Formulation and thermal sterile stability of a less painful intravenous clarithromycin emulsion containing vitamin E

Lü, Yan; Wang, Yanjiao

doi:10.1016/j.ijpharm.2007.06.003

Cited by 40 publications

(12 citation statements)

References 30 publications

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“…compound concentration and intestinal perfusion rate), and the ability to study regional differences (Song et al, 2006;Wu et al, 2004;Zakeri-Milani et al, 2009b). Clarithromycin (CLA) 6-O-methylerythromycin, is a semi-synthetic macrolide antibiotic with a broad antibacterial spectrum which is used in many infectious conditions like upper and lower respiratory tracts infections, skin, ear and other soft tissues infections, caused by different bacterial groups (Alkhalidi et al, 2008;Gomez-Burgaz et al, 2009;Lu et al, 2008). Clarithromycin is also the drug of choice to treat peptic ulcer as H. pylori resistance rate is much lower for clarithromycin as compared to other antibiotics like amoxicillin and tetracycline (Jain et al, 2006; Zakeri-Milani et al, 2005).…”

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confidence: 99%

A study on enhanced intestinal permeability of clarithromycin nanoparticles

Zakeri–Milani

Islambulchilar

Majidpour

et al. 2014

Braz. J. Pharm. Sci.

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The main objective of the present study was to determine the permeability of clarithromycin (CLA)-PLGA nanoparticles using single-pass intestinal perfusion technique in rats. Clarithromycin nanoparticles were prepared by nano-precipitation according to the modified quasi emulsion solvent diffusion technique and evaluated for their physicochemical characteristics. Permeability coefficients (P eff ) in anaesthetized rats were determined at 3 different concentrations. Drug solution or suspensions in PBS was perfused through a cannulated jejunal segment and samples were taken from outlet tubing at different time points up to 90 min. Microbiological assay of CLA and phenol red in the samples were analyzed using an agar well diffusion procedure and HPLC method respectively. The average particle size of prepared nanoparticles was 305 ± 134 nm. The mean P eff of CLA solution in concentrations of 150, 250 and 400 µg/mL was found to be 1.20 (±0.32) ×10 -3 , 9.62 (±0.46) ×10 -4 , and 1.36 (±0.95) ×10 -3 cm/sec, respectively. The corresponding values for the same concentration of nanoparticles were found to be 2.74 (±0.73) ×10 -3 , 2.45 (±0.88) ×10 -3 , and 3.68 (±0.46) ×10 -3 cm/s, respectively. The two-tailed Student's t-test showed that the intestinal permeability of CLA nanoparticle suspensions in prepared concentrations were significantly increased in comparison with its solution.Uniterms: Clarithromycin/nanoparticles/ permeability. Single-Pass Intestinal Perfusion. Intestinal permeability.O objetivo principal do presente estudo foi determinar a permeabilidade de nanopartículas de claritromicina (CLA)-PLGA, utilizando a técnica de perfusão intestinal de passo único em ratos. As nanopartículas de claritromicina foram preparadas por nanoprecipitação, de acordo com a técnica modificada de difusão de solvente quase-emulsão, e suas características físico-químicas avaliadas. Os coeficientes de permeabilidade (P eff ) em ratos anestesiados foram determinados em três concentrações diferentes. A solução, ou suspensões, do fármaco em PBS foi perfundida através do segmento de jejuno canulado e as amostras foram tomadas do tubo externo em diferentes tempos até 90 minutos. Os ensaios microbiológico de CLA e de vermelho de fenol das amostras foram realizados, utilizando-se o procedimento de difusão em poço de ágar e de CLAE, respectivamente. O tamanho médio das partículas das nanopartículas preparadas foi de 305 ± 134 nm. O P eff médio da solução de CLA em concentrações de 150, 250 and 400 µg/mL foi de 1.20(±0.32)×10 -3 , 9.62(±0. INTRODUCTIONOral administration remains the most convenient and useful route for delivering most pharmaceutical agents. However, the major problem of many orally administered drugs is to overcome several barriers before reaching their target site (Cook, Shenoy, 2003;Rao et al., 2008). Several approaches have been applied in order to improve the oral bioavailability of poorly permeable and soluble compounds intended for oral administration. Using nanoparticulate drug delivery system is considered as one of...

