Development and Evaluation of a Once-Daily Controlled Porosity Osmotic Pump of Tapentadol Hydrochloride

Abstract

Abstract. The present study aimed to prepare, optimize, and evaluate Tapentadol hydrochloride controlled porosity osmotic pump (CPOP) and to achieve the drug release at nearly zero-order. The CPOP was prepared by the coating of polymers (Eudragit RSPO and RLPO) on a directly compressed core tablet. A Box-behnken experimental design was applied to optimize the parameters for CPOP. The optimized batch was characterized for in vitro drug release study, effect of pH, osmolarity and agitation intensity, and surface morphology and stability study. In vivo pharmacokinetic studies were performed on New Zealand white rabbits for CPOP and marketed tablet. All the batches showed a drug release ranging from 29.87 to 56.92% after 12 h; and from 59.64 to 99.96% after 24 h. There was no change in the drug release pattern at different pH and agitation intensities. The drug release was found to decrease with increasing osmolarity of dissolution media.An in vivo study showed a higher mean residence time, area under the curve, and biological half-life (T 1/2 ) than the marketed tablet with low rate of elimination (Ke) and a 2.35-fold increase in relative bioavailability. The result showed that the amounts of sodium chloride and PEG 400 were contributing positively while the number of coats was negatively affecting the drug release. The drug release was found to be independent of physiological conditions. The stability testing showed that the prepared CPOP was stable for 3 months at accelerated conditions. The prepared CPOP was found to deliver Tapentadol hydrochloride at zero-order for up to 24 h.

Osmotic Drug Delivery System of Nicorandil: Design and Evaluation

“…This suggests that there is no curvature effect and that the steepest ascent method can be used for optimization simulation. The present analysis confirmed the release mechanism as osmotic-activated drug release [26].…”

“…(0 atm) no sucrose, (15 atm) 201.78 g/l of sucrose, (30 atm) 402.6 g/l of sucrose, and (45 atm) 605.34 g/l of sucrose. For formulation, FT3A, dug release studies were conducted using the above media [26]. It can be suggested from the fig.…”

<p>Quality by Design (QbD)-Based Numerical and Graphical Optimization Technique for the Development of Osmotic Pump Controlled-Release Metoclopramide HCl Tablets</p>

“…For a better understanding of the influence of input variables X 1 , X 2, and X 3 , on drug release, the total number of trial batches was grouped based on sodium chloride concentration, as shown in Figure 3A-D. Thakkar et al also grouped dissolution data of trial formulations based on different osmogen levels. 37 Burst release was observed from the comparison of drug release profile of low level (−1) group F-7, and F-13, whereas F-5, F-9, and F-18, failed to meet the recommended criteria of osmotic tablets %CDR 6 and 12 hours ( Figure 3A). Burst effect was also observed for the mediumlevel group F-4 and F-11 ( Figure 3B) and high-level group F-2 and F-20 ( Figure 3C).…”

Critical Factors for Metformin Osmotic Controlled Release Pump

“…There are three mechanisms that contribute to the release of active material from controlled porosity osmotic pump i.e., drug release driven by the mechanism of osmotic pressure, size and number of pores formed in the membrane and water uptake of the membrane. To demonstrate the role of osmotic pressure for drug release, the optimized formulation of controlled porosity osmotic pump was subjected to in vitro drug release study in different concentrations of NaCl (0.5, 1 and 2 mol/l) used as dissolution medium [11].…”