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Pulmonary delivery ciprofloxacin pharmaceutical composition and preparation method thereof

A technology of ciprofloxacin and pulmonary drug delivery, which is applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve liposome leakage, affect the quality of preparations, lipid Insufficient stability of plastids and other problems, to achieve the effect of prolonging the action time, good stability, and easy to carry

Active Publication Date: 2012-01-11
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The liposomes obtained by this method are not stable enough, and the leakage of liposomes is prone to occur, thereby affecting the quality of the preparation.

Method used

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  • Pulmonary delivery ciprofloxacin pharmaceutical composition and preparation method thereof
  • Pulmonary delivery ciprofloxacin pharmaceutical composition and preparation method thereof
  • Pulmonary delivery ciprofloxacin pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the preparation of control sample

[0022] Prepare control samples with reference to the following literature:

[0023] Tejas R. Desai et al.2001. Determination of surface freeenergy of interactive dry powder liposome formulations using capillary penetration technique. Colloids and Surfaces B: Biointerfaces.22, 107-113; W.H.Finlay, J.P.Wong, 1998, Regional iposome lung deposition of neopos -encapsulated profloxacin. International Journal of Pharmaceuticals. 167, 121-127.

[0024] Specifically, the prescription is as follows:

[0025] Ciprofloxacin Hydrochloride 0.11g

[0026] DPPC 0.55g

[0027] Cholesterol 0.45g

[0028] Lactose 2.2g

[0029] 0.6M ammonium sulfate aqueous solution 20ml

[0030] Preparation method: Dissolve the prescribed amount of DPPC and cholesterol in chloroform and evaporate under reduced pressure, hydrate with 0.6M ammonium sulfate, ultrasonically granulate, dialyze with a certain amount of normal saline for 12 hours, add the p...

Embodiment 2

[0031] Embodiment 2: the preparation of spray formulation sample of the present invention

[0032] The prescription is as follows:

[0033] Ciprofloxacin Hydrochloride 0.11g

[0034] DPPC-PEG2000 0.55g

[0035] Cholesterol 0.45g

[0036] Tween 800.1ml

[0037] 0.6M ammonium sulfate aqueous solution 20ml

[0038] Preparation method: Take the prescribed amount of DPPC-PEG2000 and cholesterol, dissolve in chloroform and evaporate under reduced pressure, hydrate with 0.6M ammonium sulfate, ultrasonically granulate, dialyze with a certain amount of normal saline for 12 hours, add the prescribed amount of drugs, and incubate in a water bath at 50°C for 5 minutes . Mix this sample with Tween 80 and put it into a specific spray bottle to get sample 2.

Embodiment 3

[0039] Embodiment 3: the preparation of aerosol formulation sample of the present invention

[0040] The prescription is as follows:

[0041] Ciprofloxacin Hydrochloride 0.11g

[0042] DPPC-PEG2000 0.55g

[0043] Cholesterol 0.45g

[0044] Tween 80 0.1ml

[0045] Tetrafluoroethane (HFA134a) 3ml

[0046] 0.6M ammonium sulfate aqueous solution 20ml

[0047] Preparation method: Dissolve the prescribed amount of DPPC-PEG2000 and cholesterol in chloroform and evaporate under reduced pressure, hydrate with 0.6M ammonium sulfate, ultrasonically granulate, dialyze with a certain amount of normal saline for 12 hours, add the prescribed amount of drugs, and incubate in a water bath at 50°C 5min. Mix this sample with Tween 80 and put it into a specific container, then fill it with tetrafluoromethane to get sample 3.

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Abstract

The invention belongs to the field of drugs and pharmaceutics and relates to a pulmonary delivery ciprofloxacin pharmaceutical composition. In particular, a liposome modified by PEG (Polyethylene Glycol) is used as a drug carrier in the composition; the liposome modified by the PEG is that PEG molecules are directly connected to the liposome; or the liposome is coated by the PEG molecules. The invention further relates to the preparation method of the composition. According to the composition disclosed by the invention, the stability is good; the action time is prolonged; the better antibacterial effect is obtained; furthermore, the pulmonary effective treatment concentration can be achieved rapidly; the bioavailability is high; the composition is convenient to carry; and the composition can be taken independently.

Description

technical field [0001] The invention belongs to the field of medicine and pharmacy, and relates to a ciprofloxacin medicinal composition for pulmonary administration and a preparation method thereof. Background technique [0002] Ciprofloxacin is a third-generation quinolone antibacterial drug, which has many characteristics such as broad antibacterial spectrum, strong antibacterial activity, simple structure, and convenient administration. It inhibits DNA synthesis and replication by acting on the A subunit of bacterial DNA helicase, leading to bacterial death. Ciprofloxacin has a broad-spectrum antibacterial effect and has strong antibacterial activity against Gram-negative bacteria. It has good antibacterial effect on the following bacteria in vitro: most bacteria of Enterobacteriaceae, including Citrobacter, Enterobacter cloacae, Enterobacter aerogenes and other Enterobacter species, Escherichia coli, Klebsiella, Proteus genera, Salmonella, Shigella, Vibrio, and Yersin...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/496A61K47/34A61P31/04A61P11/00
Inventor 郑爱萍刘春美毕芸祺张晓燕孙健绪
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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