Title of Invention

"NOVEL ORAL PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF RESPIRATORY ALLERGIC DISEASES."

Abstract

An oral pharmaceutical composition which contains an active ingredients which is Ambroxol. levo cetrizine, Ketotifen together with one or more physiologically acceptable excipients. The present invention describes process for preparation of active ingredients with pharmaceutical acceptable excipients. The compositions increase the efficacy of treatment associated with particularly allergic and respiratory related disease thereof to patient compliance.

Full Text

FORM 2 THE PATENTS ACT, 1970 (39 OF 1970) & PATENTS RULES, 2003 (COMPLETE SPECIFICATION) TITLE OF INVENTION; "NOVEL ORAL PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF RESPIROTORY ALLERGIC DISEASES." NAME OF APPLICANT: ZOTA HEALTH CARE LTD ADDRESS OF APPLICANT: ZOTA HEALTH CARE LTD ZOTA HOUSE 2/896, HIRA MODI STREET, SAGRAMPURA SURAT 395002 (GUJARAT) INDIA. The following specification particularly describes the nature of the invention and the manner in which it is to be performed. FIELD OF INVENTION - The present invention provides novel oral pharmaceutical compositions for respiratory allergic diseases comprising active agent and one or more pharmaceutical acceptable excipients. The present invention describes process for preparation and method of using compositions. Preferably the compositions increase the efficacy of treatment associated with particularly respiratory and allergic diseases, leading to grater patient compliance. BACKGROUND OF INVENTION - Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. The substance is a mucoactive drug with several properties including secretolytic and secretomotoric actions that restore the physiological clearance mechanisms of the respiratory tract, which play an important role in the body's natural defence mechanisms. Ambroxol is indicated as "secretolytic therapy in bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport. It promotes mucus clearance, facilitates expectoration and eases productive cough, allowing patients to breathe freely and deeply". There are many different formulations developed since the first marketing authorisation in 1978. Ambroxol is very effective in the form of tablets, capsule and powder thereof. Although acute upper respiratory diseases (AURDs) such as common cold and influenza are common, few interventions have been proven to be effective in their prophylactic and treatment. The aim of this study was to assess the efficacy of Ambroxol for preventing AURD including treatment of pneumonia, treatment of bronchiolitis, treatment of children with asthma, the treatment of neonatal respiratory distress syndrome. Conclusions of Ambroxol treatment of childhood respiratory disease is effective and less adverse reaction, high security, is worthy of clinical use. Respiratory diseases to cough, sputum, and dyspnea based disease. Infant tracheobronchial stenosis than in adults and the lack of elastic tissue, ciliary movement function is poor, weak cough reflex, poor alveolar macrophage function, non-specific respiratory tract and specific immune functions are poor. These characteristics make children prone to respiratory infections, and infected mucus airway obstruction and difficult to spit up. So while the cause of the treatment, timely application of expectorant drugs and asthma drugs, in order to control symptoms and prevent disease progression. Ambroxol now widely used in abnormal and expectoration of sputum associated with dysfunction of various acute and chronic respiratory diseases, expectorant treatment of respiratory diseases in children in recent years has also been widely used. A large dose of Ambroxol in alveolar type cells to promote surfactant synthesis and secretion material. In addition, surface active substances covered by respiratory epithelium, the bacteria can not directly touch the surface of the respiratory tract, can reduce the risk of infection, thus preventing respiratory tract infection, and a synergistic effect with antibiotics is the treatment of respiratory tract infection in infants and young children an effective adjuvant. In summary, Ambroxol, Ketotifen and Levocetirizine are able to treatment of respiratory diseases as a safe and effective drug by oral adjuvant especially for the respiratory infection in children with the less adverse reaction. According to United States Patent 6391886 wherein Oral compositions containing therapeutical agents wherein the undesirable consumer aesthetics associated with these agents are mitigated using coolants and sweeteners According to United States Patent 7186753 wherein Compounds or their salts of general formula (1): A—B—N(0)s wherein: s is an integer equal to 1 or 2; A=R—Tl—, wherein R is the drug radical and Tl=(CO)t or (X)t', wherein X=0, S, NRlc, Rlc is H or a linear or branched alkyl or a free valence, t and t' are integers and equal to zero or 1, with the proviso that r=l when t'=0; t=0 when t'=l; B=----TB—X2—O---- wherein TB=(CO) when t=0, TB=X when t-0, X being as above defined; X2 is equal to RIB—X—R2B radical wherein X is as above defined, RIB and R2B, equal to or different from each other, are linear or branched C1-C6 alkylenes, or X2 is a radical wherein two alkylene chains C1-C4 are linked to nonadjacent positions of a central ring having 4 or 6 atoms, said ring