Jagadish P.C

Background As lung cancer treatment has progressed, there has been an increase in awareness of the short- and long-term adverse effects of targeted cancer therapies of tyrosine kinase inhibitors, particularly cardiovascular toxicities. Methods The current study assessed the potential drug interactions using interaction drug-interaction checkers (IB...

Introduction The utilization of CDK4/6 inhibitors has led to compromised survival rates for breast cancer patients. Consequently, certain treatment aspects, involving adherence and drug-to-drug interactions, are gaining prominence. To develop chemotherapy regimens that are both effective and efficient, our main objective was to thoroughly character...

Introduction: P-glycoprotein, an ATP-dependent efflux transporter, plays a crucial role in eliminating cellular toxins and affects the intracellular concentration and bioavailability of CDK 4/6 inhibitors. Moreover, dietary flavonoids are natural bio-enhancers that can effectively inhibit the efflux function of these transporters. Therefore, this...

Palbociclib and ribociclib an orally bioavailable, potent cyclin-dependent kinase 4/6 inhibitors, with low oral bioavailability due to substrate specificity towards CYP3A and P-glycoprotein. Thus, current research aims to examine the effect of a bioenhancer (naringin), on oral pharmacokinetics of palbociclib and ribociclib. Naringin’s affinity for...

Numerous clinical concerns have been expressed regarding the potential worsening of cyclin-dependent kinase 4/6 inhibitor effects in breast cancer patients because of co-administration of proton pump inhibitors. Hence, this study evaluated the effects of proton pump inhibitors on the pharmacokinetics of palbociclib and ribociclib in terms of cytoch...

Background: The study investigated pharmacokinetic interactions between palbociclib and ribociclib with proton pump inhibitors (PPIs) using the reverse-phase high-performance liquid chromatography (RP-HPLC) method.Methods: Developed RP-HPLC method quantified palbociclib and ribociclib in biological matrices. In vitro metabolic stability assays and...

Understanding the impact of dynamic alterations in gastrointestinal fluid properties and intestinal dissolution of poorly soluble drugs, such as lapatinib, is crucial for predicting drug absorption in vivo. The current study employs a micro-dissolution pH shift model to forecast the dynamic dissolution of lapatinib in buffer and bio-relevant media...

Objectives Cyclin-dependent kinase inhibitors are subject to rapid first-pass metabolism, and their oral absorption is hindered by intestinal CYP3A4 and P-gp. The present study investigates the impact of dietary polyphenols on the oral pharmacokinetics of palbociclib and ribociclib, considering their potential as modulators of CYP3A4 and P-gp. Met...

Background: Palbociclib and ribociclib are substrates of efflux transporter, P-glycoprotein plays a key role in absorption and transport of these drugs. Proton pump inhibitors, when co-administered with them are known to show inhibitory effect on P-glycoprotein. Objective: Therefore, this study aims to investigate the role of proton pump inhibit...

The 12R-lipoxygenase (12R-LOX), a (non-heme) iron-containing metalloenzyme belonging to the lipoxygenase (LOX) family catalyzes the conversion of arachidonic acid (AA) to its key metabolites. Studies suggested that 12R-LOX plays a critical role in immune modulation for the maintenance of skin homeostasis and therefore can be considered as a potenti...

The objective of the study was to evaluate the possible pH-dependent interaction of ribociclib succinate with acid-reducing agents, which are concomitantly administered as supportive care medicines in cancer. Quality by Design-based analytical method development for a weakly basic drug ribociclib succinate supposedly having the characteristic abili...

Dietary polyphenols such as quercetin and curcumin have been extensively administered to patients with cancer in the form of herbal supplements. They may have a synergistic anticancer effect; however, a risk of pharmacokinetic interactions with selective CDK‐4/6 inhibitors that are metabolized by the CYP3A4 enzyme exists. Considering these pharmaco...

The present work is aimed to address the oral bioavailability issue of asenapine maleate with the help of bio-enhancers. Molecular modeling platform by Maestro, Schrödinger was used to screen a list of bio-enhancer molecules. The bio-enhancer with the highest docking score and the best intermolecular interactions was selected for in-vivo pharmacoki...

Background and objective Concurrent usage of proton pump inhibitors and their effect on survival and medication termination has been found in individuals receiving protein kinase inhibitor chemotherapy. To investigate the drug-drug interaction mechanism between CDK inhibitors and proton pump inhibitors, the in-silico docking approach was designed b...

