司他夫定钠

司他夫定钠是一种核苷类似物，可抑制逆转录酶并具有抗HIV的体外活性。目标：艾滋病毒RT；NRTIs Stavudine钠是一种双脱氧核苷类似物，可抑制逆转录酶并具有抗HIV的体外活性。司他夫定钠是胸苷的类似物。它被细胞激酶磷酸化为活性三磷酸。司他夫定三磷酸钠与天然底物胸苷三磷酸竞争，从而抑制了HIV逆转录酶。它也通过掺入DNA而终止DNA合成[1]。小鼠分别用司他夫定d4T（500 mg / kg /天），L-肉碱（200 mg / kg /天）或两种药物治疗2周。通过双能X线骨密度仪评估身体脂肪，并在血浆中进行研究，肝脏，肌肉和WAT。D4T降低了人体肥胖，WAT瘦素，FAO全身和血浆酮体的获得，并增加了肝甘油三酸酯和血浆氨基转移酶，并伴有轻度肝细胞超微结构异常[2]。临床适应症：HIV-1感染FDA批准日期：1994年6月24日毒性：周围神经病；无症状。脂肪营养不良。

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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.

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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.

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