CN-116473942-B - Loratadine sustained-release capsule and preparation method thereof

Abstract

The application belongs to the technical field of pharmaceutical oral solid preparations, relates to a loratadine sustained-release capsule and a preparation method thereof, provides a loratadine sustained-release capsule, wherein the loratadine, the citric acid and the salicylic acid are mixed in a melting way to prepare the pill-containing core, and the pill core is coated with a slow release layer, a quick release layer and a protective layer. Not only can effectively solve the problem of slow dissolution rate of loratadine under the condition of gastric acid deficiency of human body, but also can uniformly release the medicine, and can achieve the purposes of long-acting and increasing curative effect.

Inventors

• LI YONGXUAN
• DENG WENLEI

Assignees

• 山东新时代药业有限公司

Dates

Publication Date

20260505

Application Date

20220113

Claims (6)

1. 1. The loratadine sustained-release capsule is characterized by comprising, by weight, 70 parts of loratadine, 30-45 parts of salicylic acid, 30-45 parts of citric acid or malic acid, 400-500 parts of microcrystalline cellulose or mannitol, 20-35 parts of copovidone and 1200-1600 parts of water, wherein the sustained-release capsule comprises, by weight, 10-20 parts of gastric-soluble film-forming material ethyl cellulose, 180-280 parts of 95% ethanol, 10-20 parts of purified water and 5-20 parts of talcum powder, the quick-release layer comprises, by weight, 30 parts of loratadine, 35-50 parts of povidone k30 or copovidone, 50-70 parts of polyethylene glycol, 100-200 parts of 95% ethanol and 100-200 parts of purified water, and the protective layer comprises gastric-soluble film-forming material hydroxypropyl methyl cellulose solution.
2. 2. The loratadine sustained-release capsule according to claim 1, wherein the protective coating of the sustained-release capsule comprises the following components in parts by weight: 10-20 parts of hydroxypropyl methyl cellulose 50-100 Parts of purified water.
3. 3. A method for preparing the loratadine sustained-release capsule according to claim 1, characterized in that the method comprises the steps of; (1) The preparation process of the pill-containing core comprises the steps of preparing a soft material, extruding, rounding, drying by a fluidized bed and screening; (2) Coating the pill-containing cores by a fluidized bed coating machine through a slow release layer, a quick release layer and a protective layer; (3) And filling the capsule, namely filling the obtained loratadine sustained-release pellets into a gelatin capsule shell.
4. 4. The method for preparing the loratadine sustained-release capsule according to claim 3, wherein the loratadine sustained-release capsule is prepared by the following steps: Preparing a pill core, namely heating loratadine, citric acid and salicylic acid to be molten, adding microcrystalline cellulose, copovidone aqueous solution and purified water to prepare a soft material, using a wet granulator, and adding the purified water; Extrusion rounding, namely extrusion rounding comprises two steps of extrusion and rounding, wherein soft materials are extruded through sieve holes in the extrusion step to form compact strips, the saw tooth chassis in the rounding step shreds the extruded strips, and the shredded particles are rounded by centrifugal action; Drying by fluidized bed drying, controlling water content not to exceed 4%; Sieving to obtain micropill, sieving with 20-30 mesh sieve, collecting the sieved micropill, and coating.
5. 5. The method for preparing the loratadine sustained-release capsule according to claim 3, wherein the sustained-release layer is prepared by mixing ethyl cellulose, 95% ethanol and purified water in proportion, coating is carried out on dried pellets, the air inlet volume is set to 40-60m 3 /h, the air inlet temperature is set to 40-60 ℃, the atomization pressure is set to 200-300kPa, the material temperature is set to 30-40 ℃, talcum powder is added as an anti-adhesion agent, the quick-release layer is prepared by dissolving loratadine and copovidone in 95% ethanol, meanwhile polyethylene glycol is dissolved in water, then the two solutions are mixed to obtain a quick-release layer drug-containing coating liquid, the air inlet volume is set to 40-60m 3 /h, the air inlet temperature is set to 40-60 ℃, the atomization pressure is set to 300-400kPa, and the material temperature is set to 30-40 ℃, the protective layer is prepared by stirring and dispersing the hydroxypropyl methyl cellulose with hot water, and then adding cold water for stirring and cooling, and the air inlet volume is set to 40-60m 3 /h, the air inlet temperature is set to 40-60 kPa, and the material temperature is set to 30-40 ℃ when the material temperature is set.
6. 6. The method for preparing the loratadine sustained-release capsule according to claim 3, wherein the step (3) is as follows: and filling capsules, namely filling the obtained loratadine sustained-release pellets into gelatin capsule shells, wherein each capsule contains 10mg of loratadine.

