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CN-121987578-A - Toovilin citrate tablet and preparation method thereof

CN121987578ACN 121987578 ACN121987578 ACN 121987578ACN-121987578-A

Abstract

The invention discloses a citric acid pentovirine tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The citric acid pentofibrin tablet consists of citric acid pentofibrin, a filling agent, a disintegrating agent, an adhesive, a lubricant, a stabilizer, a light shielding agent and a wetting agent, and a compound stabilizer system consisting of sodium metabisulfite, pinoresinol diglucoside and glycine is adopted, and the components are synergistic, so that the influence of environmental factors such as light, heat, humidity and the like can be resisted pertinently. The tablet prepared by the invention has the advantages of remarkably improved stability, less degradation of active ingredients, excellent and balanced physical properties, mechanical stability and bioavailability, scientific and controllable preparation process, strong repeatability, suitability for industrial production and important clinical application value and market prospect.

Inventors

  • LIU YAFANG
  • YE WEI

Assignees

  • 常州市武进人民医院(常州市第八人民医院)

Dates

Publication Date
20260508
Application Date
20260225

Claims (10)

  1. 1. The citric acid pentofibrin tablet is characterized by comprising 25 parts by weight of citric acid pentofibrin, 150-200 parts by weight of filler, 6-10 parts by weight of disintegrating agent, 3-5 parts by weight of adhesive, 0.5-2.5 parts by weight of lubricant, 0.9-2.3 parts by weight of stabilizer, 1-3 parts by weight of opacifier and a proper amount of wetting agent, wherein the stabilizer is a combination of sodium metabisulfite, pinoresinol diglucoside and glycine.
  2. 2. The pentovirine citrate tablet according to claim 1, wherein the filler is at least one selected from lactose, microcrystalline cellulose, starch, mannitol, dextrin, sucrose.
  3. 3. The pentovirine citrate tablet according to claim 1, wherein the disintegrant is at least one selected from crospovidone, croscarmellose sodium, sodium carboxymethyl starch, low substituted hydroxypropyl cellulose.
  4. 4. The pentovirine citrate tablet according to claim 1, wherein the binder is at least one selected from povidone K30, hydroxypropyl cellulose, sodium carboxymethyl cellulose, polyethylene glycol.
  5. 5. The pentovirine citrate tablet according to claim 1, wherein the lubricant is at least one selected from magnesium stearate, calcium stearate, talc, and micro silica gel.
  6. 6. The pentovirine citrate tablet according to claim 1, wherein the opacifier is titanium dioxide and/or zinc oxide.
  7. 7. The spray-on tablet of claim 1, wherein the wetting agent is purified water.
  8. 8. The pentovirine citrate tablet of claim 1, wherein the stabilizer is 0.3-0.8 parts by weight of sodium metabisulfite, 0.1-0.3 parts by weight of pinoresinol diglucoside, and 0.5-1.2 parts by weight of glycine.
  9. 9. A method for preparing the pentovirine citrate tablet of claim 1, wherein the method comprises the following steps: 1) Pretreating stabilizer by dissolving glycine in purified water, adding pinoresinol diglucoside ethanol dispersion, adding sodium metabisulfite aqueous solution with pH=4.0-4.5, stirring in dark, vacuum freeze drying, pulverizing, and sieving to obtain stabilizer pretreated micropowder; (2) Pretreating and mixing adjuvants, namely taking the citric acid pentofibrin, the filler, the disintegrating agent and the opacifier, pulverizing, sieving, and mixing with the stabilizer pretreated micropowder; (3) Granulating, namely preparing an aqueous solution of an adhesive with the mass fraction of 5% -8%, spraying the aqueous solution to the dry-mixed material, preparing a soft material, and sieving to obtain wet granules; (4) Drying and granulating; (5) Mixing and tabletting, namely adding a lubricant into the granules after finishing, mixing and tabletting to obtain the citric acid pentofavine Lin Pianji.
  10. 10. The preparation method of the stabilizer comprises the steps of (1) pretreating pinoresinol diglucoside, adding 5-8 times of absolute ethyl alcohol to disperse to obtain pinoresinol diglucoside ethanol dispersion for later use, adding 3-5 times of purified water at 40-45 ℃ to obtain glycine, stirring and dissolving, slowly adding the dispersion, stirring and mixing to obtain mixed dispersion, adding 2-3 times of purified water to obtain sodium metabisulfite, rapidly stirring and dissolving, adding sodium dihydrogen citrate to adjust the pH value to 4.0-4.5, slowly injecting the solution into the mixed dispersion, stirring for 25-35 minutes in a dark place, obtaining stabilizer composite liquid, placing the stabilizer composite liquid in a vacuum freeze dryer, pre-freezing to below-40 ℃, preserving heat for 2 hours, heating to-10 ℃ to obtain dry antioxidant material, heating to 25 ℃ to obtain dry antioxidant material, grinding the dry material, sieving the dry material with a 120-mesh sieve, and obtaining the stabilizer composite micro powder.

