易布鲁替尼口服悬浮剂的生物可用性和兼容性为最佳的肠道注射途径
Jonas Paludo1, Lisa Nodzon2, Xavier Woot de Trixhe3
1Department of Hematology, Mayo Clinic, Rochester, MN, USA.
Therapeutic advances in hematology
|December 30, 2025
概括
易布鲁替尼口服悬浮剂的生物可用性与囊和药片相比较. 它是稳定的,与肠道管兼容,为需要不同配方的患者提供可行的替代方案.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物输送系统 药物输送系统
背景情况:
- 易布鲁丁尼布是一种布鲁顿氨酸激酶抑制剂 (BTKi),可提供口服囊,片剂和悬浮剂配方.
- 患有吞困难的患者可能需要Ibrutinib治疗的替代药物选择.
研究的目的:
- 为了评估Ibrutinib口服悬浮剂相对生物可用性,与其囊和药片形式相比.
- 通过肠道管评估易布鲁替尼口服悬浮的兼容性和最佳的施用方法.
主要方法:
- 在健康志愿者和患者中进行的相对生物利用性研究,将口服悬浮与囊/片剂配方进行比较.
- 在体外评估剂量回收,杂质,颗粒大小,并使用注射器和鼻胃/PEG管保持时间.
主要成果:
- 易布鲁替尼口服悬浮在禁食条件下的健康志愿者中显示出与囊相比的临床生物可用性.
- 药物动力学值在患者的配方中是相似的. 所有测试的肠道管都通过水冲洗实现了90%-110%的剂量恢复.
- 在60分钟的保持时间后,观察到口服悬浮防腐剂在肠道管中潜在吸附.
结论:
- 易布鲁替尼口服悬浮是无法服用囊或片剂的患者的可行的替代方案.
- 口服悬浮液是稳定的,并且与常见的肠道管 (聚氨,,聚乙烯) 兼容.
- 立即施用,然后再用两次3毫升水冲洗,可确保剂量完全恢复,并防止防腐剂吸附.
相关概念视频
Routes of Drug Administration: Enteral
6.1K
Medications can be administered through the enteral route using liquids, capsules, or tablets.
Enteral administration involves drug administration via the mouth in two ways: orally or sublingually.
Unlike sublingually drugs, drugs that are taken orally pass through the gastrointestinal (GI) tract and get metabolized by the liver. Once metabolized, the drug is absorbed into the systemic circulation, reaching different body parts via the bloodstream. However, while passing through the stomach,...
Enteral administration involves drug administration via the mouth in two ways: orally or sublingually.
Unlike sublingually drugs, drugs that are taken orally pass through the gastrointestinal (GI) tract and get metabolized by the liver. Once metabolized, the drug is absorbed into the systemic circulation, reaching different body parts via the bloodstream. However, while passing through the stomach,...
6.1K
Bioavailability: Overview
3.9K
Bioavailability refers to the proportion of an unaltered drug that, after administration, enters the systemic circulation and can be distributed to the desired action site. Factors such as gastrointestinal (GI) absorption and liver biotransformation influence the bioavailability of a drug when it is administered orally. When a drug is administered intravenously, it enters the systemic circulation directly; by definition, its bioavailability is assumed to be 100%. The bioavailability of an...
3.9K
Bioavailability: Overview
310
Bioavailability refers to the proportion of an administered drug that reaches the systemic circulation in its active, unaltered form. It is a crucial pharmacokinetic parameter that determines the effectiveness of a drug in achieving its intended therapeutic outcomes. The route of administration significantly influences bioavailability, with intravenous administration achieving 100% bioavailability as the drug directly enters the bloodstream. In contrast, oral administration often results in...
310
Drug Delivery: Enteral Route
1.5K
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
1.5K
Routes of Drug Administration: Parenteral
2.8K
The administration of drugs via parenteral routes allows for direct drug introduction into the systemic circulation, resulting in high bioavailability because the medication bypasses the harsh conditions of the gastrointestinal tract and hepatic metabolism.
The intravenous route (IV) of drug administration can be further categorized into two types. The bolus injection administers the entire dose rapidly, while an intravenous infusion slowly delivers smaller doses steadily.
The IV route is often...
The intravenous route (IV) of drug administration can be further categorized into two types. The bolus injection administers the entire dose rapidly, while an intravenous infusion slowly delivers smaller doses steadily.
The IV route is often...
2.8K
Drug Delivery: Overview
693
The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
693


