the following inactive ingredients: croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch and gelatin. The amount of such an inactive ingredient is 1-10%, 20-85%, 20-85%, 1-
It is in the range of 30% and 1 to 15%.

In a more preferred embodiment, the packaging of the present invention comprising Drug A comprises croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch and gelatin each at about 4.8% by weight relative to Drug A, 33.8%, 3
Contains 3.8%, 9.6% and 3.5%.

In another aspect of the invention, the package contains Drug A having the following inactive ingredients: microcrystalline cellulose, pregelatinized starch, gelatin, magnesium stearate, calcium carbonate and sodium starch glycolate. To do. The amount of each of these components is 20-85%, 5% by weight, based on Drug A.
-50%, 1-15%, 0.05-3%, 5-50% and 1-15%.

In a further preferred embodiment, the packaging according to the invention comprises predominantly microcrystalline cellulose, pregelatinized starch, gelatine, magnesium stearate, calcium carbonate and sodium starch glycolate as the weight% of drug A,
It contains drug A containing about 33.5%, 28.3%, 3.1%, 0.5%, 15.0% and 5.4%, respectively.

In another aspect of the invention, Agent A according to the invention contains the following inactive ingredients: croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate. The amount of such an inactive ingredient is 1 to 10% and 20 to 85%, respectively, as the weight% of the drug A.
, 20-85%, 1-30%, 1-15% and 0.05-3%.

In a more preferred embodiment, the drug A is croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate at about 4.6%, 32.
Contains 4%, 32.4%, 9.2%, 3.4% and 0.5% amounts.

In a further preferred embodiment, the packaging according to the invention comprises croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate, each in a weight percentage relative to drug A of about%.
Includes Drug A in amounts of 4.8%, 33.7%, 33.7%, 9.6%, 3.5% and 0.5%.

In another aspect of the invention, the Agent A according to the invention comprises the following inactive ingredients: microcrystalline cellulose, pregelatinized starch, magnesium stearate,
Contains calcium carbonate and sodium starch glycolate. The amount of each of these inactive ingredients is 20% to 85%, 5% to 50% by weight based on the drug A.
, 0.05-3%, 5-50% and 1-15%.

In a further preferred embodiment, the packaging according to the invention comprises microcrystalline cellulose, pregelatinized starch, magnesium stearate, calcium carbonate and sodium starch glycolate in an amount of 35.1% each by weight relative to drug A.
, 29.8%, 0.5%, 15.0% and 5.4% in amount.

Drug B is a bilayer tablet containing two regions. The first isolated area is a therapeutically effective decongestant amount of pseudoephedrine or a pharmaceutically acceptable addition salt thereof, ie, about 18 to about 39% by weight of pseudoephedrine; most preferably about 25 to 33. %
And a first carrier base material. The first carrier base material comprises (i) carnauba wax in an amount of about 59% to about 81%, and most preferably about 66% to about 74% by weight, based on the weight of pseudoephedrine, and (ii) the weight of pseudoephedrine. To about 0.25% to about 2.00
% Amount, most preferably about 0.50% to about 1.50% amount of a mixture of suitable anti-adhesives, wherein the first basic material is a sustained release of pseudo-ephedrine or a pharmaceutically acceptable addition salt thereof. I will provide a. The second isolated region is a therapeutically effective antihistamine dose formula:

[Chemical 5] Fexofenadine or a pharmaceutically acceptable addition salt thereof, such as fexofenadine hydrochloride, wherein X is a number from about 0 to about 5, and their individual optical isomers are treated with fexofenadine. Containing about 15% to about 30% by weight of phenazine, most preferably about 15% to about 24% and a second carrier base material, the second carrier base material comprising:
(I) An amount of about 27% to about 73% by weight of fexofenadine, most preferably about 27%.
Cellulose diluent in an amount of 43% to about 67%; (ii) An amount of pregelatinized starch in an amount of about 15% to about 30%, most preferably about 15% to about 24%, based on the weight of fexofenadine; iii) a suitable disintegrant in an amount of about 0.25% to about 6.00%, most preferably about 3.20% to about 4.80% by weight of fexofenadine, and (iv) about 0.25% by weight of fexofenadine. To about 2.00%, most preferably about 0.50% to about 1.00%, by a mixture of suitable lubricants. The second carrier base material provides immediate release of fexofenadine or a pharmaceutically acceptable addition salt thereof. The packaging according to the present invention contains pseudoephedrine as pseudoephedrine hydrochloride.

