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Sitafloxacin sustained-release pellet and preparation method thereof

A technology of sitafloxacin and sustained-release pellets, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., to achieve the effects of reducing irritation and improving drug bioavailability

Active Publication Date: 2009-08-05
CHONGQING LUMMY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The clinical treatment of common preparations of sitafloxacin needs to be taken more than 2 times a day. In order to reduce the number of doses and maintain a stable blood drug concentration, it is suitable to prepare sitafloxacin preparations into sustained-release dosage forms. Sustained-release preparation report

Method used

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  • Sitafloxacin sustained-release pellet and preparation method thereof
  • Sitafloxacin sustained-release pellet and preparation method thereof
  • Sitafloxacin sustained-release pellet and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Example 1 Preparation of sitafloxacin sustained-release pellets

[0045] Raw materials: sitafloxacin, starch, dextrin, ethyl cellulose aqueous solution, povidone, diethyl phthalate, titanium dioxide and ethanol;

[0046] Preparation process: mix starch and dextrin evenly according to the weight ratio of 3:1, use 50% ethanol as wetting agent to make soft material, put the soft material in the coating pot and roll the ball core, take 20-40 mesh The core of the ball is set aside.

[0047] Put the spare blank pellet core in the fluidized bed, spray the sitafloxacin aqueous solution, and dry it. After the pellet core increases in weight to 100%, wrap an ethylcellulose film coating on the surface of the pellet to increase the weight by 5%. , to obtain sitafloxacin sustained-release pellets, and to pack the pellets into capsules to obtain sitafloxacin sustained-release pellets.

Embodiment 2

[0049] Raw materials: sitafloxacin, microcrystalline cellulose, dextrin, acrylic resin, 50% ethanol solution, polyethylene glycol 6000, castor oil, polysorbate and titanium dioxide;

[0050] Preparation process: take sitafloxacin, microcrystalline cellulose, and dextrin, mix them evenly according to the weight ratio of 7:2:1, use 50% ethanol liquid to make soft materials, extrude and granulate, and put the prepared granules into Put into the ball rolling machine and make micropills, choose the micropills between 20-30 meshes, wrap the film coating with the coating solution containing acrylic resin, make the pills increase by 5%, and obtain the sitafloxacin sustained-release micropills , the above-mentioned micropills are packed into capsules to obtain the sitafloxacin sustained-release micropill capsules.

Embodiment 3

[0052] Raw materials: sitafloxacin, lactose, dextrin, 50% ethanol solution and 10% Surelease solution;

[0053] Take sitafloxacin, lactose, and dextrin, mix them evenly according to the weight ratio of 4:2:1, use 50% ethanol solution to make soft materials, and extrude the soft materials through the sieve plate of the extruder to prepare granules, and spheronize the granules Machine spheronization, screen out 14-20 mesh pellets for subsequent use, then use 10% Surelease coating solution to coat the pellets with a film coating, and increase the weight of the pellets by 7% to obtain the sitafloxacin sustained-release pellets. Take the sustained-release pellets and fill them in capsules to obtain sitafloxacin sustained-release pellets capsules.

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PUM

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Abstract

The invention discloses a slow-release micropill of sitafloxacin, which comprises a slow-release drug-containing micropill, wherein the slow-release drug-containing micropill consists of a pill core of sitafloxacin and a slow-release coating layer; the pill core of sitafluoacin is coated with the slow-release coating layer; and the weight of the slow-release coating layer is 2 to 100 percent thatof the pill core of sitafloxacin. According to different coating materials and coating thicknesses, the slow-release micropill of sitafloxacin can be prepared into the micropills with different release curves, and according to clinical need, the preparation unit finally formed is added with one or more of the micropills with different release curves so as to achieve the best clinical effect.

Description

technical field [0001] The invention relates to a sitafloxacin sustained-release pellet and a preparation method thereof. Background technique [0002] Sitafloxacin (Sitafloxacin) is a new type of oral quinolone antibiotics. The Japanese Ministry of Health and Welfare approved the broad-spectrum antibiotic sitafloxacin hydrate 50mg tablet and 10% fine granule (sitafloxacin hydrate) of Daiichi Sankyo Co., Ltd. , commercial Gracevit) marketed for severe and bacterial infections caused by drug-resistant bacteria. For most Gram-negative bacteria among more than 5,000 clinically isolated strains, sitafloxacin is more active than ciprofloxacin and ofloxacin; against Streptococcus pneumoniae, drug-resistant Staphylococcus aureus, Coccus, Enterococcus faecalis, Pseudomonas, etc. are more active than sparfloxacin, fleroxacin and ofloxacin; sitafloxacin is the compound with the strongest activity against Enterobacteriaceae. For the other tested strains, the activity of sitafloxacin ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/22A61K9/52A61K31/4709A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44A61P31/04A61K47/10A61K47/26
Inventor 安林
Owner CHONGQING LUMMY PHARMA
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