Wegmans School of Pharmacy, St. John Fisher College, Rochester, New York.
Int J Pharm Compd. 2021 Jan-Feb;25(1):82-87.
Sildenafil citrate is a phosphodiesterase-5 inhibitor that is approved by the U.S. Food and Drug Administration for the treatment of erectile dysfunction. Rapid-dissolving tablets are relatively novel dosage forms that can be prepared by extemporaneous compounding and potentially provide unique advantages for medications like sildenafil. However, such preparations may present newer stability considerations previously unreported. Therefore, the purpose of this study was to assess the physical and chemical stability of sildenafil 100-mg rapid-dissolving tablets prepared by a commonly practiced molding method, using two different proprietary rapid-dissolving tablet bases (Medi-RDT or RDTPlus) immediately after preparation and over six months of storage at ambient room temperature. To prepare the rapid-dissolving tablets, the powder ingredients were homogeneously mixed, filled, and compressed into a 96-cavity metal mold. The formulation was then heated at 110°C for 10 minutes in the mold, released from the mold, and cooled at room temperature for 15 minutes. The prepared tablets were packaged in amber-colored blister packs with cold-adhesive backing seals and stored at ambient room temperature. At predetermined time points, rapid-dissolving tablets of each formulation were retrieved to perform stability analyses. These analyses included weight variation, breaking force, disintegration, friability, and potency via high-performance liquid chromatography following the United States Pharmacopoeia methods and visual inspection. At time 0 (immediately after preparation), the results of the tests for rapid-dissolving tablets made with Medi-RDT base v. RDT-Plus base were as follows: average tablet weight (649.7 mg v. 753.6 mg); breaking force (24.01 N v. 32.34 N); friability (8.52% v. 7.55%); disintegration time (34 seconds v. 35 seconds); and potency (98.61% v. 101.41%), respectively. Over the six-month storage period, both formulations of rapid-dissolving tablets had no significant changes in visual appearance, tablet weight, breaking force, or disintegration time. High-performance liquid chromatographic-based tablet assays for both formulations were consistently above 95% label claim at each time point, with no chromatographic evidence of degradation. Thus, the studied formulations of compounded sildenafil 100-mg rapid-dissolving tablets prepared using both Medi-RDT or RDT-Plus were found to be physically and chemically stable over six months of storage at ambient room temperature.
枸橼酸西地那非是一种磷酸二酯酶-5 抑制剂，已获得美国食品和药物管理局批准用于治疗勃起功能障碍。速溶片是一种相对较新的剂型，可以通过临时调配制备，并可能为西地那非等药物提供独特的优势。然而，此类制剂可能具有以前未报道过的新的稳定性考虑因素。因此，本研究的目的是评估通过一种常用的成型方法制备的 100mg 西地那非速溶片的物理和化学稳定性，使用两种不同的专有速溶片基底（Medi-RDT 或 RDTPlus），在制备后立即以及在环境室温下储存六个月后进行评估。为了制备速溶片，将粉末成分均匀混合，填充并压缩到 96 腔金属模具中。然后将配方在模具中于 110°C 加热 10 分钟，从模具中释放出来，然后在室温下冷却 15 分钟。制备好的片剂用琥珀色泡罩包装，带有冷胶背衬密封，在环境室温下储存。在预定的时间点，从每个配方中取出速溶片进行稳定性分析。这些分析包括重量变化、断裂力、崩解、脆碎度和通过美国药典方法进行的高效液相色谱法测定的效力以及目视检查。在 0 时间（制备后立即），使用 Medi-RDT 基与 RDT-Plus 基制备的速溶片的测试结果如下：平均片剂重量（649.7mg 比 753.6mg）；断裂力（24.01N 比 32.34N）；脆碎度（8.52%比 7.55%）；崩解时间（34 秒比 35 秒）；效力（98.61%比 101.41%）。在六个月的储存期间，两种速溶片配方在外观、片剂重量、断裂力或崩解时间方面均无明显变化。两种配方的高效液相色谱法片剂测定均在每个时间点均保持在 95%标签声称以上，没有降解的色谱证据。因此，研究发现，使用 Medi-RDT 或 RDT-Plus 制备的枸橼酸西地那非 100mg 速溶片的研究配方在环境室温下储存六个月后在物理和化学上均稳定。
