Title of Invention

PHARMACEUTICAL COMPOSITIONS CONTAINING TAURINE AND RACE-METHIONINE FOR THE TREATMENT OF ALCOHOLISM.

Abstract

The present invention relates to Pharmaceutical compositions for the treatment of alcoholism which is containing taurine and race-methionine. Taurine can either promote or repress the reward effects associated with alcohol; the delineating factor being the amount of alcohol consumed its role in alcoholism. Its major metabolite taurocholic acid is responsible for the metabolic conversion of alcohol. Race Methionine has antioxidant properties. It prevents lower cholesterol levels by increasing the liver"s production of lecithin, reduces liver fat.

Full Text

FORM 2 THE PATENT ACT1970 (39 OF 1970) AND THE PATENTS RULES, 2003 (See section 10, rule 13) (COMPLETE SPECIFICATION) TITLE OF THE INVENTION - Pharmaceutical compositions containing taurine and race-methionine for the treatment of alcoholism. NAME OF APPLICANT- Zota Health Care Limited. ADDRESS OF APPLICANT- Zota House 2/896, Hira Modi Street, Sagrampura, Kurat-395002 (Gujarat) India. PREAMBLE OF INVENTION; The following specification particularly desciihes the invention anc the manner in which it is to be performed. FIELD OF THE INVENTION; The invention relates generally to pharmaceutical composition containing taurine and race-methioninc for the treatment of alcoholism. PRIOR ART; In existing method as given in, US Patent 5906811 wherein said The combination of several synergistic antioxidants, enzymatic co-factors and amino acids in appropriate delivery vehicles employed in aerosol carriers, mist and pump oral sprays, solutions, such as oral irrigators, mouth rinses and mouthwashes, or gels and solid compositions as a means of preventing and ameliorating signs and symptoms and complications to the oro-pharyngeal cavity and mouth including buccal mucosa, gums and tongue and the upper respiratory tract from damage caused by free radical species induced by tobacco smoke, smokeless tobacco, ingested or chewed noxious, malodorous or harmful substances and other inhaled environmental pollutants and particulate matter, including tobacco to secondary smokers. In another existing method as given in United States Patent 5817695 wherein said A nutritional product is provided for cancer patients comprising, as per caloric requirement, a low concentration of carbohydrate, a high concentration of fat and an imbalance of amino acids wherein L-phenylalanine, L-tyrosine and L-methionine are present in the below normal concentrations and L-leucine is present in substantial excess of normal concentrations to suppress cancer growth and as an adjunct to conventional cancer therapies In another existing method as given in European Patent EP1408988wherein said Provided is a synergistic combination of nutritional supplements classified as Nutraceuticals and further combined with antioxidant vitamins and minerals that, when orally administered to mammals, provides optimal delivery of vital metabolic precursors necessary for the production and repair of articular cartilage. Specifically provided is, a unique combination of chondroitin sulfate sodium, methylsulfonylmethane, glucosamine potassium, glucosamine hydrochloride, glucosamine sulfate sodium, N-acetyl D-Glucosamine, sodium absorbatc and chelated manganese proteinate compounded through agitation. The provided compositions and methods of administration are designed to effectively elevate and sustain blood levels of said compounds in turn enhancing the body's natural chondroprotective mechanisms while providing an efficient delivery mechanism which optimizes cellular uptake of glucosamine and chondroitin. This process of forming specified synergistic relationships between vital metabolic precursors increases the body's production of proteoglycans, chondrocytes, hyalauron glycosaminoglycans and collagen, facilitating the repair and regeneration of articular cartilage and symptomatic relief from pain and inflammation associated with articular degeneration. In another existing method as given inWO 2006/062273 Al, wherein said The present invention relates to a health supplement food utilizing, in particular, branched amino acids from among essential amino acids. More specifically, the present invention relat.s to: a health supplement food comprising branched chain amino acids (hereinafter, referred to as LIV) composed of leucine (L). isoleucine (I) and valine (V) which is made to have a composition similar to essential amino acids contained in ' naturally-occurring milk. eggs, soybeans, beef and the like, and enhancing instant impact power under anaerobic conditions, via addition of L- glutamine and taurine which are essentially required when a person is exposed to excessive exercise, stress or overwork; a health supplement food for improving a weak constitution, comprising