In vitro release of new designs of modified-release tramadol hydrochloride included in a polymer matrix.

Tramadol reaches therapeutic plasma concentrations in a time interval of 0.5 to 1.7 hours, so it is necessary to dose 4 times/day, which reduces compliance with the dose and the effectiveness of the treatment. Design formulations of tramadol that allow the release time to be prolonged, surpassing those obtained with the commercial product and tramadol without excipients. Several formulations of 5% tramadol hydrochloride were designed in a matrix system based on poloxamer 407 at different concentrations (10%, 14%, 17%, and 20%). In vitro release studies were performed, using a spectrophotometer at a wavelength of 273.15 nm; were compared the results with tramadol without polymeric supplements and with the commercial formulation samples were taken in a period of time from 0.25 to 72 hours, and also compared the use or absence of dialysis membrane with a porosity of 50 kilodaltons was. With the use of the membrane, the designed formulations had a release of 98%, 50%, 23%, 16% at 72 hours, respectively, different from the commercial product and the tramadol formulation without excipients released the 24 hours. Without using dialysis membranes, a 90-100% release was achieved in the 10% and 14% formulation at 36 hours. The 17% and 20% formulation at 48 hours and the commercial formulation and tramadol without excipient were released within 2 hours. Modified release formulations were obtained, which retain and prolong the release of tramadol compared to the commercial product. Therefore, we propose to conduct further in vivo model experiments to confirm our conclusion.

Disposition and pharmacokinetics of azithromycin in serum and a lung tissue of two modified-release formulations compared with an immediate-release product on the market.

The aim of this study was to determine the disposition and pharmacokinetics in serum and a lung tissue homogenate in guinea pig (Cavia porcellus) of two experimental formulations of azithromycin, those were included in a modified release polymer matrix (MRF) after oral administration. The results obtained are compared with a commercial form of immediate release. 3 groups of animals were randomly formed in groups of 7 for control and 14 for each group of modified-release formulations (MRFs) were treated with a single dose of 8mg/kg of active principle. In lung tissue, comparisons of concentration of azithromycin, showed statistically significant differences between commercial product, MRF1 and MRF2. All pharmacokinetic parameters for MRF1 and MRF2 were significantly different with the exception of Cmax with respect to commercial product. The treatment of the animals with MRFs may have several benefits over treatment with azithromycin alone since could increase dosing interval for the two MRFs evaluated and reduce the frequency of application, patient stress levels and toxicological risks by accumulation of the active principle.

Pharmacokinetics of an oral extended-release formulation of doxycycline hyclate containing acrylic acid and polymethacrylate in dogs.

OBJECTIVE: To determine the pharmacokinetics of doxycycline hyclate administered orally in the form of experimental formulations with different proportions of acrylic acid-polymethacrylate-based matrices. ANIMALS: 30 healthy adult dogs. PROCEDURES: In a crossover study, dogs were randomly assigned (in groups of 10) to receive a single oral dose (20 mg/kg) of doxycycline hyclate without excipients (control) or extended-release formulations (ERFs) containing doxycycline, acrylic acid polymer, and polymethacrylate in the following proportions: 1:0.5:0.0075 (ERF1) or 1:1:0.015 (ERF2). Serum concentrations of doxycycline were determined for pharmacokinetic analysis before and at several intervals after each treatment. RESULTS: Following oral administration to the study dogs, each ERF resulted in therapeutic serum doxycycline concentrations for 48 hours, whereas the control treatment resulted in therapeutic serum doxycycline concentrations for only 24 hours. All pharmacokinetic parameters for ERF1 and ERF2 were significantly different; however, findings for ERF1 did not differ significantly from those for the control treatment. CONCLUSIONS AND CLINICAL RELEVANCE: Results indicated that both ERFs containing doxycycline, acrylic acid polymer, and polymethacrylate had an adequate pharmacokinetic-pharmacodynamic relationship for a time-dependent drug and a longer release time than doxycycline alone following oral administration in dogs. Given the minimum effective serum doxycycline concentration of 0.26 µg/mL, a dose interval of 48 hours can be achieved for each tested ERF. This minimum inhibitory concentration has the potential to be effective against several susceptible bacteria involved in important infections in dogs. Treatment of dogs with either ERF may have several benefits over treatment with doxycycline alone.