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Preparation and the Biopharmaceutical Evaluation for the Metered Dose Transdermal Spray of Dexketoprofen

机译:克索洛芬计量透皮喷雾剂的制备及生物制药评价

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The objective of the present work was to develop a metered dose transdermal spray (MDTS) formulation for transdermal delivery of dexketoprofen (DE). DE release from a series of formulations was assessedin vitro. Various qualitative and quantitative parameters like spray pattern, pump seal efficiency test, average weight per metered dose, and dose uniformity were evaluated. The optimized formulation with good skin permeation and an appropriate drug concentration and permeation enhancer (PE) content was developed incorporating 7% (w/w, %) DE, 7% (v/v, %) isopropyl myristate (IPM), and 93% (v/v, %) ethanol.In vivopharmacokinetic study indicated that the optimized formulation showed a more sustainable plasma-concentration profile compared with the Fenli group. The antiinflammatory effect of DE MDTS was evaluated by experiments involving egg-albumin-induced paw edema in rats and xylene-induced ear swelling in mice. Acetic acid-induced abdominal constriction was used to evaluate the anti-nociceptive actions of DE MDTS. Pharmacodynamic studies indicated that the DE MDTS has good anti-inflammatory and anti-nociceptive activities. Besides, skin irritation studies were performed using rat as an animal model. The results obtained show that the MDTS can be a promising and innovative therapeutic system used in transdermal drug delivery for DE.
机译:本工作的目的是开发用于透皮递送右酮洛芬(DE)的定量透皮喷雾剂(MDTS)制剂。在体外评估了一系列制剂的DE释放。评估了各种定性和定量参数,例如喷雾模式,泵密封效率测试,每计量剂量的平均重量和剂量均匀性。开发了具有良好皮肤渗透性和适当药物浓度和渗透促进剂(PE)含量的优化配方,其中包含7%(w / w,%)DE,7%(v / v,%)肉豆蔻酸异丙酯(IPM)和93 %(v / v,%)乙醇。体内药代动力学研究表明,与Fenli组相比,优化的制剂显示出更可持续的血浆浓度分布。通过涉及卵白蛋白诱导的大鼠足水肿和二甲苯诱导的小鼠耳朵肿胀的实验评估了DE MDTS的抗炎作用。乙酸引起的腹部收缩被用于评估DE MDTS的抗伤害感受作用。药效学研究表明DE MDTS具有良好的抗炎和抗伤害感受活性。此外,以大鼠为动物模型进行了皮肤刺激性研究。获得的结果表明,MDTS可能是用于DE的透皮药物递送的有前途的创新治疗系统。

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