US 20130210835A1 (19) United States (12) Patent Application Publication (10) Pub. N0.2 US 2013/0210835 A1 Mitchell (43) Pub. Date: Aug. 15, 2013 (54) PHARMACEUTICAL COMPOSITIONS Publication Classi?cation (75) Inventor: Odes W. Mitchell; Arlington, TX (U S) (51) Int. Cl. A61K31/137 (2006.01) _ A611; 31/4402 (2006.01) (73) Ass1gnee: GM PHARMACEUTICAL, INC, A61K 31/485 (200601) Arhngton, TX (Us) A611; 31/09 (2006.01) _ A611; 31/495 (2006.01) (21) App1.No.. 13/703,584 A61K31/505 (200601) 22 PCT P1 d: J .13 2011 (52) us Cl ( ) 1e “n ’ CPC ........... .. A611; 31/137 (2013.01); A611;31/495 (86) PCT NO. PCT/“11,4031 (2013.01); A611;31/505 (2013.01); A611; 31/485 (2013.01); A611; 31/09 (2013.01); § 371 (0)0). A611;31/4402 (2013.01) (2), (4) Date: Feb- 2, 2013 USPC .... .. 514/255.04; 564/355; 514/653; 544/396; 544/332; 514/275; 546/74; 514/289; 514/282; Related US. Application Data 514657; 514652 (60) Provisional application No. 61/354,061; ?led on Jun. (57) ABSTRACT 11; 2010; provisional application No. 61/354,057; A composition of an antitussive; a decongestant; or an anti ?led on Jun. 11; 2010; provisional application No. histamine to treat respiratory and oral pharyngeal congestion 61/354,053; ?led on Jun. 11,2010. and related symptoms in a patient. US 2013/0210835 A1 Aug. 15,2013 PHARMACEUTICAL COMPOSITIONS mucus build-up to clear congestion in the air passages. Symp toms due to allergies or allergens are often treated With an CROSS-REFERENCES TO RELATED antihistamine. Antihistamines, often referred to as histamine APPLICATIONS class receptor blockers, are compounds that may antagonis tically block the histamine receptor from binding histamine [0001] This application claims priority from US. Provi thereby preventing the symptoms of an allergy. sional Patent Application No. 61/354,053 ?led Jun. 11, 2010, US. Provisional PatentApplication No. 61/354,057 ?led Jun. [0006] There are many different treatment medications uti 11, 2010, and US. 61/354,061 ?led Jun. 11, 2010, all of liZing a combination of agents in therapeutic doses for treat Which are hereby incorporated by reference as if fully set ing multiple symptoms of upper respiratory tract and oral forth herein. pharyngeal congestion. As one example, a single medication may include an expectorant, in combination With an antitus FIELD OF THE INVENTION sive agent, for removing phlegm or mucus that may have accumulated in the lungs and other air passages in addition to [0002] The present invention relates to the treatment and suppressing a cough. The expectorant is helpful in preventing relief of various symptoms of upper respiratory and oral the progression of a mild case of bronchitis to a more severe pharyngeal congestion, and in particular, to a combination case of pneumonia. medication for treatment and relief thereof. [0007] Combination therapy provides many bene?ts. For example, it alloWs patients suffering from congestion and BACKGROUND OF THE INVENTION related symptoms to take only a single dosage medication, as [0003] People around the World frequently suffer from opposed to multiple medications, for relief therefrom. Fur upper respiratory tract and oral pharyngeal congestion. This ther, it enhances compliance in accordance With a regimen by congestion may be caused by allergies, infections in the res eliminating the need for the patient to take different medica piratory tract and/or oral and pharyngeal cavities, changes in tions. To this end, combination therapy provides conve Weather conditions, as Well as from the overall health and nience, ensures compliance, and saves cost. genetic disposition of the person. This congestion is generally [0008] Combined treatment medications may be formu diagnosed from partially or fully blocked air passages includ lated as syrups, pills, tablets, and capsules. Formulations may ing airWays in the lungs, mouth, nose, and throat. Other include ?avoring agents to mask undesirable ?avors or tastes symptoms related to the cause typically accompany the con from desired medicinal agents and colorants to render the gestion. Cough, tickles in the throat, cold symptoms such as medication more attractive and appealing to the eye. For fever, ?u, sinus infections, and throat or gland pain are some example, many formulations have a raspberry, cherry, orange, of the more common symptoms found With upper respiratory or grape ?avor Well liked by both children and adults. More and oral pharyngeal congestion. over, these ?avors are easily identi?ed by their color. In com [0004] Congestion of the upper respiratory tract and oral bination formulations, the individual ingredients are included pharyngeal cavity and related symptoms generally have in amounts proven to be effective to treat targeted symptoms. undesirable effects for the a?llicted