HPLC for control stability of quercetin injectable dosage form

Abstract

Introduction.  Quercetin is a flavone derivatives which known  like  a substances with vitamin activity, high antioxidant, antimutagenic and anticarcinogenic activity and many other types of  biological activity. Wide usage of quercetin prevents their polyphenolic nature structure which does not allow a high bioavailability of pure quercetin when administered orally. This is associated with a wide spectrum variety of chemical reactions for the phenolic groups: from interaction with amino acid residues in proteins to reactions with amine heterocyclic alkaloids and polysaccharides. In our days  Corvitin – one from the number of quercetin based drugs with sufficiently low levels all types toxicity, allergenic and has no irritating action on intravenous administration. In the same time quercetin cannot be used in full measure because of the limited number of publications with analysis methods, especially HPLC. Determining the stability over time of concentrate quercetin solution, as well as determining the stability of the concentrate to the original autoclave sterilization conditions is a promising direction in creating new drugs. Materials and methods The objective was to research quercetin soluble formulation samples in different conditions: 1) fresh dilute concentrate (0.9% sodium chloride); 2) the original dilute concentrate, which was stored at room temperature for 14 days in light and 3) similar to the first sample dilute concentrate, which went before breeding in autoclaving at 120 0 C for 20 minutes. The objects used in the studies were industrial drug-substance quercetin (Sinkea manufactured (China)), the original pharmaceutical composition as the soluble form of quercetin for injection and aerosol applications, glycerol (Sigma), Polysorbat 80 (Merk), ethanol 96 %. For the HPLC – analysis, chromatograph "Milichrom A-02" (SiChrom, Knauer) (Econova, Novosibirsk, Russia) was used. Results and discussion Quercetin was identified using information on its retention time and spectral relations in the UV region from the database of DB-2003 spectrums. HPLC analysis results show that the quercetin is stable in ampouled form under autoclave and storage and freshly diluted quercetin concentrate for infusion are identical. Quercetin aqueous solution which was stored at room temperature for 14 days in the light, turned out to be unstable.  It was found that aqueous solutions of polysorbate-80 was full hydrolyzed to the initial compounds. Conclusions In this work the ability of  quercetin’s perspective concentrates to be stable were checked. The stability of concentrates was determined by HPLC chromatograph "Millichrome A - 02» (SiChrom, Knauer). It is shown that the HPLC methods can be used to establish the smallest difference in the samples. The quercetin’s non-aqueous concentrate is capable of withstanding retorting and remains in standard indestructible state in nonaqueous media (glycerol, ethanol, polysorbate 80). Quercetin is unstable in aqueous solutions and are destroyed during prolonged storage. HPLC- chromatogram is presented in the article and show that gradient HPLC with UV- detection can be used for quality control of quercetin.