Recently, in Korea, the importance of preparation and use of injectable drugs has been emphasized due to successive fatal accidents caused by injection infections. Parenteral nutrition (PN) has also been identified as a cause of infection. Cases of infection due to PN have been reported not only in Korea, but also abroad, and contamination occurs mainly during the preparation of PN. Because sterile preparation and compounding of injections are very important for infection control and patient safety, this article reviews the major guidelines outlined thus far. The Korea Ministry of Food and Drug Safety in 2006 published guidelines and the KSHP (Korean Society of Health-System Pharmacists) recently issued guidelines for the aseptic preparation of injections. In addition, as US guidelines, the ASHP (American Society of Health-System Pharmacists) guidelines and United States Pharmacopeia (USP) <797> are also reviewed. The recent guidelines published by the KSHP have significance in that they were adopted in accordance with the domestic reality, even though they conform to foreign guidelines, and are expected to be guidelines for hospital pharmacists performing aseptic preparation work. In addition, the Korea Ministry of Health and Welfare is considering appropriate guidelines for the safe management of medications, training staff for infection prevention and strengthening staff capacity. Furthermore, the gradual expansion of aseptic compounding facilities and human resources, as well as the provision of adequate medical costs are also considered. Based on the establishment and standardization of injectable drugs compounding guidelines for Korean hospitals, it is believed that if human resources and facilities are supported and medical charges are improved, it will be possible to expect the safer preparation and use of injections.