person. For example, the Effective amounts have varied depending on the particular congestion may affect performance in the Workplace, school, formulation, type and degree of the symptoms, and desired and at home up to and including loss of Work and loss of user or consumer. For example, a child’s dose of an elixir or school attendance. Further, congestion may reduce the ability syrup for the relief of cough and pain related to congestion to perform routine activities, such as houseWork, driving, may have the antitussive and analgesic in reduced quantities running errands, and may even totally incapacitate the person. based on siZe, Weight, and age of the child targeted, compa Severe and intolerable congestion often requires visits to the rable to a composition or formulation for an adult Which may hospital and treatment. In addition, viral or bacterial infec have double the dosage of the antitussive and analgesic. tions of the sinus passage or other airWay may be passed to [0009] Accordingly, it is desirable to have an administrable healthy persons through symptoms of the congestion. For composition to reduce symptoms of upper respiratory tract example, a cough or sneeZe may convey a bacterium or virus and oral pharyngeal congestion. It is further desirable that the to another person. Thus, upper respiratory tract and oral pha composition be effective in reducing cough, congestion, his ryngeal congestion and its symptoms need to be treated. tamine-stimulated allergy symptoms and related pain. Still [0005] Generally, there are tWo typical approaches to treat further, it is desirable for the composition to contain dosages ing symptoms of the congestion. One approach involves ini suitable for administration to a child as Well as an adult. In tially treating the underlying cause of the symptom. For addition, it is desirable to have the composition in a conve example, a bacterial infection is generally treated by admin nient and pharmaceutically acceptable dosage form. istering an antibiotic to kill the bacteria causing the infection. The second approach involves treating the symptoms them SUMMARY OF THE INVENTION selves, typically in addition to treating the underlying cause, by independently administering one or more medications for [0010] The present invention provides compositions and relief of speci?c symptoms. For example, an antitussive methods for treating upper respiratory and oral pharyngeal agent, commonly referred to as a cough suppressant, has been congestion and related symptoms in a person suffering there typically administered for the treatment or relief of cough. An from. To this end, and in accordance With the principles of the opioid medication, such as codeine and hydrocodone bitar present invention, there is provided a composition of a decon trate, has generally been administered to relieve pain consis gestant, and an antihistamine. Optionally, a composition may tent With the congestion While suppressing a cough. Also include an antitussive, an expectorant and an analgesic. The decongestants, such as phenylephrine and pseudoephedrine, combination of an antitussive, a decongestant, and an antihis have been administered to both children and adults in ?avored tamine in a single composition provides relief of cough, con formulations for reducing mucosal sWelling and draining the gestion in the air passageWays, and common allergy-type US 2013/0210835 A1 Aug. 15,2013 symptoms resulting from exposure to various allergens, in a symptoms. Thus, the present invention encompasses pallia convenient and effective dosage formulation. tive compositions and methods. [0011] The composition is formulated in pharmaceutically [0014] To this end, and in accordance With the principles of acceptable forms such as liquids, pills, capsules, tablets, and the present invention, the compositions include an antitus the like. Suitable capsule forms include, Without limitation, sive, a decongestant, and an antihistamine. Inclusion of an liquid gelatin capsules and enteric -coated capsules. The tablet antihistamine, in combination With an antitussive and a form may be cheWable, may melt or disintegrate in the mouth, decongestant provides relief of histamine-stimulated allergy or may be enteric-coated to provide delayed-release and sus symptoms in addition to relieving other symptoms, such as tained-release characteristics for the composition. In one cough, congestion, sWelling, and pain. These added bene?ts embodiment, the composition is formulated into a liquid. The provide increased ef?cacy and translate into convenience and composition may further include other components, such as cost savings for the patient. conventional excipients including binders, colorants, fra [0015] The present invention provides pharmaceutical