Meyer M C, Gollamudi R, Straughn A B
J Clin Pharmacol. 1979 Aug-Sep;19(8-9 Pt 1):435-44. doi: 10.1002/j.1552-4604.1979.tb02505.x.
The bioavailability of sustained-release papaverine HCl dosage forms were compared to equivalent doses of the drug administered as an elixir and conventional compressed tablets to 12 healthy human subjects. Papaverine plasma levels were determined using a gas-chromatographic procedure. The drug was absorbed more rapidly and completely from the two nonsustained-release formulations. There was a large intersubject variability, and the plasma half-life of the drug was esstimated to be 1 hour. The area under the plasma level-time curve for the nine sustained-release products ranged from 18 to 64% relative to the area achieved by the papaverine elixir. It was concluded that the sustained-release dosage forms of papaverine included in each study group could be considered bioequivalent, but they exhibited inadequate bioavailability relative to either the elixir or the compressed tablet dosage form.
将盐酸罂粟碱缓释剂型的生物利用度与等量的以酏剂和传统压制片形式给药的该药物对12名健康人类受试者进行了比较。使用气相色谱法测定罂粟碱的血浆水平。该药物从两种非缓释制剂中吸收更快且更完全。个体间存在很大差异，该药物的血浆半衰期估计为1小时。九个缓释产品的血浆水平-时间曲线下面积相对于罂粟碱酏剂所达到的面积范围为18%至64%。得出的结论是，每个研究组中包含的罂粟碱缓释剂型可被认为具有生物等效性，但相对于酏剂或压制片剂型，它们的生物利用度不足。
