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CN-121971631-A - Taste masking composition and preparation method thereof

CN121971631ACN 121971631 ACN121971631 ACN 121971631ACN-121971631-A

Abstract

The invention discloses a taste masking composition and a preparation method thereof. The composition comprises a pharmaceutically active ingredient and pregelatinized starch, wherein the pregelatinized starch is used as a taste masking agent. The invention also provides a specific suspension drying process. The invention covers the peculiar smell of indissolvable bitter drugs such as letrozole and the like obviously, does not influence the release rate of the drugs, and has the dissolution behavior consistent with that of the original development agent. The composition has the advantages of good quality, good taste, easy administration for patients with dysphagia such as children and old people, and convenient personalized dosage adjustment, thereby improving the compliance of patients and the accuracy of dosage, and the preparation process is simple and feasible, has good reproducibility and is suitable for industrial production.

Inventors

  • ZENG FANXIN
  • XU CHEN
  • ZENG XIANG
  • DENG BOWEN
  • WEN JIALI
  • NIE JIN

Assignees

  • 吉林福剂医药有限公司

Dates

Publication Date
20260505
Application Date
20260227

Claims (11)

  1. 1. A taste masking composition, characterized in that the composition comprises a pharmaceutically active ingredient and pregelatinized starch.
  2. 2. The taste masking composition according to claim 1, wherein the mass ratio of the pharmaceutically active ingredient to the pregelatinized starch is 1:2-1:5.
  3. 3. Taste masking composition according to claim 1 or 2, characterized in that the taste masking composition is prepared by suspending the pharmaceutically active ingredient and the pregelatinized starch in a solvent and drying.
  4. 4. A taste masking composition according to any one of claims 1-3, wherein the pharmaceutically active ingredient is a poorly soluble bitter drug, preferably the pharmaceutically active ingredient is selected from one or more of azithromycin, wu Pati, roxithromycin, of letromycin Mo Wei.
  5. 5. A taste masking composition according to any one of claims 1-4, comprising the following components in mass percent: 1% -15% of a pharmaceutical active ingredient; 2% -50% of pregelatinized starch; 5% -60% of filler; 0.1-5% of suspending agent.
  6. 6. The taste masking composition according to claim 5, wherein the filler is one or more selected from mannitol, sorbitol, lactose, and xylitol, and the suspending agent is one or more selected from xanthan gum, guar gum, acacia gum, hypromellose, hydroxypropyl cellulose, povidone, sodium carboxymethyl cellulose, and dispersible cellulose.
  7. 7. The taste masking composition according to claim 5, further comprising 0.1-10% of a sweetener, 0.1-5% of a flavoring agent, wherein the sweetener is one or more of sucralose, stevioside, sucrose and aspartame, and the flavoring agent is one or more of orange essence, strawberry essence, peppermint essence and banana essence.
  8. 8. The taste masking composition according to any one of claims 1 to 7, wherein the composition is in the form of a dry suspension, dispersible tablet, orally disintegrating tablet or powder.
  9. 9. A method of preparing a taste masking composition according to any one of claims 1 to 8, comprising the steps of: (1) Adding pregelatinized starch into a matrix solvent, and uniformly stirring; (2) Adding the active ingredients, stirring, mixing, grinding, dispersing or homogenizing to obtain suspension; (3) Drying the suspension to form a solid, and pulverizing; (4) And (3) uniformly mixing the product obtained in the step (3) with other auxiliary materials and/or preparation solvents.
  10. 10. The preparation method of claim 9, wherein the matrix solvent in the step (1) is water and an organic solvent, the organic solvent comprises at least one of ethanol, acetonitrile, acetone, 2-propanol and dimethylacetamide, and the volume concentration of the organic solvent in the solvent is not higher than 40%, preferably an ethanol aqueous solution with a volume concentration of 1-30%.
  11. 11. The method according to claim 9, wherein the drying in step (3) is selected from rotary evaporation drying, fluidized bed drying or spray drying, and the drying temperature is 40-70 ℃, preferably 50-60 ℃.

