scholarly journals Comparative Study of Chemical Stability of Two H1Antihistaminic Drugs, Terfenadine and ItsIn VivoMetabolite Fexofenadine, Using LC-UV Methods

2019 ◽  
Vol 2019 ◽  
pp. 1-10
Author(s):  
Anna Gumieniczek ◽  
Anna Berecka-Rycerz ◽  
Rafał Pietraś ◽  
Izabela Kozak ◽  
Karolina Lejwoda ◽  
...  

A comparative study of chemical stability of terfenadine (TER) and itsin vivometabolite fexofenadine (FEX) was performed. Both TER and FEX were subjected to high temperature at different pH and UV/VIS light at different pH and then quantitatively analyzed using new validated LC-UV methods. These methods were used to monitor the degradation processes and to determine the kinetics of degradation for both the compounds. As far as the effects of temperature and pH were concerned, FEX occurred more sensitive to degradation than TER. As far as the effects of UV/VIS light and pH were concerned, the both drugs were similarly sensitive to high doses of light. Using all stress conditions, the processes of degradation of TER and FEX followed the first-order kinetics. The results obtained for these two antihistaminic drugs could be helpful in developing their new derivatives with higher activity and stability at the same time.

1969 ◽  
Vol 21 (03) ◽  
pp. 580-593
Author(s):  
L. A Pálos ◽  
G Sas ◽  
A Csurgay

SummaryThe reaction kinetics of the second phase of blood clotting (conversion of fibrinogen to fibrin) has been studied in euglobulin and thrombin-antithrombin systems. It was intended to set up relationships that would make mathematical expression of the processes possible and which would, moreover, help in detecting dynamic and functional relationships characteristic of the mechanism involved in coagulation.The experiments have yielded the following results:1. In the euglobulin solution containing no antithrombin the fibrinogen-thrombin reaction can be characterized with a constant deviation from the first order kinetics.2. The process of thrombin inactivation is a reaction of first order in the initial phase.3. The two basic processes (clotting by thrombin in euglobulin solution, inactivation of thrombin in defibrinated plasma) make it possible to predetermine the thrombin time of citrated plasma. Theoretical and actual clotting times were in good agreement.4. The thrombin time of plasma can be computed even if thrombin is not introduced to the system at one stride but gradually, a manner of administration which is a better imitation of what happening in vivo. 5. In connection with the computation of the “thrombin time” of citrated blood, we determined experimentally (and expressed by means of a function) the modification produced by the corpuscular elements of the blood in the reaction between fibrinogen and thrombin under atraumatic conditions.


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)


1982 ◽  
Vol 55 (1) ◽  
pp. 181-190 ◽  
Author(s):  
Manjit S. Sambhi

Abstract Molecular degradation is the main process occurring during the high temperature oxidative aging of most commercial grades of natural rubber. The degradation as measured in terms of Wallace plasticities exhibit first-order kinetics for about 50% extent of degradation. PRI can now be expressed in terms of the first-order rate constant of degradation and is independent of the initial plasticity of the rubber. The observed first-order behavior has been explained in terms of linear intrinsic viscosities versus Wallace plasticities. PRI can be interpreted in terms of the molecular chain length. Complications can, however, arise if hardening of the rubber can occur concurrently with degradation during the PRI test. We then obtain inflated PRI values which overestimate the abilities of the rubbers to resist molecular breakdown, if PRI is considered to arise from degradation only. Perhaps, in order to nullify any possible hardening contribution to PRI values, the PRI test could be designed for rubbers which have undergone some form of controlled accelerated storage-hardening in a manner that prohibits oxidative degradation.


Author(s):  
Aman ullah Khan ◽  
Javeid Iqbal ◽  
Saif-ur-Rehman Khattak ◽  
Najam-us- Saquib ◽  
Muhammad Saleem Qazi

The effect of reconstitution solvents such as water, 0.5% metronidazole solution, 0.9% sodium chloride and 5% dextrose injections, have been investigated on the kinetics of degradation of cephradineneutralised with L-arginine contained in glass, polyvinylchloride (PVC) and polyethylene pthalate (PET) containers at 5, 15 and 30 oC. The analytical method described in USP-31 for the analysis of cephradineinjection was employed in this study and validation in respect of specificity, linearity, accuracy and precision was observed. The degradation of the compound showed first-order kinetics and the degradation rate constants ‘kobs’ were found in the range of 1.84-3.07 ´ 10-3/h (r2 = 0.990-0.999) at 5 oC, 2.3-4.2 ´ 10-3/h (r2 = 0.993-0.999) at 15 oC and 7.18-9.97 ´ 10-3/h (r2 = 0.998-0.999) at 30 oC, respectively. Cephradineshowed maximum stability in dextrose solution followed by water, sodium chloride and metronidazole injections, however, linear effect of containers on degradation rate could not be established. The  extended degradation did not change the kinetics of the reaction. The abnormal toxicity/ safety test on mice for the admixtures in different containers at various temperatures showed no abnormal toxicity.


