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CN-111773191-B - Compound solid preparation containing phenylephrine hydrochloride and preparation method thereof

CN111773191BCN 111773191 BCN111773191 BCN 111773191BCN-111773191-B

Abstract

The invention relates to a compound solid preparation containing phenylephrine hydrochloride and a preparation method thereof, which is a solid preparation prepared by taking phenylephrine hydrochloride, antipyretic analgesic, acetaminophen and antihistamine chlorpheniramine maleate serving as alpha adrenergic receptor agonists as active ingredients and adding auxiliary materials such as a coating agent, an adhesive, a filler, a lubricant and the like. Because phenylephrine hydrochloride can be degraded in the presence of oxygen, aldehyde, certain acids and metals, the phenylephrine hydrochloride is coated by a coating agent, and is obtained by mixing and tabletting particles prepared from other raw materials after dry granulation.

Inventors

  • QU YUNZHI
  • Qu tiange
  • ZHANG YU
  • ZHAO XIA

Assignees

  • 北京博智绿洲医药科技有限公司
  • 北京博达绿洲医药科技研究有限公司

Dates

Publication Date
20260421
Application Date
20200708
Priority Date
20200708

Claims (7)

  1. 1. The compound solid preparation containing phenylephrine hydrochloride is characterized by comprising, by weight, 30-60% of acetaminophen, 0.2-0.5% of chlorpheniramine maleate, 0.2-0.6% of phenylephrine hydrochloride, 30-55% of filler, 5.3-10% of packaging agent, 2-10% of adhesive, 1-5% of antioxidant and 0.3-0.5% of lubricant; the wrapping agent is at least one of PEG4000 or PEG 6000; The antioxidant is vitamin C or sodium metabisulfite; the preparation method of the phenylephrine hydrochloride-containing compound solid preparation comprises the following steps: (1) Heating and melting the wrapping agent in the components at 55-70 ℃, adding phenylephrine hydrochloride in a stirring state, stirring uniformly, cooling, crushing, sieving, granulating by a dry method, and finishing to obtain granules 1 for later use; (2) Uniformly mixing acetaminophen, chlorpheniramine maleate, filler and antioxidant in the components, adding an adhesive to prepare a soft material, granulating, drying and finishing to obtain granules 2 for later use; (3) And (3) placing the particles 1 and the particles 2 into a mixer, adding a lubricant, uniformly mixing, and tabletting.
  2. 2. The compound solid preparation containing phenylephrine hydrochloride according to claim 1 is characterized by comprising the following components, by weight, 32.5% of acetaminophen, 0.2% of chlorpheniramine maleate, 0.5% of phenylephrine hydrochloride, 47% of filler, 8% of coating agent, 8% of adhesive, 3.5% of antioxidant and 0.3% of lubricant.
  3. 3. The compound solid preparation containing phenylephrine hydrochloride according to claim 1 is characterized by comprising the following components, by weight, 32.5% of acetaminophen, 0.4% of chlorpheniramine maleate, 0.4% of phenylephrine hydrochloride, 48% of filler, 7% of coating agent, 8% of adhesive, 3.3% of antioxidant and 0.4% of lubricant.
  4. 4. The compound solid preparation containing phenylephrine hydrochloride according to claim 1 is characterized by comprising the following components, by weight, 50.0% of acetaminophen, 0.2% of chlorpheniramine maleate, 0.2% of phenylephrine hydrochloride, 35% of filler, 5.3% of packaging agent, 6% of adhesive, 3% of antioxidant and 0.3% of lubricant.
  5. 5. The phenylephrine hydrochloride-containing compound solid preparation according to any one of claims 1-4, wherein the filler comprises, but is not limited to, lactose, sucrose, glucose or starch.
  6. 6. The phenylephrine hydrochloride-containing compound solid preparation according to any one of claims 1-4, wherein the binder comprises, but is not limited to, PVP or carboxymethyl cellulose, and when the binder is used, the binder is used after being soaked in cold water for 10-18 hours.
  7. 7. The phenylephrine hydrochloride-containing compound solid preparation according to any one of claims 1-4, wherein the lubricant comprises, but is not limited to, micro silica gel or talcum powder or magnesium stearate.

