司他夫定鈉是一種核苷類似物，可抑制逆轉(zhuǎn)錄酶并具有抗HIV的體外活性。目標：艾滋病毒RT；NRTIs Stavudine鈉是一種雙脫氧核苷類似物，可抑制逆轉(zhuǎn)錄酶并具有抗HIV的體外活性。司他夫定鈉是胸苷的類似物。它被細胞激酶磷酸化為活性三磷酸。司他夫定三磷酸鈉與天然底物胸苷三磷酸競爭，從而抑制了HIV逆轉(zhuǎn)錄酶。它也通過摻入DNA而終止DNA合成[1]。小鼠分別用司他夫定d4T（500 mg / kg /天），L-肉堿（200 mg / kg /天）或兩種藥物治療2周。通過雙能X線骨密度儀評估身體脂肪，并在血漿中進行研究，肝臟，肌肉和WAT。D4T降低了人體肥胖，WAT瘦素，F(xiàn)AO全身和血漿酮體的獲得，并增加了肝甘油三酸酯和血漿氨基轉(zhuǎn)移酶，并伴有輕度肝細胞超微結(jié)構(gòu)異常[2]。臨床適應(yīng)癥：HIV-1感染FDA批準日期：1994年6月24日毒性：周圍神經(jīng)??；無癥狀。脂肪營養(yǎng)不良。

---

1.Oral Disintegration Tablets of Stavudine for HIV Management: A New Technological Approach.
Sankar V1, Ramakrishna B, Devi PS, Karthik S. Indian J Pharm Sci. 2012 Nov;74(6):556-63. doi: 10.4103/0250-474X.110602.

Stavudine oral disintegration tablets were formulated to minimize the bitter taste and to reduce the first-pass hepatic metabolism. The various precompression parameters like the angle of repose, bulk density, compressibility index and Hausner's ratio were determined for the powder blend. In this study, 14 formulations of stavudine oral disintegration tablet were prepared by direct compression method. The tablets were evaluated for weight variation, percentage friability, disintegration time, hardness, wetting time and water absorption ratio. The in vitro dissolution study results of the batch S1 (stavudine+crospovidone+sodium starch glycollate) are encouraging as highest dissolution rate (99.2% in 100 min) and lowest time of disintegration (56 s) was achieved. The in vivo drug release studies were carried out in rabbits and the relative bioavailability of formulation S1 was found to be 2.83 times greater than that of conventional tablets.

---

2.Formulation and evaluation of floating matrix tablet of stavudine.
Prajapati PH1, Nakum VV, Patel CN. Int J Pharm Investig. 2012 Apr;2(2):83-9. doi: 10.4103/2230-973X.100047.

BACKGROUND/AIM: The purpose of the study was to prolong the gastric residence time of stavudine by designing its floating tablets and to study the influence of different polymers on its release rate.

---