herbal materials such as ginseng, red ginseng and Acanthopanax; and a diet food or beverage further comprising dietary fibers such as inulin, polydextrose and crystalline cellulose, and carnitine and hydroxy citric acid. In another existing method as given in WO 2007/115112 A2wherein said An exemplary dried, meat-based product includes meat and plant seed where the plant seed comprises at least approximately 3% caffeine by weight. For example, an exemplary product includes guarana plant seed. According to various products and processes, plant seed may be provided as a powder In another existing method as given in US 2009/0005320 Al wherein said The invention relates to compositions comprising one or more ionic salts, each of said ionic salts consisting of a bicarbonate anion and a cation selected from the group consisting of an amino acid, an amino acid derivative, a di-peptide and a tri-peptide, and to methods of making and using said compositions. BACKGROUND OF INVENTION: The present invention is basically based on treatment of alcoholism by pharmaceutical composition. Alcoholism is a disease. It is often diagnosed more through behaviors and adverse effects on functioning than by specific medical symptoms. Alcoholics, when confronted, will often deny excess consumption of alcohol. Alcoholism is a diverse disease and is often influenced by the alcoholic's personality as well as by other factors. Therefore, signs and symptoms often vary from person to person. There are. however, certain behaviors and signs that indicate someone may have a problem with alcohol. These behaviors and signs include insomnia, frequent falls, bruises of different ages, blackouts, chronic depression, anxiety, irritability, tardiness or absence at work or school, loss of employment, divorce or separation, financial difficulties, frequent intoxicated appearance or behavior, weight loss, or frequent automobile collisions. Late signs and symptoms include medical conditions such as pancreatitis, gastritis, cirrhosis, neuropathy, anemia, cerebellar atrophy, alcoholic cardiomyopathy (heart disease). Wernicke's encephalopathy (abnormal brain functioning), Korsakoff s dementia, central pontine myelinolysis (brain degeneration), seizures, confusion, malnutrition, hallucinations, peptic ulcers, and gastrointestinal bleeding. EFFECT OF ALCOHOLISM IN LIVER- Alcohol abuse can cause a condition called "fatty liver" or another called "alcohol hepatitis" - both of'which can be treated, but only if alcohol consumption is stopped. If drinking continues, these conditions will cause cirrhosis of the liver. Alcoholism is called a progressive disease, meaning that over time the symptoms and effects of drinking alcohol become more intense and severe. The symptoms in the early stages differ from those during later stages as the disease progresses from binge drinking to alcohol abuse to alcohol dependence. The liver detoxifies poisons, both those produced by the body and those from outside; filters bacteria from the blood; regulates fat metabolism; stores and manufactures vitamins; regulates and manufactures cholesterol and fats: synthesizes proteins; maintains the body's water and salt balance; secretes bile for the digestion of fat; stores energy (in the form of glycogen) helps regulate overall body metabolism; transforms the highly toxic ammonia (produced by exercise and by metabolism of proteins) into urea t which is eliminated in the urine: manufactures lipoproteins for fat and cholesterol transport; and metabolizes alcohol. If the liver stops doing any of these jobs, or numerous others it does constantly, the result is fatal. Self Care Information dissemination. This strategy provides awareness and knowledge of the nature and extent of alcohol, tobacco, and other drug use, abuse, and addiction and their effects on individuals, families, and communities, as well as information to increase perceptions of risk. It also provides knowledge and awareness of prevention policies, programs, and services. It helps set and reinforce norms (for example, underage drinking and drug dealers will not be tolerated in this neighborhood). Prevention education. This strategy aims to affect critical life and social skills, including decision making, refusal skills, critical analysis (for example, of media messages), and systematic and judgmental abilities. Alternatives- This strategy provides for the participation of targeted populations in activities that exclude alcohol, tobacco, and other drug use by youth. Constructive and healthy activities offset the attraction to, or otherwise meet the needs usually filled by. alcohol, tobacco, and other drug use. Problem identification and referral. This strategy calls for identification, education, and counseling for those youth who have indulged in age-inappropriate use of tobacco products