ObjectiveHistory of the utilization of various parts of Camellia sinensis such as seed oil in different folklore medicaments and plants leaves for preparing green tea is very old. Pharmacokinetics (PK) plays a key role in the drug discovery stage by channelizing the medicinal chemist in the optimization process of chemical sequences and lends a hand to pharmacologists to invent in vivo studies. The objectives of the present study were to elaborate quantitative determination of phytochemicals and nutritional assessment of C. sinensis especially on the composition of seed oil of the local C. sinensis plant and to evaluate the pharmacokinetics of leaves extract in healthy volunteers. MethodDetermination of secondary metabolites and nutritional assessment of C. sinensis were carried out. The composition of seed oil was elaborated with the help of GC–MS analysis for its potential significance and evidence-based household uses as folklore but also for industrial applications. Pharmacokinetics of water extract of C. sinensis leaves was compared in 9 healthy human volunteers and divided into three groups (n = 3, in each) fasting, fed and fed with coke. Plasma concentrations were noted in each group and were quantified using a validated HPLC method. ResultsPhytochemical analysis and proximate analysis of C. sinensis suggests the presence of alkaloids, flavonoids, tannins, saponins sterols; and protein, lipids fiber and carbohydrate respectively. GC–MS of the C. sinensis seed oil shows the presence of linoleic acid 100%, palmitic acid 33.55%, stearic acid 21.96, caffeine 21.72 and vitamin E 14.49%. Pharmacokinetic studies suggest that in the fasting group, higher plasma concentration was found among all the volunteers. ConclusionThe phytochemical analysis of green tea suggests that it is a good source of secondary metabolites full of important nutrients. GC–MS of seed oil reveals that seed of C. sinensis is a rich source of fatty acid, and can be used to fulfill the pharmaceutical need. Pharmacokinetic studies may help to develop the biomarkers for the green tea utilization and also would help to design the dose and dose frequency for achieving the significant absorption level. PK and PD also help to determine its plasma concentration and therapeutic efficacy.