4- [4- [4- (hydroxydiphenylmethyl) -1-piperidinyl] -1-hydroxybutyl] -α, α-dimethylbenzeneacetic acid hydrochloride has a chemical name of other chemical name: fexofenadine Equivalent to the hydrochloride salt. See US Pat. No. 5,855,912. This is incorporated herein by reference.

The term “fexofenadine or a pharmaceutically acceptable addition salt thereof” as used herein corresponds to compounds where X is about 0-5 in the above formulas and individual optical isomers thereof. . Compound, 4- [4- [4- (hydroxydiphenylmethyl)
-1-Piperidinyl] -1-hydroxybutyl] -α, α-dimethylbenzeneacetic acid hydrochloride (
X in formula (I) is 0 or 1) is the most preferred form of fexofenadine. The package according to the invention contains pseudoephedrine as pseudoephedrine hydrochloride.

A suitable glidant, such as colloidal silicon dioxide, included in the first carrier base material of Pseudoephedrine is 0.005% by weight of Pseudoephedrine.
% To about 3.00%, more preferably 0.00 based on the weight of pseudoephedrine.
% To about 0.75%.

Stearic acid is a suitable anti-adhesive for pseudoephedrine, a suitable disintegrant for fexofenadine is croscarmellose sodium, and a suitable lubricant is magnesium stearate. Pseudoephedrine hydrochloride, pseudoephedrine carnauba wax, stearic acid and colloidal silicon dioxide are about 28.17%, about 70.42%, about 1.15% by weight of the pseudoephedrine composition, respectively.
% And about 0.25%, wherein fexofenadine, fexofenadine cellulose diluent, pregelatinized starch, croscarmellose sodium, and magnesium stearate are each about 17.09% by weight of the fexofenadine composition. %, About 61.67%, about 17.09%, about 3.42% and about 0.75%.
The term fexofenadine means fexofenadine hydrochloride.

Cellulose diluents used herein are AVICEL® PH101 and AVI
Consists of formulations of CEL PH102 in amounts of about 12% and 88% respectively. In addition, fexofenadine hydrochloride is present in an amount of about 60 mg, and pseudoephedrine hydrochloride is about 120 mg.
Present in the amount of mg. Bilayer tablets may be coated with a suitable coating such as OPADRY® YS
-1-7006 and has a hardness of about 15 kp to about 25 kp. The coating agent OPADRY® YS-1-7006 is present in an amount of about 2.9% by weight of the composition.

“Fexofenadine hydrochloride” (see US Pat. No. 6,039,974, incorporated herein by reference) or “pharmaceutically acceptable addition salt thereof” has the formula:

[Chemical 6] Equivalent to.

The term “pharmaceutically acceptable salt” is of the formula (), which is substantially non-toxic at the doses administered to achieve the desired effect, and which independently has no significant pharmacological activity. I
) And (II) salts. Salts included within the scope of this term are pharmaceutically acceptable acid addition salts of suitable inorganic or organic acids. Suitable inorganic acids are, for example, hydrochloric acid, hydrobromic acid, sulfuric acid and phosphoric acid. Suitable organic acids include carboxylic acids such as acetic acid, propionic acid, glycolic acid, lactic acid, pyruvic acid, malonic acid, succinic acid, fumaric acid, apple acid, tartaric acid, citric acid, cyclamic acid, ascorbic acid,
Maleic acid, hydroxymaleic acid, dihydroxymaleic acid, benzoic acid, phenylacetic acid, 4-aminobenzoic acid, 4-hydroxybenzoic acid, anthranilic acid, cinnamic acid, salicylic acid, 4-aminosalicylic acid, 2-phenoxybenzoic acid, 2- Acetoxybenzoic acid and mandelic acid, sulphonic acids such as methanesulphonic acid, ethanesulphonic acid and β-hydroxyethanesulphonic acid are included. further,
Pharmaceutically acceptable salts include inorganic and organic bases such as alkali metals such as sodium, potassium and lithium, such as alkaline earth metals such as calcium and magnesium, Group IIIA light metals such as aluminum, organic amines such as primary amines. Included are salts of formulas (I) and (II) formed with secondary, secondary or tertiary amines such as cyclohexylamine, ethylamine, pyridine, methylaminoethanol and piperazine. These salts are prepared by conventional methods well known to the person skilled in the art, for example by treating the compounds of formula (I) and (II) with a suitable acid or base. Such salts exist in either hydrate or substantially anhydrous form. Preferred acid addition salts are salts prepared from hydrochloric acid, sulfuric acid and tartaric acid.

