Tablet composition containing paracetamol, chlorpheniramine, and ascorbic acid.

Abstract

Containing paracetamol (acetaminophen), chlorpheniramine maleate, and ascorbic acid (vitamin C); cold It has analgesic, antipyretic and antihistamine effects in the symptomatic treatment of colds and flu. It relates to the composition of film-coated tablets.

Description

Tablet containing paracetamol, chlorpheniramine, and ascorbic acid. COMPOSITION Technical Area The invention relates to Paracetamol (Acetaminophen), Chlorpheniramine maleate, and Ascorbic Acid (Vitamin C). Containing; pain relievers, fever reducers, and used in the symptomatic treatment of colds and flu. This relates to the composition of film-coated tablets with antihistamine effects. State of the Art Paracetamol (acetaminophen) is a pharmaceutical active ingredient with analgesic and antipyretic effects. (Formula 1). Caffeine, codeine, hydrocodone, oxycodone, propoxyphen, tramadol, diphenhydramine, Dual combinations with phenylephrine; aspirin and caffeine, triple combinations with butalbital and caffeine. There are combinations. Paracetamol, also known by its chemical name 4-Acetamidophenol CH NO 8 9 2 It has the following molecular formula and chemical structure: Formula 1 Chlorpheniramine is an antihistamine compound used to treat allergic symptoms (Formula 1) 2). Used in the form of maleate salts. Ibuprofen and pseudoephedrine, dextromethorphan and paracetamol. Triple combinations with; quadruple combinations with dextromethorphan, paracetamol, and phenylephrine. There are combinations. Formula 2 Ascorbic acid (vitamin C or ascorbate) is found in citrus fruits and other fruits and vegetables. It is a water-soluble vitamin (Formula 3). Ascorbic acid has the molecular formula C6H8O6 and the following: It has a chemical structure: Formula 3 1 Fervex granular sachets contain 500mg paracetamol, 200mg ascorbic acid, and 25mg feniramine. Contains maleate. Coldrex tablets contain 500mg Paracetamol, 25mg Caffeine, and 5mg Phenylephrine Hydrochloride. Antipyretic, analgesic, and decongestant containing 20mg Terpin Hydrate and Vitamin C (ascorbic Acid). and it has expectorant effects. Coldrex HotRem chassis 750 mg paracetamol, 10 mg phenylephrine hydrochloride and 60 mg It contains ascorbic acid. In the case of the technique, 160mg paracetamol, 1mg chlorpheniramine maleate and 50mg ascorbic acid An OTC medicine in powder form containing [container name] has been mentioned. (*) (*) https: / / dailymed.nlm.nih.gov / dailymed / drugInfo.cfm?setid=827fd66b-9574-cbb5-e053- 2991aa0a5077) In the treatment of colds and flu, paracetamol and ascorbic acid are used in combination for adults. The maximum dosage for paracetamol is 4 g per day; ascorbic acid can be given at a dose of 2 g per day. In the case of the technique, it is preferably used for the symptomatic treatment of mild to moderate pain and fever. It is clear that effective and stable compositions are needed. Detailed Description of the Invention A configuration of the invention is a film-coated mixture containing paracetamol, chlorpheniramine maleate, and ascorbic acid. It relates to tablet compositions. Composition: Excipients that function as binders, fillers, dispersants, and lubricants. It may contain. The composition subject to the invention has a paracetamol:ascorbic acid ratio of 1.5:1 to 2.5:1. It is preferably between 60% Paracetamol by weight and 24% to 40% by weight. It contains ascorbic acid. The composition subject to the invention includes paracetamol and chlorpheniramine. Maleate is found in the inner phase, and ascorbic acid is found in the outer phase. In pharmaceutical tablet composition containing paracetamol, chlorpheniramine maleate and ascorbic acid. Paracetamol granules are produced using the wet granulation technique, while ascorbic acid is processed into granules using dry powder. It is added as follows. In pharmaceutical tablet composition containing paracetamol, chlorpheniramine maleate and ascorbic acid. Chlorpheniramine maleate is dissolved in a suitable solvent and added to the granulation process. The Paracetamol D90 used should have a particle size under 300 microns, preferably 200 microns. It is below, preferably below 150 microns. Microcrystalline cellulose and powdered cellulose are used as fillers in pharmaceutical tablet production. cellulose derivatives such as; lactose, sugar, sorbitol, dextrose, mannitol, dibasic calcium phosphate, 2 Starches such as tribasic calcium phosphate, calcium sulfate, calcium carbonate, and pregelatinized starch. The compounds include gelatin, acacia, alginic acid, sodium alginate, starch, and pregelatinized oil as binders. Natural polymers such as starch; synthetic polymers such as povidone and polyvinyl acetate; methyl cellulose, HPMC includes cellulose derivatives such as sodium carboxymethylcellulose and ethyl cellulose, as well as glucose and sucrose. carbohydrate derivatives; sugar alcohols such as sorbitol; starch as a dispersant, pregelatinized starch, microcrystalline cellulose, calcium carbonate, methyl cellulose, alginic acid, veegum, kaolin, bentonite, Cross-linked cellulose (croscarmellose) and cross-linked PVP (crospovidon) act as super-dispersants. Cross-linked starch (sodium starch glycolate), ion exchange resins; used as a lubricant. metallic stearates such as magnesium stearate, stearic acid, hydrogenated vegetable oils, sodium stearyl fatty acid esters such as fumarate, glyceryl behenate, and glyceryl palmitostearate, tribasic calcium, colloidal silicon dioxide, talc, calcium stearate, sodium acetate, sodium benzoate, glycol, Polyethylene glycol and silica can be used. Polyvinyl alcohol and ethyl cellulose can be used as film-forming agents. Hydroxypropyl cellulose and hydroxypropyl methylcellulose-based agents can be selected. The invention composition, produced by wet granulation, contains paracetamol and chlorpheniramine in its internal phase. Paracetamol granules containing maleate, a binder, and a diluent; ascorbic acid in the outer phase, Other diluents, binders, and dispersants are