or alcohol, or who have indulged in the first use of illicit drugs. Activities under this strategy would include screening for tendencies toward substance abuse and referral for preventive treatment for curbing such tendencies. Community-based process. This strategy aims to enhance the ability of the community to provide prevention and treatment services to alcohol, tobacco, and other drug use disorders more effectively. Activities include organizing, planning, enhancing efficiency and effectiveness of services implementation, interagency collaboration, coalition building, and networking. Building healthy communities encourages healthy lifestyle choices. Environmental approach. This strategy sets up or changes written and unwritten community standards, codes, and attitudes-influencing incidence and prevalence of alcohol, tobacco, and other drug use problems in the general population. Included are laws to restrict availability and access, price increases, and community-wide actions. OBJECT OF THE INVENTION: The main object of the invention is to provide the composition of pharmaceutical which is comparatively more effective than others as it contains taurine and race-methionin. Taurine, or 2-aminoethanesulfonic acid, is an organic acid. Taurine can either promote or repress the reward effects associated with alcohol; the delineating factor being the amount of alcohol consumed its role in alcoholism. Its major metabolite taurocholic acid is responsible for the metabolic conversion of alcohol. Race Methionine has antioxidant properties. It prevents lower cholesterol levels by increasing the liver's production of lecithin, reduces liver fat and protects the kidneys. STATEMENT OF THE INVENTION: This invention is based on a pharmaceutical composition containing taurine and race-methionine for treating alcoholism. Both arc helpful for protection to liver by alcohol. DETAILED DESCRIPTION OF INVENTION: The liver is the largest glandular organ of the body. The liver has many functions. Some of the functions are: to produce substances that break down fats, convert glucose to glycogen, produce urea (the main substance of urine), make certain amino acids (the building blocks of proteins), filter harmful substances from the blood (such as alcohol), storage of vitamins and minerals (vitamins A, D, K. and B12) and maintain a proper level or glucose in the blood. The liver is also responsible for producing cholesterol. It produces about 80% of the cholesterol in your body. The main disease of liver is Alcohol alters the metabolism of the liver, which can have overall detrimental effects if alcohol is taken over long periods of time Short-term effects Depending on how much you drink, your experience with alcohol and the environment in which you arc drinking, alcohol can cause: • relaxation, feeling of well-being • loss of inhibitions • dizziness, unclear judgement • uncoordinated movements, slow reactions • blurred vision, slurred speech • unconsciousness • death Taurine or 2-aminoethanesulfonic acid- It is an organic acid. Taurine is one of the most abundant amino acids in the body. It is also a major constituent of bile and can be found in the lower intestine and in small amounts in the tissues of many animals, including humans. Taurine is a derivative of the sulfur-containing (sulfhydryl) amino acid, cysteine. Taurine is one of the few known naturally occurring sulfonic acids. It has a number of roles regarding normal functioning of the brain, heart, gallbladder, eyes and vascular system. It functions to facilitate the movement of mineral and salt ions in and out of the cells and to stabilize cell membranes. Among several taurine derivatives, Ca N-acetylhomotaurinate (Ca AOTA) appears to be the most active anti-acetaldehyde and anti-alcohol agent. Large numbers of 1 taurine derivatives have been reported in the literature with partial to marked activity. Taurine derivatives like taltrimide, acamprosate and tauromustine, are already in the market as anticonvulsant, anti-alcoholic and anti-cancer agents. Taurine derivatives like taltrimide, acamprosate and tauromustine, are already in the market as anticonvulsant, anti-alcoholic and anti¬cancer agents. MECHANISM OF TAURINE - Taurine can either promote or repress the reward effects associated with alcohol, the delineating factor being the amount of alcohol consumed. Its major metabolite taurocholic acid is responsible for the metabolic conversion of alcohol. The correlation of taurine with alcohol consumption, scientists synthesized the drug acamprosate, the calcium salt of N-acetyl-homotaurinate. It is the first agent specifically designed to maintain abstinence in alcohol-dependent patients who have completed detoxification. It interacts with glutamanergic neurotransmission channels (NMDA receptors) to reduce calcium flux., resulting in