The In Vitro Degradation Kinetics of Polyurethane Prodrug Materials

2011 ◽  
Vol 399-401 ◽  
pp. 1067-1070
Author(s):  
Chun Yan Li ◽  
Cong Cong Hu ◽  
Zhi Guo Wen ◽  
Sheng Xiong Dong

The method of high performance liquid chromatography (HPLC) is established to determine the content of antibacterial agent — ciprofloxacin (CF) in the degradation solution of ciprofloxacin-polyurethane (CFPU) and investigate the in vitro degradation kinetics by plotting and fitting the cumulative release curves to inspect the effects of different medium and different concentrations on drug release. The results showed that the HPLC method is accurate, reliable and simple. The drug-release of CFPU was bioresponsive and could be accorded with first order kinetics. It was observed that CF was released from CFPU by a combination of diffusion and erosion mechanism, mainly in the manner of diffusion in the absence of infection while erosion mechanism in the presence of infection.


2020 ◽  
Vol 16 ◽  
Author(s):  
M. Alarjah

Background: Prodrugs principle is widely used to improve the pharmacological and pharmacokinetic properties of some active drugs. Much effort was made to develop metronidazole prodrugs to enhance antibacterial activity and or to improve pharmacokinetic properties of the molecule or to lower the adverse effects of metronidazole. Objective: In this work, the pharmacokinetic properties of some of monoterpenes and eugenol pro metronidazole molecules that were developed earlier were evaluated in-vitro. The kinetic hydrolysis rate constants and half-life time estimation of the new metronidazole derivatives were calculated using the validated RP-HPLC method. Method: Chromatographic analysis was done using Zorbbax Eclipse eXtra Dense Bonding (XDB)-C18 column of dimensions (250 mm, 4.6 mm, 5 μm), at ambient column temperature. The mobile phase was a mixture of sodium dihydrogen phosphate buffer of pH 4.5 and methanol in gradient elution, at 1ml/min flow rate. The method was fully validated according to the International Council for Harmonization (ICH) guidelines. The hydrolysis process carried out in an acidic buffer pH 1.2 and in an alkaline buffer pH 7.4 in a thermostatic bath at 37ºC. Results: The results followed pseudo-first-order kinetics. All metronidazole prodrugs were stable in the acidic pH, while they were hydrolysed in the alkaline buffer within a few hours (6-8 hr). The rate constant and half-life values were calculated, and their values were found to be 0.082- 0.117 hr-1 and 5.9- 8.5 hr., respectively. Conclusion: The developed method was accurate, sensitive, and selective for the prodrugs. For most of the prodrugs, the hydrolysis followed pseudo-first-order kinetics; the method might be utilised to conduct an in-vivo study for the metronidazole derivatives with monoterpenes and eugenol.



2017 ◽  
Vol 48 ◽  
pp. 468-478 ◽  
Author(s):  
Xuan Li ◽  
Chenglin Chu ◽  
Yalin Wei ◽  
Chenxi Qi ◽  
Jing Bai ◽  
...  


Author(s):  
ARGELIA M. L. LENARDÓN ◽  
PATRICIA M. DE LA SIERRA ◽  
FERNANDA MARINO

Estudou-se a cinética de degradação da mistura dos isômeros alfa e beta Endosulfan em diferentes condições de trabalho. Os compostos foram adicionados em água ultrapura, água do rio, água de rio filtrada e água ultrapura com sais (salinidade similar à agua do rio utilizada). As condições de degradação escolhidas foram: escuridão e duas temperaturas (14+1 ºC e 26+1 ºC). As amostragens foram programadas de modo a se obter dados periódicos mais freqüentes no início da experiência e posteriormente mais espaçados até o seu final (230 dias). As amostras foram submetidas à microextração e analisadas por cromatografia em fase gasosa com detector de Ni63 e coluna Megabore DB-5. A degradação foi descrita de acordo com a cinética de primeira ordem, determinando-se os tempos de meia vida (t1/2) e as energias de ativação (Ea). Os dados obtidos evidenciaram que a temperatura é o fator preponderante, sendo possível deduzir que o alfaendosulfan, exceto para água ultrapura (AU), é mais influenciado pela temperatura do que o beta-endosulfan. O segundo efeito mais importante refere-se ao tipo de água utilizada como matriz, devido à influência da salinidade. PERSISTANCE OF ENDOSULFAN IN STATIC AQUEOUS MEDIUM Abstract Degradation kinetics of a mixture of alpha- and beta-Endosulfan isomers was studied under different conditions. The compounds were spiked in ultrapure water, river water, filtered water and ultrapure water with salts (similar salinity condition to that of the river water used). The degradation conditions chosen were: darkness, two temperatures (14+1 ºC e 26+1 ºC). Samplings were programmed in order to obtain more frequent periodical data in the beginning of the experience and after more spaced until its end (230 days). The samples were submitted to microextraction and then analyzed by gas chromatography through a Ni63 detector equipped with a Megabore DB-5 column. Degradation was described using first-order kinetics to determine half-life times (t1/2) and activation energies (Ea). The data obtained evidenced that temperature is the predominant factor, it can possibly be inferred that alfa-endosulfan is much more influenced than beta-endosulfan except for ultrapure water (UW). The second important effect is the water type used as matrix, due to the influence of salinity.



