Exploring thiocolchicoside injection: Mechanism, formulation development, and analytical validation

Abstract

Globally, musculoskeletal disorders – which include ailments such as osteoarthritis, lower back pain, and cervical spondylosis – are major contributors to pain and disability. To reduce related muscular spasms and discomfort, doctors frequently prescribe muscle relaxants, particularly those that target pathways in the central nervous system. Thiocolchicoside (THC), a semi-synthetic version of colchicine, is derived from the Gloriosa superba plant. It helps lower pain and inflammation and relaxes muscles mostly in the brain and spinal cord. The injectable version of THC is becoming more and more popular for the treatment of acute and severe musculoskeletal problems due to its low oral bioavailability and gastrointestinal side effects. The formulation creation of THC injection is the main topic of this work, which also addresses important issues including stability, isotonicity, sterility, and solubility optimization. To choose the best excipient and store it in the right method, the physicochemical characteristics – such as solubility, partition coefficient, and degradation pathways – are investigated. Franz diffusion cell-based in vitro permeability studies provide additional insight into the drug’s absorption properties and possible parenteral delivery-based bioavailability increase. Furthermore, an examination of contemporary analytical techniques, such as reverse-phase high-performance liquid chromatography and ultraviolet spectrophotometry, enables International Council for Harmonizationcompliant quality control and validation procedures. All things considered, the study offers thorough insights into the injectable form of THC, confirming its cliHnical effectiveness and providing a dependable substitute for oral administration in the treatment of musculoskeletal conditions.