a depressed interest in alcohol consumption.Acomprosate decreases glutamate elevations that are characteristic of alcohol withdrawal. It's also use for Hepatic steatosis (Tatty liver') and lipid peroxidation by administering alcohol .hepatic steatosis was greatly reduced and lipid per oxidation completely prevented. Fatty liver was prevented in animals receiving taurine supplementation. The protective effect of taurine was attributed to the potential of taurine conjugated bile acids (particularly taurocholic acid) to inhibit adverse enzymatic functions associated with alcohol consumption. This elucidates the very crucial tasks that taurine performs to protect against the deleterious effects of chronic alcohol consumption. RACE- METHIONINE (Essential) 1 .-Methionine has antioxidant properties. Methionine is one of the three amino acids needed by the body to manufacture Creatine, an amino acid essential for energy production and muscle building MECHANISM OF RACE-METHIONINE It prevents disorders of the hair, skin and nails, helps lower cholesterol levels by increasing the liver's production of lecithin, reduces liver fat and protects the kidneys. Methionine is a natural chelating agent for heavy metals. It regulates the formation of ammonia and creates ammonia-free urine, which reduces bladder irritation. Methionine is used in the liver as a detoxifying agent. It has also been used to treat depression, arthritis pain and chronic liver disease. Procedure of Manufacturing . QUANTITATIVE FORMULA; 12 Magnesium Stearate BP 12.0 - 12.0 1.200 13. Talc BP 20.0 - 20.0 2.00 14 Sodium Starch Glycolate BP 20.0 20.0 2.00 15 Aerosil(colloidal Silicon dioxide) USP 3.00 3.00 0.300 Total Material Weight per Tablet : 981.60 mg • PART IV: COATING Film coat Ready mix White(INSTACOAT) HIS 24.60 24.60 2.460 ISOPROPYL ALCOHOL BP 0.200ML 0.200ML 20.00LTS METHYLENR DICHLORIDE BP 0.390GM 0.390GM 39.00KGS • LIST OF EQUIPMENTS / MACHINES TO BE USED FOR MANUFACTURING SR. NO. NAME OF EQUIPMENT / MACHINE 1 Sifter 2 Octagonal Blender Planetary Mixer [ 100 Lits. ] 4 Fluid Bed Dryer capacity 60 Kg. with SS Trolleys / Tray Dryer 5 Multi-mill 6 Tablet compression machine 7 Stainless steel scoops 8 Infrared moisture balance 9 Digital balance capacity 150 Kg. & 5 Kg. 10 D.T Apparatus 11 Hardness Tester 12 Friability Test Apparatus 13 Micrometer / Vernier 14 Plastic, lnprocess containers 15 Stirrer MANUFACTURING PROCESS: 4.1 GRANULATION SR. NO ACTIVITY 1. Sift Race methionine and taurine sieve in sifter. For geometrically mixing. 2. Load Above sifted materials in PLM & mix for 30 minutes at slow speed. [ Bitter : 12 rpm & Sun : 25 rpm j Prepare Starch & Gelatin (P): Starch 4.00 Kgs . Gelatin 0.500 Kgs., & Sodium Benzoate 0.400 Kgs., in 15.00 Lits. Of Purified Water & add in P.L.M.& granulate at fast speed for 20 minutes \ Bitter : 25 rpm & Sun : 50 rpm ]& than at slow speed for two minutes. [ Bitter : 12 rpm & Sun : 25 rpm ] 4. Pass Wet mass through Multimill using 12 mm # at medium-speed f 1525 rpm ] 5. Unload the wet mass in FBD trolleys and dry at inlet air temperature of 60°C + 5 °C. Check the LOD. (Limit: Not More Than 3.0%). 6. Sift the dried granules through 16 # sieve in sifter and mill the oversized granules through 2.5 mm # in Multimill at medium speed. | 1525 rpm ] 7. Sift Magnesium stearate 1.200 Kgs,., Talc 2.00 Kgs., Sodium Starch Glycolate 2.00 Kgs, & Aerosil 0.300 Kgs., through 60 # sieve in sifter. 8. Blend granules from Step (6) and lubricants from Step (7) in PLM for 10 minutes. [ Bitter: 12 rpm & Sun : 25 rpm ] (Add mag. Stearate last 5.0 minuts) 9. Check the total weight of lubricated granules & record. Intimate Q.A dept to collect the CLAIMS: I Claim; (1) Pharmaceutical compositions for the treatment of alcoholism which is containing taurine and race- methionine. (2) The Pharmaceutical composition comprises of taurine and race-methionine. (3) The Pharmaceutical composition as recited in Claim 2 wherein said Taurine can either promote or repress the reward effects associated with alcohol, the delineating factor being the amount of alcohol consumed. (4) The Pharmaceutical composition as recited in Claim 1 wherein said race methionine prevents disorders of the hair, skin and nails, helps lower cholesterol levels by increasing the liver's production of lecithin, reduces liver fat. (5) The Pharmaceutical composition as recited in Claim 1 wherein said methionine is a natural chelating agent for heavy metals. It regulates the formation of ammonia and creates ammonia-free urine, which reduces bladder irritation. (6) The Pharmaceutical composition as recited in Claim 1 wherein said methionine is used in the liver as a detoxifying agent. It has also been used to treat depression, arthritis pain and chronic liver disease. Signature of Applicant- Place- Surat Name of Applicant- MR.KAMLESH RAJN1KANT ZOTA