2013 ◽  
Vol 63 (1) ◽  
pp. 59-69 ◽  
Author(s):  
Atul Awasthi ◽  
Majid Razzak ◽  
Raida Al-Kassas ◽  
Joanne Harvey ◽  
Sanjay Garg

The aim of this study was to evaluate stability characteristics and kinetics behavior of abamectin (ABM) as a 1 % (m/V) topical veterinary solution. During the study, samples stressed at 55 and 70 °C were regularly analyzed for several parameters over 8 weeks on a chromatographic (HPLC) system, using a Prodigy C18, 250 x 4.6 mm, 5-μm, column eluting with 15 : 34 : 51 (V/V/V) water/methanol/ acetonitrile as mobile phase. The HPLC method was validated for precision, accuracy, linearity and specificity, and was found to be stability indicating. The results showed that degradation of ABM followed first-order kinetics and data on loss in kobs (s-1) and half life (t1/2, days) demonstrated ABM showing the maximum stability in glycerol formal. The degradation behavior of ABM varies from solvent to solvent. The effect of added alkali on pH change and loss of ABM was studied and found to be unique for all solvents and very distinct from typical hydrolysis degradation. The present study may serve as a platform to design and develop topical non-aqueous solutions of ABM for veterinary use given no such comprehensive efforts have been published to date on the stability profile of ABM in non-aqueous solvents.



2013 ◽  
Vol 63 (2) ◽  
pp. 223-229 ◽  
Author(s):  
Iqbal Ahmad ◽  
Raheela Bano ◽  
Muhammad Ali Sheraz ◽  
Sofia Ahmed ◽  
Tania Mirza ◽  
...  

The kinetics of photodegradation of levofloxacin in solution on UV irradiation in the pH range 2.0-12.0 has been studied using a HPLC method. Levofloxacin undergoes first-order kinetics in the initial stages of the reaction and the apparent first-order rate constants are of the order of 0.167 to 1.807×10-3 min-1. The rate-pH profile is represented by a curve indicating the presence of cationic, dipolar and anionic species during the reaction. The singly ionized form of the molecule is non-fluorescent and is less susceptible to photodegradation. The increase in the degradation rate in the pH range 5.0-9.0 may be due to greater reactivity of the ionized species existing in that range. The rate appears to vary with a change in the degree of ionization of the species present in a particular pH range and their susceptibility to photodegradation. Above pH 9, the decrease in the rate of photodegradation may be a result of deprotonation of the piperazinyl group. The levofloxacin molecule is more stable in the pH range around 7, which is then suitable for formulation purposes. The photodegradation of levofloxacin was found to be affected by the dielectric constant and viscosity of the medium



2022 ◽  
Vol 52 (5) ◽  
Author(s):  
Renata Oliveira Santos ◽  
Laura Monteiro Keller ◽  
Vanessa Sales de Oliveira ◽  
Carlos Alberto Bucher ◽  
José Lucena Barbosa Junior ◽  
...  

ABSTRACT: This study evaluated the effects of temperature on the pH of extracts of ascorbic acid and anthocyanins from petals of butterfly pea, as well as their in vitro digestive stability in model systems at 60, 70, and 80 °C. The pH values significantly decreased with an increase in the temperature (P < 0.05). The findings were similar for the degradation of anthocyanins and ascorbic acid, which followed first-order kinetics in all the systems. The samples heated at 80 °C presented the highest degradation rate (kobs), as well as higher percentages of degradation at the end of digestive stability in vitro.



