scholarly journals COMPARATIVE STUDY OF PHARMACOKINETICS OF OFLOXACIN IN A FREE AND NIOSOMAL FORMS IN EXPERIMENTS ON WHITE MICE WHEN ADMINISTERED Per Os

2015 ◽  
Vol 69 (1-2) ◽  
pp. 80-84
Author(s):  
A. N. Kulichenko ◽  
M. E. Mikhailova ◽  
D. A. Kovalev ◽  
S. V. Pisarenko ◽  
U. V. Siriza ◽  
...  

Aim: to study features of pharmacokinetics of ofloxacin as a part of anion PEGylated niosomes on a basis of sorbitan monostearate (Span 60) to experimental white mice per os. Materials and methods: ofloxacin was entrapped in niosomes consisting of Span 60, cholesterol, PEG 4000 and dicetylphosphate. Sizes of niosomes estimated by means of probe microscopy. Efficiency of inclusion of an antibiotic in niosomes defined after removal of free drug by a centrifugation. The analysis of the quantitative contents of ofloxacin in samples carried out a method of a high performance liquid chromatography. Results: we studied the main pharmacokinetic parameters of ofloxacin when used free and niosomal forms of antibiotic to experimental white mice per os. It is shown that use of oral niosomal forms leads to decrease of maximal concentration in serum and increase of ofloxacin half-life by 7,4 times in average compared to the free form. It is determined that bioavailability of ofloxacin in the niosomal form is 154% relative to the free form of the antibiotic. Conclusions: niosomal microcontainers are perspective technology of encapsulation and the directed transport of antibacterial preparations through biological barriers. Using of niosomal formulation of ofloxacin is able to afford to increase considerably efficiency of treatment in comparison with a free form and significantly decrease negative effects of antibiotic therapy.

Author(s):  
Yan Xiong ◽  
Yong-Hong Liu ◽  
Jian-Sha Li ◽  
Yu-Ying Zhang ◽  
Jing Zhang ◽  
...  

Abstract A simple high performance liquid chromatography (HPLC) method was developed and validated for the determination of coumarin-3-carboxylic acid analogues (C3AA) in rat plasma and a preliminary study on pharmacokinetics. Ferulic acid (FA) was used as the internal standard substance, and coumarin-3-carboxylic acid (C3A) was used as a substitute for quantitative C3AA. After protein precipitation with methanol, the satisfactory separation was achieved on an ODS2 column when the temperature was maintained at 30 ± 2°C. The correlation coefficient r in the C3A linear equation is equal to 0.9990. Pharmacokinetic parameters for t1/2, Tmax, Cmax, area under the curve (AUC)0-t, average residence time (MRT), apparent volume of distribution (V z/F) and clearance (Cl/F) were 1.89 ± 0.03 h, 0.39 ± 0.14 h, 1.81 ± 0.10 g· mL−1 ·h, 7.88 ± 0.24 g·mL−1·h, 3.23 ± 0.14 h, 0.43 ± 0.03 (mg·kg−1)·(g·mL−1)−1·h−1, respectively. The high performance liquid chromatography-photo diode array detector (HPLC-PDA) method established in this study can be used to separate and determine the content of C3AA in plasma of rats after 60% ethanol extraction by gavage. The plasma concentration-time curve and pharmacokinetic parameters reflect the absorption of C3AA in rat blood after oral administration to some extent.


2020 ◽  
Vol 11 (4) ◽  
pp. 7289-7292
Author(s):  
Seema Saini ◽  
Rajeev Garg

In the present study, fast disintegrating tablets of Lercanidipine Hydrochloride (LFDT) were tested in vivo in the buccal cavity of the rabbits. Various pharmacokinetic parameters were analysed in the study, including maximum measured plasma concentration (Cmax), time of maximum measured plasma concentration (tmax) and area under the plasma concentration vs time curve (AUC). Also, the comparative study of the Lercanidipine Hydrochloride fast disintegrating tablets (LFDT) was performed with the marketed conventional tablets of the drug (LMKT). The technique selected for the bioanalytical analysis of the blood samples of the rabbits for pharmacokinetic data computation was High-Performance Liquid Chromatography. An already well-established and validated method was used to analyse the blood samples of the rabbits. The results revealed that the rate of absorption was improved for fast disintegrating tablets of Lercanidipine Hydrochloride (LFDT) as compared to the marketed conventional tablets of the drug (LMKT). This indicated that drug was rapidly absorbed from the fast disintegrating tablet and attained elevated plasma concentration in a short interval after dosing than the marketed formulation. However, the value of tmax was drastically shorter for LFDT than the LMKT. The average peak plasma concentration also designated a rise in the extent of absorption (AUC). From the present study, it was concluded that the fast disintegrating tablet batch (LFDT) had much more improved pharmacokinetic parameters as compared to its conventional marketed counterpart (LMKT).