1985 ◽  
Vol 86 (1) ◽  
pp. 135-165 ◽  
Author(s):  
M Mahler

In frog sartorius muscle, after a tetanus at 20 degrees C, during which an impulse-like increase occurs in the rate of ATP hydrolysis, the rate of O2 consumption (QO2) reaches a peak relatively quickly and then declines monoexponentially, with a time constant not dependent on the tetanus duration (tau = 2.6 min in Rana pipiens and 2.1 min in Rana temporaria). To a good approximation, these kinetics are those of a first-order impulse response, and the scheme of reactions that couple O2 consumption to extramitochondrial ATP hydrolysis thus behaves as a first-order system. It is first deduced and then demonstrated directly that while QO2(t) is monoexponential, it changes in parallel with the levels of creatine and phosphorylcreatine, with proportionality constants +/- 1/tau p, where p is the P/O2 ratio in vivo. From this, it is further deduced that the mitochondrial creatine kinase (CK) reaction is pseudo-first order in vivo. The relationship between [creatine] and QO2 predicted by published models of the control of respiration is markedly different from that actually observed. As shown here, the first-order kinetics of QO2 are consistent with the hypothesis that respiration is rate-limited by the mitochondrial CK reaction; this has as a corollary the "creatine shuttle" hypothesis.


2019 ◽  
Author(s):  
Chem Int

The kinetics of oxidation of methyl orange by vanadium(V) {V(V)} has been investigated in the pH range 2.3-3.79. In this pH range V(V) exists both in the form of decavanadates and VO2+. The kinetic results are distinctly different from the results obtained for the same reaction in highly acidic solution (pH < 1) where V(V) exists only in the form of VO2+. The reaction obeys first order kinetics with respect to methyl orange but the rate has very little dependence on total vanadium concentration. The reaction is accelerated by H+ ion but the dependence of rate on [H+] is less than that corresponding to first order dependence. The equilibrium between decavanadates and VO2+ explains the different kinetic pattern observed in this pH range. The reaction is markedly accelerated by Triton X-100 micelles. The rate-[surfactant] profile shows a limiting behavior indicative of a unimolecular pathway in the micellar pseudophase.


1939 ◽  
Vol 23 (1) ◽  
pp. 21-39 ◽  
Author(s):  
Aurin M. Chase ◽  
Emil L. Smith

1. Measurements of visual purple regeneration in solution have been made by a procedure which minimized distortion of the results by other color changes so that density changes caused by the regenerating substance alone are obtained. 2. Bleaching a visual purple solution with blue and violet light causes a greater subsequent regeneration than does an equivalent bleaching with light which lacks blue and violet. This is due to a photosensitive substance which has a gradually increasing effective absorption toward the shorter wavelengths. It is uncertain whether this substance is a product of visual purple bleaching or is present in the solution before illumination. 3. The regeneration of visual purple measured at 560 mµ is maximal at about pH 6.7 and decreases markedly at more acid and more alkaline pH's. 4. The absorption spectrum of the regenerating material shows only a concentration change during the course of regeneration, but has a higher absorption at the shorter wavelengths than has visual purple before illumination. 5. Visual purple extractions made at various temperatures show no significant difference in per cent of regeneration. 6. The kinetics of regeneration is usually that of a first order process. Successive regenerations in the same solution have the same velocity constant but form smaller total amounts of regenerated substance. 7. In vivo, the frog retina shows no additional oxygen consumption while visual purple is regenerating.


1985 ◽  
Vol 18 (4) ◽  
pp. 251-255 ◽  
Author(s):  
A. L. Melo ◽  
L.H. Pereira

To study the cercaria-schistosomulum transformation in vivo, underthe influence of an antischistosomal compound (oxamniquine), a model using cercarial infections into the abdominal cavity of mice was chosen. This procedure provided easy and reproducible recoveries of larvae from peritoneal washings with appropriate solutions for a long time (30 to 180 min) after inoculation. The results show that high doses of oxamniquine (given intramuscularly one hour before the infection) produce a marked delay in the kinetics of the cercaria-schistosomulum transformation. Cercariae, tail-less cercarial bodies and schistosomula were recovered from the peritoneal cavity ofdrug treated mice in numbers significantly different from those recovered from untreated mice.


1992 ◽  
Vol 73 (5) ◽  
pp. 1939-1945 ◽  
Author(s):  
E. M. Postlethwait ◽  
S. D. Langford ◽  
A. Bidani

We previously showed, during quasi-steady-state exposures, that the rate of inhaled NO2 uptake displays reaction-mediated characteristics (J. Appl. Physiol. 68: 594–603, 1990). In vitro kinetic studies of pulmonary epithelial lining fluid (ELF) demonstrated that NO2 interfacial transfer into ELF exhibits first-order kinetics with respect to NO2, attains [NO2]-dependent rate saturation, and is aqueous substrate dependent (J. Appl. Physiol. 71: 1502–1510, 1991). We have extended these observations by evaluating the kinetics of NO2 gas phase disappearance in isolated ventilating rat lungs. Transient exposures (2–3/lung at 25 degrees C) employed rebreathing (NO2-air) from a non-compliant continuously stirred closed chamber. We observed that 1) NO2 uptake rate is independent of exposure period, 2) NO2 gas phase disappearance exhibited first-order kinetics [initial rate (r*) saturation occurred when [NO2] > 11 ppm], 3) the mean effective rate constant (k*) for NO2 gas phase disappearance ([NO2] < or = 11 ppm, tidal volume = 2.3 ml, functional residual capacity = 4 ml, ventilation frequency = 50/min) was 83 +/- 5 ml/min, 4) with [NO2] < or = 11 ppm, k* and r* were proportional to tidal volume, and 5) NO2 fractional uptakes were constant across [NO2] (< or = 11 ppm) and tidal volumes but exceeded quasi-steady-state observations. Preliminary data indicate that this divergence may be related to the inspired PCO2. These results suggest that NO2 reactive uptake within rebreathing isolated lungs follows first-order kinetics and displays initial rate saturation, similar to isolated ELF.(ABSTRACT TRUNCATED AT 250 WORDS)


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