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Sustained-release injection containing netilcosin

A slow-release injection and test-taking technology, which is applied in the field of medicine, can solve the problems of side effects of increasing doses, difficulty in obtaining effective bactericidal concentration, etc., and achieve the effects of reducing the course of treatment, facilitating drug application, and reducing costs

Inactive Publication Date: 2008-10-15
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there are many new antibacterial drugs, especially aminoglycoside antibiotics, which have shown good curative effect. However, for many chronic lesions, especially local lesions, it is difficult to obtain an effective bactericidal concentration with conventional therapy.
Increased dose or long-term use of drugs will have many side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] Put 90, 90 and 80 mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymers into (A), (B) and (C) three In two containers, add 100 milliliters of dichloromethane to each, after dissolving and mixing, add 10 mg arbekacin, 10 mg amikacin, and 20 mg asmitacin respectively, shake them up again, and use spray-drying method to prepare the mixture containing 10% arbekacin, 10% amikacin and 20% asmitacin microspheres for injection. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 350cp-550cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 7-14 days, and the drug release time in mice subcutaneous is about 15-25 days.

Embodiment 2

[0101] The method steps of being processed into sustained-release injections are the same as in Example 1, but the difference is that the antibacterial active ingredients and their weight percentages are: 2-50% paromomycin, dibekacin, ribomycin, carbane Namycin, kanamycin B, amikacin B, dideoxykanamycin B, amikacin, rivamycin, tilmicosin, netilmicin , Tobramycin, Sisomicin, Etimicin, Penicillin A, Gentamicin, Vertimicin, Doxycycline, Small Normicin, Isopamicin, Isopamicin, Tylosin, Virginmycin, Salinomycin, Flavomycin, Tylomycin, Telosin, Virginmycin, Hiduramycin, Sisomycin, Lidamycin, Fluoride Benicol, rifaximin, or daptomycin.

Embodiment 3

[0103] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 10,000 into three containers (A), (B) and (C) respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well , add 30mg paromomycin, 30mg dibekacin, 30mg ribomycin respectively in three containers, shake up again and use spray-drying method to prepare containing 30% paromomycin, 30% dibekacin, 30 % Ribomycin Microspheres for Injection. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 500cp-650cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 7-15 days, and the drug release time in mice subcutaneous is about 15-25 days.

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Abstract

A sustained-release injection containing netilmicin comprises sustained-release microspheres and solvent. The microspheres contain sustained-release adjuvants and aminoglycoside antibiotics, and the solvent is a special solvent containing suspending agent such as sodium carboxymethylcellulose and having viscosity of 100-3000cp (20-30 DEG C); and the sustained-release adjuvants are selected from poly(ethylene-co-vinylacetate) (EVAc), polifeprosan, poly(lactic acid) (PLA), poly(lactic-co-glycolic acid) (PLGA), sebacic acid copolymer, albumin glue and gelatin; the sustained-release microspheres can also be made into sustained-release implant or ointment. The sustained-release implant or injection can be locally placed or injected into foci to locally sustained-release of drug for 5-30 days, so as to obtain and maintain local drug effective concentration while remarkably reduce the systemic toxicity of the drug. The sustained-release injection has distinct and unique therapeutic effect on local infection diseases caused by Staphylococci, Streptococci, Peptostreptococcus, Propionibacterium acnes, Enterobacter, Mycobacterium tuberculosis, Gonococcus or Meningococcus, such as chronic osteomyelitis, severe decubital ulcer, refractory skin ulcer, diabetic foot, femoral head necrosis, abscess, etc.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing aminoglycoside antibiotics and an application thereof, belonging to the technical field of medicines. Specifically, the present invention provides a sustained-release injection and a sustained-release implant containing aminoglycoside antibiotics. The sustained-release agent is mainly applied locally, and can obtain and maintain effective drug concentration in the local area of ​​bacterial infection. (2) Background technology [0002] With the advent of antibiotics, bacterial infection became a treatable disease. However, because the treatment is not standardized and the treatment time is long, many patients may forget to dose the medicine in time, which often leads to the emergence of drug resistance. Many bacterial infections that should have been cured have recurred and become chronic lesions. On the one hand, the treatment of drug-resistant patients or recurrent chronic lesion...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/08A61K9/10A61K31/7036A61K47/34A61P31/04A61K47/26A61K47/32A61K47/36A61K47/42
Inventor 孙娟
Owner JINAN SHUAIHUA PHARMA TECH
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