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Ciprofloxacin thermo-sensitive type in-situ gel composition and preparing method thereof

A technology of ciprofloxacin lactate and in-situ gelation, which is applied in the fields of pharmaceutical formulation, drug delivery, and medical preparations of non-active ingredients, etc. It can solve problems such as increased gelation temperature, oxidation of pharmaceutical preparations, and impact on the quality of preparations. Achieve increased compliance, uniform drug distribution, and good drug distribution

Active Publication Date: 2013-06-19
NANJING AGRICULTURAL UNIVERSITY +1
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  • Abstract
  • Description
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AI Technical Summary

Problems solved by technology

①The gelling temperature of the composition is 29°C, and the temperature in summer often reaches 29°C. The preparation has become a gel before use in this temperature environment, and the preparation needs to be cooled before it can be used. At the same time, there are higher requirements for the storage temperature; ②Poor The concentration of Loxamer 407 is low, and the gelation temperature may be significantly increased or even lose gelation ability under the dilution of tissue fluid or secretion fluid at the application site; ③ lack of metal ion complexing agent affects the quality of the preparation, because the lactic acid ring Profloxacin in an appropriate amount of heavy metal ions such as Fe 3+ It is easy to make the color of the preparation turn yellow under the action (Tan Rijian. Chinese Journal of Hospital Pharmacy, 2000, 20(3): 175
(Wang Rushan et al. Chinese Journal of Hospital Pharmacy, 1998, 18(12): 570) ④ Lack of pH regulator: CPFL is prone to precipitate crystals when the pH>5.0 (Xie Benshu. Medical Anthology, 2004, 23(6): 735 -736), making the quality of the preparation not up to standard
⑤ Lack of antioxidants: Oxygen in the atmosphere can easily cause oxidation of pharmaceutical preparations, and more attention should be paid to liquid preparations
The gelling temperature of the preparation is 25.3°C. When stored at room temperature (25°C) or above, it becomes very viscous or has formed a gel, which makes it impossible to administer the preparation. After cooling down, the preparation returns to liquid and administered to the eye. But cold stimulation will make the compliance worse
In addition, according to the research results of the above-mentioned ciprofloxacin lactate ordinary injection, it can be known that the quality of the preparation is unreliable due to the lack of metal ion complexing agents, antioxidants and pH regulators, etc.
[0012] After searching, no report was found on the temperature-sensitive in situ gel composition of ciprofloxacin lactate for injection or rectal administration

Method used

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  • Ciprofloxacin thermo-sensitive type in-situ gel composition and preparing method thereof
  • Ciprofloxacin thermo-sensitive type in-situ gel composition and preparing method thereof
  • Ciprofloxacin thermo-sensitive type in-situ gel composition and preparing method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0064] The preparation of embodiment 1 acetic acid-sodium acetate buffer solution

[0065] Proceed as follows:

[0066] (1) Add 1.6410 g of analytically pure sodium acetate to 100 mL of water for injection to dissolve, mix well, and filter through a 0.22 μm microporous membrane to obtain a 0.2 mol / L sodium acetate solution.

[0067] (2) Add 12.0100 g or 11.5 mL of anhydrous acetic acid into 1000 mL of water for injection to dissolve, mix well, and filter through a 0.22 μm microporous membrane to obtain a 0.2 mol / L acetic acid solution.

[0068] (3) Mix 75 mL of sodium acetate solution in (1) and 925 mL of acetic acid solution in (2), and filter through a 0.22 μm microporous membrane to obtain 0.2 mol / L acetic acid-sodium acetate buffer solution (pH=3.6 ), about 1L.

