A novel insulin-sodium oleate complex for oral administration: preparation, characterization and in vivo evaluation

2008 ◽  
Vol 18 (4) ◽  
pp. 239-243 ◽  
Author(s):  
S. Sun ◽  
F. Cui ◽  
Y. Kawashima ◽  
N. Liang ◽  
L. Zhang ◽  
...  
2009 ◽  
Vol 12 (1) ◽  
pp. 129 ◽  
Author(s):  
Zhihong Zhang ◽  
Bo Peng ◽  
Xinggang Yang ◽  
Chao Wang ◽  
Guangmei Sun ◽  
...  

PURPOSE. Find a novel delivery system for oral administration of drugs that have absorption window in the upper part of gastrointestinal (GI) track. METHODS. Dipyridamole was chosen as the model drug. A novel system, which combined the osmotic pump controlled release system and the floating system, was designed; matrix tablets (MT) were prepared for compares. The effects of pH, temperature and hydrodynamic conditions on drug release and the floating behavior of floating osmotic pump system (FOP) were investigated. In vivo evaluation was performed by a three-crossover study in six Beagle dogs relative to the conventional tablet (CT). Cumulative percent input in vivo was compared with that of in vitro release profiles. RESULTS. Floating behavior of FOP, drug releases from FOP and MT were sensitive to pH of dissolution media but not sensitive to temperature; the release of dipyridamole from MT was influenced by stirring rate while drug release from FOP was not. AUC of FOP was larger than MT and CT. The linear correlations between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP-a true zero-order release formula, whereas only a nonlinear correlation was obtained for MT. CONCLUTIONS. FOP could be a novel way for the oral administration for drugs like dipyridamole.


2015 ◽  
Vol 305 (1) ◽  
pp. 139-145 ◽  
Author(s):  
So-Young Ma ◽  
You Ree Nam ◽  
Jongho Jeon ◽  
Jong Kook Rho ◽  
Dong-Eun Lee ◽  
...  

2014 ◽  
Vol 194 ◽  
pp. 323-331 ◽  
Author(s):  
Bettina Ralay-Ranaivo ◽  
Didier Desmaële ◽  
Elsa P. Bianchini ◽  
Elise Lepeltier ◽  
Claudie Bourgaux ◽  
...  

2007 ◽  
Vol 57 (1) ◽  
pp. 111-122 ◽  
Author(s):  
Pradeep Patil ◽  
Vandana Patil ◽  
Anant Paradkar

Formulation of a self-emulsifying system for oral delivery of simvastatin: In vitro and in vivo evaluation The objective of the present work was to formulate a self-emulsifying drug delivery system (SEDDS) for simvastatin, which is widely used in the treatment of hypercholesterolemia and dyslipidemia as an adjunct to diet. Simvastatin SEDDS were formulated using a 1:1 (V/V) mixture of diesters of caprylic/capric acids and polyglycolyzed glycerides with varying concentrations of polyoxy castor oil and C8/C10 mono-/diglycerides. The developed SEDDS were evaluated for turbidimetry, droplet size analysis, drug content and in vitro diffusion profiles. In vivo performance of the optimized formulation was evaluated in rats using pharmacodynamic marker parameters like plasma total cholesterol (CH), triglycerides (TG) and high-density lipoprotein (HDL-CH) for 21 days. SEDDS containing 9.1% (m/m) simvastatin and 23.0% (m/m) of each excipient showed minimum mean droplet size (124 nm) and optimal drug diffusion. This test formulation showed significant reduction in plasma CH and TG (around 5-fold and 4-fold, respectively), while HDL-CH concentration was markedly higher (2-fold) compared a reference simvastatin suspension formulation after oral administration for 21 days of study. Test formulation has shown enhanced pharmacodynamic performance compared to reference formulation in rats. The study illustrated the potential of simvastatin SEDDS for oral administration and its biopharmaceutic performance.


2015 ◽  
Vol 87 (3) ◽  
pp. 1823-1831 ◽  
Author(s):  
MUHAMMAD NAEEM ◽  
NISAR UR RAHMAN ◽  
GUILHERME. D. TAVARES ◽  
SÁVIO F. BARBOSA ◽  
NÁDIA B. CHACRA ◽  
...  

ABSTRACTFlurbiprofen, a potent nonsteroidal anti-inflammatory drug, is widely used for relief of pain in patients suffering from rheumatic diseases, migraine, sore throat and primary dysmenorrheal. However, this drug has many gastrointestinal side effects produced by its oral administration, such as gastric bleeding and peptic ulcer. These effects were responsible for non-compliance among patients, which ultimately results in treatment failure. The physicochemical properties of flurbiprofen, make it a suitable candidate for transdermal drug delivery, which can overcome the drawbacks of oral administration. In this sense, microemulsions have been proved to increase the cutaneous absorption of lipophilic drugs when compared to conventional drug delivery systems. The purpose of this study was to formulate and characterize gel based microemulsions, for topical delivery of flurbiprofen. Different gel bases, containing microemulsion and hydro-alcoholic solution of flurbiprofen, were developed and compared. In vitro study showed that gels containing microemulsion had a higher permeation rate than those containing hydro-alcoholic solutions. Additionally, formulation of Carbopol-I (microemulsion) showed higher percent of inhibition of inflammation than others bases. Further, skin irritation study demonstrated that Carbopol-I was none irritating. Flurbiprofen microemulsion incorporated on Carbopol-I showed physicochemical, in vitro and in vivo characteristics suitable for the development of alternative transdermal delivery formulation.


Toxins ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 489
Author(s):  
Andrea Boente-Juncal ◽  
Sandra Raposo-García ◽  
Carmen Vale ◽  
M. Carmen Louzao ◽  
Paz Otero ◽  
...  

Palytoxin (PLTX) is one of the most poisonous substances known to date and considered as an emergent toxin in Europe. Palytoxin binds to the Na+-K+ ATPase, converting the enzyme in a permeant cation channel. This toxin is known for causing human fatal intoxications associated with the consumption of contaminated fish and crustaceans such as crabs, groupers, mackerel, and parrotfish. Human intoxications by PLTX after consumption of contaminated fishery products are a serious health issue and can be fatal. Different reports have previously explored the acute oral toxicity of PLTX in mice. Although the presence of palytoxin in marine products is currently not regulated in Europe, the European Food Safety Authority expressed its opinion on PLTX and demanded assessment for chronic toxicity studies of this potent marine toxin. In this study, the chronic toxicity of palytoxin was evaluated after oral administration to mice by gavage during a 28-day period. After chronic exposure of mice to the toxin, a lethal dose 50 (LD50) of 0.44 µg/kg of PLTX and a No-Observed-Adverse-Effect Level (NOAEL) of 0.03 µg/kg for repeated daily oral administration of PLTX were determined. These results indicate a much higher chronic toxicity of PLTX and a lower NOAEL than that previously described in shorter treatment periods, pointing out the need to further reevaluate the levels of this compound in marine products.


2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S598-S598 ◽  
Author(s):  
Laurent Martarello ◽  
Vincent J Cunningham ◽  
Julian C Matthews ◽  
Eugenii Rabiner ◽  
Steen Jakobsen ◽  
...  

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