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

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...

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

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