The term “stereoisomer” is a general term for isomers of all individual molecules that differ only in the orientation of their atoms in space. It has
Included are geometric (cis / trans) isomers and isomers of compounds that have two or more chiral centers and are not mirror images of one another (diastereomers).

As used herein, the term “cellulose diluent” includes microcrystalline cellulose, AV
ICEL PH101, AVICEL PH102, AVICEL PH301, AVICEL PH302, AVICEL PH200, AVIC
EL PH112, AVICEL PH113, AVICEL PH103, AVICEL PH105, etc. are included. Preferred cellulose diluents are microcrystalline cellulose, AVICEL PH101 and AVICEL PH102, and most preferred cellulose diluents are blends of AVICEL PH 101 and AVICEL PH 102. AVICEL PH101 consisting of about 12% AVICEL PH101 and about 88% AVICEL PH102
Particularly preferred is a mixture of PEG and AVICEL PH102.

The term “suitable anti-adhesive” as used herein includes stearic acid, cetyl alcohol, stearyl alcohol, paraffin, white wax, glycerin, lanolin, talc, mineral oil and the like. A preferred suitable anti-adhesive is stearic acid.

As used herein, the term “suitable disintegrant” includes croscarmellose sodium, crospovidone, alginic acid, sodium alginate, DVB methacrylate,
Crosslinked PVP, microcrystalline cellulose, polacrilin potassium, sodium starch glycolate, starch, pregelatinized starch and the like are included. A preferred suitable disintegrant is croscarmellose sodium.

The term “suitable lubricant” as used herein includes magnesium stearate, calcium stearate, zinc stearate, stearic acid, talc, hydrogenated vegetable oils and the like. A preferred suitable lubricant is magnesium stearate.

As used herein, the term “suitable glidant” means silicon dioxide, talc and the like. A preferred suitable glidant is silicon dioxide.

The term “inert ingredient” as used herein is a therapeutically inactive ingredient well known in the field of pharmacology that can be used alone or in various formulations, eg Includes binders, diluents, lubricants, glidants, sweeteners, disintegrants, colorants, fragrances, antioxidants, solubilizers, coatings, etc., The United States Ph
armacopeia, XXII, 1990 (1989 The United States Pharmacopeial Convention,
Inc.), 1857-1859. This is incorporated herein by reference. For example, the following inert ingredients: binders such as gelatin, polyvinylpyrrolidone (PVP), pregelatinized starch, providone; diluents such as calcium carbonate, lactose, starch, microcrystalline cellulose, etc .; lubricants such as magnesium stearate. , Calcium stearate, zinc stearate, stearic acid, talc, hydrogenated vegetable oil, etc .; glidants such as silicon dioxide, talc, etc .; disintegrants such as alginic acid, methacrylic acid DVB, crosslinked PVP, microcrystalline cellulose, croscarmellose sodium, crospovidone, Polacrylin potassium,
Sodium starch glycolate, starch, pregelatinized starch and the like; sweeteners; coloring agents; flavoring agents; antioxidants and the like can be used alone or in various formulations.

Description of the Preferred Embodiments One embodiment of the present invention will now be described with reference to the accompanying drawings. Referring to FIG. 1, the package is in the form of a rectangular box, the medicaments A and B respectively.
The front view of the inside of the box 3 which attaches the lids 1a and 2a to the medicine bottles 1 and 2 containing is fractured and shown. The vial 1 is placed on a platform 7, the cover flap 5 on the top of the box is shown in the closed position and the side flaps 6 on the top are shown in the closed position. 4 is a side view of the box, and 8 is a top view of the box.

Referring to FIG. 2, the packaging is in the form of a rectangular box, showing an unbroken front view 3'of the box. Top cover flap 5'and top side flap 6
′ Is open. A cushion 6a 'is attached to the upper side flap 6'. 4 is a side view of the box.

Referring to FIG. 3, the container is shown as an open view of the vial 1 and 2 with the vial lids 1a and 2a located just above the vial.

[Brief description of drawings]

FIG. 1 is a partially cutaway front view of a single package as a box, showing how the containers are placed inside the package.

FIG. 2 is a view of a single package as a box with flaps, with the flaps open to show the position where the container is inserted into the box.

[Figure 3]   Figure 6 shows an open container with a screw top cap located just above the vial.

