Preparation and evaluation of bilayer-core osmotic pump tablets contained topiramate

Abstract

Topiramate (TPM) was an antiepileptic agent commonly used in clinical. Studies showed that an oral preparation of TPM with extended-release manner could bring some benefits for epileptics. In this paper, controlled release push-pull osmotic pump (PPOP) tablets of sparingly water-soluble TPM were successfully prepared. This bi-layer tablet core mainly consisted of sodium chloride as osmotic promoting agent and polyethylene oxide as suspending and pushing agents. The influences of osmotic agents, pushing agents and the compositions of coating membrane on TPM release profiles were evaluated. An optimal formulation of TPM-PPOP was obtained through single-factor experiments. In vitro release tests showed that the optimum formulation could release TPM at an approximate zero-order rate up to 8 h. Pharmacokinetic behaviors of TPM-PPOP tablets were evaluated and compared with the immediate release capsules after an oral single dose in beagle dogs. Pharmacokinetics results demonstrated that the TPM-PPOP tablet was able to provide a prolonged release of TPM with longer tmax and mean residence time. Lower fluctuations of drug plasma levels could also be achieved with TPM-PPOP tablets. These results suggested that sparely water-soluble drugs as TPM can be designed to PPOP for efficacy and safety use.

Osmotic Release Oral Tablet Formulation, Development, and Evaluation of an Anti-epileptic Drug

“…The tablets were found to be mechanically stable and adhere to applicable pharmacopeia specifications, a comparable innovator product in the dissolution test, and several other physicochemical criteria. 10 As a whole, F9 is the most successful batch of the formulation. Trial F9 was created with 7% and 6% weight growth, and the drug's release at 3 hours was found to be 21 and 21, respectively, both of which are within the ranges specified by the USP 11 .…”

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“…Drugs having shorter biological half-life (2-6 h), low dose, compatible with osmotic agent, and other excipients are preferred for the delivery The drug having absorption in the proximal region of the GIT and have shorter stomach retention period, can be given by this way to prolong residence time which will significantly enhance the effectiveness of the dose In these cases, the osmotic drug delivery which work on osmotic principle, floating principles is used to improve the GRT. [7] Many prospective medications are developed for osmotic distribution, such asazilsartan, [17] diethylcarbamazine citrate [18] diltiazem HCl, [19] carbamazepine, [20] metoprolol, and nifedipine, [21] Theophylline, salbutamol, [22] topiramate, [23] gliclazide, [24] domperidone maleate, [25] etc.…”

SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™

“…The compressed tablets were coated in a conventional tablet coating pan, which was rotated at a 3-6 rpm speed till the inlet and outlet air temperatures were maintained at ~45 and ~28 °C, respectively (Okimoto et al, 2004;Seo et al, 2020). The speed of the coating pan was then increased up to 18-24 rpm (Lin et al, 2022). The automation pressure was set at 1 kg/cm 2 , and the coating solution was applied at a spraying rate of 8-10 ml/min.…”