being an unsaturated cycloaliphatic ring, or a saturated or aromatic heterocylic ring, containing one or two heteroatoms, equal or different, selected from O, S, N; wherein the unsaturated cycloaliphatic ring does not have aromatic character according to Huckel's rule. According to WTPO Patent Application WO/1997/004808 wherein The present invention relates to compositions and methods for providing improved treatment, management or mitigation of cold cold-like, allergy, sinus and/or flu symptoms by administering a safe and effective amount of a composition comprising an analgesic agent along with certain pyrrolidine and piperidine ether antihistaminic agents. According to Patent 7175854 wherein said the present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for the production of a large number of pharmaceutical dosage forms. SUMMARY OF THE INVENTION- It is an objective of the present invention to provide novel oral pharmaceutical composition comprising one active agent and one or more pharmaceutically acceptable excipients. Preferably the composition is administered to a subject particularly human by oral form wherein the composition forms a drug that releases the pharmaceutically active agent over a desired period of time, thereby increasing the efficacy of treatment associated with particularly respiratory and allergic diseases thereof leading to greater patient compliance. The novel compositions of the present invention preferably provide the active agent to localize in certain tissues, thereby increasing the efficacy of treatment, associated with such tissues. The compositions of the present invention may be used for especially respiratory and allergic diseases in a subject in need thereof. The present invention provides a novel therapeutic oral pharmaceutical composition for the treatment of respiratory allergic diseases. This composition comprises Ambroxol, levocetirizine, Ketotifen thereof. DETAILED DESCRIPTION OF THE INVENTION -The present invention provides a novel therapeutic oral pharmaceutical administration for respiratory and allergic diseases and thereof. This comprises Ambroxol, levocetirizine, Ketotifen thereof. This is a need for the development of a pharmaceutical formulation that contains a high concentration of active ingredient where the formulation is storage able According to another preferred embodiment of the present invention Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. It is a mucoactive drug with several properties including secretolytic and secretomotoric actions that restore the physiological clearance mechanisms of the respiratory tract, which play an important roie in the body's natural defence mechanisms. According to another preferred embodiment of the present, Ketotifen is a second-generation H1 receptor antagonist /mast cell and basophile stabilizer. The main function of ketotifen in this invention is that it's working as an active bronchodilator. "An active bronchodilator is a substance that dilates the bronchi and bronchioles, decreasing resistance in the respiratory airway and increasing airflow to the lungs. They are used for the treatment of breathing difficulties specially in the case of obstructive lung diseases such as Asthma, Emphysema, Bronchitis ,Chrom'c obstructive pulmonary disease and thereof." Ketotifen is used to up-regulate beta-2 adrenergic receptors down-regulated by beta-2 adrenergic agonists. It upregulates adrenergic receptors due to its phosphodiesterase inhibition. It provides symptom relief and a minimal decrease in beta-agonist use but no significant change in pulmonary function In the case of asthma, Ketotifen is an antihistamine preparation with prolonged preventive effect on the frequency and intensity of the asthma attacks. Its mechanism of action ultimately is associated with reduction of histamine, serotonine and other mast cell mediators release, and simultaneous selective blocking of the H1-receptors. As a result of the latter effects the level of the cell cAMP in enhanced and eosinophilic infiltration is inhibited. Although the preparation influences favorably expectoration, Ketotifen is used to minimize the frequency and severity of asthma attacks. It is used on a long-term basis to prevent symptoms of mild to moderate allergic asthma and may allow for reduction of doses of other asthma medication. Ketotifen may also be used to prevent hay fever and allergic skin reactions and thereof. Ketotifen decreases the actions of histamine, a substance that is released by the body to cause an allergic reaction. Allergic reactions may include asthma, hay fever, nasal congestion, skin rash and swelling and thereof. According to another preferred embodiment of the present invention levocetirizine is safe and effective for the treatment of allergic rhinitis and chronic idiopathic urticaria. The compound shows a rapid onset of action, high bioavailability and affinity for the H1 receptor. It demonstrates many anti-inflammatory effects that enhance the clinical therapeutic benefit not only in short-term but also in long-term treatments. Its safe effective activity for treatment of allergic disease in both adults and children. Furthmore, the compatible composition according to the invention can be used to produce respiratory and allergic protective preparation for the prophylactic or treatment of related respiratory and allergic diseases