Formulation and In Vitro and In Vivo Evaluation of Lipid-Based Terbutaline Sulphate Bi-layer Tablets for Once-Daily Administration

Abstract

Abstract. The objective of this study was to prepare and evaluate terbutaline sulphate (TBS) bi-layer tablets for once-daily administration. The bi-layer tablets consisted of an immediate-release layer and a sustained-release layer containing 5 and 10 mg TBS, respectively. The sustained-release layer was developed by using Compritol®888 ATO, Precirol® ATO 5, stearic acid, and tristearin, separately, as slowly eroding lipid matrices. A full 4×2 2 factorial design was employed for optimization of the sustainedrelease layer and to explore the effect of lipid type (X 1 ), drug-lipid ratio (X 2 ), and filler type (X 3 ) on the percentage drug released at 8, 12, and 24 h (Y 1 , Y 2 , and Y 3 ) as dependent variables. Sixteen TBS sustained-release matrices (F1-F16) were prepared by melt solid dispersion method. None of the prepared matrices achieved the targeted release profile. However, F2 that showed a relatively promising drug release was subjected to trial and error optimization for the filler composition to develop two optimized matrices (F17 and F18). F18 which consisted of drug-Compritol®888 ATO at ratio (1:6 w/w) and Avicel PH 101/dibasic calcium phosphate mixture of 2:1 (w/w) was selected as sustained-release layer. TBS bilayer tablets were evaluated for their physical properties, in vitro drug release, effect of storage on drug content, and in vivo performance in rabbits. The bi-layer tablets showed acceptable physical properties and release characteristics. In vivo absorption in rabbits revealed initial high TBS plasma levels followed by sustained levels over 24 h compared to immediate-release tablets.

Development and In vitro-In vivo Characterization of Chronomodulated Multi-Particulate Drug Delivery System of Terbutaline Sulphate for Treatment of Nocturnal Asthma by box–Behnken Statistical Design

“…The value of MRT was found to be 9.51± 0.201 h for formulation MP1 and 6.26 ± 0.698 h for immediate release tablet (Table 7). In a study conducted by Hashem et al, (2016) similar results for C max, were obtained which supports present study. From the statistical analysis of pharmacokinetic parameters, there was a significant difference in the values of AUC 0-∞ and MRT between immediate release tablet and MP1, demonstrating that formulation MP1 was able to sustain the release and had a longer MRT.…”

“…At predetermined time intervals (0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14 and 24 h post dose), 1ml of blood samples were collected from the marginal ear vein and analysis of the samples were done. Pharmacokinetic parameters including C max , T max , AUC 0-t , AUC 0-∞, t 1/2 and MRT were determined from plasma profile by the using software Kinetica 5.0 (Hashem et al, 2016;Chandaa et al, 2010;Bajwa et al, 2017a).…”

Preparation and Pharmacokinetics Evaluation of Solid Self-Microemulsifying Drug Delivery System (S-SMEDDS) of Osthole

“…The polymeric materials play an important role in the formation of microspheres and drug release. Taking the pH sensitivity of osthole in gastric juice into account, application of enteric coating played a key role in solving the problem (44)(45)(46)(47). In the current study, four polymers, including Eudragit S100, EC, CA, and HPMCP-HP55, were evaluated based on sphere formation and product yield.…”

Facile Preparation of Drug-Loaded Tristearin Encapsulated Superparamagnetic Iron Oxide Nanoparticles Using Coaxial Electrospray Processing

“…For example, genistein has been explored for chemotherapeutic applications and is known to be an excellent molecule for several other biological functions. 29 Similarly, tristearin has been explored in numerous therapeutic dosage forms involving solid lipid nanoparticles 30 and as solid oral drug delivery systems (e.g., tablets) 31 displaying good in vitro and in vivo outcomes. SPIONs have been investigated as nontoxic MRI imaging agents and theranostic agents.…”