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Claims (65)

[Claims] 1. A container 1 containing (a) a therapeutically effective amount of fexofenadine or a drug A having a pharmaceutically acceptable addition salt thereof; (b) a therapeutically effective amount of fexofenadine and sudo. A container 2 in which a drug B having ephedrine or a pharmaceutically acceptable addition salt thereof is dispensed, and the drug A in the containers 1 and 2
And a package which dispenses two or more pharmaceutically active compounds which provide an indication identifying B and B. 2. The addition salt has the formula: The package of claim 1 which is fexofenadine hydrochloride having the formula: wherein X is a number in the range of about 0 to 5 and its individual optical isomers. 3. The addition salt has the formula: The package according to claim 1, wherein the package is pseudo-ephedrine hydrochloride. 4. The package according to claim 1, wherein the medicine A in the container 1 is instructed to be used at night, and the medicine B in the container 2 is indicated to be used in the daytime. 5. The package of claim 4, wherein the indicia is used to identify container 1 and container 2. 6. The package of claim 5, wherein the indicia are sized or colored. 7. The package according to claim 6, wherein the drug A is placed in a smaller container. 8. The package according to claim 6, wherein the medicine B is contained in a larger container. 9. The package according to claim 1, wherein the containers 1 and 2 are in the form of vials. 10. Containers 1 and 2 are enclosed in a unipackage.
Stated packaging. 11. The unipackage of claim 10, wherein the packaging is a convenient packaging. 12. Unipackage according to claim 11, in the form of a box. 13. The package according to claim 1, wherein the drugs A and B in the containers 1 and 2 are in the form of capsules, caplets, tablets or liquid formulations. 14. The container according to claim 13, wherein the drug A in the container 1 is a capsule. 15. The container according to claim 13, wherein the drug B in the container 2 is a tablet. 16. The package according to claim 1, wherein the drug A and the drug B further include a pharmaceutical carrier and a formulation aid. 17. The package of claim 16, wherein Drug A comprises fexofenadine hydrochloride, has a particle surface area of greater than or equal to about 1.0 m ² / g, and further has at least one inert ingredient. 18. At least one inactive ingredient is selected from the group consisting of croscarmellose sodium, lactose, microcrystalline cellulose, pregelatinized starch, gelatin, calcium carbonate, magnesium stearate and sodium starch glycolate. Item 17. The packaging according to Item 17. 19. The inactive ingredient comprises croscarmellose sodium, lactose, microcrystalline cellulose, pregelatinized starch and gelatin.
Stated packaging. 20. Croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, and gelatin are each about 1% to about 10%, 20% to about 85%, 20% to about 85% by weight relative to drug A. %, 1% to about 3
20. The package of claim 19 present in an amount of 0% and 1% to about 15%. 21. Croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch and gelatin are about 4.8%, 33.8%, 33.8% and 9.6%, respectively, as the weight% of drug A. 20. The package according to claim 19, which is present in an amount of 3.5% and 3.5%. 22. The packaging of claim 18, wherein the inactive ingredients include microcrystalline cellulose, pregelatinized starch, gelatin, magnesium stearate, calcium carbonate and sodium starch glycolate. 23. Microcrystalline cellulose, pregelatinized starch, gelatin,
Magnesium stearate, calcium carbonate and sodium starch glycolate are about 20% to about 85% and 5% to about 50% by weight, respectively, relative to drug A.
%, 1% to about 15%, 0.05% to about 3%, 5% to about 50% and 1% to about 15%
23. The package of claim 22, which is present in an amount of%. 24. Microcrystalline cellulose, pregelatinized starch, gelatin,
Magnesium stearate, calcium carbonate and sodium starch glycolate are about 33.5%, 28.3% and 3.1%, respectively, as the weight% of drug A.
23. The package of claim 22, present in an amount of 0.5%, 0.5%, 15.0% and 5.4%. 25. The package of claim 18, wherein the inactive ingredients include croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate. 26. Croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate are respectively about 1% to about 10%, 20% to about 85% by weight of drug A, respectively.
20% to about 85%, 1% to about 30%, 1% to about 15% and 0.05% to about 3.0.
