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首页> 外文期刊>Colloids and Surfaces, B. Biointerfaces >A novel oil-based suspension of a micro-environmental, pH-modifying solid dispersion for parenteral delivery: Formulation and stability evaluation
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A novel oil-based suspension of a micro-environmental, pH-modifying solid dispersion for parenteral delivery: Formulation and stability evaluation

机译：微环境的新型油基悬浮液，对肠胃外递送的微环境，pH-改性固体分散体：配方和稳定性评估

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The objective of this study was to evaluate a novel oil-based suspension as a potential parenteral drug delivery system for drugs with poor water solubility. Most of the new active pharmaceutical ingredients are weak acid or basic drugs with pH-dependent solubility. To limit this dependence, use of micro-environmental pH-modifying solid dispersions (micro pHm SD) has been proved to increase the bioavailability of these drugs. Toltrazuril (TOL), a weakly acidic drug with poor aqueous and pH-dependent solubility, was studied as a model drug. Recently, studies on TOL with focus on the parenteral injection are rarely to find in the literature. A novel parenteral oil-based TOL suspension was prepared containing TOL micro pHm SD (TSD) powders suspended in oil-based vehicles and the optimal formulation was screened. The stability of this formulation was assessed considering particle size distribution, settling volume ratio, redispersibility, thermal stability, and drug content. The optimized white oil-based TOL pHm SD suspension (W-TSDS) showed significant improved stability and shear-thinning behavior. In particular, fumed silica as suspending agent positively influenced the physical stability of the formulation. Furthermore, W-TSDS showed good injectability using 21 G needles and more rapid and sustained drug release compared to TSD powders in vitro. In the in vivo safety evaluation, W-TSDS showed good histocompatibility in rabbits injected subcutaneously or intramuscularly. We believe these findings provide an alternative choice of dosage form for the delivery of new active pharmaceutical ingredients.
机译：本研究的目的是评估一种新的油基悬浮液作为水溶性差的药物肠胃外药物递送系统。大多数新的活性药物成分是弱酸或具有pH依赖性溶解度的碱性药物。为了限制这种依赖性，已经证明了使用微环境pH调制固体分散体（微pHM SD）以增加这些药物的生物利用度。作为模型药物，研究了含有差的水性和pH依赖性溶解度的弱酸性药物。最近，对肠外注射的重点的研究很少在文献中找到。制备新的肠胃外油基Tol悬浮液，含有悬浮在油基载体中的Tol Micro PHM Sd（TSD）粉末，筛选最佳制剂。考虑粒度分布，沉降体积比，再分散性，热稳定性和药物含量评估该配方的稳定性。优化的白油基Tol PHM SD悬浮液（W-TSDS）显示出显着的稳定性和剪切稀疏行为。特别地，烟雾二氧化硅作为悬浮剂积极影响配方的物理稳定性。此外，与体外TSD粉末相比，W-TSDS使用21g针头和更快速和持续的药物释放显示出良好的可注射性。在体内安全评估中，W-TSD在皮下或肌肉内注射的兔子中表现出良好的组织相容性。我们认为这些发现提供了用于提供新的活性药物成分的替代选择剂型。

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