Application of a novel particle coating technology for paediatric formulation development

儿科用药配方所面临的挑战是有据可查的。最重要的是，必须考虑这一患者群体的独特特征，以及可能在新型固体制剂中引入的辅料的耐受性和阈值--例如口服分散片。给药途径、不同儿童的偏好以及对剂量释放的影响都是在考虑儿科配方时必须考虑的挑战。在初级保健中，要求为儿科患者提供即兴配方的次数很昂贵，即使这样，也可能达不到改善依从性的预期结果，导致临床疗效降低，以及这些配方没有在儿科人群中进行适当研究的明显警告。欧洲药品管理局规定，在以患者为中心的角度接近儿科人群时，有各种好处，因为儿童可能会拒绝服用被认为令人不快的药物。可供儿科人群使用的口服制剂包括迷你片剂、颗粒剂/喷雾剂和口腔分散片(ODT)。然而，在实践层面上，仍然有儿科患者与其中一些配方作斗争，特别是初级保健药剂师报告说，质地和感知味道仍然是一个问题。这些固体剂量配方“最适合于高可溶性药物，尽管药物的溶解度需要与味觉掩蔽相平衡，因为如果高可溶性药物溶解在口腔内的唾液中，它们将激活舌头上的味觉感受器”。这导致需要对其他可行的剂型进行更多的研究。味觉掩蔽和可预测的剂量释放的挑战，特别是对于更高剂量的剂型，仍然与儿科人口有关。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，拟议的项目将需要评估新的干涂技术的可行性和优化需求。为了改善儿童的口感和接受性问题，但重要的是认识到需要探索基线药物释放概况，当然还有干衣剂兼容性的适用性。该项目的关键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，用一系列不同的聚合物评估其可行性。此外，探索如何使用干燥包衣颗粒将ODT配方并入，然后评估药物释放性能。为了确保一致性，需要使用预测建模方法来利用干包衣工艺优化、药物特性、赋形剂/聚合物特性和片剂制造工艺的结果。

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.