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Medicament for treatment of diabetic foot infections

一种糖尿病足、细菌感染的技术，应用在药物输送、医药配方、抗细菌药等方向，能够解决患者置之不理等问题

Pending Publication Date: 2018-11-09
DEBIOPHARM INTERNATIONAL SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The infection may remain undetected by the patient, or may be ignored by the patient

Method used

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  • Medicament for treatment of diabetic foot infections
  • Medicament for treatment of diabetic foot infections
  • Medicament for treatment of diabetic foot infections

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0118] A preferred embodiment of the present invention uses Compound A or a pharmaceutically acceptable salt thereof to treat diabetic foot osteomyelitis. A particularly preferred aspect of this preferred embodiment is the use of the bis(ethanolammonium) salt of Compound A. Another particularly preferred aspect of this preferred embodiment is the treatment of diabetic foot osteomyelitis caused by S. aureus infection. Another particularly preferred aspect of this preferred embodiment is the treatment of diabetic foot osteomyelitis associated with severe ischemia. Another particularly preferred embodiment is the administration of Compound A by intravenous administration in the dose range of 40 mg BID to 160 mg BID or TID, or by oral administration in the dose range of 40 mg BID to 240 mg BID or TID. Even more preferred embodiments are characterized by simultaneous realization of two or more of these particularly preferred aspects.

Embodiment 1

[0120] Embodiment 1: PDE3 inhibition test

[0121] Introduction: Cyclic nucleotide phosphodiesterases (PDEs) are enzymes that regulate cellular levels of cAMP and cGMP by controlling the rate of degradation of the second messengers cAMP and cGMP. PDE3A and PDE3B are members of the PDE3 family. Inhibition of PDE3 prevents cAMP fragmentation, thereby increasing its intracellular concentration. The intracellular concentration of cAMP plays an important second messenger role, such as regulating myocardial contraction and vascular smooth muscle contraction (1. Bender AT, Beavo JA: Cyclic nucleotidephosphodiesterases: molecular regulation to clinical use. Pharmacol. Rev. (2006) 58 (3 ):488-520).

[0122] Materials / Methods: Caliper mobility assay was used in the enzyme phosphodiesterase assay (2. Card A1, Caldwell C, Min H et al.: High-throughput biochemical kinase selectivity assays: panel development and screening applications, J Biomol Screen.( 2009); 14(1):31-42) The inhibitor...

Embodiment 2

[0125] Example 2: In vitro vasodilation test of rabbit saphenous vein model

[0126] Materials / Methods: The vasodilatory effect of Compound B was assessed using isolated rabbit saphenous vein tissue. Rabbits were killed by blows on the head, followed by cervical dislocation and exsanguination. A segment of the saphenous vein is carefully excised. The vein was cleared of all fat and connective tissue and cut into 2.5 mm long rings. Mount the ring horizontally in a 20 ml organ bath filled with Krebs solution maintained at 37.7 ± 0.5 °C and filled with 95% O 2 and 5% CO 2 of mixed gas. The composition of Krebs solution is as follows (mM): NaCl:118.0 / KCl:5.0 / CaCl 2 :2.6 / MgSO 4 (7H 2 O): 1.2 / NaHCO 3 :24.9 / KH 2 PO 4 :1.2 / glucose: 10.0. The pH is 7.40 ± 0.05. The rings were equilibrated for 60 minutes at an optimal resting tension of 1 g. Contraction tension was measured using an isometric force transducer and the signal was analyzed using dedicated software (IOX version...

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Abstract

The present invention provides means and methods for treating diabetic foot infections. In particular, drug compounds are provided that combine a high therapeutic activity against Staphylococcus Spp.bacteria with a high degree of bone penetration and vasodilatory effects. This unique combination of properties allows to accomplish high local concentrations of the drug at the site of infection evenin diabetic foot patients typically having poor blood perfusion at the site of infection.

Description

technical field [0001] The present invention provides means and methods for treating bacterial infections associated with diabetic foot syndrome or other bacterial infections of the foot associated with peripheral ischemia. Background technique [0002] Diabetic foot syndrome is a pathology often associated with ulcers and bacterial infections. This bacterial infection is hereinafter identified as a diabetic foot infection. Treatment of diabetic foot infections is often hampered by the ischemia that is often associated with diabetic foot syndrome. Thus, systemic administration of antibiotics will enable low plasma levels of antibiotic drugs only at the site of infection. This problem is especially acute if the infection is caused by resistant bacteria such as methicillin-resistant Staphylococcus aureus (MRSA). [0003] The condition is further exacerbated by the fact that diabetics often suffer from peripheral neuropathy. These people may have a diabetic foot infection w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/675A61K31/4375A61P31/04
CPCA61K31/4375A61K31/675A61P31/04A61K45/06A61K9/0019A61K9/0053
Inventor G·乌阿尼奥克斯L·卡迪F·威特基
Owner DEBIOPHARM INTERNATIONAL SA