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Levofloxacin tablet

A technology of levofloxacin tablets and levofloxacin, which is applied in the direction of antibacterial drugs, organic active ingredients, drug delivery, etc., can solve the problem of slow release effect decline, and achieve the effect of overcoming incomplete and unstable release

Pending Publication Date: 2022-08-02
ZHEJIANG POLY PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for people with insufficient gastric acid secretion and people who cannot strictly follow the doctor's advice to use it about half an hour after meals, the sustained-release effect of these slow-release agents will be significantly reduced

Method used

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Examples

Experimental program
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Effect test

preparation example Construction

[0039] Preparation of levofloxacin sustained-release tablets

[0040] After passing the raw material drug and the auxiliary materials except magnesium stearate through a 100-mesh sieve, weigh the required amount of ingredients and mix them thoroughly; add 55% ethanol to make a soft material, dry the wet granules and sieve them through a 20-mesh sieve for granulation; Add magnesium stearate and mix well; tablet (specification 500mg, hardness 9Kg).

[0041] Coating (JGB-150 coating pan, Jian brand) parameters: tablet bed temperature 40 degrees Celsius, air outlet temperature 47 degrees Celsius, atomization pressure 0.5Mpa, rotation speed 10rpm, spray volume 110g / min, coating weight gain 10%.

Embodiment 1

[0042] Example 1 Preliminary study on levofloxacin sustained-release tablets

[0043] After trying a large number of sustained-release tablet formulations, the applicant constructed the following sustained-release tablet formulations, which can release the drug smoothly in about 12 hours and have good sustained-release performance (see figure 1 Curve pH3): by weight: levofloxacin hydrochloride 55%, hypromellose K100M 20%, ethylcellulose N50 15%, lactose 7.5%, magnesium stearate 2.5%.

[0044] However, further research found that the release performance of the sustained-release tablet formulation was obviously limited at higher pH, the drug could not be fully released, the release degree within 12 hours was only slightly higher than 80%, and the release amount after 8 hours was obviously insufficient (see figure 1 The curve in the pH5, pH7), which will significantly affect the efficacy and limit the convenience of drug use for patients with insufficient gastric acid or those wh...

Embodiment 2

[0045] Example 2 Study on the coating of levofloxacin sustained-release tablets

[0046] The applicant tried to solve the problem of the reference document 1 by adjusting the formula, but the effect was not satisfactory (the formulas of hypromellose K100M, ethyl cellulose N50, and lactose have been obtained by the applicant after a large number of formula screening). Applicants then attempted to use coatings to solve the above problems while providing taste-masking or taste-correcting functions to ofloxacin with a strong bitter taste. Based on production experience, the applicant has successively tried various existing coatings, such as Opadry II 85G (HPMC, aqueous solution) with 4% by weight of the tablet core, and Aquacoat ECD 30 (EC, aqueous solution) with 6% by weight of the tablet core. Except for a certain time delay, these coatings had no significant effect on the release properties of ER tablets.

[0047]According to the characteristics of the previously used self-mad...

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Abstract

The invention provides a levofloxacin tablet. The levofloxacin tablet is composed of a tablet core and a coating layer, wherein the tablet core contains levofloxacin hydrochloride, hydroxypropyl methylcellulose, ethyl cellulose, lactose and magnesium stearate; the coating layer contains PVP (Polyvinyl Pyrrolidone), diethyl phthalate and glycerol triacetate; the combination of the tablet core and the coating layer can provide 12-hour stable release for levofloxacin in a pH range of 2-7.

Description

technical field [0001] The application belongs to the field of pharmacy, specifically, the application provides a levofloxacin sustained-release tablet, the levofloxacin sustained-release tablet comprises levofloxacin hydrochloride, hypromellose, ethylcellulose, lactose, magnesium stearate and a coating Element. Background technique [0002] Ofloxacin is a third-generation quinolone antibacterial drug, which achieves antibacterial by inhibiting the mechanism of DNA replication enzymes, and has spectral effects on Gram-positive and gram-negative bacteria. At present, oral preparations, injections, eye drops and other dosage forms are widely used in the clinical treatment of bacterial infections of the respiratory system, urinary system, reproductive system, skin, and eyes. [0003] Ofloxacin is rapidly metabolized, its biological half-life is only about 6 hours, and its antibacterial effect is obviously concentration-dependent. Therefore, the current clinical oral administra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/32A61K9/22A61K31/5383A61K47/32A61K47/38A61P31/04
CPCA61K31/5383A61K9/2054A61K9/2018A61P31/04A61K9/284
Inventor 朱逸凡范敏华周学来
Owner ZHEJIANG POLY PHARMA
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