Elucidation of pharmacokinetics of novel DNA ligase I inhibitor, S012-1332 in rats: Integration of in vitro and in vivo findings

Riyazuddin, Mohammed; Valicherla, Guru R.; Husain, Athar; Shukla, Minakshi; Katekar, Roshan; Gupta, Anand P.; Singh, Punj Lata; Banerjee, Dibyendu; Hussain, Mohd Kamil; Gayen, Jiaur R.

doi:10.1016/j.jpba.2018.09.031

Cited by 11 publications

(8 citation statements)

References 25 publications

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“…14 Plasma stability was performed in fresh plasma collected from non-treated rats. Microsomal stability was performed in RLM prepared in house and the conditions are similar to as reported by Riyazuddin et al 15 Briey, the contents of reaction mixture are RLM (0.5 mg mL À1 ), 40 mM MgCl 2 , 1 mM NADPH in 0.8 mL of 50 mM Tris-HCl buffer (pH 7.4). All the stability studies were performed at 37 C in a shaking water bath incubator and the reactions were initiated by spiking 100 mg mL À1 of COEE into respective reaction media.…”

Section: Methods Validationmentioning

confidence: 99%

Simultaneous quantification of five biomarkers in ethanolic extract ofCassia occidentalisLinn. stem using liquid chromatography tandem mass spectrometry: application to its pharmacokinetic studies

et al. 2020

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Section: Methods Validationmentioning

confidence: 99%

Simultaneous quantification of five biomarkers in ethanolic extract ofCassia occidentalisLinn. stem using liquid chromatography tandem mass spectrometry: application to its pharmacokinetic studies

et al. 2020

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“…Gastrointestinal stability was performed in different pH conditions of gastric intestinal simulated media fluids such as FaSSGF (pH‐1.6) and FaSSIF (pH‐6.8). [ 22 ] In which media was prepared according to previously reported protocols containing pepsin (0.1 mg/mL) for FaSSGF and pancreatin (10 mg/mL) for FaSSIF, respectively. This stability study is essential for oral pharmacokinetic study, the drug is administered via an oral route and distributed to the GIT site.…”

Section: Methodsmentioning

confidence: 99%

The combined effect of Raspberry Ketone with Resveratrol against oxidative stress and steatohepatitis in rats: Pharmacokinetic and pharmacodynamic studies

Verma

Goand

Rathaur

et al. 2023

J Biochem & Molecular Tox

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Raspberry Ketone (RK) and Resveratrol (RSV) are natural phenolic antioxidants and anti-inflammatory agents. However, its combined pharmacokinetic and pharmacodynamics potentials are not reported. The study aims to assess the combined effect of RK with RSV to protect rats from carbon-tetrachloride (CCl4) induced oxidative stress and NASH. The toxicant CCl4 was employed at a concentration of 1 mL/kg as a 1:1 (v/v) mixture with olive oil twice weekly for 6 weeks to induce liver toxicity.Animal treatment was followed for 2 weeks. Silymarin was used as a standard control drug to compare the hepatoprotective effect of RK and RSV. Hepatic histology, oxidative stress, MMP, reduced glutathione (GSH), plasma levels of SGOT, SGPT, and lipid profile (total cholesterol and triglycerides) were measured. Antiinflammation genes (IL-10), and fibrotic genes (TGF-β) were also examined in liver tissue. Oral administration of combined RK with RSV (50 + 50 mg/kg for 2 weeks) showed significantly more hepatoprotection by significantly decreasing elevated plasma markers and lipid profile than alone RK and RSV (100 mg/kg daily for 2 weeks). It also significantly alleviated the hepatic lipid peroxidation, restoring the activities of GSH levels in the liver. RT-PCR and Immunoblotting studies confirmed that significantly upregulation of anti-inflammation genes and protein expression (MMP-9) ameliorated the disease. Pharmacokinetic studies confirmed more synergistic stability in simulated gastric-intestinal fluids (FaSSGF, FaSSIF) and rat liver microsomes (CYP-450, NADPH oxidation & glucuronidation. Moreover, coadministration of drugs augmented the relative bioavailability, V d/ F (L/Kg), and MRT 0-∞( h), which leads to more efficacy. This pharmacokinetic and pharmacodynamic reveals a new adjuvant therapy for the treatment of steatohepatitis.

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“…P eff,rat = Q in * In( C in / C out )/2πrL equation for calculating the effective permeability in the small intestine of the rat (Riyazuddin, Husain, et al, 2019). Where Q in is the flow rate (0.2 ml/min), C out is the outlet concentration of perfusate after correction, C in is the concentration of entering of perfusate, r is the inner radius of the intestine (0.18 cm) and L is the length of the intestine (Riyazuddin, Valicherla, et al, 2019).…”

Section: Evaluation Of the Effect Of P‐gp On Drug Permeabilitymentioning

confidence: 99%

Approaches to minimize the effects of P‐glycoprotein in drug transport: A review

Husain

Makadia

Valicherla

et al. 2022

Drug Development Research

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P-glycoprotein (P-gp) is a transporter protein that is come under the ATP binding cassette family of proteins. It is situated on the surface of the intestine epithelium, where P-gp substrate binds to the transporter and is pumped into the intestine lumen by the ATP-driven energy-dependent process. In this review, we summarize the role of the P-gp efflux transporter situated on the intestine, the clinical importance of P-gp related drug interactions, and approaches to minimize the effect of P-gp in drug transport. This review also focuses on the impact of P-gp on the bioavailability of the orally administered drug. Many drug's oral bioavailabilities can improve by concomitant use of P-gp inhibitors. Multidrug resistance are reduced by using some naturally occurring compounds obtained from plants and several synthetic P-gp inhibitors. Formulation strategies, one of the most important approaches to mimic the P-gp transporter's action, finally enhancing the oral bioavailability of the drug by inhibiting its P-gp efflux. Vitamin E TPGS, Gelucire 44/14 and other pharmaceutical/formulation excipients inhibit the P-gp efflux. A prodrug approach might be a useful strategy to overcome drug resistance.Prodrug helps to enhance the solubility or alter the pharmacokinetic properties but does not diminish the pharmacological action.

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Elucidation of pharmacokinetics of novel DNA ligase I inhibitor, S012-1332 in rats: Integration of in vitro and in vivo findings

Cited by 11 publications

References 25 publications

Simultaneous quantification of five biomarkers in ethanolic extract ofCassia occidentalisLinn. stem using liquid chromatography tandem mass spectrometry: application to its pharmacokinetic studies

Simultaneous quantification of five biomarkers in ethanolic extract ofCassia occidentalisLinn. stem using liquid chromatography tandem mass spectrometry: application to its pharmacokinetic studies

The combined effect of Raspberry Ketone with Resveratrol against oxidative stress and steatohepatitis in rats: Pharmacokinetic and pharmacodynamic studies

Approaches to minimize the effects of P‐glycoprotein in drug transport: A review

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