Roxatidine acetate pharmaceutical salt drug-loading pellets and preparation method and applications thereof

Abstract

The invention relates to roxatidine acetate pharmaceutical drug-loading salt pellets. The pellets comprise a blank pellet core and a drug-loading layer, wherein a 95% or above ethanol aqueous solventor absolute ethyl alcohol by weight is taken as a drug-loading layer coating solvent, so that the defect of coating hardening in the preparation process of the roxatidine acetate pharmaceutical salt drug-loading pellets can be overcome, and in addition, the stability of active ingredients in the drug-loading pellets can be improved.

Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations. Specifically, the invention relates to a drug-loaded pellet of roxatidine acetate medicinal salt, a preparation method and application thereof. Background technique

[0002] Roxatidine aidcetate hydrochlore (ROX) is another H 2 A selective antagonist of the receptor, it can block the histamine H2 receptor of the parietal cell of the gastric mucosa to show continuous inhibition of gastric acid secretion, and also has mucosal protection. It is clinically suitable for the treatment of peptic ulcer disease and has moderate acid suppression ideal drug. Compared with proton pump inhibitors (PPI), roxatidine acetate hydrochloride has many clinical advantages: ① It acts on the histamine activation pathway, moderately inhibits gastric acid secretion, and has a definite preventive effect on stress ulcers in hospitalized patients , effectively prevent and treat stress ulcers, and its preventive ...

Examples

Embodiment 1

[0057] Example 1 Preparation of Roxatidine Hydrochloride Acetate-loaded Pellets

[0058] Sucrose core 65mg

[0059] Roxatidine Hydrochloride Acetate 75mg

[0060] Hydroxypropyl Cellulose-SL 3.75mg

[0061] Talc 15mg

[0062] 95% ethanol 656.25mg

[0063] Mechanically pulverize the raw material, weigh 95% ethanol in the prescribed amount, add hydroxypropyl cellulose-SL and the main ingredient under stirring, add talcum powder after stirring evenly, stir, sieve, and set aside. Use a fluidized bed granulation coating machine to spray the drug-loaded coating solution onto the blank pellet core. The fluidized bed coating conditions are: air intake air volume: 120-160m 3 / h, air inlet temperature: 30-50°C, atomization pressure 1.6-2.2kg / cm 2 . During the coating process, the coating pellets were cohesive and hardened, and the coating could not be completed and the theoretical weight gain could not be achieved.

Embodiment 2

[0064] Example 2 Preparation of Roxatidine Hydrochloride Acetate-loaded Pellets

[0065] Sucrose core 65mg

[0066] Roxatidine Hydrochloride Acetate 75mg

[0067] Hydroxypropyl Cellulose-SL 3.75mg

[0068] Talc 15mg

[0069] Absolute ethanol 656.25mg

[0070] Mechanically pulverize the raw materials, weigh the prescribed amount of absolute ethanol, add hydroxypropyl cellulose-SL under stirring, stir until dissolved, add the main ingredient, stir evenly, then add talcum powder, stir evenly, sieve, and set aside . Spray the drug-loaded coating solution onto the blank pellet core with a fluidized bed granulator, dry and sieve to obtain the drug-loaded pellets. The coating conditions are the same as in Example 1, the absolute ethanol is chemically pure or above, and the weight fraction of ethanol alcohol is greater than 99.5%.

