Department of Organic Chemistry and Technology, Budapest University of Technology and Economics (BME), H-1111 Budapest, Műegyetem rakpart 3, Hungary.
Oral Solids Development, Janssen R&D, B-2340 Beerse, Turnhoutseweg 30, Belgium.
J Control Release. 2019 Feb 28;296:162-178. doi: 10.1016/j.jconrel.2019.01.023. Epub 2019 Jan 21.
In chronic intestinal diseases like inflammatory bowel disease, parenteral administration of biopharmaceuticals is associated with numerous disadvantages including immune reactions, infections, low patient compliance, and toxicity caused by high systemic bioavailability. One alternative that can potentially overcome these limitations is oral administration of biopharmaceuticals, where the local delivery will reduce the systemic exposure and furthermore the manufacturing costs will be lower. However, the development of oral dosage forms that deliver the biologically active form to the intestines is one of the greatest challenges for pharmaceutical technologists due to the sensitive nature of biopharmaceuticals. The present article discusses the various drug delivery technologies used to produce orally administered solid dosage forms of biopharmaceuticals with an emphasis on colon-targeted delivery. Solid oral dosage compositions containing different types of colon-targeting biopharmaceuticals are compiled followed by a review of currently applied and emerging drying technologies for biopharmaceuticals. The different drying technologies are compared in terms of their advantages, limitations, costs and their effect on product stability.
在慢性肠道疾病（如炎症性肠病）中，生物制药的肠胃外给药与许多缺点相关，包括免疫反应、感染、低患者顺应性和高全身生物利用度引起的毒性。一种潜在的替代方法是生物制药的口服给药，局部给药将降低全身暴露，并且制造费用将更低。然而，由于生物制药的敏感性，开发将生物活性形式递送至肠道的口服剂型是制药技术人员面临的最大挑战之一。本文讨论了用于生产生物制药口服固体制剂的各种药物递送技术，重点是结肠靶向递药。包含不同类型结肠靶向生物制药的固体制剂进行了汇编，然后对目前应用和新兴的生物制药干燥技术进行了综述。不同的干燥技术在优势、局限性、成本及其对产品稳定性的影响方面进行了比较。
