Synthesis and Characterization of Nanoporous Carbon Carriers for Losartan Potassium Delivery

Losartan potassium is most commonly used for the treatment of hypertension. In recent years, new applications of this drug have emerged, encouraging the design of novel nanoporous carriers for its adsorption and release. The purpose of this study was to synthesize ordered mesoporous carbon vehicles via a soft-templating method altered with the use of nitrogen precursors and via a hard-templating method followed by chitosan functionalization. As a result, the materials obtained differed in nitrogen content as well as in the number of total surface functional groups. The impact of the modification on the physicochemical properties of carbon carriers and their interaction with losartan potassium during adsorption and release processes was examined. The materials were characterized by various morphologies, specific surface areas (101–1180 m2 g−1), and the amount of acidic/basic oxygen-containing functional groups (1.26–4.27 mmol g−1). These features, along with pore sizes and volumes, had a key effect on the sorption capacity of carbon carriers towards losartan potassium (59–161 mg g−1). Moreover, they contributed to the differential release of the drug (18.56–90.46%). Losartan potassium adsorption onto the surface of carbonaceous materials was mainly based on the formation of hydrogen bonds and π–π interactions and followed the Langmuir type isotherm. It has been shown that the choice of the method of carbon carriers’ synthesis and their modification allows for the precise control of the kinetics of the losartan potassium release from their surface, resulting in rapid or sustained drug liberation.

Synthesis and Characterization of calcium Starch: A New Controlled Release Polymer for floating tablets of Losartan Potassium

Losartan potassium is used to treat high blood pressure (hypertension). The present study was aimed to prepare a floating drug delivery system to design a controlled release oral dosage form of Losartan potassium. This helps to overcome the demerit of limited residence time of the drug in the gastrointestinal track and hence to increase the duration of release. Hence objective of the present study is to develop Losartan potassium floating tablets by direct compression method using calcium starch as release retarding polymer. The calcium starch was synthesized by gelatinizing potato starch in the presence of sodium hydroxide and cross linking by treatment with calcium chloride. The micromeritic properties studies indicated that calcium starch is a promising pharmaceutical excipient in tablets. Floating tablets of Losartan potassium was formulated by direct compression technique, using different concentration of calcium starch and compared with HPMC K-100 as release retard polymer. As the amount of calcium starch in the tablet increased, the drug release decreased. The formulation F5 containing 125 mg calcium starch showed better controlled release of 76.38% after 12 hours.

Design and Evaluation of Losartan Potassium Effervescent Floating Matrix Tablets: In Vivo X-ray Imaging and Pharmacokinetic Studies in Albino Rabbits

Losartan potassium (LP) is an angiotensin receptor blocker used to treat hypertension. At higher pH, it shows poor aqueous solubility, which leads to poor bioavailability and lowers its therapeutic effectiveness. The main aim of this research was to develop a direct compressed effervescent floating matrix tablet (EFMT) of LP using hydroxyl propyl methylcellulose 90SH 15,000 (HPMC-90SH 15,000), karaya gum (KG), and an effervescent agent, such as sodium bicarbonate (SB). Therefore, an EFMT has been developed to prolong the stomach residence time (GRT) of a drug to several hours and improve its bioavailability in the stomach region. The blended powder was evaluated for pre-compression characteristics, followed by post-compression characteristics, in vitro floating, water uptake studies, and in vitro studies. The optimized formulation of EFMT was investigated for in vivo buoyancy by X-ray imaging and pharmacokinetic studies in Albino rabbits. The results revealed that the parameters of pre- and post-compression were within the USP limits. All tablets showed good floating capabilities (short floating lag time <1 min and floated for >24 h), good swelling characteristics, and controlled release for over 24 h. The Fourier-transform infrared (FTIR) and differential scanning calorimetry (DSC) spectra showed drug–polymer compatibility. The optimized formulation F3 (HPMC-90SH 15,000-KG) exhibited non-Fickian diffusion and showed 100% drug release at the end of 24 h. In addition, with the optimized formulation F3, we observed that the EFMT floated continuously in the rabbit’s stomach area; thus, the GRT could be extended to more than 12 h. The pharmacokinetic profiling in Albino rabbits revealed that the relative bioavailability of the optimized LP-EFMT was enhanced compared to an oral solution of LP. We conclude that this a potential method for improving the oral bioavailability of LP to treat hypertension effectively.

Simultaneous Determination of Hydrochlorothiazide and Losartan Potassium in Pharmaceutical Product by UV-Vis Spectrophotometric Method with Kalman Filter Algorithm

In this paper, hydrochlorothiazide (HCT) and losartan potassium (LSP) in tablets are simultaneously determined with UV-Vis spectrophotometry and chemometrics without separation. The spectra of standard and sample solutions were recorded in the wavelength from 220 to 300 nm at 1.0 nm intervals. The concentrations of HCT and LSP in the sample solutions were computed with the Kalman filter algorithm written on the Microsoft Excel 2016 and Visual Basic for Applications (VBA) platform. The method validation was determined via the accuracy and repeatability of measurements when analyzing HCT and LSP in the Splozarsin Plus tablet and comparing the mean values of their contents in the sample with those analyzed with HPLC. The proposed method is simple with a low cost compared with the standard HPLC method.