直肠布洛芬黏附水凝胶的制备与研究

IF 0.1 Q4 MEDICINE, GENERAL & INTERNAL Medical-Surgical Journal-Revista Medico-Chirurgicala Pub Date : 2022-09-30 DOI:10.22551/msj.2022.03.18
E. Rédai
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引用次数: 0

摘要

摘要):直肠途径代表了儿科口服给药的另一种选择。布洛芬是一种非甾体抗炎药,用于所有年龄组,以减轻疼痛,发烧和炎症。目的:研制并表征含布洛芬黏附直肠凝胶。材料与方法:以卡波波尔940、海藻酸钠和低粘度羟丙基甲基纤维素HPMC为成胶剂,丙烯乙二醇和甘油为渗透增强剂。5%的布洛芬被纳入所有配方。制备了三种凝胶,分别含有1%卡波波尔、0.5%卡波波尔和5% HPMC以及5%海藻酸钠。研究了配方变量对药技参数(黏附性、pH值和扩散)的影响。使用Franz细胞在受体介质中测量API通过膜释放的量。用数学模型模拟了活性物质的释放过程。结果:凝胶的pH值在4.2 ~ 5.0之间。粘度在165 - 212 mpa之间变化。分离力范围为0.02 ~ 0.12 n,三种凝胶均适用于儿童和成人。结论:实验结果表明,5%海藻酸钠凝胶释放布洛芬效果较好。
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Formulation and study of rectal ibuprofen mucoadhesive hydrogels
HYDROGELS Abstract): The rectal route represents an alternative to oral administration in pediat-rics. Ibuprofen is a non- steroidal anti-inflammatory agent, used in all age groups to reduce pain, fever, and inflammation. Aim: to develop and characterize ibuprofen-containing mucoadhesive rectal gels. Material and methods: Carbopol 940, sodium alginate, and low viscosity hydroxypropyl methylcellulose HPMC were used as gel-forming agents and propyl-ene-glycol and glycerin as permeation enhancers. 5% of ibuprofen was incorporated in all formulations. Three gels have been prepared containing 1% Carbopol, 0.5% Carbopol and 5% HPMC, and 5% sodium alginate. The influence of formulation variables on the pharma-co-technical parameters (adhesivity, pH, and diffusion) was studied. The amount of API released through the membrane using a Franz cell in the acceptor media was measured. Mathematical models were applied to model the release of the active substance. Results: The pH of gels ranged between 4.2-5.0. Viscosity varied between 165 and 212 mPas. The detachment force was from 0.02 to 0.12 N. All three gels were formulated suitable for children and adults. Conclusions: The obtained experimental results showed a superior release of ibuprofen from the 5% sodium alginate gel.
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