Ferreira Anderson de Oliveira, Polonini Hudson
Fagron BV, Rotterdam, The Netherlands.
Int J Pharm Compd. 2022 Jul-Aug;26(4):283-291.
The development of an efficient formulation for hardshell capsules needs to consider pharmaceutical and biopharmaceutical aspects to assist in the careful selection of excipients, which are essential ingredients for the formulation's good performance. They ensure correct bioavailability, solubility, stability, dose accuracy (weight variation and content uniformity), and organoleptic characteristics. Given this, DiluCap was developed as a line of excipients so that the pharmacist can compound every capsule formulation with ease and trust in its final characteristics. The line is composed of six excipients: 1) Dilucap SLD, for soluble active pharmaceutical ingredients Class I and III from the Biopharmaceutical Classification System - it promotes disintegration without a negative impact on dissolution; 2) Dilucap PSD, for poorly soluble active pharmaceutical ingredients Class II and IV - it favors the disintegration and dissolution of the active pharmaceutical ingredients; 3) Dilucap SR, for active pharmaceutical ingredients requiring modified/ slow release - it reduces the disintegration and release rate of the active pharmaceutical ingredients, promoting its slow release, and, also, prevents plasma peaks responsible for adverse effects; 4) DiluCap Hygro, for hygroscopic or deliquescent active pharmaceutical ingredients - it reduces hygroscopicity, deliquescence, and eutectic mixture formation; 5) DiluCap Antioxi, for active pharmaceutical ingredients susceptible to oxidation - it provides chemical stabilization due to antioxidant ingredients and reduces water activity and chemical degradation; 6) DiluCap OD, for orodispersible active pharmaceutical ingredients that can be compounded as sprinkle capsules or sublingual capsules - it favors transmucosal permeation. The testing conducted for the DiluCap line of excipients showed that all products have suitable flow properties (angle of repose and Carr's compressibility index), hygroscopicity, biopharmaceutical performance (dissolution profiles), and stability. This corroborates the allegations that DiluCap provides a science based line of excipients to the compounding pharmacies with proven functionality that saves time (reduces the preprocessing and the number of items in stock) and guarantees efficacy and safety of hard-shell oral capsules formulations.
开发一种高效的硬胶囊制剂需要考虑药学和生物药学方面的因素，以帮助谨慎选择辅料，辅料是制剂良好性能的关键成分。它们确保正确的生物利用度、溶解度、稳定性、剂量准确性（重量差异和含量均匀度）以及感官特性。鉴于此，DiluCap作为一系列辅料而开发，以便药剂师能够轻松地调配每种胶囊制剂，并对其最终特性充满信心。该系列由六种辅料组成：1）Dilucap SLD，用于生物药剂学分类系统中的I类和III类可溶性活性药物成分——它促进崩解，且对溶出无负面影响；2）Dilucap PSD，用于II类和IV类难溶性活性药物成分——它有利于活性药物成分的崩解和溶出；3）Dilucap SR，用于需要缓释/控释的活性药物成分——它降低活性药物成分的崩解和释放速率，促进其缓释，还可防止导致不良反应的血药浓度峰值；4）DiluCap Hygro，用于吸湿性或潮解性活性药物成分——它降低吸湿性、潮解性和低共熔混合物的形成；5）DiluCap Antioxi，用于易氧化的活性药物成分——它因含有抗氧化成分而提供化学稳定性，并降低水分活度和化学降解；6）DiluCap OD，用于可制成撒粉胶囊或舌下胶囊的口腔崩解活性药物成分——它有利于透粘膜渗透。对DiluCap系列辅料进行的测试表明，所有产品都具有合适的流动性质（休止角和卡尔压缩性指数）、吸湿性、生物药学性能（溶出曲线）和稳定性。这证实了如下说法：DiluCap为复方药房提供了一系列基于科学的辅料，其功能经过验证，节省时间（减少预处理和库存项目数量），并保证硬壳口服胶囊制剂的有效性和安全性。