Embodiment 3

[0071] Example 3 Roxatidine Hydrochloride Acetate Loaded Pellets

[0072] Sucrose core 65mg

[0073] Roxatidine Hydrochloride Acetate 75mg

[0074] Hydroxypropyl Cellulose-L 3.75mg

[0075] Talc 15mg

[0076] Absolute ethanol 656.25mg

[0077] Mechanically pulverize the raw materials, weigh the prescribed amount of absolute ethanol, add hydroxypropyl cellulose-L while stirring, stir until dissolved, add the main ingredient, stir evenly, then add talcum powder, stir evenly, sieve, and set aside . Using a fluidized bed granulation coating machine, using the same conditions as in Example 2, the drug-loaded coating solution was sprayed onto the blank core, dried and sieved to obtain drug-loaded pellets.

technical field

[0001] The invention belongs to the field of pharmaceutical preparations. Specifically, the invention relates to a drug-loaded pellet of roxatidine acetate medicinal salt, a preparation method and application thereof. Background technique

[0002] Roxatidine aidcetate hydrochlore (ROX) is another H 2 A selective antagonist of the receptor, it can block the histamine H2 receptor of the parietal cell of the gastric mucosa to show continuous inhibition of gastric acid secretion, and also has mucosal protection. It is clinically suitable for the treatment of peptic ulcer disease and has moderate acid suppression ideal drug. Compared with proton pump inhibitors (PPI), roxatidine acetate hydrochloride has many clinical advantages: ① It acts on the histamine activation pathway, moderately inhibits gastric acid secretion, and has a definite preventive effect on stress ulcers in hospitalized patients , effectively prevent and treat stress ulcers, and its preventive ...

Examples

Embodiment 1

[0057] Example 1 Preparation of Roxatidine Hydrochloride Acetate-loaded Pellets

[0058] Sucrose core 65mg

[0059] Roxatidine Hydrochloride Acetate 75mg

[0060] Hydroxypropyl Cellulose-SL 3.75mg

[0061] Talc 15mg

[0062] 95% ethanol 656.25mg

[0063] Mechanically pulverize the raw material, weigh 95% ethanol in the prescribed amount, add hydroxypropyl cellulose-SL and the main ingredient under stirring, add talcum powder after stirring evenly, stir, sieve, and set aside. Use a fluidized bed granulation coating machine to spray the drug-loaded coating solution onto the blank pellet core. The fluidized bed coating conditions are: air intake air volume: 120-160m 3 / h, air inlet temperature: 30-50°C, atomization pressure 1.6-2.2kg / cm 2 . During the coating process, the coating pellets were cohesive and hardened, and the coating could not be completed and the theoretical weight gain could not be achieved.

Embodiment 2

[0064] Example 2 Preparation of Roxatidine Hydrochloride Acetate-loaded Pellets

[0065] Sucrose core 65mg

[0066] Roxatidine Hydrochloride Acetate 75mg

[0067] Hydroxypropyl Cellulose-SL 3.75mg

[0068] Talc 15mg

[0069] Absolute ethanol 656.25mg

[0070] Mechanically pulverize the raw materials, weigh the prescribed amount of absolute ethanol, add hydroxypropyl cellulose-SL under stirring, stir until dissolved, add the main ingredient, stir evenly, then add talcum powder, stir evenly, sieve, and set aside . Spray the drug-loaded coating solution onto the blank pellet core with a fluidized bed granulator, dry and sieve to obtain the drug-loaded pellets. The coating conditions are the same as in Example 1, the absolute ethanol is chemically pure or above, and the weight fraction of ethanol alcohol is greater than 99.5%.

Embodiment 3

[0071] Example 3 Roxatidine Hydrochloride Acetate Loaded Pellets

[0072] Sucrose core 65mg

[0073] Roxatidine Hydrochloride Acetate 75mg

[0074] Hydroxypropyl Cellulose-L 3.75mg

[0075] Talc 15mg

[0076] Absolute ethanol 656.25mg

[0077] Mechanically pulverize the raw materials, weigh the prescribed amount of absolute ethanol, add hydroxypropyl cellulose-L while stirring, stir until dissolved, add the main ingredient, stir evenly, then add talcum powder, stir evenly, sieve, and set aside . Using a fluidized bed granulation coating machine, using the same conditions as in Example 2, the drug-loaded coating solution was sprayed onto the blank core, dried and sieved to obtain drug-loaded pellets.

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