Yunchao He,Yaling Wu,Lingping Cheng,Shanshan He,Qiuhua Wang,Huiying Wang,Yanxiong Ke
Ketorolac has been widely applied in clinical medicine for its antipyretic, analgesic and anti-inflammatory pharmacological activity. Research showed that the analgesic effect of the S enantiomer is 230 times stronger than that of the R enantiomer. Getting the high-purity S enantiomer of Ketorolac has profound significance but still remains a challenging topic. In this work, the separation of the R and S enantiomers of Ketorolac was investigated on polysaccharide-based chiral stationary phases. Chiralcel AD-H, OD-H, OJ-H and AS-H columns were evaluated using polar organic and normal phase mode, respectively, in which the OJ-H column showed the best performance with high selectivity and resolution for Ketorolac with α = 2.43 and R S = 9.04 by using methanol/formic acid (100:0.1, v/v) as the mobile phase. The influences of acid additive, composition of mobile phase and temperature were examined. The coating amount of cellulose tris- (4-methylbenzoate) has significant influence on the sample loadability. The high loadability of chiral stationary phases coated with 40% of cellulose tris- (4-methylbenzoate) allows preparative separation up to 16 mg on an analytical column of 250 × 4.6 mm id in a single run for Ketoroac using methanol/formic acid (100:0.1, v/v) as mobile phase, which shows a potential application in industrial preparation.
Aortic dissection is a serious health risk and has led to interest in creating effective drug treatments like ketorolac. However, conventional administration techniques lack specificity, which limits their effectiveness and may result in adverse effects. A microneedle patch system (MNPS) offers a minimally invasive, pain-free alternative with a high capacity for drug delivery, but there is still a gap in the direction of treating aortic dissection. Here, we present a novel biodegradable MNPS with a pagoda-shaped structure designed for drug loading. These MNPS were fabricated using a stepwise mold replication method, with the medication embedded in the top layer of the MNPS. The double-layered pagoda structure enhances MNPS adhesion, enabling it to withstand the impact of aortic blood flow and enhancing drug targeting. In conclusion, our pagoda MNPS introduces a new approach for treating aortic dissection, providing hope for affected patients.
Chenxi Li,Chunyan Li,Zheshuo Liu,Qiuhong Li,Xueying Yan,Yu Liu,Weiyue Lu
The objective of this study was to construct a new in situ gel system based on the combination of poloxamer 407 and carrageenan (carrageenan–poloxamer 407 hydrogel, CPH) for intranasal delivery of ketorolac tromethamine . CPH showed potassium ion concentration - dependent erosion characteristics which ensured slow erosion in aqueous environment containing potassium ion at the physiological level. Loading with ketorolac tromethamine influenced erosion, drug release and thermosensitive properties of CPH. CPH containing 15% ketorolac tromethamine showed suitable gelation temperature (near 35 °C) and in vitro sustained release profiles. Pharmacokinetic study of intranasal CPH containing 15% ketorolac tromethamine in rats demonstrated enhanced absolute bioavailability (68.8 ± 23.3%) and prolonged mean residence time (8.8 ± 3.5 h) in comparison with the intranasal solution group (24.8 ± 13.8%, 3.9 ± 0.6 h). Nasal ciliotoxicity evaluation on an in situ toad palate model preliminarily showed the safety of CPH for intranasal use. All results suggested the potential of CPH as a new sustained - release platform for the intranasal delivery of ketorolac tromethamine.
危险品化学品经营许可证（带存储）