ABSTRACT
@#In order to evaluate the consistency of the release behavior between the self-made saxagliptin and metformin hydrochloride sustained-release tablets and the reference preparations in vitro, the similarity of the dissolution curves between the self-made preparations and the reference preparations in four dissolution mediums: HCl (pH 1.0), acetate buffer saline (pH 4.5), phosphate buffer saline (pH 6.8) and pure water, and the gel morphology and strength of the self-made preparations and the reference preparations in the HCl (pH 1.0) solution medium were compared.Results showed that in four dissolution mediums, the dissolution rates of saxagliptin in the self-made preparations and the reference preparations at 15 min were greater than 85%, and the ?2 similarity factors of metformin hydrochloride were 89, 83, 80, 86, all greater than 50, so the dissolution of the self-made preparations was consistent with those of the reference preparations.The volume expansion rate, water absorption rate and erosion rate were consistent with those of the reference preparations, and the gel strength of the self-made preparations was the same as that of the reference preparations.The in vitro release behaviors of the self-made preparations and the reference preparations are consistent, which provide a good guarantee for bioequivalence.
ABSTRACT
@#Solid dispersions of the insoluble compound CHMFL-KIT-110 were prepared by solvent method with polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus),Poloxamer 407,PEG 6000,Copovidone (Kollidon VA64) as carriers and SLS,Tween 80,Cremophor RH40 as solubilizers. The optimal formulation was screened and obtained with dynamic solubilities and supersaturation performances as indexes. The final product was characterized by Fourier transform infrared (FT-IR),differential thermal analysis (DTA) and X-ray powder diffraction (XRPD). The stability and pharmacokinetic behavior in rats were also investigated. Results suggested that when the weight ratio of CHMFL-KIT-110/Soluplus/SLS was 1∶4∶0.5,dynamic solubility of the solid dispersions was significantly improved with no recrystallization. In the accelerated condition (40 °C,75% RH) for 30 days,CHMFL-KIT-110 in the solid dispersions was still amorphous with no crystal observed. The results of pharmacokinetics in rats showed that the cmax and AUC0→t of CHMFL-KIT-110 solid dispersions were 373.1 times and 358.7 times higher than those of free drugs,respectively. These results help to understand the formulation development and clinical practice of CHMFL-KIT-110.
ABSTRACT
OBJECTIVE:To establish and compare the HPLC characteristic Spectrum Erycibe obtusifolia from different habi-tats. METHODS:HPLC was performed on the column of Hypersil ODS C18 with the mobile phase of acetonitrile-0.1% phosphoric acid at flow rate of 1.0 ml/min,detection wavelength was 347 nm,the column temperature was 30℃and the sample size was 20μl. 12 different batches of samples were determined and the characteristic spectrums of those were established. TCM fingerprint evalu-ation software(2004 edition)was used to evaluate the similarity of 12 batches of samples. RESULTS:10 characteristic peaks were identified in the characteristic spectrum of E. obtusifolia. Peak 3 was scopolamine glycosides,peak 4 was chlorogenic acid and peak 6 was scopoletin. The similarities of 10 batches of samples were proved to be higher than 0.90 and 2 batches were proved to be less than 0.90. CONCLUSIONS:The method is simple,accurate and reproducible,and can provide scientific evidence for effectively controlling the internal quality standards.