present. Preferably, povidone is used as a binder in the internal phase. Pregelatinized starch as a diluent; hydroxypropylcellulose as a binder in the outer phase, diluent. Microcrystalline cellulose is used as the base. The composition may contain at least one binder. The proportion of each binder in the composition. Preferably between 0.5-5% by weight. Povidone and / or hydroxypropyl alcohol are preferred as binders. May contain cellulose. Povidone as Povidone K-30, hydroxypropyl cellulose as Klusel Exf Farm. Trademarks may be used. The composition subject to the invention is used as a binder. Povidone is in the inner phase, and hydroxypropylcellulose is in the outer phase. The composition may contain at least one filler. The ratio of each filler in the composition... Preferably between 5-25% by weight. Preferably pregelatinized starch as a filler. and / or may contain microcrystalline cellulose. Microcrystalline cellulose should preferably be microcrystalline. Cellulose pH 102 can be used. The composition that is the subject of this invention is used as a filler. Pregelatinized starch is in the inner phase, and microcrystalline cellulose is in the outer phase. The composition may contain a dispersant. The dispersant ratio in the composition should preferably be 1-5% by weight. It is among them. It may preferably contain crospovidon as a dispersant. The composition may contain a lubricant. The proportion of lubricant in the composition should preferably be 1% by weight. It is among them. It may preferably contain magnesium stearate as a lubricant. The composition subject to this invention has a paracetamol content of at least 60% by weight (m / m). The composition subject to the invention contains ascorbic acid with a content between 24% and 30% (m / m) by weight. It could be 35. The amount of paracetamol in the composition subject to this invention may be between 300 and 650 mg. 3 The amount of ascorbic acid in the composition subject to this invention may be between 200 and 300 mg. The amount of chlorpheniramine maleate in the composition subject to this invention may be between 2 and 4 mg. The amount of Paracetamol / Chlorpheniramine maleate / Ascorbic Acid in the composition that is the subject of the invention. For example, it could be 650 / 4 / 300mg, 650 / 2 / 300mg, 325 / 2 / 150mg, 500 / 4 / 250mg, or 500 / 2 / 250mg. The composition subject to this invention uses povidone and hydroxypropylcellulose as binders. The ratio is typically 1:10 to 10:1 (a / a) by weight, preferably 1:5 to 5:1 (a / a), with 1:1 being the most preferred. When povidone and hydroxypropylcellulose are used as binders in the indicated ratio, the tablets Its disintegration and dissolution were found to be very good. Furthermore, the cap detachment event was distinctly evident. It has been observed that it has decreased. The subject matter of the invention is pregelatinized starch and microcrystalline protein used as diluents in the composition. Cellulose content should be 1:10 to 10:1 (w / w) by weight, preferably 1:5 to 5:1 (w / w), whichever is most preferred. It is 1:1. Pregelatinized starch, which has good flow and lubricity properties, is indicated by microcrystalline cellulose. When used together in these ratios, it has shown better compressibility in tablet production and more Good friability has been achieved. Specified with pregelatinized starch and microcrystalline cellulose. When used together in proportions, tablets have good storage properties. It has been observed. Specified ratios of binders and diluents in the inner and outer phases of the composition subject to the invention. Preparation with this method has been found to be more suitable in terms of production and stability. The composition that is the subject of the invention is used symptomatically in cases of colds and flu. available. Example Composition: STARTING POINTS Task % (a / a) Paracetamol (650mg) Active Ingredient Min 60.0% Ascorbic acid (300 mg) Active ingredient 24.0-30.0% Chlorpheniramine maleate (4 mg) Active ingredient 0.4-0.5 Povidone Binder 0.5-5.0 Hydroxypropylcellulose Binder 0.5-5.0 Pregelatinized starch filler 5.0-25.0 Microcrystalline cellulose PH102 Filler 5.0-25.0 Crospovidon Dispenser 0.5-5.0 Magnesium stearate lubricant 0.5-5.0 *Pure water Solvent - Total 100.00 *It evaporates during the process. 4 Another configuration of the invention is a film containing paracetamol, chlorpheniramine maleate, and ascorbic acid. It relates to the process of preparing coated tablet compositions. 1- Solution Preparation: Chlorpheniramine maleate is slowly added to pure water and stirred (Mechanically) Mixer). 2- Once chlorpheniramine maleate has dissolved, povidone is added to the mixture and stirring continues. (Mechanical Mixer) 3- Dry Mixture: Paracetamol and pregelatinized starch are mixed dry (Planetary Stirrer). 4- Wet Granulation: The prepared solution is slowly added to the dry mixture and mixed thoroughly. (Planetary Stirrer) 5- Pre-drying: The binder is dried in an oven at 50˚C. 6- Sieving: The sieving process is done using an 18 mesh (1000 µm) sieve. (Wet Granulator) 7- Drying: The binder is dried further in an oven at 50˚C. (Drying time depends on the moisture content.) adjustable.) 8- Final Mixture: Dry granulated, microcrystalline cellulose, crospovidon, ascorbic acid, Klucel Added and mixed. (Cube Mixer) 9- Finally, magnesium stearate is added and mixed. (Cube Mixer) 10- Tablet Printing: In the final mixture tablet printing machine, hardness, brittleness, and dispersion control are performed. It is printed by being processed. 11- Film Coating: The core tablets are coated with a film. The developed compositions are suitable in terms of dissolution, and the dissolution results are shown in Table 1. Given in section 1. (Pedal method, Rotation speed 100 rpm, Temperature 37°C) Table 1 - Dissolution Results Paracetamol, Ascorbic Acid, Chlorpheniramine Maleate Time (min) pH 1.2 medium, % water medium, % pH 1.2 medium, % 94.0 85.6 85.9 96.3 94.2 91.5 98.4 95.4 95.8 100.1 95.6 96.2 100.3 96.2 97.3 45 100.5 96.4 97.9 60 100.5 96.6 99.1