In search of potent and new anti-inflammatory agents, we explored a new class of isocoumarin derivatives possessing the 3-oxoalkyl moiety at C-4 position. These compounds were synthesized via the FeCl3 catalyzed construction of isocoumarin ring. The methodology involved coupling of 2-alkynyl benzamides with alkyl vinyl ketone and proceeded via a re...

Background The bioavailability of a drug in a solid oral dose depends on its release from the drug product and its balance in dissolution. Compared with a reference drug, the newly developed formulation needs to establish bioequivalence by comparing the dissolution profile. Objective To compare dissolution profiles of a newly developed maraviroc o...

A stability-indicating reverse phase high-performance liquid chromatography method was developed and validated for simultaneous quantification of apremilast (APL) and betamethasone dipropionate (BD) in bulk as well as drug loaded microsponges. Various mobile phase systems were screened to check the system suitability followed by force degradation a...

An HPLC-ECD analytical method with high reproducibility and wide linearity range has been developed and validated. Moxifloxacin was separated and identified using this method with a simple mobile phase comprising Britton Robinson buffer pH 5.0 and methanol (93: 7 v/v) flowing at a rate of 0.5 mL/min through Acclaim C18 column (150 mm × 4.6 mm × 5 i...

Background: Radical cure of Plasmodium vivax malaria requires treatment with a blood schizonticide and a hypnozoitocide (primaquine) to eradicate the dormant liver stages. There has been uncertainty about the operational effectiveness and optimum dosing of the currently recommended 14-day primaquine (PQ) course. Methods: A two centre, randomized...

The aim of the work was to prepare co-crystals of valsartan, a BCS Class II drug to enhance its aqueous solubility and bioavailability. The solvent evaporation method was used to prepare co-crystals by using different co-formers and varying the drug to co-former molar ratios. Succinic acid was found to be suitable co-former to prepare co-crystals w...

Ethnopharmacological relevance: The rhizomes of an acaulescent perennial herb, Kaempferia galanga Linn (Family: Zingiberaceae), used as traditional ayurvedic herb to get relief from indigestion, swelling, pain, high blood pressure and dyslipidemia. Aim of the study: To prepare and characterize various extracts of Kaempferia galanga (K. galanga)...

The purpose of this study was to develop nanosuspension based on combinative technology to enhance the intestinal absorption of Olmesartanmedoxomil(OLM), a potent antihypertensive agent with limited oral bioavailability. Two combinative approaches were employed and then characterized. In vitro intestinal absorption of OLM nanosuspension and plain O...

Aripiprazole is an atypical neuroleptic drug used to manage conditions like schizophrenia and bipolar disorder. The aim of current work is to compare UV spectrophotometric and derivative techniques of aripiprazole to establish simple, sensitive method. In different spectrophotometric orders of aripiprazole, zero order has shown maximum absorbance a...

Breast cancer is a major health concern, with a mortality rate worldwide. Targeted therapy has emerged as a promising option for cancer treatment, particularly through the inhibition of cyclin-dependent kinase-2 (CDK-2), holding a promise for combating this disease. The potential of 4-aryl-4H-chromene derivatives as inhibitors of CDK- 2 was evaluat...

Mannich base of pyrazolines 3(a–e) under both conventional and microwave irradiation was synthesized. All the synthesised compounds were purified by recrystallisation, characterized on the basis of UV, IR, and NMR spectroscopy, and further supported by mass spectroscopy. The result obtained confirms superiority of microwave irradiation method over...

There are 27 European Union (EU) member states, 3 European Economic Area (EEA) and European Free Trade Association (EFTA) states. For a company willing to market the medicinal product in to the EEA, marketing authorization (MA) for the respective product must be issued by competent authority of member state or authorization granted according to Reg...

A chemometric UV-spectrophotometric method of analysis was successfully developed for the simultaneous determination of stavudine, lamivudine and nevirapine in pharmaceutical formulation. The application of multivariate method to the obtained spectrophotometric data is a new idea for the simultaneous quantitative analysis of stavudine, lamivudine a...

The term medical device includes a wide category of products ranging from therapeutic medical devices exerting their effects locally such as tissue cutting, wound covering or propping open clogged arteries, to highly sophisticated computerized medical equipment and diagnostic medical devices. To achieve uniformity among the national medical device...

Crude ethanol extract of the rhizome Kaempferia galanga L. and the successive extracts prepared with increasing polarity viz., petroleum ether, ethyl acetate and ethanol. The extracts and fractions were screened for cytotoxic activities by standard MTT and SRB assays against four cancerous viz., DU145, PA1, SW620, B16F10 and a normal Vero cell cult...