Slow release type linezolid preparation for eyes as well as preparation method and application thereof
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A linezolid eye and linezolid technology are applied in the field of sustained-release linezolid ophthalmic preparations and their preparation, which can solve the problems of increasing the incidence of infectious endophthalmitis and the like, and achieve high intraocular bioavailability, The effect of strong targeting effect and good intraocular penetration
Inactive Publication Date: 2018-09-21
广州君博医药科技有限公司
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Subconjunctival and intravitreal injections can achieve effective drug concentrations in ocular tissues, but intraocular injections are, after all, a traumatic method of administration, and repeated injections will greatly increase the risk of infectious endophthalmitis. incidence rate
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Embodiment 8
[0032] (1) Embodiment 8 pharmacokinetic test
[0033] Healthy New Zealand rabbits (half male and half female) were used as experimental animals. A single dose of linezolid eye drops (at 20, 40, 60, 80, 100, 120, 150, 210, 270, 360, 480 minutes after administration, the aqueous humor 30 μl) and multiple times (7 days of continuous administration, 4 times a day, once every 6 hours. Take 30 μl of aqueous humor before the last administration on the 6th day, before the 1st and 2nd administration on the 7th day, At 20, 40, 60, 80, 100, 120, 150, 210, 270, 360, 480 min after the third administration, 30 μl of aqueous humor was extracted) After administration, the aqueous humor samples were determined by HPLC-MS.
[0034]After a single administration, the Cmax of linezolid in aqueous humor was 38.754±9.426g / ml; Tmax was 102.00±12.55min; T1 / 2 was 81.52±13.64min; AUC0-t was 5179.60±1881.16gminml-1, AUC0- was 5374.01±2056.85gminml-1; Ke is 0.01±0.001min-1. After repeated eye drops, the...
Embodiment 7
[0053] Pharmacokinetic test of linezolid eye drops prepared from sustained-release linezolid eye drops and DuraSite ophthalmic delivery system in Example 7
[0054] The left and right eyes of New Zealand rabbits were administered at the same time, and the dosage was 50 μL. At 20, 40, 60, 80, 100, 120, 150, 210, 270, 360, and 480 minutes after administration, 30 μl of aqueous humor was extracted for testing; aqueous humor samples were determined by LC-MS, and the results are shown in Table 4 below:
[0055] Table 4: The main pharmacokinetic parameters of the sustained-release linezolid eye drops and DuraSite linezolid eye drops in Example 7 administered to the eyes of New Zealand rabbits in a single dose
[0056]
[0057]
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Abstract
The invention relates to a slow release type linezolid preparation for eyes as well as a preparation method and application thereof. The slow release type linezolid preparation is prepared from the following components: linezolid, polycarbophil, disodium edetate, an auxiliary material and water for injection, wherein the mass ratio of linezolid to polycarbophil to disodium edetate is 1 to (0.5 to2) to (0.05 to 0.2); the mass percent of linezolid is 0.1 percent to 1 percent. Dosage form of the preparation comprise eye drops, eye ointment and eye gel. The slow release type linezolid preparationhas a remarkable and long-lasting pharmaceutical effect, has good intraocular penetrability and relatively high intraocular bioavailability and has the advantages of strong penetration force, strongtargeting effect and small toxic and side effects; the slow release type linezolid preparation is suitable for treating and preventing outer eye and anterior segment diseases caused by non-infection inflammations and postoperative inflammations, and has good antibacterial and inflammation-diminishing effects, small irritation and high safety; raw materials are easy to obtain, a preparation processis simple and the cost is low; industrialized large-scale production can be realized and the economic benefit is remarkable.
Description
technical field [0001] The invention relates to an ophthalmic pharmaceutical preparation for treating bacterial infection, in particular to a slow-release linezolid ophthalmic preparation and its preparation method and application. Background technique [0002] Linezolid is a synthetic oxazolidinone antibiotic approved by the US FDA in 2000 for the treatment of infections caused by Gram-positive (G+) cocci, including suspected or confirmed hospital-acquired pneumonia (HAP) caused by MRSA, Community-acquired pneumonia (CAP), complicated skin or skin and soft tissue infection (SSTI), and vancomycin-resistant enterococci (VRE) infection. Linezolid is a brand-new class of oxazolone antibacterial drugs, which comprehensively covers drug-resistant strains of Gram-positive bacteria - Staphylococcus aureus / Enterococcus / Streptococcus, etc. It is an inhibitor of bacterial protein synthesis and acts on bacterial 50S ribosomes subunit and is closest to the site of action. Unlike o...
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