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Havlickova B.,Intendis GmbH | Havlickova B.,Charles University
Alimentary Pharmacology and Therapeutics | Year: 2010

Topical corticosteroids and local anaesthetics have been used for many years to relieve symptoms of anorectal diseases, such as pain, pruritus and bleeding. Few clinical trials have been published to allow comparisons of different combinations or different formulations, mainly because many of these products came to market before stringent peer review of clinical trials data was a prerequisite for registration. This article highlights why topical medications are necessary for the treatment of anorectal diseases, especially of inflammatory symptoms of haemorrhoids, anal eczema and others, particularly with respect to improving the quality of life of patients living with the pain and discomfort associated with such symptoms. It also demonstrates the efficacy and safety of combinations of topical corticosteroids and local anaesthetics in cream and suppository through reference to published clinical trials data, previously unpublished clinical trials data and real life clinical experience with these products. © 2010 Blackwell Publishing Ltd.


Lenhard D.C.,Bayer AG | Pietsch H.,Bayer AG | Sieber M.A.,Intendis GmbH | Ernst R.,Bayer AG | And 3 more authors.
Investigative Radiology | Year: 2012

OBJECTIVE: Nonionic iodinated contrast agents (CAs) can be divided into monomeric, low-osmolar, and dimeric, iso-osmolar classes. In clinical practice, renal tolerance of CAs is a concern, especially in patients with impaired renal function. With regard to renal safety, we wanted to evaluate the role of osmolality and viscosity in renal tolerance. MATERIAL AND METHODS: We generated a formulation (iodixanol/mannitol) consisting of the dimeric iodixanol with an osmolality of the monomeric iopromide. Male Han-Wistar rats were intravenously injected with low-osmolar iopromide 300, iso-osmolar iodixanol 320, and iodixanol/mannitol. Saline and diatrizoate were used as controls. A total number of 227 rats were used in the following experiments. We compared the impact of osmolality on renal iodine retention using computed tomography 2 and 24 hours postinjection (p.i.). The animals were killed 2, 24, and 72 hours after injection, and the kidneys were excised for further investigations. Changes in renal cell proliferation were analyzed by 5-bromo-2′-deoxyuridine incorporation 48 hours p.i. as a degree of tissue regeneration after induced injury. To specify potential renal injury, we quantified the expression of acute kidney injury (AKI) markers (kidney injury marker-1 [KIM-1], neutrophil gelatinase-associated lipocalin [NGAL], and plasminogen activator inhibitor-1 [PAI-1]) by quantitative real-time polymerase chain reaction. Furthermore, the kidneys were analyzed histologically, including immunofluorescence analysis. RESULTS: After intravenous application of the CAs into Han-Wistar rats, renal iodine concentration was increased (3-fold) for iodixanol 2 hours p.i. and iodine retention was detected to be prolonged 24 hours p.i. compared with iopromide injection (iodixanol, 520 ± 50 Hounsfield Units [HU] vs iopromide, 42 ± 5 HU). The higher iodine concentration 2 hours p.i. upon iodixanol injection was reduced almost to the level of iopromide when injecting iodixanol/mannitol (iopromide: 289 ± 68 HU vs iodixanol/mannitol: 343 ± 68 HU). In addition, iodixanol application induced increased renal cell proliferation (2.7-fold vs saline), indicating renal injury, which was significantly lower in iopromide-treated animals (1.6-fold vs saline). More detailed analysis of markers for AKI revealed that iodixanol significantly induced the expression of PAI-1 (7.7-fold at 2 hours) as well as KIM-1 (2.1-fold) and NGAL (3.2-fold) at 2 and 24 hours when compared with saline treatment. In contrast, the expression of markers for AKI was low after iopromide (1.4-fold NGAL, 1.7-fold PAI-1, KIM-1 not significant) and iodixanol/mannitol (1.6-fold NGAL, 2.6-fold PAI-1, KIM-1 not significant) injection. CONCLUSION: The present results clearly show that prolonged iodine retention and the enhanced expression of kidney injury markers are caused mainly by the explicitly higher urine viscosity induced by iodixanol. We conclude that the osmolality of low-osmolar CAs such as iopromide induces a positive diuretic effect that is responsible for rapid iodine clearance and prevents increased expression of acute injury markers in the kidney. ©2012 by Lippincott Williams & Wilkins.


