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Pimecrolimus
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Pimecrolimus is a derivative of the macrolactam ascomycin with immunosuppressant and immunomodulating properties. Its mechanism of action involves calcineurin inhibition, blockage of T-cell activation, blocking signal transduction pathways in T-cells, reducing the ability of mast cells to release chemicals that promote inflammation, and inhibition of the synthesis of inflammatory cytokines, specifically Th1- and Th2-type cytokines. Pimecrolimus is indicated for topical treatment of mild to moderate atopic dermatitis (1).
Hand Dermatitis
Published in Donald Rudikoff, Steven R. Cohen, Noah Scheinfeld, Atopic Dermatitis and Eczematous Disorders, 2014
Nina C. Botto, Erin M. Warshaw
Topical pimecrolimus and tacrolimus, ascomycin-derived agents that inhibit inflammatory cytokine production by T lymphocytes and mast cells, have been studied in the treatment of atopic dermatitis and allergic contact dermatitis (Grassberger et al. 1999). In a double-blind, vehicle-controlled study of patients with chronic hand dermatitis, twice-daily application of pimecrolimus 1% cream with overnight occlusion was superior to vehicle alone, especially in those without palmar involvement (Belsito et al. 2004). On the other hand, a questionnaire survey of patients with hand dermatitis failed to show any significant change in quality of life or work productivity with pimecrolimus treatment compared with vehicle (Reilly et al. 2003). A prospective, open, multicenter study of 29 patients with mild-to-moderate occupational hand dermatitis suggests that topical tacrolimus ointment 0.1% can also be an effective treatment option (Schliemann et al. 2008).
Effect of Soluplus on the supersaturation and absorption of tacrolimus formulated as inclusion complex with dimethyl-β-cyclodextrin
Published in Pharmaceutical Development and Technology, 2019
Chun Tao, Taotao Huo, Qian Zhang, Hongtao Song
The separation was carried out using an Agilent Poroshell 120 EC-C18 column (50 × 2.1 mm, 2.7 μm; Agilent, Santa Clara, CA). Methanol and water (9: 1) containing 2 mmol/l ammonium acetate and 0.1% formic acid were used as the mobile phase at a flow rate of 0.3 ml/min. The column temperature was set at 40 °C, and 1 μl of sample was injected. The detection was performed by a triple quadrupole detector (SCIEX QTRAP® 5500; AB, US). The mass spectrometer was operated using an electrospray ionization interface in positive ionization mode, and using a multiple reaction monitoring mode. The selected reaction monitoring (SRM) of FK506 and ascomycin was m/z 821.5 → 768.4 and m/z 809.5 → 759.5 for quantitation, respectively. The concentration of FK506 was determined by a standard linear calibration curve in the concentration range of 0.2–25 ng/ml.
Preparation and study of two kinds of ophthalmic nano-preparations of everolimus
Published in Drug Delivery, 2019
Zhan Tang, Lina Yin, Yawen Zhang, Wenying Yu, Qiao Wang, Zhajun Zhan
Everolimus (EVR, purity > 98%) was purchased from Lunan Pharmaceutical Group Corporation (Shandong, China), and internal standard ascomycin (IS) was purchased from Gene Operation (Ann Arbor, MI, USA, purity > 99%, QAS1212). Tween-80 and polyoxyethylene (40) stearate (P40S) were supplied by Sigma-Aldrich (St. Louis, MO, USA). Pluronic P407 was from BASF (Ludwigshafen, Germany). Hydroxypropylmethylcellulose and glutamine were purchased from Aladdin (Shanghai, China). Polyvinyl alcohol with low viscosity was obtained from Jiangxi Alpha Gaoke Pharmaceutical Corporation (Jiangxi, China). Methanol was purchased from Merk (Darmstadt, Germany), acetonitrile was from Tedia (Fairfield, OH, USA), and formic acid was from ACS (Wilmington, DE, USA) and all were of HPLC-grade. Ammonium formate was supplied by Sinopharm Chemical Reagent Co., Ltd (Shanghai, China). Water purification was carried out with the Milli-Q ultra-pure water system (Millipore, Darmstadt, Germany). Other reagents were of analytical grade and commercially available.
Design of novel tacrolimus formulations with chemically synthesized oils for oral lymphatic delivery
Published in Drug Development and Industrial Pharmacy, 2020
Takayuki Yoshida, Kazuhiro Sako, Hiromu Kondo
Tacrolimus was provided by Astellas Pharma Inc. (Tokyo, Japan). Sunflower oil (Nikko Chemicals Co. Ltd., Tokyo, Japan), MCT (Miglyol 810, Watahan Trading Co. Ltd., Tokyo, Japan), and GMS (F75MV, F50MV, Nikko Chemicals Co. Ltd.) were used for the oil formulations. Ascomycin and concanavalin A (Lot: S0619) were purchased from Wako Pure Chemical Industries Ltd. (Tokyo, Japan) and Funakoshi Co. Ltd. (Tokyo, Japan), respectively. Methanol, acetonitrile, hexane, zinc sulfate, and ammonium acetate were provided by Kanto Chemical Co. Inc. (Tokyo, Japan). Lymphosepar® II (Immuno-Biological Laboratories Co. Ltd., Gunma, Japan) was used for separation of lymphocytes from blood.