Description

Taste masking composition and preparation method thereof Technical Field The invention belongs to the field of pharmaceutical preparations, and relates to a taste masking composition and a preparation method thereof. Background Drug palatability (taste, smell, dosage form and the like) is a core influencing factor of children medication, and medication compliance and treatment effect are directly determined. Children have far higher taste sensitivity than adults, have extremely low tolerance to bitter taste and peculiar smell of the medicine, have poor palatability, are easy to cause refusal to take, spit medicine and miss taking, lead the concentration of the medicine in the body to be unable to reach the standard, prolong the course of disease if light and induce the medicine resistance if heavy. The medicines such as azithromycin, letrozole and Wu Pati are common medicines in clinical treatment of children, but have obvious bitter taste, so that the medicines become a big pain point for children to take medicines. The poor taste of the medicine is very easy to cause the child to resist and cry, the medicine feeding difficulty of parents is greatly increased, even the situations of choking, vomiting and the like caused by forced feeding occur, the medicine feeding experience is affected, the medicine feeding dosage is more easily insufficient, the medicine curative effect is directly weakened, and the recovery of illness state is delayed. Meanwhile, repeated medication resistance can also lead children to psychological fear, reduce medication compliance of other subsequent treatments and form vicious circle. Therefore, the improved taste of the bitter drugs is an urgent need for improving the medication compliance of children and guaranteeing the clinical treatment effect. The common technology in the existing preparation taste masking technology has own limitations. For example, the coating of the pellets has the defects of uneven thickness of the coating layer, easy rupture of the membrane and taste leakage, large influence of pH of gastrointestinal fluid on the coating material, possibility of delayed drug dissolution, complex process, high equipment requirement and high production cost. Taste masking of the flavoring agent mixture has limited effect on strongly bitter drugs, and excessive flavoring agent may affect drug stability and dissolution behavior. Other taste masking technologies such as cyclodextrin inclusion masking, cyclodextrin auxiliary materials are high in cost, inclusion rate is easy to be interfered by temperature and concentration, ion exchange resin is used for masking the taste, the binding force between the resin and the medicine is unstable, the medicine release is easy to be delayed, and the standard reaching efficiency of the blood concentration is easy to be influenced. Therefore, research on a taste masking composition which is easy to administer, good in taste, easy to obtain auxiliary materials and low in material and production cost is a problem which needs to be solved in the field. Disclosure of Invention Aiming at the defects of the prior art, particularly the problems of obvious bitter taste of bitter drugs and difficulty in meeting the medicine taking requirements of dysphagia patients such as pediatrics or geriatrics, the invention provides a taste masking composition which is easy to administer, good in taste, easy to obtain auxiliary materials and low in material and production cost. A taste masking composition, characterized in that the composition comprises a pharmaceutically active ingredient and pregelatinized starch. Preferably, the mass ratio of the active pharmaceutical ingredient to the pregelatinized starch is 1:2-1:5. Preferably, the taste masking composition described above is prepared by suspending the pharmaceutically active ingredient and the pregelatinized starch in a solvent and drying. Further, the pharmaceutical active ingredient is a poorly soluble bitter drug. For example, the active ingredient is selected from one or more of azithromycin, wu Pati, roxithromycin from lett Mo Wei. The invention is particularly applicable to letromycin. The invention discovers that the strong bitter taste of the raw material medicine cannot be effectively covered by simply mixing or conventional granulating the flavoring agent with the medicines such as azithromycin, wu Pati Ni, letrozole and the like with obvious bitter taste. The invention creatively combines bitter drugs and pregelatinized starch into a taste-masking layer. In the field of pharmaceutical formulations, pregelatinized starch is generally used as filler, disintegrant or binder. The invention creatively finds that pregelatinized starch can be used as a taste masking agent of bitter drugs, and is particularly suitable for insoluble drugs. The pregelatinized starch can form a physical barrier for the poorly soluble bitter drug, blocking bitter substances from contacting with taste buds, and reducing