Description

Toovilin citrate tablet and preparation method thereof Technical Field The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a citric acid pentovirine tablet and a preparation method thereof. Background The disclosure of this background section is only intended to increase the understanding of the general background of the invention and is not necessarily to be construed as an admission or any form of suggestion that this information forms the prior art already known to those of ordinary skill in the art. The pentovirine citrate is a classical non-addictive antitussive drug and has dual antitussive action mechanisms of central nature and peripheral nature. The cough relieving effect intensity is about 1/3 of that of codeine, and the cough relieving effect is superior to that of adults by directly inhibiting the medullary respiratory center to block cough reflex, meanwhile, the cough relieving effect has a slight atropine-like effect, can relax the bronchosmooth muscle of spasms, reduce airway resistance, is suitable for dry cough caused by various reasons, including dry cough without phlegm, pertussis and the like caused by upper respiratory tract infection, and has better curative effect on children than adults. Compared with the addictive antitussive such as codeine, the citric acid pentovirine has higher safety, no addiction, slight adverse reaction, and occasionally reactions such as constipation, slight headache, dizziness, somnolence, dry mouth, nausea, abdominal distention, skin allergy and the like, and can be widely applied clinically. Currently, commercial dosage forms of pentovirine citrate mainly include syrups and tablets. The syrup is one of the mainstream dosage forms because of convenient administration, but has obvious quality defects that in a syrup system, the medicament is easy to precipitate due to the change of the solution environment, and in addition, the syrup has the problem of inaccurate metering in the use process, thereby affecting the accuracy and clinical curative effect of the medicament dosage, easily generating the solution bacteria-staining phenomenon, and seriously affecting the use experience of consumers and the stability of products. In order to solve the defects of the syrup, the tablet is gradually the key point of research and development due to the advantages of accurate dosage, convenient carrying, stable storage and the like. Chinese patent publication No. CN116492307a discloses a tablet of pentovine citrate and a preparation method thereof, wherein talcum powder is mixed with the raw material of pentovine citrate in advance, and a coating powder film is formed on the raw material of pentovine citrate Lin Waiceng, so that the raw material of pentovine citrate is prevented from directly contacting with a tabletting punch die, and further the problem of sticking and punching in the punching process is solved. The Chinese patent publication No. CN112315931A discloses a citric acid pentovirine tablet and a preparation method thereof, wherein the tablet core is prepared from the following components, by mass, 0.5-2 parts of citric acid pentovirine, 1-5 parts of a filling agent, 0.1-1 part of an adhesive and 0.1-1 part of a lubricant, and a coating layer is prepared from a gastric-soluble film coating premix, wherein the weight of the coating layer is 3% -5% of the weight of the tablet core. However, aiming at the core problems of stability such as degradation of storage period, increase of related substances, content reduction and the like caused by citric acid spray-on-vitamin Lin Duiguang and heat and humidity sensitivity, an effective solution is not formed, and the prolongation of the effective period of the product and the further improvement of the safety and reliability of clinical application are still restricted. Therefore, the citric acid pentovirine tablet which can give consideration to the feasibility of the preparation process and the long-term stability of the product, has controllable quality and stable curative effect and the preparation method thereof have important clinical application value and market prospect, and are also the core research and development starting point of the invention. Disclosure of Invention In order to overcome the technical defects that the citric acid pentovirine tablet is sensitive to light, heat and humidity, so that the effective components are degraded and the content is reduced in the storage period and the physical properties of part of the preparation are poor in the prior art, the invention provides the citric acid pentovirine tablet with long-term stability and excellent physical properties and a preparation method thereof, and the specific technical scheme is as follows: The citric acid pentovirine tablet adopts the component combination with accurate proportion, and the components have synergistic effect, so that the preparation formability is ensured, the stabil