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Preclinical Research The purpose of this work was to synthesize a series of symmetrical analogs (CA2 – CA7) of curcumin and determine their efficacy as antioxidant and anticancer agents in vitro. The six analogs were successfully synthesized and characterized, one of which, CA6, had not been previously reported in the literature. With the exception of CA2, the analogs had lower predicted aqueous solubilities and higher partition coefficients than curcumin. Two analogs, CA2 and CA3, had lower potencies as anticancer agents compared with curcumin, while CA6 had a slightly higher IC50 value. Two different trends in the antioxidant capabilities of curcumin and its analogs were determined when assessed in vitro or in cell culture. The in vitro DPPH assay clearly showed curcumin as the strongest antioxidant as compared with the analogs when tested at the same concentration or at their IC50 value. The cell culture ‐ based reactive oxygen species/reactive nitrogen species assay indicated that CA3 and CA6 were equal to curcumin in their free radical scavenging ability at the same concentration, but when curcumin and its analogs were tested at their respective IC50 values, CA4 and CA5 showed excellent antioxidant capacities. These results indicate that in cell culture, the ability of these analogs to produce antioxidant effects may be tied to their downstream effects. [ABSTRACT FROM AUTHOR]

Fibromyalgia is a syndrome associated with chronic, widespread musculoskeletal pain, fatigue, depression, and cognitive dysfunction. With few U.S. Food and Drug Administration-approved treatment options, there is evidence that low-dose naltrexone, an opioid antagonist approved for opioid and alcohol dependence at high doses, may have efficacy in the treatment of fibromyalgia and chronic pain. At the doses required for fibromyalgia treatment, naltrexone needs to be compounded, and no data currently exists regarding the long-term stability of low-dose naltrexone capsules. This limits pharmacies to a maximum beyond-use date of 180 days. Our study examined the stability of compounded capsules of low-dose naltrexone in Avicel over 360 days. Naltrexone was extracted from compounded capsules and assessed using reversed-phase high-performance liquid chromatography validated to differentiate between the degraded and undegraded naltrexone. United States Pharmacopeia guidelines state that compounded medications must remain within 10% of the labeled potency at all times during the assigned expiration date for a preparation. Our results show that low-dose naltrexone is stable for 360 days when stored at room temperature and away from light remaining within 90% to 110% of the labeled potency throughout the study period. Based on our study results, the beyond-use date for compounded low-dose naltrexone formulations stored at room temperature and protected from light can be extended to 1 year. The longer beyond-use dating allows patients greater flexibility in using these capsules during the flare-ups associated with fibromyalgia without needing a refill immediately at the onset of symptoms. In addition, it may help compounding pharmacies reduce waste associated with small-batch preparation of these capsules., (Copyright© by International Journal of Pharmaceutical Compounding, Inc.)

The purpose of this research was to collect, analyze, and compare stability data for levothyroxine (T4) powder in the anhydrous and pentahydrate form when prepared as an aliquot and in capsules. Two different compounding pharmacies, Central Iowa Compounding and Gateway Medical Pharmacy, used different forms of T4 and aliquot formulations, which were studied to determine the beyond-use date at ±5% or ±10% of labeled strength. T4 was extracted from aliquot and capsule formulations and assessed using reverse-phase high- performance liquid chromatography validated to differentiate between the degraded and original forms of T4. The results indicate that T4 1:100 aliquot formulation prepared with silica gel or Avicel as filler are stable for 120 days at ±10% labeled potency, but at ±5% labeled potency, the silica gel and Avicel aliquot formulations are stable for 45 and 30 days, respectively. The silica gel capsules prepared from fresh aliquot were stable for 120 days at ±10% labeled potency and 90 days at ±5% labeled potency, while the Avicel capsules prepared from fresh aliquot were stable for 180 days at both ±10% and ±5% labeled potency. Avicel capsules prepared from old aliquot (120 days) and fresh aliquot (1 day) were also compared for stability. The old aliquot Avicel capsules were stable for 14 days at ±5% labeled potency and 150 days at ±10% labeled potency, while new aliquot Avicel capsules were stable for 180 days at both ±10% and ±5% labeled potency. Based on our data, there can be significant variation in the beyond-use dates assigned to T4 capsules based on the diluents used for aliquots, the final capsule formulations, and the potency standards applied. These results also indicate that pharmacists must exercise caution when using older aliquots and may have to assign shorter beyond-use dates.