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The characterization and dissolution performances of spray dried solid dispersion of ketoprofen in hydrophilic carriers

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Asian Journal of Pharmaceutical Sciences 2015年第5期10卷 372-385页

作者： Siok-Yee Chan Yin-Ying Chung Xin-Zi Cheah Eryn Yen-Ling Tan Joan Quah School of Pharmaceutical Sciences Universiti Sains Malaysia11800 Pulau PinangMalaysia

Solid dispersion is one of the most promising strategies to improve oral bioavailability of poorly soluble ***,there are inconsistent dissolution performances of solid dispersion reported which entails further *** this study,solid dispersions of ketoprofen in three hydrophilic carriers,*** K30,PVPVA 6:4 and PVA were prepared and *** characterization of the physical mixture of ketoprofen and carriers shows certain extent of amorphization of the *** result is coinciding to evaluation of drug-polymer interaction using ATR-FTIR whereby higher amorphization was seen in samples with higher drug-polymer *** scanning confirms that fully amorphous solid dispersion was obtained for SD KTP PVP K30 and PVPVA system whereas partially crystalline system was obtained for SD KTP ***,dissolution profiles of the solid dispersion had shown that degree of amorphization of KTP was not directly proportional to the dissolution rate enhancement of the solid dispersion ***,it is concluded that complete amorphization does not guarantee dissolution enhancement of an amorphous solid dispersion system.

关键词： Solid dispersion Amorphous Polymer PVP PVPVA ketoprofen

Two kinds of ketoprofen enteric gel beads(CA and CS-SA) using biopolymer alginate

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Asian Journal of Pharmaceutical Sciences 2018年第2期13卷 120-130页

作者： Bingchao Cheng Dongyang Li Qiye Huo Qianqian Zhao Qi Lan Mengsuo Cui Weisan Pan Xinggang Yang Department of Pharmaceutics School of Pharmaceutical Sciences Shenyang Pharmaceutical University State Key Laboratory of New-tech for Chinese Medicine Pharmaceutical Process

To obtain expected rapid-release and sustained-release of ketoprofen gel beads, this paper adopted biopolymer alginate to prepare alginate beads and chitosan-alginate gel beads. Formulation factors were investigated and optimized by the single factor test. The release of ketoprofen from calcium alginate gel beads in pH 1.0 hydrochloric acid solution was less than 10% during 2 h, then in pH6.8 was about 95% during 45 min, which met the requirements of rapid-release preparations. However, the drug release of chitosan-alginate gel beads in pH1.0 was less than 5% during 2 h, then in pH6.8 was about 50% during 6 h and reached more than 95% during 12 h, which had a good sustained-release behavior. In addition, the release kinetics of keteprofen from the calcium alginate gel beads fitted well with the Korsmeyer–Peppas model and followed a case-II transport mechanism. However, the release of keteprofen from the chitosan-alginate gel beads exhibited a non-Fickian mechanism and based on the mixed mechanisms of diffusion and polymer relaxation from chitosanalginate beads. In a word, alginate gel beads of ketoprofen were instant analgesic, while chitosan-alginate gel beads could control the release of ketoprofen during gastrointestinal tract and prolong the drug's action time.

关键词： Gel beads Enteric rapid-release Enteric sustained-release ketoprofen

Resolving ketoprofen Using n-Octyl-d-glucamine as an Optical Resolution Agent

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Chinese Journal of Chemical Engineering 2005年第4期13卷 568-571页

作者：朱圣东吴元欣喻子牛 School of Chemical Engineering and Pharmacy Wuhan Institute of Chemical Technology College of Life Science and Technology Huazhong Agricultural University

The process of resolution of racemic ketoprofen using n-octyl-d-glucamine as an optical resolution agent was investigated. The process consists of preparation of the diastereomer salt of ketoprofen with n-octyl-d-glucamine, liberation of S-(+)-ketoprofen from its diastereomer salt and recovery of the remaining ketoprofen and n-octyl-d- glucamine. The suitable conditions for preparation of the diastereomer salt were methanol and ethyl acetate (1.1 by volume) as the solvent, the ratio of solvent volume to ketoprofen mass at 8ml:1g, and the molar ratio of ketoprofen to n-octyl-d-glucamine at 1:1. The preferred approach to liberate S-(+)-ketoprofen from its diastereomer salt was alkali dissolution, acid adjustment and ethyl acetate extraction. Racemization of the recovered ketoprofen could be achieved by reacting the recovered ketoprofen with 10% NaOH at 507 kPa for 6h. The recovered n-octyl-d- glucamine could be refined by acid dissolution and alkali adjustment. S-(+)-ketoprofen can be obtained with high optical purity and yield, showing that the present process is a practical and efficient one which can be used in industrial scale for preparation of S-(+)-ketoprofen.