OENO One ◽  
1999 ◽  
Vol 33 (1) ◽  
pp. 9
Author(s):  
Béchir Ezzili ◽  
Gérard Darné ◽  
M. Bejaoui

<p style="text-align: justify;">Under some laboratory conditions, it is possible to obtain a production of anthocyanins by the leaves of grape cuttings.</p><p style="text-align: justify;">The objective of this work consists in the comparison between contents in anthocyanin pigments of leaves of stemming Carignan of one eye cuttings cultivated in various conditions of laboratory with those of leaves of the same cultivated grape to the vineyard in the area of El Khenguet UCP Sidi Slama (Tunisia).</p><p style="text-align: justify;">We have measured the growth in length and in diameter of stems of the cuttings processed 30 days in total darkness and compared to cuttings witnesses raised in greenhouse. The same comparison has been undertaken on cuttings having undergone 30 days stay in total darkness and 21 days of maintenance in greenhouse with witness that has undergone 51 days in greenhouse.</p><p style="text-align: justify;">The total darkness during 30 days favors the growth in length and in diameter of shoots, reduced the leaf surface, and blocks the synthesis of anthocyanin as compared to the photoperiod of 12 hours of darkness/12 hours of light. The total darkness during 30 steady days by a photoperiod of 12 hours light/12 hours darkness during 21 days induces a resumption of the leaf growth and a synthesis of anthocyanins in leaves and in stems.</p><p style="text-align: justify;">The analysis of the anthocyanin, undertaken by High Performance Liquid Chromatography (HPLC) allowed to detect the five anthocyanin 3-monoglucosides following: Delphinidin MG3 - Cyanidin MG3 - Petunidin MG3 - Pæonidin MG3 and Malvidin MG3.</p><p style="text-align: justify;">They are in the free form and in the combined form, esterified by acetic, cafeic and coumaric acids in stemming leaves of the vineyard as well as in those developed in the laboratory. The combined anthocyanins are better represented in the cutting cultivated in laboratory.</p><p style="text-align: justify;">The Cyanidin 3-monoglucoside, the Pæonidin 3-monoglucoside and the Malvidin 3-monoglucoside present a maximal content at the period of the fall of leaves. The other anthocyanin pigments have similar contents always weaker than those of Cyanidin MG3 and Pæonidine MG3.</p><p style="text-align: justify;">The output in total anthocyanin obtained of the cuttings of the laboratory is equal to 25 p. cent of that of the vineyard.</p>


1997 ◽  
Vol 41 (8) ◽  
pp. 1668-1672 ◽  
Author(s):  
J A Zix ◽  
H F Geerdes-Fenge ◽  
M Rau ◽  
J Vöckler ◽  
K Borner ◽  
...  

In an open, randomized, triple crossover study, the effects of cisapride and sucralfate on the pharmacokinetics of sparfloxacin were assessed. Fifteen healthy volunteers received 400 mg of sparfloxacin as a single oral dose on day 0. In a random order, concomitant doses of 10 mg of cisapride three times daily from day -2 to day 2 and 1 g of sucralfate four times daily from day -2 to day 0 were administered. Sparfloxacin concentrations were measured by bioassay and high-performance liquid chromatography. Pharmacokinetic parameters for sparfloxacin alone were as follows (mean +/- standard deviation): maximum concentration of drug in serum (C(max)), 1.27 +/- 0.39 microg/ml; time to C(max) (T(max)), 4.1 +/- 1.9 h; area under the concentration-time curve (AUC), 35.0 +/- 9.7 microg x h/ml; mean residence time, 28.5 +/- 5.7 h; half-life (t1/2), 20 +/- 4 h; urinary recovery (UR x f), 11.0% +/- 2.7%; and metabolite-sparfloxacin ratio in urine, 2.6. For the cisapride group there was a significant decrease in the sparfloxacin T(max) (1.9 +/- 2.1 h) and a significant increase in C(max) (1.74 +/- 0.73 microg/ml). The QTc interval for patients receiving sparfloxacin and cisapride was prolonged by 7.7% compared to the QTc interval during medication-free periods. Significant differences in the values for the group receiving sucralfate compared to the values for the group receiving sparfloxacin alone were found: C(max), 0.77 +/- 0.31 microg/ml; AUC, 18.6 +/- 5.8 microg x h/ml; t1/2, 26 +/- 10 h; and UR x f, 5.8 +/- 1.8%. Concomitant adminstration of cisapride accelerates the absorption and increases the peak concentration of sparfloxacin without having a significant effect on the extent of bioavailability. Coadministration of sucralfate leads to a 44% decrease in the bioavailability of sparfloxacin.


