Stability and thermophysical properties of azithromycin dihydrate

Timoumi, S.; Mangin, Denis; Peczalski, Roman; Zagrouba, Féthi; Andrieu, Julien

doi:10.1016/j.arabjc.2010.10.024

Cited by 30 publications

(24 citation statements)

References 8 publications

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“…This corroborated rates of recrudescence reported on the disease and the possibility of paying less attention to a seemingly resolved BU lesion. Recurrence is an important reality in BU management and antimicrobials such as azithromycin can play a very important role, particularly in the preulcerative and postsurgical periods in BU disease due to their stability and their penetrative capacity [33–35]. Additionally, multidrug regimens containing azithromycin may help control secondary bacterial infections sometimes seen in BU patients.…”

Section: Discussionmentioning

confidence: 99%

In Vitro Susceptibility ofMycobacterium ulceransIsolates to Selected Antimicrobials

Owusu

Newman

Addo

et al. 2017

Canadian Journal of Infectious Diseases and Medical Microbiolog

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Background. The current definitive treatment of Buruli ulcer with antibiotics makes the issue of antimicrobial drug resistance an unavoidable one. This is as a result of drug misuse by health personnel and patients' noncompliance to treatment regimen. Monitoring of these factors and screening for new effective antimicrobials are crucial to effective management of Buruli ulcer disease. This study therefore investigated the inhibitory activity of some antibiotics against isolates of Mycobacterium ulcerans. Methods. Activity of eight antibiotics was tested against twelve M. ulcerans isolates (2 reference strains and 10 clinical isolates). The anti-M. ulcerans activities were determined by the agar dilution method and the minimum inhibitory concentrations (MICs) were determined by the agar proportion method. Results. All antimicrobials investigated had activity against M. ulcerans isolates tested. The MICs ranged from 0.16 μg/mL to 2.5 μg/mL. Azithromycin recorded the highest inhibitory activity at a mean MIC of 0.39 μg/mL, whilst clofazimine a second-line antileprosy drug, recorded the lowest at a mean MIC of 2.19 μg/mL. Among the four antituberculosis drugs, rifampicin had the highest activity with a mean MIC of 0.81 μg/mL. Conclusion. Azithromycin could be considered as a lucrative alternative to existing treatment methods for inhibiting M. ulcerans in Ghana.

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Section: Discussionmentioning

confidence: 99%

In Vitro Susceptibility ofMycobacterium ulceransIsolates to Selected Antimicrobials

Owusu

Newman

Addo

et al. 2017

Canadian Journal of Infectious Diseases and Medical Microbiolog

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“…According to the Biopharmaceutical Classification System, AZT can be classified as a class II drug; therefore, the rate-limiting step in the process of drug absorption is the dissolution of the drug, which accounts for its low bioavailability. 6,7 Furthermore, it is a substrate of the p-glycoprotein transport system, which is further responsible for its low bioavailability due to ileal clearance (biliary plus intestinal excretion clearance). 8,9 Therefore, the present investigation aimed to prepare and characterize azithromycin loaded SLNs using stearic acid with different surfactant combinations with a view to improve the solubility of AZT.…”

Section: Introductionmentioning

confidence: 99%

Effect of Surfactant on Azithromycin Dihydrate Loaded Stearic Acid Solid Lipid Nanoparticles

Bhattacharyya¹,

Reddy²

2019

tjps

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ÖZAmaç: Azitromisin dihidrat, çeşitli bakteriyel enfeksiyon tiplerinin tedavisinde kullanılan bir makrolid antibiyotiktir. Etkin madde düşük çözünürlüğü nedeniyle düşük oral biyoyararlanım gösterir. Bu çalışmada, etken maddenin çözünürlüğünü ve çözünme hızını arttırmaya yönelik olarak azitromisin dihidratın katı lipit nanopartikülleri formüle edilmiştir. Gereç ve Yöntemler: Azitromisin dihidrat yüklü stearik asit nanopartikülleri, etken madde miktarını sabit tutarken, farklı lipit yüzey aktif madde oranında üç farklı yüzey aktif madde, Tween 20, Poloksamer 188 ve Poloksamer 407 kullanılarak yüksek hızlı homojenizasyon yöntemi ile formüle edilmiştir. Bu yöntemle on iki formülasyon hazırlanmıştır. Elde edilen nanopartiküller etken madde içeriği, % etken madde yükleme, % enkapsülasyon etkinliği, partikül boyutu analizi, zeta potansiyeli, yüzey morfolojisi, Fourier Transmisyon kızılötesi spektroskopisi, in vitro etken madde salımı, stabilite çalışması için değerlendirilmiştir. Bulgular: Tüm formülasyonlar, iyi yükleme etkinliği ve lenfatik absorpsiyon için uygun bir partikül büyüklüğü ile yüksek oranda in vitro salım göstermiştir. Poloksamer 188 ile formüle edilen nanopartiküller, diğer sürfaktanlara kıyasla daha iyi özellikler göstermiştir. Sonuç: Bu çalışma, yüksek hızlı homojenizasyon yöntemiyle hazırlanan azitromisin dihidratın stearik asit nanopartiküllerinin, çözünmenin ve dolayısıyla ilacın oral biyoyararlanımının iyileştirilmesi için kullanılabileceğini göstermiştir. Anahtar kelimeler: Azitromisin dihidrat, katı lipit nanopartiküller, zeta potansiyeli, partikül büyüklüğü, enkapsülasyon verimi, ilaç salımı Objectives: Azithromycin dihydrate is a macrolide antibiotic used for the treatment of several types of bacterial infections. The drug shows low oral bioavailability due to its low solubility. In the present work solid lipid nanoparticles of azithromycin dihydrate were formulated, keeping in view enhancement of the solubility and rate of dissolution of the drug. Materials and Methods: Azithromycin dihydrate loaded stearic acid nanoparticles were formulated by high shear homogenization using three different surfactants, namely Tween 20, poloxamer 188, and poloxamer 407, at a varied lipid surfactant ratio while keeping the quantities of the active ingredient constant. Twelve such formulations were prepared. The nanoparticles obtained were evaluated for drug content, % drug loading, % entrapment efficiency, particle size analysis, zeta potential, surface morphology, Fourier transmission infrared spectroscopy, in vitro drug release, and stability. Results: All the formulations showed good entrapment efficiency and high percentage of in vitro release with a particle size suitable for lymphatic absorption. The nanoparticles formulated with poloxamer 188 showed better characteristics compared to the other surfactants. Conclusion: This study indicates that stearic acid nanoparticles of azithromycin dihydrate prepared by high shear homogenization can be successively used for improvement of dissolution and thereby ora...

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“…The temperature of the second endotherm matches with the reported melting point of anhydrous AZI. 25 It is interesting to note that the product phase obtained by dehydration of the MH melted at 116 • C, whereas the dehydration product of the DH melted at 125 • C (Fig. 4).…”

Section: Characterization Of Drug Substancementioning

confidence: 96%