目的:含透明质酸钠(SH)的阿奇霉素(AZI)滴眼液最优处方的筛选及制备工艺的考察。方法:采用Box-Behnken设计,以滴眼液p H、透明质酸钠的相对分子质量和透明质酸钠的质量浓度为因素,以药物在泪液中的动力学行为作为评价指标,考察各因素的...目的:含透明质酸钠(SH)的阿奇霉素(AZI)滴眼液最优处方的筛选及制备工艺的考察。方法:采用Box-Behnken设计,以滴眼液p H、透明质酸钠的相对分子质量和透明质酸钠的质量浓度为因素,以药物在泪液中的动力学行为作为评价指标,考察各因素的影响,确定最合理的处方。进一步制备了阿奇霉素滴眼液,根据《中国药典》要求考察滴眼液的渗透压,黏度及表面张力。结果:阿奇霉素滴眼液的最优处方为溶液p H 5.5,透明质酸钠相对分子质量150万,透明质酸钠质量浓度为0.6 g·(100 m L)-1。为保证滴眼液的无菌要求,制剂不耐受高压蒸汽灭菌,需无菌操作。结论:采用Box-Behnken设计筛选处方是可行的,依据最优处方制备的阿奇霉素滴眼液能有效延长药物结膜滞留时间,同时满足药典对滴眼液渗透压及黏度的要求。展开更多
The therapeutic application of deoxypodophyllotoxin(DPT) is limited due to its poor water solubility and stability. In the present study, the micelles assembled by the amphiphilic block copolymers(m PEG-PDLLA) were co...The therapeutic application of deoxypodophyllotoxin(DPT) is limited due to its poor water solubility and stability. In the present study, the micelles assembled by the amphiphilic block copolymers(m PEG-PDLLA) were constructed to improve the solubility and safety of DPT for their in vitro and in vivo application. The central composite design was utilized to develop the optimal formulation composed of 1221.41 mg m PEG-PDLLA, the weight ratio of 1 : 4(m PEG-PDLLA : DPT), 30 m L hydration volume and the hydration temperature at 40 oC. The results showed that the micelles exhibited uniformly spherical shape with the diameter of 20 nm. The drug-loading and entrapment efficiency of deoxypodophyllotoxin-polymeric micelles(DPT-PM) were about(20 ± 2.84)% and(98 ± 0.79)%, respectively, indicating that the mathematical models predicted well for the results. Compared to the free DPT, the cytotoxicity showed that blank micelles possessed great safety for Hela cells. In addition, the DPT loaded micelle formulation achieved stronger cytotoxicity at the concentration of 1 × 10^(-7) mol·L^(-1), which showed significant difference from free DPT(P < 0.05). In conclusion, the micelles were highly promising nano-carriers for the anti-tumor therapy with DPT.展开更多
文摘目的:含透明质酸钠(SH)的阿奇霉素(AZI)滴眼液最优处方的筛选及制备工艺的考察。方法:采用Box-Behnken设计,以滴眼液p H、透明质酸钠的相对分子质量和透明质酸钠的质量浓度为因素,以药物在泪液中的动力学行为作为评价指标,考察各因素的影响,确定最合理的处方。进一步制备了阿奇霉素滴眼液,根据《中国药典》要求考察滴眼液的渗透压,黏度及表面张力。结果:阿奇霉素滴眼液的最优处方为溶液p H 5.5,透明质酸钠相对分子质量150万,透明质酸钠质量浓度为0.6 g·(100 m L)-1。为保证滴眼液的无菌要求,制剂不耐受高压蒸汽灭菌,需无菌操作。结论:采用Box-Behnken设计筛选处方是可行的,依据最优处方制备的阿奇霉素滴眼液能有效延长药物结膜滞留时间,同时满足药典对滴眼液渗透压及黏度的要求。
基金supported by the Ministry of Science and Technology of China(No.2014ZX09507001006)the National Natural Science Foundation of China(No.81501579)+2 种基金the Natural Science Foundation of Jiangsu Province(No.BK20150702)the Science and Technology Development Fund of Nanjing Medical University(No.2016NJMU105)the Priority Academic Program Development of Jiangsu Higher Education Institutions
文摘The therapeutic application of deoxypodophyllotoxin(DPT) is limited due to its poor water solubility and stability. In the present study, the micelles assembled by the amphiphilic block copolymers(m PEG-PDLLA) were constructed to improve the solubility and safety of DPT for their in vitro and in vivo application. The central composite design was utilized to develop the optimal formulation composed of 1221.41 mg m PEG-PDLLA, the weight ratio of 1 : 4(m PEG-PDLLA : DPT), 30 m L hydration volume and the hydration temperature at 40 oC. The results showed that the micelles exhibited uniformly spherical shape with the diameter of 20 nm. The drug-loading and entrapment efficiency of deoxypodophyllotoxin-polymeric micelles(DPT-PM) were about(20 ± 2.84)% and(98 ± 0.79)%, respectively, indicating that the mathematical models predicted well for the results. Compared to the free DPT, the cytotoxicity showed that blank micelles possessed great safety for Hela cells. In addition, the DPT loaded micelle formulation achieved stronger cytotoxicity at the concentration of 1 × 10^(-7) mol·L^(-1), which showed significant difference from free DPT(P < 0.05). In conclusion, the micelles were highly promising nano-carriers for the anti-tumor therapy with DPT.