Biomaterials ◽  
2000 ◽  
Vol 21 (23) ◽  
pp. 2443-2452 ◽  
Author(s):  
C.M Agrawal ◽  
J.S McKinney ◽  
D Lanctot ◽  
K.A Athanasiou


2012 ◽  
Vol 441 ◽  
pp. 549-554
Author(s):  
Ying Jie Cai ◽  
Xiao Jun Yang ◽  
Dong Sheng Xia ◽  
Qing Fu Zeng

Abstract. Degradation of reactive brilliant red X-3B (X-3B) by a UV/Mn2+/H2O2/micro- aeration method was investigated. The influencing factors of degradation of X-3B including UV irradiation, aeration, pH value, H2O2 concentration and X-3B concentration were examined. The results show that X-3B was effectively degraded by the UV/Mn2+/H2O2/micro-aeration method. The degradation rate of X-3B was obtained from weighted linear least squares analysis of the experimental data, and accorded with the pseudo-first order kinetics equation.



2018 ◽  
Vol 17 (2) ◽  
pp. 167-173
Author(s):  
Md Mokaram Hossain ◽  
Reza Ul Jalil ◽  
Mohammad A Rashid

Ramosetron hydrochloride is the hydrochloride salt of ramosetron, a selective serotonin (5-HT3) receptor antagonist with potential antiemetic activity. Upon administration, ramosetron selectively binds to and blocks the activity of 5-HT subtype 3 (5-HT3) receptors located in the vagus nerve terminal and the vomiting center of central nervous system (CNS), suppressing chemotherapy-induced nausea and vomiting. Degradation of Ramosetron HCl was conducted with 0.1N NaOH at 60°C, 70°C and 80°C to study the reaction kinetics. The reaction rate constants (k) for degradation at 60°C, 70°C and 80°C were -2.2680 molL-1s-1 , -3.3714 molL-1s-1 and -5.3686 molL-1s-1 for zero order and -1.05 x 10-2s-1, -1.60 x 10-2s-1 and -2.70 x 10-2s-1 for first order kinetics, respectively. The activation energy of Ramosetron HCl was found as 10.05 kcalmol-1 by using Arrhenius equation. Dhaka Univ. J. Pharm. Sci. 17(2): 167-173, 2018 (December)



Author(s):  
Xingang Meng ◽  
Lingzhu Chen ◽  
Yuping Zhang ◽  
Deyu Hu ◽  
Baoan Song

Hydrolysis and photolysis kinetics of Fubianezuofeng (FBEZF) in water were investigated in detail. The hydrolysis half-lives of FBEZF depending on pH, initial concentration, and temperature were (14.44 d at pH = 5; 1.60 d at pH = 7), (36.48 h at 1.0 mg L−1; 38.51 h at 5.0 mg L−1; and 31.51 h at 10.0 mg L−1), and (77.02 h at 15 °C; 38.51 h at 25 °C; 19.80 h at 35 °C; and 3.00 h at 45 °C), respectively. The photolysis half-life of FBEZF in different initial concentrations were 8.77 h at 1.0 mg L−1, 8.35 h at 5.0 mg L−1, and 8.66 h at 10.0 mg L−1, respectively. Results indicated that the degradation of FBEZF followed first-order kinetics, as the initial concentration of FBEZF only had a slight effect on the UV irradiation effects, and the increase in pH and temperature can substantially accelerate the degradation. The hydrolysis Ea of FBEZF was 49.90 kJ mol−1, which indicates that FBEZF belongs to medium hydrolysis. In addition, the degradation products were identified using ultra-high-performance liquid chromatography coupled with an Orbitrap high-resolution mass spectrometer. One degradation product was extracted and further analyzed by 1H-NMR, 13C-NMR, 19F-NMR, and MS. The degradation product was identified as 2-(4-fluorobenazyl)-5-methoxy-1,3,4-oxadiazole, therefore a degradation mechanism of FBEZF in water was proposed. The research on FBEZF can be helpful for its safety assessment and increase the understanding of FBEZF in water environments.



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