26. The package of claim 25, present in an amount of%. 27. Croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate are respectively about 4.6%, 32.4% and 32.4% as weight% relative to drug A. , 9.
26. The package of claim 25 present in an amount of 2%, 3.4% and 0.5%. 28. Croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate are respectively about 4.8%, 33.7% and 33.7% as weight% relative to drug A. , 9.
26. The package of claim 25 present in an amount of 6%, 3.5% and 0.5%. 29. The package of claim 18, wherein the inactive ingredients include microcrystalline cellulose, pregelatinized starch, magnesium stearate, calcium carbonate and sodium starch glycolate. 30. Microcrystalline cellulose, pregelatinized starch, magnesium stearate, calcium carbonate and sodium starch glycolate are about 20% to about 85%, 5% to about 50% and 0.0% by weight, respectively, relative to drug A. 0
30. Present in an amount of 5% to about 3%, 5% to about 50% and 1% to about 15%.
Stated packaging. 31. Microcrystalline cellulose, pregelatinized starch, magnesium stearate, calcium carbonate and sodium starch glycolate are about 35.1%, 29.8%, 0.5% and 15% by weight with respect to drug A, respectively. 0.0%
30. The package of claim 29, which is present in an amount of 5% and 5.4%. 32. The package according to claim 18, wherein the drug A is fexofenadine hydrochloride. 33. The package of claim 32, wherein fexofenadine hydrochloride is present in an amount of about 14.4% by weight of Drug A. 34. Fexofenadine hydrochloride about 2m ² / g to about 10 m ² / g
33. The package of claim 32 having a particle surface area of. 35. Fexofenadine hydrochloride packaging of claim 32 having a particle surface area of about 2m ² / g to about 6 m ² / g. 36. Fexofenadine hydrochloride packaging of claim 32 having a particle surface area of about 2m ² / g to about 4m ² / g. 37. The package of claim 32, wherein fexofenadine hydrochloride is present in an amount of about 5 mg to about 180 mg. 38. Drug B comprises: (a) a therapeutically effective decongestive amount of pseudoephedrine or a pharmaceutically acceptable addition salt thereof, ie, about 18% to about 39% by weight of pseudoephedrine; and ( i) Carnauba wax in an amount of about 59% to about 81% by weight of the sudoephedrine and (ii) a suitable anti-adhesion amount of about 0.25% to about 2.00% by weight of the sudoephedrine. A first separated region containing a first carrier base material consisting of a mixture of agents, wherein the first carrier base material provides a sustained release of pseudo-ephedrine or a pharmaceutically acceptable addition salt thereof. And (b) a therapeutically effective antihistamine amount of fexofenadine or a pharmaceutically acceptable addition salt thereof, ie about 15% to about 30 fexofenadine.
%, And (i) about 27% to about 73% by weight of the fexofenadine cellulose diluent; (ii) about 15% to about 3% by weight of the fexofenadine.
0% amount of pregelatinized starch; (iii) about 0.25% to about 6.00% by weight of fexofenadine of a suitable disintegrant and (iv) about of weight of fexofenadine. A second carrier base consisting of a mixture of suitable lubricants in an amount of 0.25% to about 2.00%, wherein the second carrier base material is fexofenadine or a pharmaceutically acceptable addition salt thereof. 17. A package according to claim 16 which is a bilayer tablet composed of a second separated area containing a). 39. The addition salt has the formula: 39. The package of claim 38 which is fexofenadine hydrochloride having the formula: wherein X is a number from about 0 to about 5 and their individual optical isomers. 40. A bilayer tablet of Drug B comprises: (a) about 25% to about 33% by weight of a therapeutically effective decongestant amount of pseudoephedrine or a pharmaceutically acceptable addition salt thereof. %; And (i) about 66% to about 74% by weight of carnauba wax, and (ii) about 0.50% to about 1.50% by weight of suedoephedrine. A first separated region containing a first carrier base material consisting of a mixture of suitable anti-adhesives, wherein the first carrier base material is of sudoephedrine or a pharmaceutically acceptable addition salt thereof. Providing a sustained release); and (b) a therapeutically effective antihistamine amount formula: Fexofenadine hydrochloride (where X is a number from about 0 to about 5) and their individual optical isomers, about 15% to about 24% by weight; and (i) the weight of fexofenadine. A cellulose diluent in an amount of about 43% to about 67%; (ii) a pregelatinized starch in an amount of about 15% to about 24% by weight of fexofenadine;
