Application of a novel particle coating technology for paediatric formulation development

儿科给药制剂中存在的挑战已得到充分记录。最重要的是，必须考虑该患者人群的独特特征以及可能引入新型固体制剂（如Oro分散片）的辅料的耐受性和阈值。在考虑儿科制剂时，给药途径、不同儿童的偏好以及对剂量释放的影响都是必须考虑的挑战。在初级保健中，儿科患者临时配制的要求数量是昂贵的，即使这样，也可能无法实现改善依从性的期望结果，欧洲药品管理局规定，当以患者为中心的观点接近儿科人群时，孩子可能会拒绝服用被认为不好吃的药物。可用于儿科人群的口服途径制剂包括微型片剂、颗粒剂/喷雾剂和口服分散片（ODT）。然而，在实践层面上，仍然有儿科患者与这些制剂中的一些制剂斗争，特别是初级保健药剂师报告质地和感知味道仍然是一个问题。这些固体剂型“最适合高度可溶性药物，尽管药物的溶解度需要与掩味平衡，因为高度可溶性药物如果溶解在口腔内的唾液中，将激活舌头上的味觉受体”。这导致需要对其他可行形式的剂型进行更多的研究。掩味和可预测剂量释放的挑战，特别是对于较高剂量的制剂，仍然与儿科人群相关。能够提供具有剂量灵活性、安全性和商业可行性的儿科制剂将为制药业和患者带来优势。为了应对这些挑战，拟议项目需要评估新型干法涂层技术的可行性和优化需求。为了改善儿童的口味和可接受性问题，但重要的是认识到需要探索基线药物释放曲线，当然还有干包衣相容性的适用性。该项目的主要目标是评估包衣过程的参数，并了解这些参数如何与中性聚合物对潜在候选药物的包衣效率相关联。下一步是根据确定的优化参数评估其与一系列不同聚合物的可行性。此外，探索如何使用干燥包衣颗粒掺入用于ODT的制剂，然后评价药物释放特性。为确保一致性，需要采用预测建模方法，以利用干法包衣工艺优化、药物特性、辅料/聚合物特性和片剂生产工艺的结果。

The challenges presented in paediatric dosage formulations is well documented. Most importantly the unique profiles of this patient population must be considered as well as tolerances and thresholds for excipients that may be introduced in novel solid formulations -such as Oro-dispersible tablets. Drug administration routes, varied children's preferences and the impact on dosage release are all challenges that have to be considered when considering paediatric formulations. In primary care the number of requests for extemporaneous formulations for paediatric patients is expensive and even then, may not achieve the desired result of improved compliance, resulting in diminished clinical efficacy as well as the obvious caveat that these formulations have not been properly studied in paediatric populations.The European Medicines Agency stipulates various benefits when approaching paediatric populations with a patient centred perspective as a child may refuse to take medicine that is considered unpalatable. Oral route formulations available for paediatric populations include mini-tablets, granules/sprinkles and Oro-dispersible tablets (ODT). On a practical level however, there are still paediatric patients that struggle with some of these formulations, in particular primary care pharmacists report texture and perceived taste still being an issue. These solid dose formulations "are most suited to highly soluble drugs, although the solubility of the drug needs to be balanced with taste-masking as highly soluble drugs will activate taste receptors on the tongue if they dissolve in saliva within the oral cavity". Which leads to the need for more research into other viable forms of dosage formulations.The challenge of taste masking and predictable dose release, especially for higher dose formulations is still as relevant to the paediatric population. Being able to offer paediatric formulations that offer dose flexibility, safety and commercial feasibility would offer advantages to the pharmaceutical industry as well as to patients. To address these challenges the proposed project would need to evaluate the feasibility and optimisation needs of novel dry coating technologies. To ameliorate issues of taste and acceptability amongst children but importantly recognise the need to explore a base line drug release profile and of course the applicability of dry coating compatibility.Key objectives for the project would be to evaluate the parameters of the coating process and understand how these parameters are linked to the coating efficiency of neutral polymers on potential drug candidates. The next step is to assess it's viability with a range of different polymers based on the determined optimised parameters. Furthermore, to explore how a formulation for ODT would be incorporated using dry coated particles and then evaluating the drug release properties. To ensure consistency a predictive modelling approach would be need to utilising the outcomes from the dry coating process optimisation, the drug properties, excipient/polymer properties and the tablet manufacturing processes.