Yurtdaş-Kırımlıoğlu Gülsel
Department of Pharmaceutical Technology, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.
Pharm Dev Technol. 2021 Apr;26(4):476-489. doi: 10.1080/10837450.2021.1889584. Epub 2021 Mar 1.
The aim of this study was the development of hard-cellulose capsules containing cefpodoxime proxetil (CEF) (BCS Class II) loaded novel Pluronic F127 (P127)/Polyvinylpyrrolidone K30 (PVP) solid dispersions (SDs) using ultrasonic probe induced solvent-lyophilization method for effective antibacterial treatment by means of improved saturated aqueous solubility, dissolution rate, reduced particle size, and wettability. SDs were evaluated for physical and solid-state analyses. The solubility of pure CEF was calculated as 0.269 ± 0.005 mg/mL, SDs formulated with P127/PVP exhibited increased solubility from 3.5- to 8-fold. Molecular distribution of CEF in SDs and formation of CEF loaded amorphous polymeric network were confirmed with morphological study, thermal analysis, Fourier-transform infrared spectroscopy (FT-IR), and H-NMR studies. (ATCC 29213), (ATCC 25922), and (ATCC 700603) were used to investigate the antibacterial effectiveness of the SDs. The minimum inhibitory concentration (MIC) values of the P127/PVP SDs were found 2-8 times lower than the pure CEF. All SDs from hard-cellulose capsules exhibited significantly faster release than unprocessed CEF. The profiles of SDs and reference were detected to be dissimilar according to difference (f) and similarity factor (f). Hard-cellulose capsules containing CEF loaded P127/PVP SDs appear to be feasible alternative to commercially available CEF tablets for effective antibacterial therapy at lowest dose.
本研究的目的是利用超声探头诱导溶剂冻干法开发含头孢泊肟酯(CEF)(BCS II类)的硬胶囊,负载新型普朗尼克F127(P127)/聚乙烯吡咯烷酮K30(PVP)固体分散体(SDs),以通过提高饱和水溶液溶解度、溶解速率、减小粒径和润湿性来实现有效的抗菌治疗。对固体分散体进行了物理和固态分析评估。计算出纯CEF的溶解度为0.269±0.005mg/mL,用P127/PVP配制的固体分散体的溶解度提高了3.5至8倍。通过形态学研究、热分析、傅里叶变换红外光谱(FT-IR)和氢核磁共振(H-NMR)研究证实了CEF在固体分散体中的分子分布以及负载CEF的无定形聚合物网络的形成。使用(ATCC 29213)、(ATCC 25922)和(ATCC 700603)来研究固体分散体的抗菌效果。发现P127/PVP固体分散体的最低抑菌浓度(MIC)值比纯CEF低2至8倍。硬胶囊中所有的固体分散体均表现出比未处理的CEF释放速度明显更快。根据差异因子(f)和相似性因子(f)检测到固体分散体和参比制剂的溶出曲线不同。含有负载CEF的P127/PVP固体分散体的硬胶囊似乎是市售CEF片剂的可行替代品,可在最低剂量下实现有效的抗菌治疗。