Objective This study is aimed to investigate the differences in pharmaceutical quality and therapeutic efficacy of calcipotriol ointments between the original product and the generics.Methods We evaluated the pharmace...Objective This study is aimed to investigate the differences in pharmaceutical quality and therapeutic efficacy of calcipotriol ointments between the original product and the generics.Methods We evaluated the pharmaceutical quality of the original product and the generics including pH,content and related substance,and calcipotriol stability in the matrix.Intradermal retention of calcipotriol ointments in vitro was investigated using skin of Bama miniature pig.The pharmacodynamics study was performed in psoriasis guinea pig models.Results The matrix of original product is better than the generics,and influenced the drug diffusion,stability and in vitro retention,thus resulted in the difference in pharmacodynamics.The retention amount of calcipotriol in the original product was significantly higher than that of generic B,and approximately 4 folds higher than that of generic A.All of the three ointments improved pathological indexed in psoriasis guinea pigs,and there was a significant difference between the preparation group and the model group (P =0.001).Guinea pigs in the original group had the lowest interleukin-17 level (35.7 ± 1.13 μg/ml) and Baker Score (2.70 ± 0.97) compared with generic A (37.9 ±3.3 μg/ml,3.10 ± 0.22,respectively) and generic B (39 ± 4.6μg/ml,3.80 ± 0.57,respectively),but no statistical difference was found among the three groups (all P ＞ 0.05).Conclusions Difference occurs in the internal quality between the original product and the generics.The original preparation owns suitable balance between matrix stability and transdermal ability so that showes superiority in pharmaceutical properties,intradermal retention and therapeutic effect in vitro and in vivo,which suggests that more attention should be paid to the formulation and process during the research and development of the generics.The original product is recommended with priority for treatment especially at emergency.展开更多
文摘Objective This study is aimed to investigate the differences in pharmaceutical quality and therapeutic efficacy of calcipotriol ointments between the original product and the generics.Methods We evaluated the pharmaceutical quality of the original product and the generics including pH,content and related substance,and calcipotriol stability in the matrix.Intradermal retention of calcipotriol ointments in vitro was investigated using skin of Bama miniature pig.The pharmacodynamics study was performed in psoriasis guinea pig models.Results The matrix of original product is better than the generics,and influenced the drug diffusion,stability and in vitro retention,thus resulted in the difference in pharmacodynamics.The retention amount of calcipotriol in the original product was significantly higher than that of generic B,and approximately 4 folds higher than that of generic A.All of the three ointments improved pathological indexed in psoriasis guinea pigs,and there was a significant difference between the preparation group and the model group (P =0.001).Guinea pigs in the original group had the lowest interleukin-17 level (35.7 ± 1.13 μg/ml) and Baker Score (2.70 ± 0.97) compared with generic A (37.9 ±3.3 μg/ml,3.10 ± 0.22,respectively) and generic B (39 ± 4.6μg/ml,3.80 ± 0.57,respectively),but no statistical difference was found among the three groups (all P ＞ 0.05).Conclusions Difference occurs in the internal quality between the original product and the generics.The original preparation owns suitable balance between matrix stability and transdermal ability so that showes superiority in pharmaceutical properties,intradermal retention and therapeutic effect in vitro and in vivo,which suggests that more attention should be paid to the formulation and process during the research and development of the generics.The original product is recommended with priority for treatment especially at emergency.
