2015, Number 3
Technological development and stability study of a 100 mg oxaliplatinum formulation in injectable solution
González CA, Martínez ALO, Achón TO
Full text
Language: Spanish
References: 12
Page: 425-440
PDF size: 180.33 Kb.
ABSTRACT
Introduction: oxaliplatinum is an analogue of the platinum-derived complexes in which the central platinum atom is surrounded by an oxalate and 1,2?diaminocyclohexane in transposition. The link kinetics of oxaliplatinum on the DNA occurs in 15 minutes at most and if compared with the cysplatinum, it presents a 4-8 h biphasic kinetics and higher efficacy over certain tumors.Objective: to design an oxaliplatinum formulation, for injection solution that contains 100mg of the active ingredient per ampoule, comply with the quality parameters for this pharmaceutical form and provides the desired therapeutic effect.
Methods: the corresponding formulation studies were performed together with the testing of five technological variants in which the formulation pH was adjusted according to the requirements of a parenteral product. A temperature study was also conducted to reach dissolving the active principle without any damage to its properties, given that it is poorly water-soluble. Different packing materials and storage temperatures of the product were studied in addition to standardizing an analytical technique based on high performance liquid chromatography for the stability of the formulation, estimation of the expiry date and for the quality control.
Results: the technological development was satisfactory in one of the tested variants. The obtained product complied with all the described specifications in the monograph for the quality control of the product; its physical, chemical and microbiological properties remained unchanged for a period of 18 months and stored at room temperature, with pilot scale-up with no further technological problems.
Conclusions: there was obtained the formulation of a drug in its injectable form that contains oxaliplatinum as active ingredient, complies with all the quality specifications for this pharmaceutical form and increases the therapeutical arsenal available in Cuba.
REFERENCES