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Hydrochloric acid ciprofloxacin lipidosome preparation and preparation method thereof

A technology of ciprofloxacin hydrochloride and liposome preparations, which is applied in the field of new preparations of ciprofloxacin hydrochloride, can solve the problems of frequent medication, short elimination half-life, etc., to improve bioavailability, reduce adverse reactions, and reduce toxicity side effects

Inactive Publication Date: 2016-01-13
ZHENGZHOU HOUYI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Common clinical dosage forms include oral dosage forms and injections; however, the elimination half-life of conventional dosage forms of the drug is short, frequent medication, and widely distributed in the body

Method used

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  • Hydrochloric acid ciprofloxacin lipidosome preparation and preparation method thereof

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Experimental program
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Embodiment 1

[0024] A ciprofloxacin hydrochloride liposome preparation is prepared from the following raw materials in parts by weight: 1 part of ciprofloxacin hydrochloride, 10-50 parts of soybean lecithin, and 5-40 parts of cholesterol.

[0025] The preparation method of ciprofloxacin hydrochloride liposome preparation as above, comprises the following steps:

[0026] (1) Weigh ciprofloxacin hydrochloride, add phosphate buffer with a concentration of 100~200mmol / L, add 20~25mL of phosphate buffer per mg of ciprofloxacin hydrochloride; stir to make ciprofloxacin hydrochloride solution , placed in a 65-70°C water bath, kept warm, and set aside;

[0027] (2) Preparation of blank liposomes: Mix soybean lecithin and cholesterol, add chloroform, place in a water bath at 65-70°C, stir to dissolve, remove the solvent under reduced pressure, and obtain a blank phospholipid film. Each mg of soybean lecithin and Add 2~4mL of chloroform to cholesterol;

[0028] (3) Dissolve the phospholipid film o...

Embodiment 2

[0030] A ciprofloxacin hydrochloride liposome preparation is prepared from the following raw materials in parts by weight: 1 part of ciprofloxacin hydrochloride, 10 parts of soybean lecithin, and 5 parts of cholesterol.

[0031] The preparation method of ciprofloxacin hydrochloride liposome preparation as above, comprises the following steps:

[0032] (1) Weigh 1mg of ciprofloxacin hydrochloride and add 20ml of 0.2mol / L phosphate buffered saline water, stir to make a ciprofloxacin hydrochloride solution, place it in a 65°C water bath, keep warm, and set aside;

[0033] (2) Preparation of blank liposomes: Mix 10 mg of soybean lecithin and 5 mg of cholesterol, add 50 ml of chloroform, place in a 65°C water bath, stir to dissolve, remove the solvent under reduced pressure, and obtain a blank phospholipid film;

[0034] (3) Dissolve the film in 5 mL of chloroform, add the ciprofloxacin hydrochloride solution prepared in (1) and 5 mL of 0.2 mol / L phosphate buffer, and sonicate at 6...

Embodiment 3

[0036] A ciprofloxacin hydrochloride liposome preparation is prepared from the following raw materials in parts by weight: 1 part of ciprofloxacin hydrochloride, 11 parts of soybean lecithin, and 5 parts of cholesterol.

[0037] The preparation method of ciprofloxacin hydrochloride liposome preparation as above, comprises the following steps:

[0038] (1) Weigh 5mg of ciprofloxacin hydrochloride and add 120ml of 0.2mol / L phosphate buffered saline water, stir to make a ciprofloxacin hydrochloride solution, place it in a water bath at 65°C, keep warm, and set aside;

[0039] (2) Preparation of blank liposomes: Mix 55 mg of soybean lecithin and 25 mg of cholesterol, add 200 ml of chloroform, place in a 65°C water bath, stir to dissolve, remove the solvent under reduced pressure, and obtain a blank phospholipid film;

[0040] (3) Dissolve the film in 5 mL of chloroform, add the ciprofloxacin hydrochloride solution prepared in (1) and 6 mL of 0.2 mol / L phosphate buffer, and sonicat...

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Abstract

The invention discloses a preparation method of a hydrochloric acid ciprofloxacin lipidosome preparation. The preparation method includes the steps that one part of hydrochloric acid ciprofloxacin is weighed, a phosphate buffer solution is added and stirred, and a hydrochloric acid ciprofloxacin solution is obtained; 2, blank liposome is prepared, wherein 10-50 parts of soya bean lecithin and 5-40 parts of cholesterol are weighed and mixed, chloroform is added and stirred for being dissolved, decompression is conducted for removing solvent, and a blank phospholipid membrane is prepared; 3, the membrane is dissolved through a small amount of chloroform, the hydrochloric acid ciprofloxacin solution obtained in step 1 and the phosphate buffer solution are taken for being added into an acetate solution, ultrasound treatment is conducted for 10-30 minutes through a bath type ultrasonic instrument at the temperature of 45-60 DEG C, a stable solution is formed, the obtained lipidosome solution is filtered twice through a microfiltration membrane, granulation is conducted, and the hydrochloric acid ciprofloxacin lipidosome preparation is obtained. The lipidosome produced through the ultrasonic instrument has the advantages that the particle size is small, particle size distribution is narrower, and the lipidosome has good preparation nature and target ability, can improve the curative effect, has a long-term effect, can reduce drug toxicity and can improve the drug stability.

Description

technical field [0001] The invention relates to a new preparation of ciprofloxacin hydrochloride, in particular to a ciprofloxacin hydrochloride liposome preparation and a preparation method thereof. Background technique [0002] Liposome is a targeted drug carrier, which belongs to a new dosage form of targeted drug delivery system. It can embed drug powder or solution in particles with a diameter of nanometer scale. This particle has a cell-like structure. It enters the human or animal body and is mainly swallowed by the reticuloendothelial system to activate the body's autoimmune function and change the encapsulation. By controlling the distribution of drugs in the body, the drugs are mainly accumulated in tissues and organs such as the lung, spleen, liver and bone marrow, thereby improving the therapeutic index of the drug, reducing the therapeutic dose of the drug and reducing the toxicity of the drug. Liposomes are continuous bilayer lipid molecules containing an aque...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/496A61P31/04A61P11/00
Inventor 李亚娥朱丽平
Owner ZHENGZHOU HOUYI PHARMA
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