Aim: Sickle cell home remedy mixture for the relief of symptoms associated with sickle cell disease has been toxicologically investigated and ascertained in the rat model in the previous study. However, this study was designed to ascertain the level of absorption, distribution, bioavailability, metabolism and excretion of the drug which is medically refers to as pharmacokinetic (PK) to ensure its effectiveness and safety. Methods: The structural profiles, metabolites and the in vivo concentration of the mixture in blood plasma and different tissues homogenate (liver, kidney, liver, blood, heart and lung) of rats model collected at different time points after oral and intravenous (IV) administration at a single dose of 200mg/kg body weight were done using high performance liquid chromatography (HPLC) and LTQ-Orbitrap XL mass spectrometer (Thermo Electron, Begin China). Results: A 55.3% bioavailability was recorded in both the male and female rats after 30 minutes of oral administration. There was no significant difference (P<0.05) increase in the level of plasma concentration between male and female rats at the same time points of administration. Three distinct metabolites (alkoxide, acetaldehyde and sodium triglycerides) were identified in the rat’s feces and urine 24 h after administration of which the metabolic pathway were mainly hydrolysis and oxidation using cytochrome P450. Regarding the study data, One-way ANOVA was done employing Statistical Package for Social Science (SPSS) software version 21. Significant differences between male and female experimental rat groups were judged by Waller Duncan test. All data were articulated as mean ± and standard deviation (SD). Conclusion: With the results of this Pharmacokinetic study, sickle cell home remedy mixture dose intervals can be determined and adjusted more accurately for effectiveness and safety of the end users. Moreover, the clinical trial will be used to fully understand in vivo disposition of this mixture and evaluate the mechanism of its biological response.