Background: Monitoring of plasma concentrations is a necessity for narrow therapeutic index potent drugs. Development of non-invasive methods can save the patients from the trauma of needles and hence is considered as a research priority. Introduction: Gabapentin, an anti-epileptic drug requires therapeutic monitoring because of its narrow therapeutic index. The objective of the study was to develop a suitable method for the non-invasive extraction of gabapentin for the same. Methods: Transdermal reverse iontophoresis was performed using pig ear skin as a barrier membrane. Three compartment iontophoretic cells were used for the extraction study. Extractions were carried out under low intensity electric field (current intensity- 0.5 mA/cm2, electrical field approximately 5 V). The donor compartment was charged with aqueous gabapentin (10 µg/ml in phosphate buffer of pH 7.4). For studying the effect of receiving vehicle (pH, ionic strength, and enhancer) on the extraction efficiency of gabapentin, the two receiver chambers were charged with media having varying concentration of these factors. Drug content was determined by HPLC. Results: Compared to other pHs, cumulative extraction of gabapentin at pH 5 was significantly higher at both anode and cathode (p<0.001). At low ionic strength, extraction of gabapentin increased linearly with the increase in concentration of ions up to a certain value but at very high ionic strength the pattern reversed. Similar results were obtained with enhancer (polyethylene glycol 400). Extraction increased with increase in polyethylene glycol 400 up to 3% and then decreased. Conclusion: Extraction flux can be optimized by manipulation of the receiver media.
The world is currently witnessing a pandemic crisis caused by SARS CoV-2 having its origin in Wuhan, China. Transformation from epidemic to pandemic within a very short time-gap resulting in massive global mortality has created a sudden global deadlock affecting both human health and wealth. Clinical symptoms expressed by affected patients include dry cough, dyspnea, fever, bilateral lung infiltration and ultimately severe acute respiratory distress in advanced stages. The disease is spread over 150 countries and termed as COVID-19 by the World Health Organization (W.H.O). As per W.H.O report on 2 nd May 2020 there are over 3000000 infected cases distributed throughout the globe claiming more than 200000 lives. Mortality rate is accelerating at high speed and presently crossing 6%. The entire global healthcare system is exposed and found to be inadequate to mitigate the deadly virus. At present there is no medicine or vaccine available or clinically proven for COVID-19 management. However, the global research spotlight is now focused on development of drugs or vaccine against the virus. This has created a long pipeline of such agents which are now under preclinical or clinical evaluation stage. Some existing drugs are also under efficacy evaluations against COVID-19 whereas some are allowed to be used as a prophylactic measure. WHO has framed clear guidelines for all countries to manage the spread of the virus and these are being implemented through existing government & regulatory bodies of specific countries. The present work will give detailed outline on the pandemic spread, transmission mode, therapeutic strategies and its impact on day to day human life.
As gabapentin carried no net charge at pH 7.4, orientation mediated electromigration was suggested to be the cause.
The main aim of the present research work is to evaluate the pharmacokinetic parameters as well as therapeutic efficacy of Hydrochlorothiazide along with Losartan used as a fixed dose combined drug in treatment of hypertension. This study is carried out by utilizing a typical two periods; randomized and two way complete cross over design. All the 6 volunteers are received fixed dose and single dose product based on the randomization code in each clinical period. Then blood samples are taken and the comparative Pharmacokinetic study was carried out. Matrix effect for internal standard (Letrozole and Candesartan) and analytes (Losartan, LCA & HTCZ) were also carried out as per US-FDA guideline. Maximum plasma concentration of fixed dose combining drug (in which Losartan combined with HCTZ) was found 49 ± 8.87 ng/ml (Cmax) at time 2.75 ± 0.25 hours (tmax) for HCTZ and the average maximum plasma concentration of 6 volunteers was 49.87 ng/ml and Tmax 2.75 hours, AUC0-t was 227.02 ng/ml at 48 hours and AUC0-α227.67 ng/ml at infinite time and plasma half-life (T1/2) of HCTZ 4.91 hours and Ket value is 0.14 hour -1 . The matrix effect of internal standard (letrozole) ranged between 87.32% -89.71% and for HCTZ it was between 88.47% -89.86%. And the matrix effect of internal standard (Candesartan) ranged between 93.77% -98.28% and same was found between 95.97% -96.78% in case of Losartan and for LCA it was 95.41% -98.39%. From the comparative pharmacokinetic study it can be concluded that after fixed dose combined drug treatment the maximum plasma concentration of losartan and losartan carboxylic acid were too much higher than the maximum concentration of losartan and LCA after single drug containing losartan only. And fixed dose combination drug is more susceptible than single dose of Losartan for the treatment of hypertension with better therapeutic efficacy.
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