納布啡(Nalbuphine)為一個半合成的鴉片類(opioids)藥物，用於緩解疼痛。而其優點包含呼吸抑制的副作用較嗎啡(Morphine)輕微、不會產生欣快感也沒有成癮的問題。然而Nalbuphine的口服生體可用率(Bioavailability, BA)偏低，以及在人體中的半衰期約5小時，使用上必須要頻繁得給藥，增加使用上的不便。若能設計Nalbuphine長效藥物，可以改善使用上的問題。
Dinalbuphine sebacate (DNS)是Nalbuphine的前驅藥物，藉由兩個Nalbuphine與sebacic acid以共價鍵相連接而成。相較於Nalbuphine，DNS的水溶性下降，適合用來設計為油針注射液(Oily injection)。
本論文主要在研究DNS油針注射液 的配方與藥物釋放速率間的相關性。在進行配方開發的過程中，一個能夠預測體內釋放的體外溶離方法是很重要的。經過文獻尋找與初步的測試，現階段已知的體外釋放模型並不適合用於我們的研究。在本論文中，我們試著建立新的體外釋放模型，並選擇三種配方進行比格犬之藥物動力學實驗(Pharmacokinetics, PK)。實驗結果證明，我們建立的體外釋放模型的結果與藥物體內釋放速率有所關聯。此模型應能夠使用於油針注射液配方開發時的篩選並加速配方開發過程。

Nalbuphine is a semi-synthetic opioid indicated for the relief of moderate to severe pain. Dinalbuphine sebacate (DNS) is a prodrug of nalbuphine for which we have developed long-acting lipophilic formulations in a benzyl benzoate/sesame oil mixture for intramuscular (IM) injection. In this study, we found that the in vitro release profile of DNS could be affected by adjusting the weight ratio of benzyl benzoate to sesame oil (the solvent/oil ratio). A longer release period could be attained by increasing the solvent/oil ratio in the formulation.
A pharmacokinetic study was conducted in beagle dogs to verify the relationship between the in vitro release and the drug release from the formulations in vivo. The pharmacokinetic study confirmed that the formulation with a higher benzyl benzoate to oil ratio exhibits a longer drug release profile with a lower maximum concentration (Cmax) and a longer time to peak blood concentration level (Tmax) than the formulation with a lower benzyl benzoate to oil ratio.

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