Embodiment 2

[0069] Example 2 Preparation of ciprofloxacin lactate temperature-sensitive in-situ gel composition (composition 1)

[0070] Prepare according to the following method: EDTA-2Na 0.012g, sodium bisulfite 0.060g, 80 microliters of 5% benzalkonium bromide solution (5% benzalkonium bromide solution is to dissolve benzalkonium bromide in water for injection according to weight percentage Obtained in. The weight-to-volume ratio that is equivalent to benzalkonium bromide here is 0.01%) adds in the acetic acid-sodium acetate buffer solution 40mL that embodiment 1 prepares, stirs to make it dissolve; Then add ciprofloxacin lactate 3.2g, Stir and dissolve; 0.45 μm microporous membrane filtration, add Poloxamer 407 (Germany BASF Company) 9.60g and Poloxamer 188 (Germany BASF Company) 0.80g in the obtained filtrate, leave standstill 20min, stir; Put it in the refrigerator at 4°C for 60 minutes, take it out, stir it evenly; put it in the refrigerator at 4°C for 20 hours, and then get the cl...

Embodiment 3

[0071] Example 3 Preparation of ciprofloxacin lactate temperature-sensitive in-situ gel composition (composition 2)

[0072] Prepared according to the following method: EDTA-2Na 0.008g, sodium bisulfite 0.080g, 120 microliters of 5% benzalkonium bromide solution (the weight-to-volume ratio of benzalkonium bromide here is 0.015%) was added to the preparation of Example 1 Add ciprofloxacin lactate 3.2g, stir and dissolve in 40mL of acetic acid-sodium acetate buffer solution; add poloxamer 407 (Germany BASF company) to the filtrate 9.60g and 1.20g of poloxamer 188 (Germany BASF company), let it stand for 15min, stir evenly, then put it in a refrigerator at 4°C for 80min, take it out, stir evenly, and put it in a refrigerator at 4°C for 24 hours to get a clear lactic acid ring Profloxacin thermosensitive in situ gel composition. Autoclave at 115°C for 20 minutes, let cool, and pack aseptically after passing the product inspection.

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Abstract

The invention discloses ciprofloxacin thermo-sensitive type in-situ gel composition and belongs to the field of veterinary drug preparations. The thermo-sensitive type in-situ gel composition comprises, by weight volume (g / ml), 5%-10% of ciprofloxacin, 20%-26% of poloxamer 407, 0.5%-10% of poloxamer 188, 0.01%-0.04% of edetic acid, 0.009%-0.03% of bacteriostatic agent, and 0.1%-0.2% of antioxidant. Solvent of the composition is acetic acid - sodium acetate buffer solution. The invention further discloses a preparing method of the composition. The ciprofloxacin thermo-sensitive type in-situ gel composition is liquid at room temperature, jelling temperature is close to body temperature, and therefore dosing is convenient and jelling speed is high, jelling strength and adhering function are good, the dosing can be achieved with accurate positioning, and loss of drug is reduced. Furthermore, the ciprofloxacin thermo-sensitive type in-situ gel composition and the preparing method thereof have controlled-releasing and long-acting functions, dosage is low, the number of times of dosing is small, harm caused by implants normally used is avoided, and pain of patients is relieved.

Description

technical field [0001] The invention belongs to the field of veterinary in-situ gel preparations, and in particular relates to a temperature-sensitive in-situ gel composition of ciprofloxacin lactate and a preparation method of the composition. Background technique [0002] Ciprofloxacin Lactate (CPFL), the lactic acid salt of Ciprofloxacin (Ciprofloxacin), is easily soluble in water, and is a strong broad-spectrum antibacterial drug among quinolones used in veterinary clinical practice. It has the advantages of broad antibacterial spectrum, strong bactericidal power, good pharmacokinetic characteristics, low incidence of adverse reactions, long postantibiotic effect, low price, and no cross-resistance, and is widely used. in medicine and veterinary practice. It is widely used clinically to control gastrointestinal infections, lung infections, obstetrical infections and local infections caused by sensitive pathogens, while veterinary medicine is used clinically for infectio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/496A61K47/34A61P31/04
Inventor 江善祥曹礼华张东娟彭麟季辉万荣峰蔡冬张军忍施宗傲
Owner NANJING AGRICULTURAL UNIVERSITY
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