Description

Loratadine sustained-release capsule and preparation method thereof Technical Field The invention belongs to the technical field of pharmaceutical oral solid preparations, and in particular relates to a loratadine sustained-release capsule and a preparation method thereof. Background Allergy is also known as anaphylaxis and modern medicine refers to this reaction as an antigen-antibody reaction. About 10% -45% of the general population in the world have allergic diseases, and the incidence rate is increasing, about 2 hundred million people in China have allergic diseases, the world and health organization has classified the allergic diseases as diseases which are mainly researched and prevented in the 21 st century, along with the change of the living environment of human beings, the incidence rate of allergic diseases is increasing, allergic population in China is increasing, especially the rising curve change of the allergic population in seasons is obvious, the prevention and the treatment of allergic diseases become an unprecedented task, and the development potential of the antiallergic medicine market is huge. Loratadine is a zwitterionic feature in the molecular structure of the second generation antihistamine drug, so that the loratadine has no obvious central inhibition effect, and is clinically used for preventing and treating diseases such as allergic rhinitis, chronic idiopathic urticaria, allergic asthma, atopic dermatitis and the like. The FDA publication in the United states shows that preparation of loratadine tablets, orally disintegrating tablets, and the like, all employ micronized raw materials. The drug micronization can obviously improve the dissolution rate of the preparation, but the micronization also has the defects that the drug powder is easy to reagglomerate, the raw materials and the auxiliary materials are difficult to mix uniformly, and the like. Loratadine is a water-insoluble substance that has the solubility characteristics of being soluble in strong acid solutions and almost insoluble in weak acid solutions or water. Currently, the quality standard of loratadine tablet is only measured on the dissolution rate of loratadine tablet in a strong hydrochloric acid solution (ph=2), in fact, the dissolution rate of loratadine tablet in the market is high in the environment, but the dissolution rate of loratadine tablet in the environment is low in the weak acid environment and the neutral environment, and the release of loratadine tablet in the stomach is influenced by the rise of pH when the conventional loratadine tablet is taken, and the release rate of loratadine tablet in the intestinal tract is lower when the medicament is taken, so that the clinical effect of loratadine tablet is influenced. Aiming at the problem, the invention adopts the melt combination of the loratadine, the citric acid and the salicylic acid to prepare the pill-containing core by extrusion and spheronization, then uses a fluidized bed coating machine to coat a slow release layer, a quick release layer and a protective layer, and finally fills the loratadine slow release capsule into the capsule. The preparation of a proper acidic environment for the dissolution and the dissolution of the loratadine can obviously optimize the high pH dissolution performance of the loratadine and better adapt to the requirements of patients with gastric acid deficiency. Disclosure of Invention The invention aims to overcome the defects and shortcomings of the prior art and provide the loratadine sustained-release capsule which has the advantages of lasting effect, less administration times, stable blood concentration and higher safety. The prior art adopts wet granulation, extrusion spheronization and fluidized bed coating processes for production, and has complex process flow and higher control requirement. The invention provides a loratadine sustained-release capsule which consists of sustained-release pellets and hollow capsules, wherein the preparation process of the sustained-release pellets comprises a pellet-containing core, a sustained-release layer, a quick-release layer and a protective layer. The sustained-release pellet consists of 70-75% of pill-containing core, 5-10% of sustained-release coating layer, 10-15% of quick-release coating layer and protective layer according to weight percentage. The loratadine sustained-release capsule, wherein the pellet-containing core ensures acceptable formability, roundness, friability and the like of the granules, and optional auxiliary materials comprise microcrystalline cellulose, starch, mannitol, sucrose, silicon dioxide or a combination thereof, preferably mannitol, microcrystalline cellulose, silicon dioxide or a combination thereof, and finally preferably microcrystalline cellulose, and the prepared granules have high roundness and low friability because of good formability. The invention particularly adopts a method of combining loratadine with citric acid and sa