Claims

1. It is a tablet composition containing paracetamol, ascorbic acid and chlorpheniramine maleate, and its characteristic feature is... Paracetamol:ascorbic acid ratio should be between 1.5:1 and 2.5:1, with a minimum of 60% by weight. paracetamol, 24% to 30% ascorbic acid by weight, binder in a ratio of 1:10 to 10:1 by weight. (a / a) between povidone and hydroxypropyl cellulose, as fillers, 1:10 to 10:1 by weight. (a / a) contains pregelatinized starch and microcrystalline cellulose.

2. A composition according to claim 1, with a binding ratio of 1:5 to 5:1 (w / w) by weight. It contains povidone and hydroxypropyl cellulose.

3. A composition according to claim 1, characterized by having povidone as a binder in a 1:1 ratio by weight. and it contains hydroxypropyl cellulose.

4. A composition according to Claim 1, with a filler ratio of 1:5 to 5:1 (w / w) by weight. It contains pregelatinized starch and microcrystalline cellulose.

5. A composition according to claim 1, characterized by a filler material ratio of 1:1 (w / w) by weight. It contains a certain percentage of pregelatinized starch and microcrystalline cellulose.

6. A composition according to claim 1, characterized by having povidone as a binder in a 1:1 ratio by weight. and hydroxypropyl cellulose, pregelatinized starch as a filler in a 1:1 ratio by weight. It contains microcrystalline cellulose.

7. It is a composition according to any of the previous requirements, and its characteristic is distributive. It contains crospovidon.

8. It is a composition according to any of the previous requirements, and its feature is a slider. It contains magnesium stearate.

9. A composition according to any of the previous requests, and its characteristic is paracetamol D90. particle size below 300 microns, preferably below 200 microns, even more preferably 150 It means being below a micron.

10. A composition according to any of the previous requests, and its characteristic feature is paracetamol. The amount is 650 mg.

11. A composition according to any of the previous requirements, and its characteristic is ascorbic acid. The amount is 300 mg.

12. A composition according to any of the previous requirements, and its characteristic is chlorpheniramine. The maleate content is 4 mg.

12. A composition according to any of the previous requests, with a characteristic of 650mg It contains paracetamol, 4 mg chlorpheniramine maleate, and 300 mg ascorbic acid.

13. Previously used for symptomatic treatment of colds and flu. A composition for any of the requests. 35 6