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Levofloxacin slow release micropill, its preparation method and uses

A technology of levofloxacin and sustained-release pellets, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, and bulk delivery, etc., and can solve the problems of increased side effects, sudden release, and high blood drugs of patients.

Inactive Publication Date: 2006-10-04
CHINA PHARM UNIV +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional sustained-release preparations have the possibility of burst release of the drug, resulting in high levels of blood drug in patients and increasing the hidden danger of side effects

Method used

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  • Levofloxacin slow release micropill, its preparation method and uses
  • Levofloxacin slow release micropill, its preparation method and uses
  • Levofloxacin slow release micropill, its preparation method and uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Preparation of levofloxacin sustained-release pellets

[0057] The prescription composition of the blank ball core:

[0058] Starch: dextrin 4: 1 (weight ratio)

[0059] Isolation layer coating material: 2% hydroxypropyl methylcellulose (HPMCE5) aqueous solution, which also contains 5% polyethylene glycol, 2% polysorbate 80

[0060] Sustained release layer coating material: 20% ethyl cellulose water dispersion, also contains 10% povidone, 5% diethyl phthalate, 10% titanium dioxide

[0061] Preparation Process:

[0062] Mix starch and dextrin at a weight ratio of 4:1, use an appropriate amount of 30% ethanol as a binder to make a soft material, and roll into a ball in a coating pan to make a blank core, and take a blank core between 20-40 mesh spare.

[0063] Place the blank pellet core in a fluidized bed, prepare an aqueous solution of levofloxacin, apply the drug, and make the pellets increase in weight by about 100%, use the HPMC aqueous solution to wrap the isola...

Embodiment 2

[0065] Isolation layer coating material: 5% Opadry aqueous solution (Shanghai Colorcon Company)

[0066] Sustained-release layer coating material: 10% Sulisi aqueous dispersion (Shanghai Colorcon Company)

[0067] Preparation Process:

[0068] Mix microcrystalline cellulose and levofloxacin in a weight ratio of 3:7, make a wet material with 40% ethanol solution, extrude the wet material through the sieve plate of an extruder to prepare granules, place it in a spheronizer, and use Opadry aqueous solution Wrap an isolation coat to increase the weight of the pills by about 6%, and then use the Sulisi water dispersion to coat them with a slow-release coating to increase the weight by 5% to obtain slow-release pellets. The prepared sustained-release pellets were aged at 80° C. for 1 hour. Release curve see image 3 .

Embodiment 3

[0070] starch

[0071] dextrin

[0072] Levofloxacin

[0073] Isolation layer coating material: 10% Opadry 50% ethanol aqueous solution

[0074] Sustained release layer coating material: 15% Suli silk aqueous dispersion

[0075] Preparation Process:

[0076] Mix starch, dextrin, and levofloxacin in a weight ratio of 3:3:4, make a wet material with 3% HPMC50% ethanol solution, extrude the wet material through an extruder sieve plate to prepare granules, place it in a spheronizer, and The opadry ethanol aqueous solution is used to coat the isolation coat, so that the weight of the pills is increased by about 8%, and then the Sulisi aqueous dispersion is used to coat the slow-release coating, so that the weight is increased by 7%, and the slow-release pellets are obtained. Release curve see Figure 4 .

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Abstract

The invention relates to a slow release micro-pellet preparation containing Levofloxacin, its preparation process and therapeutic use, wherein the micro-pellet preparation contains 0-40% of conventional medicinal particles and 60-100% of slow release medicinal micro-pellet, the micro-pellet contains medicinal core including Levofloxacin, and slow release coating layer whose content being 4-100% of the pellet core.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to sustained-release pellet preparations containing levofloxacin, a preparation method and therapeutic use thereof. Background technique [0002] Levofloxacin (levofloxacin) is the L-type photoactive isomer of ofloxacin. It is a third-generation fluoroquinolone broad-spectrum antibacterial drug. Its antibacterial activity is twice that of ofloxacin, and the incidence of adverse reactions is low. At present, it is widely used in clinical practice. Levofloxacin lactate and levofloxacin hydrochloride are commonly used in clinical practice. Different salts have similar drug effects. Since the biological half-life of levofloxacin is less than 6 hours, the clinical treatment of common preparations of levofloxacin needs to be taken 2 to 3 times a day. In order to reduce the number of times of taking medicine and maintain a stable blood drug concentration, the slow and controlled...

Claims

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Application Information

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IPC IPC(8): A61K31/5383A61K9/16A61P31/04
Inventor 尹莉芳陈矛张陆勇赵存婕江振洲叶放方毓新赵钢
Owner CHINA PHARM UNIV
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