66635-74-3Relevant academic research and scientific papers
Ketorolac derivative, pharmaceutical composition and preparation method and application thereof
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Paragraph 0302-0306, (2022/01/08)
The present invention provides a ketorolac derivative shown in formula (I), a pharmaceutical composition and a method and application thereof. As a drug, the ketorolac derivative has better half-life, stability, good pharmacokinetic properties, high stabi
Effective mamagement of acute postoperative pain using intravenous emulsions of novel ketorolac prodrugs: in vitro and in vivo evaluations
Chen, Yong,Huang, Qian,Niu, Bixi,Qiu, Nanqing,Yin, Zongning,Yu, Yuting,Zhu, Qing,Zhuang, Xiaoxiao
, (2020/04/29)
The aim was to prepare intravenous fat emulsions (IFEs) of ketorolac (KTL) ester prodrugs and to investigate the pharmacokinetics and pharmacodynamics of these formulations. Three prodrugs of KTL (KTL-IS, KTL-AX and KTL-BT) were synthesized as a means to increase the lipid solubility of KTL. All KTL prodrugs with higher Log P values presented increased tendency to partition into a blank IFE using extemporaneous addition method – the encapsulation efficiency of KTL-IS IFE and KTL-BT IFE was more than 97percent. The particle sizes and zeta potentials of these two formulations were comparable to that of the blank IFE. PK studies in rabbits showed significant larger AUC0-8h (646.969 ± 154.326 mg/L?h?1 for KTL-IS IFE and 559.426 ± 103.057 mg/L?h?1 for KTL-BT IFE) than that of ketorolac tromethamine (KTL-T) injectable (286.968 ± 63.045 mg/L?h?1) and approximately 2-fold increases in the elimination t1/2 over KTL-T. In a rat postoperative pain model, the paw withdrawal thresholds and the paw withdrawal latency after I.V. KTL prodrug IFEs were significantly higher than that after I.V. KTL-T at 3~4 h. Effective controlling of acute postoperative pain in a longer duration can be achieved by using non-addictive ketorolac derivatives intraveneous emulsions.
Ketorolac ester derivative intravenous injection lipid emulsion, preparing method and application
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Paragraph 0073; 0080-0082, (2019/10/29)
The invention belongs to the field of pharmaceutic preparations, and particularly relates to a ketorolac ester derivative intravenous injection lipid emulsion, a preparing method and application. According to the intravenous injection lipid emulsion, ketorolac ester derivatives and caffeine are dissolved in an intravenous emulsion to form emulsion grains as the medicine carrier; a ketorolac esterpro-drug can be dissolved in small oil drops (emulsion grains) of the intravenous emulsion or on an interface membrane, the physical and chemical properties can be kept stable in the storage process under certain conditions, the slow release performance is improved, and the drug function time is prolonged.
Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids and related compounds
Muchowski,Unger,Ackrell,Cheung,Cooper,Cook,Gallegra,Halpern,Koehler,Kluge
, p. 1037 - 1049 (2007/10/02)
5-Acyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids and the homologous pyridine and azepine derivatives were synthesized and assayed for antiinflammatory and analgesic activity. 5-Benzoyl-1,2-dihydro-3H-pyrrolo-[1,2-a]pyrrole-1-carboxylic acid and the corresponding p-methoxy compound were selected for evaluation as analgesic agents in humans on the basis of their high potency in the mouse phenylquinone writhing assay as well as on their minimal liability to elicit gastrointestinal erosion in rats on chronic administration. Extensive quantitative structure-activity relationship (QSAR) studies of the benzoylpyrrolopyrrolecarboxylic acids have demonstrated that the analgesic (mouse writhing) and antiinflammatory (rat carrageenan paw) potencies of these compounds are satisfactorily correlated with the steric and hydrogen-bonding properties of the benzoyl substituent(s). The 4-vinylbenzoyl compound, which was correctly predicted to be highly active in both assays on this basis, is undergoing advanced pharmacological evaluation in animals as a potential antiinflammatory agent.
