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Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists

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5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
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Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists01:29

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Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
Phenothiazines, such as prochlorperazine...
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Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

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Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates...
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Chemotherapy-Induced Nausea and Vomiting: Cannabinoids01:21

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Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
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Drug Delivery: Enteral Route01:18

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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.
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子供の化学療法による吐き気と嘔吐の予防のために3Dプリントされたデキサメタゾンの錠の開発

Adrin Dadkhah1,2, Tobias Gutowski1, Eva-Maria Wansing1

  • 1University Medical Center Hamburg-Eppendorf, Hospital Pharmacy, Hamburg, Germany.

International journal of pharmaceutics: X
|September 2, 2025
PubMed
まとめ

3Dプリントされたデキサメタゾン (Dexa) タブレットは,小児がん患者のために開発されました. この革新的なアプローチは 投与の精度と味覚を改善し,現在の小児化学療法の 嘔吐抑制剤の治療に伴う課題を解決します.

キーワード:
3Dプリント配方開発パーソナライズド医療半固体挤出味覚を隠す

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科学分野:

  • 製薬技術
  • 薬物投与システム
  • 小児腫瘍学

背景:

  • デキサメタゾン (Dexa) は,化学療法による吐き気と嘔吐 (CINV) の管理に不可欠です.
  • 現在の小児用投与方法は,錠剤の操作を伴うため,誤差があり,苦い味のために患者の受け入れが悪い.
  • 子供に優しい,正確に投与され,美味しいDexaの製剤が必要である.

研究 の 目的:

  • 半固体挤出 (SSE) を用いて3Dプリントしたデキサメタゾン錠剤を開発する.
  • 効果的味覚マスクを実現し,小児患者の受容性を向上させる.
  • 小児腫瘍学における臨床使用のための正確な用量と安定性を確保するためです.

主な方法:

  • 3Dプリントでデキサメタゾン錠剤を製造するために,半固体挤出 (SSE) が使用されました.
  • 副成分は,印刷可能性と味覚マスクの有効性を評価した.
  • 熱安定性 (DSC,TGA),分解,in vitro溶解,含量/質量均一性,および短期安定性が評価されました.
  • 感覚評価は健康な成人のボランティアで行われました.

主要な成果:

  • 質量均一性 (RSD 0. 75%) とAPI含有量 (99. 35% ± 2. 92%) が良好でした.
  • 2時間以内に完全に薬剤を放出する.
  • 熱分析ではデキサメタゾンの分解は認められず,5週間以上の安定性が確認された.
  • 痛みの有意な減少は,感覚評価で報告されました.

結論:

  • SSEは,子供に適した個別投与デキサメタゾンの錠の複製可能な製造を容易にする.
  • 開発された配合は,小児患者の味覚を高め,効果的な味覚マスクを提供します.
  • この3Dプリントによるアプローチは,小児腫瘍学におけるデキサメタゾンの臨床応用を改善することを支援します.