iii) a suitable disintegrant in an amount of about 3.20% to about 4.80% by weight of fexofenadine and (iv) about 0.50% to about 1.00% by weight of fexofenadine. Containing a second carrier base consisting of an amount of a mixture of suitable lubricants, wherein the second carrier base material provides immediate release of fexofenadine or a pharmaceutically acceptable addition salt thereof. 39. The package of claim 38, wherein the package comprises a second separated area. 41. A suitable glidant is included in a first carrier base material of pseudoephedrine in an amount of 0.00% to about 3.00% by weight of pseudoephedrine. Packaging. 42. A suitable glidant is 0.000% to about 0.750% based on the weight of pseudoephedrine in the first carrier base material of pseudoephedrine.
42. The package of claim 41, which is included in an amount of. 43. The package of claim 42, wherein the suitable glidant is colloidal silicon dioxide. 44. The package of claim 43, wherein the pseudoephedrine is pseudoephedrine hydrochloride. 45. The package of claim 40, wherein the pseudoephedrine is pseudoephedrine hydrochloride. 46. A suitable anti-adhesive agent for pseudoephedrine is stearic acid, and in fexofenadine, a suitable disintegrant is croscarmellose sodium and a suitable lubricant is magnesium stearate. Item 44. The packaging according to Item 44. 47. A suitable anti-adhesive agent for pseudoephedrine is stearic acid, and in fexofenadine, a suitable disintegrant is croscarmellose sodium and a suitable lubricant is magnesium stearate. Item 45. The package according to Item 45. 48. Pseudoephedrine hydrochloride, carnauba wax of pseudoephedrine, stearic acid, and colloidal silicon dioxide are about 28.17%, about 70.42%, and about 70% by weight, respectively, of the weight of the pseudoephedrine composition. 1.15
% And about 0.25%, wherein fexofenadine, a cellulosic diluent for fexofenadine, pregelatinized starch, croscarmellose sodium and magnesium stearate are each about per weight of the fexofenadine composition. 17.09%, about 61.67%, about 17.09%, about 3.42% and about 0.09%.
47. The package of claim 46, which contains an amount of 75%. 49. Pseudoephedrine hydrochloride, pseudoephedrine carnauba wax, stearic acid, and colloidal silicon dioxide are about 28.17%, about 70.42%, and about 70,42% by weight of the pseudoephedrine composition, respectively. 1.15
% And about 0.25%, wherein fexofenadine, a cellulosic diluent for fexofenadine, pregelatinized starch, croscarmellose sodium and magnesium stearate are each about per weight of the fexofenadine composition. 17.09%, about 61.67%, about 17.09%, about 3.42% and about 0.09%.
48. The package of claim 47, which comprises an amount of 75%. 50. The package of claim 48, wherein the fexofenadine is fexofenadine hydrochloride. 51. The package of claim 49, wherein fexofenadine is fexofenadine hydrochloride. 52. The package of claim 50, wherein the cellulose diluent comprises a blend of AVICEL PH101 and AVICEL PH102. 53. The package of claim 51, wherein the cellulose diluent comprises a blend of AVICEL PH101 and AVICEL PH102. 54. A blend of AVICEL PH101 and AVICEL PH102 has an AV of about 12%.
53. The package of claim 52, which comprises ICEL PH101 and about 88% AVICEL PH102. 55. A blend of AVICEL PH101 and AVICEL PH102 has an AV of about 12%.
54. The package of claim 53, which comprises ICEL PH101 and about 88% AVICEL PH102. 56. The package of claim 54, wherein fexofenadine hydrochloride is present in an amount of about 60 mg and sudoephedrine hydrochloride is present in an amount of about 120 mg. 57. The package of claim 55, wherein fexofenadine hydrochloride is present in an amount of about 60 mg and sudoephedrine hydrochloride is present in an amount of about 120 mg. 58. The package according to claim 56, wherein the bilayer tablet is coated with a suitable coating agent. 59. The package of claim 57, wherein the bilayer tablet is coated with a suitable coating agent. 60. The package of claim 58, wherein the bilayer tablet is coated with OPADRY® YS-1-7006. 61. The package of claim 59, wherein the bilayer tablet is coated with OPADRY® YS-1-7006. 62. OPADRY® YS-1-7006 is about 2. per weight of composition.
61. The package of claim 60, which is present in an amount of 9%. 63. OPADRY® YS-1-7006 is about 2. per weight of composition.
62. The package of claim 61, which is present in an amount of 9%. 64. The package of claim 56, wherein the bilayer tablet has a hardness of about 15 kp to about 25 kp. 65. The package of claim 57, wherein the bilayer tablet has a hardness of about 15 kp to about 25 kp.