关键词： ketoprofen resolution n-octyl-d-glucamine

Effects of ketoprofen, Ketamine, Lidocaine and Propofol on Fentanyl-Induced Hyperalgesia in Rats

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Journal of Biosciences and Medicines 2022年第7期10卷 53-63页

作者： Camila dos Santos Leite Naira Correia Cusma Pelógia Eliane Stevanato Marília Hidalgo Uchôas Gabriela Apóstulo Silva Guilherme Apóstulo Silva Carlos Augusto Pires Zerbini Marta Helena Rovani Pires Oscar César Pires Laboratory of Immunopharmacology and Molecular Biology S&atilde o Francisco University Medical School Bragan&ccedil a Paulista Brazil Laboratory of Cell and Molecular Tumor Biology and Bioactive Compounds S&atilde o Francisco University Medical School Bragan&ccedil a Paulista Brazi Laboratory of Pharmacology and Physiology Medicine Department Taubaté University Taubaté Brazil Vera Cruz Hospital Campinas Brazil

Opioid-induced hyperalgesia negatively affects physiological pain management and presents a complex causal mechanism, involving, pharmacodynamic and pharmacokinetic factors of interactions with receptors, opioid-independent ascending systems and with pro-nociceptive systems. After approval by the CEUA, 42 male Wistar rats were divided into 7 groups: In group 1 (GCSSL) the animals received 1 ml of 0.9% saline solution intraperitoneally (IP);in group 2 (GFTSL), they received fentanyl at a dose of 100 ug·kg-1 IP;in the remaining groups (3, 4, 5, 6 and 7) the animals received IP, fentanyl at a dose of 100 ug·kg-1 followed also by IP route of: group 3 (GFTKP) ketoprofen at a dose of 5 mg·kg-1;group 4 GFTKT), ketamine up to a dose of 10.0 mg·kg-1;group 5 (GFTLI), incisional lidocaine up to a dose of 10 mg·kg-1;group 6 (GFTLP), intraperitoneal lidocaine up to a dose of 10 mg·kg-1 and group 7 (GFTPP), propofol up to a dose of 60 mg·kg-1. Under general anesthesia, all animals with a plantar surgical incision. Hyperalgesia was evaluated by applying Von Frey filaments on the 2nd, 1st, 3rd and 5th days after treatment. In the 2nd hour and on the 5th day after the procedure, there was no hyperalgesia associated with the use of fentanyl, however, on the 1st and 3rd postoperative days there was hyperalgesia that was attenuated by ketoprofen, ketamine, lidocaine infiltrated in the incision and intraperitoneally, an effect not observed with the use of propofol. The results suggest fentanyl-induced hyperalgesia and the efficacy of ketoprofen, ketamine, incisional lidocaine and intraperitoneal lidocaine in reducing this effect.

关键词： Hyperalgesia Fentanyl ketoprofen Ketamine Lidocaine Propofol Rats

Determination of ketoprofen in Human Plasma by RP-HPLC

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American Journal of Analytical Chemistry 2013年第5期4卷 252-257页

作者： Farya Zafar Muhammad Harris Shoaib Asia Naz Rabia Ismail Yousuf Huma Ali Department of Pharmaceutical Chemistry Faculty of PharmacyUniversity of Karachi Karachi Pakistan Department of Pharmaceutics Faculty of Pharmacy University of Karachi Karachi Pakistan Ziauddin College of Pharmacy Ziauddin University Karachi Pakistan

For in vivo pharmacokinetic studies, it is pre-requisite to quantify drug concentrations in plasma. In the present study a RP-HPLC procedure was developed and validated for the assessment of ketoprofen in human plasma. For this purpose mobile phase consisting of methaol:water (70:30) adjusted to pH 3.3 with phosphoric acid was used, and chromatography was carried out on Discovery HS C18 column, 5 μm (25 cm × 4.6 mm). The flow rate was 1 mL·min-1 and quantitative assessment was performed at 260 nm. The retention time was found to be was found to be accurate and illustrated linearity from 0.2441 to 125 μg·mL-1 with the determination coefficient (r2) of 0.9999, also accuracy and precision were found to be ketoprofen in human plasma.

关键词： RP-HPLC ketoprofen Linearity Accuracy Precision Specific

The Extent of Solubilization of Flurbiprofen and ketoprofen by Cetyltrimethylammonium Micelles Using Semi-Equilibrium Dialysis

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Advances in Materials Physics and Chemistry 2020年第4期10卷 97-109页

作者： Jimmy D. Roach Ibrahim Laswi Malik Mushannen Ali Chaari Mandy Bondaruk Pre-Medical Education Unit Weill Cornell Medical College-Qatar Doha Qatar

The partitioning of two non-steroidal anti-inflammatory drugs (NSAIDs), flurbiprofen and ketoprofen, into cationic cetyltrimethylammonium micelles was investigated using semi-equilibrium dialysis at 37℃ in phosphate buffered saline. The micellar-water solubilization equilibrium constants for both NSAIDs, in their deprotonated forms, were observed to decrease linearly with increasing mole fraction of drug in micelles. For flurbiprofen, the solubilization constant in the limit as mole fraction of drug in micelles approaches zero was found to be 11,200 (co = 1 M), while for ketoprofen the value was 1950 (co = 1 M). Using 1H-NMR and UV spectroscopic techniques, the locus of solubilization for ketoprofen was found to be towards the charged exterior of the micelles, in the Stern layer, whereas flurbiprofen was found to solubilize more in the micellar interior.

关键词： Flurbiprofen ketoprofen CTAB Micelle Solubilization

Effects of Ginsenosides and ketoprofen on Smoke Inhalation Injury in Rabbits and Rats

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