Description

Compound solid preparation containing phenylephrine hydrochloride and preparation method thereof Technical Field The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a compound solid preparation containing phenylephrine hydrochloride and a preparation method thereof. Background Phenylephrine hydrochloride is an alpha-adrenergic receptor agonist, has the effects of contracting blood vessels and increasing blood pressure, is a very strong vasoconstrictor, is used as a nasal decongestant and an electrocardio agent, can cause pulmonary vasoconstriction and subsequent pulmonary arterial pressure increase, and is often combined with antiallergic drugs, expectorants, antitussives, antipyretics and the like to treat symptoms such as fever, nasal obstruction, runny nose, cough, sneeze or headache and the like caused by cold. Acetaminophen, also known as paracetamol, is an in vivo metabolite of phenacetin, which regulates central prostaglandin synthase by inhibiting hypothalamic body temperature. Reduces synthesis and release of prostaglandin PGE1, bradykinin, histamine, etc. Is a antipyretic analgesic with antipyretic effect stronger than analgesic effect. Chlorpheniramine maleate, also known as chlorphenamine, is an antihistamine, which has antiallergic effect by antagonizing H1 receptor. Is mainly used for treating rhinitis, skin mucosa allergy and cold symptoms such as lacrimation, sneeze, watery nasal discharge and the like. The three medicines are combined to relieve symptoms such as fever, headache, cough, nasal obstruction and the like caused by cold. Disclosure of Invention Brief description of the invention: the invention relates to a compound solid preparation containing phenylephrine hydrochloride and a preparation method thereof, which is a solid preparation prepared by taking phenylephrine hydrochloride, antipyretic analgesic, acetaminophen and antihistamine chlorpheniramine maleate serving as alpha adrenergic receptor agonists as active ingredients and adding auxiliary materials such as a coating agent, an adhesive, a filler, a lubricant and the like. Because phenylephrine hydrochloride can be degraded in the presence of oxygen, aldehyde, certain acids and metals, the phenylephrine hydrochloride is coated by a coating agent, and is obtained by mixing and tabletting particles prepared from other raw materials after dry granulation. Detailed description of the invention: the tablet is prepared through two granulating processes, including the first coating phenylephrine hydrochloride with coating agent, crushing, dry granulating and pelletizing, the second crushing acetaminophen and chlorpheniramine maleate into fine powder, mixing with crushed stuffing, pelletizing with adhesive, drying, pelletizing, adding phenylephrine hydrochloride granule and lubricant, mixing and tabletting. In order to make phenylephrine hydrochloride more stable, the invention also adds an antioxidant. All weights herein are as indicated for the active pharmaceutical ingredient in the composition and the excipients required for tablet manufacture at 18-25 ℃. All percentages herein are by weight, and all percentages are based on the total composition, unless otherwise indicated. Various embodiments are disclosed in the examples of the present specification, all combinations of which are possible and preferred by those skilled in the art. The specific technical scheme for realizing the invention is as follows: The compound solid preparation containing phenylephrine hydrochloride and the preparation method thereof are characterized by comprising the following components in percentage by weight: 30-60% of acetaminophen, 0-0.5% of chlorpheniramine maleate, 0-0.6% of phenylephrine hydrochloride, 30-55% of filler, 0-10% of coating agent, 2-10% of adhesive, 1-5% of antioxidant and 0-0.5% of lubricant, The phenylephrine hydrochloride compound solid preparation and the preparation method thereof are characterized by comprising the following components in percentage by weight: 32.5 percent of parachlorophenol, 0.2 percent of chlorpheniramine maleate, 0.5 percent of phenylephrine hydrochloride, 47 percent of filler, 8 percent of coating agent, 8 percent of adhesive, 3.5 percent of antioxidant and 0.3 percent of lubricant, The phenylephrine hydrochloride compound solid preparation and the preparation method thereof are characterized by comprising the following components in percentage by weight: 32.5 percent of acetaminophen, 0.4 percent of chlorpheniramine maleate, 0.4 percent of phenylephrine hydrochloride, 48 percent of filler, 7 percent of coating agent, 8 percent of adhesive, 3.3 percent of antioxidant and 0.4 percent of lubricant, The phenylephrine hydrochloride compound solid preparation and the preparation method thereof are characterized by comprising the following components in percentage by weight: 50.0 percent of acetaminophen, 0.2 percent of chlorpheniramine maleate, 0.2 percent