Rosuvastatin Calcium 10 Mg

Rosuvastatin Calcium 10 mg: Pharmacokinetics, Efficacy, and Formulation

Pharmacokinetics of Rosuvastatin Calcium 10 mg

Bioequivalence and Food Effects

A study on the pharmacokinetics of rosuvastatin calcium 10 mg in healthy Chinese subjects revealed that the drug's bioequivalence was maintained under both fasted and fed conditions. The study used a randomized, open-label, two-formulation, two-sequence, two-period, single-dose crossover design. The results showed that the 95% confidence intervals of the test/reference geometric mean ratios for Cmax, AUC0–t, and AUC0–∞ were within the acceptable range of 80%-125%. However, high-fat meals were found to reduce the Cmax, AUC0–t, and AUC0–∞, although they did not significantly affect the Tmax or elimination rate of rosuvastatin.

Pharmacokinetic Characteristics in Chinese Volunteers

Another study focused on the pharmacokinetics of rosuvastatin in healthy Chinese volunteers. It was found that systemic exposure (AUC) to rosuvastatin was approximately two-fold higher in Asian subjects compared to white subjects. The study involved ascending single and multiple doses of 5, 10, and 20 mg. The results indicated minimal accumulation of rosuvastatin with repeated administration, and all doses were well tolerated.

Efficacy of Rosuvastatin Calcium 10 mg

Lipid-Lowering Effects in Hemodialysis Patients

In a double-blind, randomized, placebo-controlled trial involving hemodialysis patients, rosuvastatin calcium 10 mg/day significantly reduced total cholesterol, LDL cholesterol, and non-HDL cholesterol over a three-month period. Additionally, high-sensitivity C-reactive protein (hs-CRP) levels were significantly lower in the rosuvastatin group compared to the placebo group.

Treatment of Primary Hypercholesterolemia

Phase II clinical trials evaluated the efficacy and safety of rosuvastatin calcium in patients with primary hypercholesterolemia. The study found that rosuvastatin calcium 10 mg was as effective as atorvastatin calcium 10 mg in lowering LDL-C levels. Both doses were well tolerated, and the lipid-lowering effect of rosuvastatin was not inferior to that of atorvastatin.

Effects on Elderly Patients with Cerebral Ischemic Stroke

A study on elderly patients with cerebral ischemic stroke showed that rosuvastatin calcium 10 mg significantly improved blood lipid levels, including reductions in total cholesterol, LDL-C, and triglycerides, while increasing HDL-C levels. The high-dose treatment group (10 mg) exhibited more pronounced changes compared to the low-dose group (5 mg).

Formulation and Stability of Rosuvastatin Calcium 10 mg Tablets

Immediate Release Formulations

Several studies have focused on developing immediate release formulations of rosuvastatin calcium 10 mg to enhance its bioavailability. One study used superdisintegrants like Crospovidone to speed up disintegration and dissolution, resulting in a formulation that released 80% of the drug within 15 minutes. Another study confirmed that formulations containing Crospovidone released up to 102.4% of the drug in 30 minutes, demonstrating better efficacy compared to conventional tablets.

Stability with Tribasic Calcium Phosphate

A formulation study used tribasic calcium phosphate to stabilize rosuvastatin calcium in immediate release tablets. The tablets exhibited good mechanical properties, rapid disintegration, and a fast dissolution rate, with 85% of the drug substance dissolved within 15 minutes. The formulation also showed satisfactory chemical stability during storage under stress conditions.

Conclusion

Rosuvastatin calcium 10 mg is a highly effective and well-tolerated statin for lowering cholesterol levels and improving lipid profiles in various patient populations, including those on hemodialysis and elderly patients with cerebral ischemic stroke. Its pharmacokinetic profile is influenced by food intake, and systemic exposure is higher in Asian populations. Immediate release formulations using superdisintegrants and stabilizing agents like tribasic calcium phosphate have been developed to enhance its bioavailability and stability.

Summary

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