Swarna Makshika (chalcopyrite), an ore of copper, is used since ancient days in India to treat various ailments. Swarna Makshika Bhasma (SMB) preparation involves two main processes: Shodhana (detoxification) and Marana (incineration in a controlled manner). The present study is designed to compile and assess all the relevant and standard work done related to SMB preparation in addition to standardization in terms of its pharmaceutical, analytical, and safety parameters. These drugs may accumulate contaminants at various stages of manufacturing, transit, and storage, making them dangerous to administer and necessitating their detection and quantification. Analytical instrumentation and procedures are crucial in this regard. Sophisticated analytical analysis (X-ray diffraction, energy dispersive X-ray, Raman spectroscopy, Fourier-transform infrared spectroscopy, scanning electron microscope, transmission electron microscope, and nuclear magnetic resonance) may improvize our understanding on drugs’ overall response in terms of their structure, behavior, and response in the body. Relevant literatures of ancient India related to ayurvedic pharmaceutics for preparation of SMB along with contemporary research databases such as Scopus, PubMed, and various other appropriate contents on the internet were thoroughly searched. This work may provide an insight into its potential effect in characterization and therapeutics, eventually leading to the betterment of human life. Though this compilation has some limitations due to less standard works available, the concise perimeter may provide further quality studies to be done in near future.