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Medicinal composition containing lipid material nocathiacin antibiotic

A technology of nocafloxacin and lipid materials, applied in antibacterial drugs, drug delivery, liposome delivery, etc., to achieve the effects of low efficiency, easy process steps, simple and safe equipment

Inactive Publication Date: 2011-04-27
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] But there is no report about making nocafloxacin into liposomes, lipid vesicle preparations or solid lipid nanoparticles

Method used

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  • Medicinal composition containing lipid material nocathiacin antibiotic

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1: Liposome with main drug ratio of phospholipid 1:10 and cholesterol ratio of phospholipid 1:1

[0046] prescription:

[0047] Soy Lecithin 100mg; Cholesterol 100mg;

[0048] Nocafloxacin I 10mg phosphate buffer (pH7.4) 1ml.

[0049] Preparation Process:

[0050] Dissolve the prescribed amount of phospholipids, cholesterol and main drug in dichloromethane, centrifuge to remove insolubles, and then rotate the solution in the flask below 30°C to form a film on the inner wall; then add phosphate buffer to the flask and Stir continuously until a uniformly dispersed liposome solution is formed; the solubility of nocafloxacin I detected by high performance liquid chromatography is 6.96 mg / ml; the solution is diluted 500-1000 times and there is no precipitation within 72 hours.

Embodiment 2

[0051] Example 2: Liposomes with main drug ratio of phospholipid 1:10 and cholesterol ratio of phospholipid 1:2

[0052] prescription:

[0053] Cereblin 100mg; Cholesterol 50mg;

[0054] Nocafloxacin I 10mg; Phosphate buffer (pH7.4) 1ml.

[0055] Preparation Process:

[0056] Dissolve the prescription amount of phospholipid, cholesterol and main drug in ethanol, centrifuge to remove insoluble, then slowly drip the solution into the stirred phosphate buffer, keep stirring until the ethanol is exhausted, and then pass through the high-pressure milk homogenizer twice , A uniformly dispersed liposome solution was obtained; the solubility of nocafloxacin I was 7.61 mg / ml as determined by high performance liquid chromatography; no precipitation was precipitated within 72 hours after the solution was diluted 500-1000 times.

Embodiment 3

[0057] Example 3: Liposomes with main drug ratio of phospholipid 1:10 and cholesterol ratio of phospholipid 1:4

[0058] prescription:

[0059] Egg yolk phospholipid 100mg; cholesterol 50mg;

[0060] Oleic acid 3μl; Polysorbate 80 5μl;

[0061] Nocafloxacin I 10mg; Phosphate buffer (pH7.4) 1ml.

[0062] Preparation Process:

[0063] Add the phosphate buffer to chloroform or dichloromethane containing the prescribed amount of phospholipid, cholesterol, oleic acid, polysorbate 80 and the main drug, stir and evaporate to remove the organic solvent, and the residual liquid is dispersed by ultrasonic to separate the lipid Resuspended in phosphate buffer to obtain a uniformly dispersed liposome solution; the solubility of nocafloxacin I detected by HPLC is 7.98mg / ml; within 72 hours after the solution is diluted 500-1000 times There is no precipitation.

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Abstract

The invention belongs to a medicinal composition and particularly relates to a medicinal composition containing a lipid material nocathiacin antibiotic as well as a corresponding liposome, a noisome and a solid lipid nanoparticle form thereof. The invention discloses a medicinal composition containing a nocathiacin antibiotic which comprises the main medicine nocathiacin and a lipid material, wherein the lipid material is phospholipid or phospholipid. With the medicinal composition, a lipid containing nocathiacin, a noisome preparation or a solid lipid nanoparticle form can be prepared. The medicinal composition can obviously improve the solubility of nocathiacin, the preparation process is safe, the materials are economical, the equipment is simple and the process steps are few; and moreover, due to the remarkable drug-resistant bacteria activity of nocathiacin, the invention has important values in clinical application.

Description

Technical field [0001] The invention belongs to a pharmaceutical composition, and specifically relates to a pharmaceutical composition of nocafloxacin antibiotic containing lipid materials, and corresponding liposomes, lipid vesicles and solid lipid nanoparticle dosage forms. Background technique [0002] In the history of humans fighting against diseases, bacterial infections have always been the number one killer of human deaths. As people use more and more antibiotics to treat diseases, they have also exercised the resistance of bacteria, so with antibiotics The abuse of pathogenic bacteria and the rapid evolution of pathogenic bacteria, more and more drug-resistant strains have appeared clinically, especially strains resistant to many antibiotics such as methicillin-resistant Staphylococcus aureus (MRSA), Penicillin-resistant Streptococcus pneumoniae (PRSP), as well as the recently discovered "super bacteria", are often helpless in the face of the rapid infection rate of thes...

Claims

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Application Information

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IPC IPC(8): A61K38/12A61K9/127A61K9/14A61K9/00A61P31/04
Inventor 冯坤陈依军张志伟
Owner CHINA PHARM UNIV
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