Documents:

1868-mum-2009-abstract.doc

1868-mum-2009-abstract.pdf

1868-MUM-2009-AFFIDAVIT(21-10-2013).pdf

1868-MUM-2009-CLAIMS(AMENDED)-(2-11-2012).pdf

1868-MUM-2009-CLAIMS(AMENDED)-(21-10-2013).pdf

1868-MUM-2009-CLAIMS(MARKED COPY)-(21-10-2013).pdf

1868-mum-2009-claims.doc

1868-mum-2009-claims.pdf

1868-mum-2009-description(complete).doc

1868-mum-2009-description(complete).pdf

1868-MUM-2009-DRAWING(2-11-2012).pdf

1868-MUM-2009-DRAWING(21-10-2013).pdf

1868-mum-2009-drawing.pdf

1868-mum-2009-form 1.pdf

1868-mum-2009-form 18.pdf

1868-mum-2009-form 2(title page).pdf

1868-mum-2009-form 2.doc

1868-mum-2009-form 2.pdf

1868-MUM-2009-FORM 3(2-11-2012).pdf

1868-MUM-2009-FORM 3(21-10-2013).pdf

1868-MUM-2009-FORM 5(2-11-2012).pdf

1868-MUM-2009-FORM 5(21-10-2013).pdf

1868-mum-2009-form 9.pdf

1868-MUM-2009-REPLY TO EXAMINATION REPORT(2-11-2012).pdf

1868-MUM-2009-REPLY TO HEARING(21-10-2013).pdf

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