Controlled release of a self-emulsifying formulation from a tablet dosage form: Stability assessment and optimization of some processing parameters

• Published in: International journal of pharmaceutics 2006-06, Vol.315 (1), p.110-121
• Main Authors: Nazzal, Sami, Khan, Mansoor A.
• Format: Article
• Language: English
• Subjects: Biological and medical sciences; Coenzyme Q 10; Coenzymes; Controlled release; Delayed-Action Preparations - chemistry; Delayed-Action Preparations - pharmacokinetics; Drug Carriers - chemistry; Drug Industry - methods; Drug Stability; Emulsifying Agents - chemistry; Emulsifying Agents - therapeutic use; Face-centered cubic design; General pharmacology; Lipids; Medical sciences; Optimization; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Self-emulsified drug delivery system; Stability; Tablets - chemistry; Tablets - pharmacokinetics; Temperature; Ubiquinone - analogs & derivatives
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2006.02.019

The objective of this study was to evaluate the effect of some processing parameters on the release of lipid formulation from a tablet dosage form. A 17-run, face-centered cubic design was employed to evaluate the effect of colloidal silicates ( X 1), magnesium stearate mixing time ( X 2), and compression force ( X 3) on flow, hardness, and dissolution of Coenzyme Q 10 (CoQ 10) lipid formulation from a tablet dosage form. The optimized formulation was subsequently subjected to a short-term accelerated stability study. All preparations had a flowability index values ranging from 77 to 90. The cumulative percent of CoQ 10 released within 8 h ( Y 5) ranged from 40.6% to 90% and was expressed by the following polynomial equation: Y 5 = 49.78 − 16.36 X 1 + 2.90 X 2 − 3.11 X 3 − 0.37 X 1 X 2 + 1.06 X 1 X 3 − 1.02 X 2 X 3 + 11.98 X 1 2 + 10.63 X 2 2 − 7.10 X 3 2 . When stored at 4 °C, dissolution rates were retained for up to 3 months. Storage at higher temperatures, however, accelerated lipid release and caused leakage, and loss of hardness. Processing parameters have a profound effect on the release of lipid formulations from their solid carriers. While optimized controlled release formulations could be attained, further considerations should be made to prepare “liquisolids” that are physically stable at higher storage temperatures.