caused by active ingredients like Ambroxol. levocetirizine, Ketotifen. An active ingredient represents a promising respiratory protection in the case of hay fever, asthma, They are taken orally as tablets, capsules, granules or powder but according to the invention, the compatible solutes can be used to produce a medicine in the oral form to treat disease that are caused by Ambroxol,levocetirizine, Ketotifen and thereof. Such diseases are in particular allergic or respiratory diseases. The preparation of the oral composition is following Exemple 1 In this example an oral pharmaceutical composition for the respiratory allergic diseases is prepared as per the invention. The composition comprises of the main ingredients such as ambroxol 50mg. Ketotifen 0.5 mg, levocetirizine 3mg. The result indicated that the composition is satisfactory. Example 2 In this example an oral pharmaceutical composition for the respiratory allergic diseases is prepared as per the invention. The composition comprises of the main ingredients such as ambroxol 55mg, Ketotifen 0.75mg, Levocetirizine 4mg. The result indicated that the composition is satisfactory. Example 3 In this example an oral pharmaceutical composition for the respiratory allergic diseases is prepared as per the invention. The composition comprises of the main ingredients such as ambroxol 60mg, Ketotifen lmg, Levocetirizine 5mg. The result indicated that the composition is appropriate. Example 4 In this example an oral pharmaceutical composition for the respiratory allergic diseases is prepared as per the invention. The composition comprises of the main ingredients such as ambroxol 62rng . Ketotifen 1.5mg , Levocetirizine 5.5mg . The result indicated that the composition is satisfactory. Example 5 In this example an oral pharmaceutical composition for the respiratory allergic diseases is prepared as per the invention. The composition comprises of the main ingredients such as ambroxol 65mg, Ketotifen 2mg, Levocetirizine 6mg. The result indicated that the composition is satisfactory. CLAIMS, We Claim, 1. An oral pharmaceutical composition comprising Ambroxol, Levocetirizine , Ketotifen and thereof. 2. An oral pharmaceutical composition as claimed as claim 1 wherein said the pharmaceutical acceptable excipients are selected from the group comprising organic solvents, stabilizers, preservatives, lubricants, chelating agents and thereof 3. An oral pharmaceutical composition as claimed as claim 1 wherein said compound can be enhanced and the volatility can be reduced .it can easily increase the permeability of Ambroxol, Levocetirizine, Ketotifen and thereof. 4. An oral pharmaceutical composition as claimed as claim 1 wherein said Ambroxol, levo cetirizine, Ketotifen and other pharmaceutical acceptable excipients can create synergy, efficacy increased significantly and no significantly adverse reactions. It boosts the human body's defence system and has anti-inflammatory effects. 5. An oral pharmaceutical composition as claimed as claim 1 wherein said It can be used to produce preparation for the prophylactic or treatment of respiratory and allergic related disease caused by poilen,dust,bacteria,fungus,foods,air pollution and thereof. 6. An oral pharmaceutical composition as claimed as claim 1 wherein said Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. It is a mucoactive drug with several properties including secretolytic and secretomotoric actions that restore the physiological clearance mechanisms of the respiratory tract, which play an important role in the body's natural defence mechanisms. . It used in the range between 50mg to 65 mg more preferably in 60 mg. 7. An oral pharmaceutical composition as claimed as claim 1 wherein said levocetirizine is safe and effective for the treatment of allergic and respiratory diseases. It shows a rapid onset of action, high bioavailability and affinity for the H1 receptor. It demonstrates many anti-inflammatory effects that enhance the clinical therapeutic benefit not only in short-term but also in long-term treatments. It's safe effective activity for treatment of allergic disease in both adults and children. It used in the range between 3mg to 6 mg more preferably in 5mg. 8. An oral pharmaceutical composition as claimed as claim 1 Ketotifen is a H1 receptor antagonist or mast cell and basophile stabilizer. Ketotifen is used to up-regulate beta-2 adrenergic receptors down-regulated by beta-2 adrenergic agonists. It up regulates adrenergic receptors due to its phosphodiesterase inhibition. Ketotifen is used as a bronchodilator in this invention. It dilates the bronchi and bronchioles, decreasing resistance in the respiratory airway and increasing airflow to the lungs. It provides symptom relief and a minimal decrease in beta-agonist use but no significant change in pulmonary function. It used in the range between 0.5mg to 2 mg more preferably in lmg.

Documents:

1402-mum-2011-abstract.doc

1402-mum-2011-abstract.pdf

1402-MUM-2011-CLAIMS(AMENDED)-(20-2-2014).pdf

1402-mum-2011-claims.doc

1402-mum-2011-claims.pdf

1402-mum-2011-description(complete).pdf

1402-mum-2011-form 1.pdf

1402-MUM-2011-FORM 18.pdf

1402-mum-2011-form 2(title page).pdf

1402-mum-2011-form 2.doc

1402-mum-2011-form 2.pdf

1402-MUM-2011-FORM 9.pdf

1402-MUM-2011-OTHER DOCUMENT(20-2-2014).pdf

1402-MUM-2011-REPLY TO EXAMINATION REPORT(20-2-2014).pdf