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confidence: 99%

A study on enhanced intestinal permeability of clarithromycin nanoparticles

Zakeri–Milani

Islambulchilar

Majidpour

et al. 2014

Braz. J. Pharm. Sci.

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“…Poloxamer 188 (Pluronic F68 [F68], Sigma Chemical Co., St Louis, MO; MW 8400) is a nonionic block copolymer chemical surfactant known to be cytoprotective against hydrodynamic stress. The pluronic polymers have also been widely used as additives in the preparation of intravenously (IV) administered drugs 9,10 or cell cultures 11 . However, there are no reports describing the effect of this additive on in vitro mass production of RBCs, despite its wide usage and safe IV application in vivo 12 .…”

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Stroma‐free mass production of clinical‐grade red blood cells (RBCs) by using poloxamer 188 as an RBC survival enhancer

Baek

Kim

et al. 2009

Transfusion

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“…The optimal emulsifier dosage was 3 and 0.4% for Lipoid S75® and F‐68, respectively. Less emulsifier could not adequately strengthen and uniformly disperse in the emulsifier interfacial film to obtain a good emulsification effect 14 and, at low surfactant concentration, the emulsion was not stable due to agglomeration of the oil droplets, also at high surfactant concentrations, the emulsion destabilization would occur as a result of rapid coalescence 15. Sodium oleate (SO), with a concentration of 0.05% was often used in commercial parenteral emulsions (Lipofundin®MCT, Abbolipid®, Schiwalipid®, and others) to obtain stable formulations during the autoclaving process 16.…”

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confidence: 99%

Intravenous bufadienolides‐loaded lipid microspheres for improving chemical stability

Weng

Chen

et al. 2010

Euro J Lipid Sci & Tech

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This study focused on the degradation kinetics of bufalin (B), cinobufagin (C), and resibufogenin (R) in bufadienolides-loaded lipid microsphere (BU-LM) and bufadienolides-loaded aqueous solution (BU-S). The chemical stability of bufadienolides both in BU-LM and BU-S at different pH values and temperatures was monitored by HPLC. Photon correlation spectroscopy and electrophoretic light scattering technology were used to evaluate the physical characteristic of BU-LM. Under the most stable pH range of 6.0-6.5, the half-lives of B, C, and R in BU-LM were 22, 15, and 20 days at 80 8C but 4510, 1717, and 3300 days at 25 8C, whereas for BU-S only 11, 3, and 10 days at 80 8C and 71, 18, and 49 days at 25 8C. The results indicated that BU-LM significantly increased the chemical stability of bufadienolides, especially at low temperatures. The degradation of bufadienolides took place mostly in the aqueous phase and the diffusion process of bufadienolides from the oil phase through the interfacial layer to the aqueous phase was the rate-limiting step for the drug degradation. A low temperature slowed down of the diffusion rate leading to a slower degradation and longer half-lives. Among the three bufadienolides in BU-LM, C was protected from degradation to the greatest extent.Practical applications: Bufadienolides, consisting of bufalin (B), cinobufagin (C), and resibufogenin (R) have poor aqueous solubility between 20 and 60 mg/mL and are easily degradable by acids or bases. Here we propose a new strategy to overcome stability problems by using lipid microspheres (LM) as the drug vehicle. By incorporating the drugs into the interior oil phase and the oil-water interfacial film, a direct contact of the drug with body fluids and tissues is avoided. Thus the drug is protected from degradation and possible side effects are minimized. Our results indicate that BU-LM significantly increased the chemical stability of bufadienolides, especially at low temperatures. Among the three bufadienolides in BU-LM, C was protected from degradation to the greatest extent.

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Formulation and thermal sterile stability of a less painful intravenous clarithromycin emulsion containing vitamin E

Cited by 40 publications

References 30 publications

A study on enhanced intestinal permeability of clarithromycin nanoparticles

A study on enhanced intestinal permeability of clarithromycin nanoparticles

Stroma‐free mass production of clinical‐grade red blood cells (RBCs) by using poloxamer 188 as an RBC survival enhancer

Intravenous bufadienolides‐loaded lipid microspheres for improving chemical stability

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