Author(s):  
Elahehnaz Parhizkar ◽  
Zahra Mohammadi ◽  
Shohreh Alipour

Abstract Levodopa is widely administered orally in clinical treatment of Parkinson’s disease; however, due to levodopa various oral absorption and low bioavailability, intranasal delivery seems to be a suitable alternative route of administration. Pluronic F-127 is a thermosensitive polymer, which can form gel at nasal cavity temperature and increase drug residence time. In this study, a rapid High Performance Liquid Chromatography (HPLC) method was validated in presence of internal standard to determine pharmacokinetic parameters following levodopa administration to rats in three different intravenous solution, intranasal solution and intranasal thermosensitive gel groups. A precised (96.7%) and accurate (95.0%) HPLC method was validated at low UltraViolet (UV) wavelength of 208 nm that showed limit of detection and limit of quantitation of 59 and 177 ng/mL, respectively. Specificity results showed no interference for levodopa with endogenous serum materials, and serum extraction efficacy was 93%. Pharmacokinetic parameters including bioavailability of 75 and 85% with mean residence time of 78 and 94 min were estimated for intranasal solution and thermosensitive gel using the validated HPLC method, which indicated that levodopa nasal gel may be a good alternative with appropriate pharmacokinetic outcome. Therefore, the validated levodopa HPLC analysis method at low UV wavelength was efficiently applied in pharmacokinetic study.


2020 ◽  
Vol 3 (1) ◽  
pp. 122-129
Author(s):  
Christica Ilsana Surbakti

Paracetamol is a safe analgesic and antipyretic drug with low side effects, effective and well tolerated. In some cases there is a drug interaction between paracetamol and other drugs. The purpose of this study is to determine the effect of cimetidine administration on paracetamol pharmacokinetic profiles. The method used in this study was an experimental method using 3 rabbits. Rabbits are divided into 3 groups. The first treatment group was given paracetamol suspension, the second treatment group was giving cimetidine 1 hour before paracetamol and the third group was giving cimetidine and paracetamol simultaneously. The dose of the drug has been adjusted to each rabbit. Measurement of plasma paracetamol drug levels was carried out using a High Performance Liquid Chromatography (HPLC) tool. The results of the study showed that the pharmacokinetic parameter values ​​did not show any significant effect on each group. Cimetidine administration simultaneously affects paracetamol pharmacokinetic parameters but not significantly. Likewise with the administration with a time span of 1 hour, did not show any significant changes in the pharmacokinetics of paracetamol.


2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Nabil K. Alruwaili

The use of analytical quality by design (AQbD) approach in the optimization of the high-performance liquid chromatography (RP-HPLC) method is a novel tool. Three factors and three levels of Box–Behnken statistical design (BBD) were used for method optimization and analysis of atorvastatin. The mobile phase (acetonitrile: water), flow rate (Rt), and UV wavelength were used as independent variables. Their effects were observed in the area of the chromatogram (AU), retention time (Rt, min), and tailing factor (%). The optimized HPLC condition was found as acetonitrile:water (50 : 50), flow rate (0.68 ml/min), and UV wave length (235 nm). It gives the retention time of 2.43 min with the linearity range of 5–30 μg/ml with a high regression value (r2 = 0.999). The method was found to be precise and accurate with low % RSD (<5%). The refrigeration stability indicated that atorvastatin was stable. The force degradation study showed that the atorvastatin was fully unstable in UV light and stable in 0.1 M basic condition. It concluded that this QbD optimized method is suitable for quantification of the atorvastatin from the formulation as well as pharmacokinetic parameters.


Sign in / Sign up

Export Citation Format

Share Document