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Cefpiramide sodium micro-spheres and preparing method thereof

A technology of cefpiramide sodium and microspheres, which is applied in the field of medicine, can solve the problems of insufficient drug sensitivity, low drug concentration, and short action time, and achieve the effects of short biological half-life, reduced damage, and increased compliance

Inactive Publication Date: 2011-10-12
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of its strong water solubility, it is difficult to penetrate the cell membrane and cannot accumulate in the cell, resulting in a low intracellular drug concentration, bacteria, etc. are not sensitive enough to the drug, and the effect of treating intracellular bacterial infection is not good, so it is generally administered in the form of intravenous injection. ; However, due to the short duration of action, intravenous administration is required 2 to 3 times a day, causing inconvenience to patients

Method used

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  • Cefpiramide sodium micro-spheres and preparing method thereof
  • Cefpiramide sodium micro-spheres and preparing method thereof
  • Cefpiramide sodium micro-spheres and preparing method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Embodiment 1: the preparation of cefpiramide sodium microspheres

[0030] Dissolve 10 mg of cefpiramide sodium in 3 ml of 30 mg / ml carboxymethyl chitosan aqueous solution, and ultrasonically dissolve it to form a water phase; take 40 ml of liquid paraffin, add 4.0 g of span-80 to it, and prepare 100 mg / ml span -80 liquid paraffin solution to form the organic phase. Under magnetic stirring, the drug-containing carboxymethyl chitosan solution was added dropwise to the liquid paraffin containing span-80, and after the dropwise addition was completed, the dispersion was continued for 30 minutes. Add 1ml of glutaraldehyde to cross-link and solidify at about 30 minutes, and observe the morphology of the microspheres under an optical microscope. The morphology of the microspheres was observed after stirring for 3 h with an electromagnetic stirrer at 1500 rpm. The microspheres are collected by suction filtration, washed with petroleum ether and then with isopropanol, filtered...

Embodiment 2

[0031] Embodiment 2: the preparation of cefpiramide sodium microspheres

[0032]Dissolve 10 mg of cefpiramide sodium in 3 ml of 30 mg / ml carboxymethyl chitosan aqueous solution, and ultrasonically dissolve it to form a water phase; take 25 ml of liquid paraffin, add 1.25 g of span-80 to it, and prepare a 50 mg / ml span -80 liquid paraffin solution to form the organic phase. Under magnetic stirring, the drug-containing carboxymethyl chitosan solution was added dropwise to the liquid paraffin containing span-80, and after the dropwise addition was completed, the dispersion was continued for 30 minutes. Add 1ml of glutaraldehyde to cross-link and solidify at about 30 minutes, and observe the morphology of the microspheres under an optical microscope. The morphology of the microspheres was observed after stirring for 3 h with an electromagnetic stirrer at 1500 rpm. The microspheres are collected by suction filtration, washed with petroleum ether and then with isopropanol, filtere...

Embodiment 3

[0033] Embodiment 3: the preparation of cefpiramide sodium microspheres

[0034] Dissolve 10 mg of cefpiramide sodium in 3 ml of 30 mg / ml carboxymethyl chitosan aqueous solution, and ultrasonically dissolve it to form an aqueous phase; take 40 ml of liquid paraffin, add 2.0 g of span-80 to it, and prepare a 50 mg / ml span -80 liquid paraffin solution to form the organic phase. Under magnetic stirring, the drug-containing carboxymethyl chitosan solution was added dropwise to the liquid paraffin containing span-80, and after the dropwise addition was completed, the dispersion was continued for 30 minutes. Add 1ml of glutaraldehyde to cross-link and solidify at about 30 minutes, and observe the morphology of the microspheres under an optical microscope. The morphology of the microspheres was observed after stirring for 2 h with an electromagnetic stirrer at 1000 rpm. The microspheres are collected by suction filtration, washed with petroleum ether and then with isopropanol, filt...

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Abstract

The invention relates to cefpiramide sodium micro-spheres and a preparing method thereof, belonging to the technical field of medicaments. A carrier material of each cefpiramide sodium micro-sphere is carboxy methyl chitosan while a slow release medicament of each cefpiramide sodium micro-sphere is cefpiramide sodium, wherein the content of the cefpiramide sodium is 5.3% to 5.5% of mass of the overall micro-sphere; each micro-sphere is 17.920 mum to 20.749 mum in average grain diameter and 2.799 in span of the grain diameter. The preparing method comprises the following step of: with biodegradable high molecular material, i.e., carboxy methyl chitosan as the carrier material, preparing highly water-soluble antibiotic-medicament, i.e., cefpiramide sodium into the slow release micro-sphere by using an emulsifying and dispersing-curing cross-linking method, wherein the micro-sphere is taken orally. The cefpiramide sodium micro-spheres disclosed by the invention can be used for reducing damage of intravenous drip to skins and mucous membranes of a patient, improving absorption of oral taking, and increasing bioavailability of the medicament; meanwhile, the cefpiramide sodium micro-sphere can be used for prolonging action time of the medicament, reducing dosage and improving compliance of the patient. The preparing method disclosed by the invention has the advantages of simpleness in operation, gentle conditions and strong controllability and is suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a cefpiramide sodium microsphere and a preparation method thereof. Background technique [0002] Clinically, antibiotics mainly inhibit the growth of pathogenic bacteria and are used to treat most bacterial infectious diseases. There are many kinds of antibiotics, mainly penicillins, cephalosporins, sulfonamides and quinolones and other drugs. [0003] Because penicillin has been found to have shortcomings such as allergic reactions, drug resistance, narrow antibacterial spectrum and unstable properties in use, so its structure has been modified. Since the 1960s, a series of broad-spectrum, acid-resistant, and enzyme-resistant semi-synthetic penicillins have emerged. In 1945, Brotzu discovered cephalosporins. In 1962, the first generation of cephalosporins was developed. Through structural modification and transformation, cephalosporin antibiotics were developed rapidly, and the...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/546A61K47/36C08J3/24A61P31/04
Inventor 黄桂华张志岳胡玥
Owner SHANDONG UNIV
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