Jost G.,Bayer AG | Lenhard D.C.,Bayer AG | Sieber M.A.,Intendis GmbH | Lengsfeld P.,Bayer AG | And 2 more authors.
Investigative Radiology | Year: 2011

Objective: X-ray contrast agents (CA) possess specific physicochemical properties and are excreted renally by glomerular filtration. Thereby, they may affect the diffusion of water molecules within the kidney. The aim of our preclinical study was to investigate potential changes in the apparent diffusion coefficient (ADC) of the kidney after administration of monomeric, low-osmolar, and dimeric, iso-osmolar CA by using diffusion-weighted magnetic resonance imaging (DWI). MATERIAL AND METHODS:: First, the relationship between CA viscosity and the ADC of water was assessed by phantom measurements. Subsequently, Han Wistar rats (8 per group) received an intravenous injection of iso-osmolar CA (iodixanol) or low-osmolar CA (iopromide) at a dosage of 4 gI/kg body weight. The control group received saline (0.9% NaCl) at the same volume. The renal ADC was dynamically monitored up to 40 minutes postinjection (p.i.) by DWI using a 1.5-T clinical MR unit. After DWI, the animals were killed and the kidneys were removed for iodine measurements by X-ray fluorescence analysis. RESULTS:: The in vitro measurements yielded an inverse relationship between increasing viscosity and decreasing water diffusion. In vivo, a slight increase in ADC was observed immediately after administration of the low-osmolar iopromide (ΔADC = 80 ± 78 μm/s) and saline (ΔADC = 89 ± 53 μm/s), which normalized to the baseline level at 40 minutes p.i. In contrast, a strong decrease in ADC was observed after administration of the iso-osmolar iodixanol. This was most prominent 12 minutes p.i. (ΔADC =-555 ± 194 μm/s) and persisted throughout the investigation. Concomitantly, the kidney iodine concentration 50 minutes p.i. was significantly higher after iodixanol (58.6 ± 5.3 mgI/g kidney) compared with iopromide injection (18.4 ± 4.5 mgI/g kidney). CONCLUSION:: A significant difference in the renal ADC was observed between the low-osmolar CA/saline and the iso-osmolar CA. The in vitro measurements suggest that the substantial decrease in ADC observed after administration of the iso-osmolar CA is based on the high viscosity of the agent during renal passage. This, in turn, may explain the delayed iodine retention after administration of iso-osmolar CA and demonstrates the importance of the physicochemical properties of CA during their renal elimination. © 2011 by Lippincott Williams & Wilkins.


Patent
Intendis Gmbh | Date: 2011-05-26

The present patent application relates to an azelaic acid-comprising pharmaceutical composition, preferably an azelaic acid-comprising gel, with added pigment, which composition can be used, inter alia, for treating rosacea and acne, and also to a process for its preparation.


The present patent application is related to a hydrogel composition which is essentially free of active drugs for the manufacture of a product for the treatment of dermatological disorders, especially perioral dermatitis, acne or seborrheic dermatitis which hydrogel comprises propylene glycol, polyacrylic acid, lecithin and medium chain triglycerides or macrogol-glycerol hydroxystearate.


The present invention related to a pharmaceutical composition which is esentially free of pharmaceutically active ingredients for the treatment of human skin. The composition according to the invention is especially useful in the treatment of rosacea, acne, atopic dermatitis, contact dermatitis, perioral dermatitis, psoriasis or neurodermitis.


The present invention related to the use of a pharmaceutical composition which is essentially free of pharmaceutically active ingredients for the treatment of human skin, especially in the treatment of rosacea, acne, atopic dermatitis, contact dermatitis, perioral dermatitis, psoriasis or neurodermitis, as well as for prophylactic and/or cosmetic purposes.


In order to make available another therapeutic possibility for rosacea the use of at least one ,-n-alkanedicarboxylic acid with 7 to 13 carbon atoms or its esters and at least one retinoid for producing a pharmaceutical preparation is proposed. The suggested formulation is also effective in treatment of other inflammatory skin diseases such as psoriasis, atopic dermatitis and common acne.


The present patent application is related to a hydrogel composition which is essentially free of active drugs for the manufacture of a product for the treatment of dermatological disorders, especially perioral dermatitis, acne or seborrheic dermatitis.


The current invention describes novel chiral synthetic routes and intermediates for the manufacture of chiral anti-inflammatory agents of general formula VIII in which at least one of the groups X^(1), X^(2), X^(3 )is selected from fluoro, chloro, bromo, hydroxy, methoxy, ethoxy, trifluoromethyl, amino whereas the other groups X^(1), X^(2), X^(3 )have the meaning of a hydrogen atom,in which at least one of the groups Z^(1), Z^(2), Z^(3 )is selected from O, S, N(CH_(3)), whereas the other groups Z^(1), Z^(2), Z^(3 )have the meaning of a CH_(2) group,and in which Ar is an aromatic group.

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