No abstract

Sodium alginate, calcium carbonate, and guar gum were mixed with oils such as olive oil (OO), sesame oil (SO), and medium chain triglyceride (MCT). The oily formulations were found to simplify the preparation of in situ floating gel. This was the aim of this study using ketoconazole (keto) as a model drug. The investigations for the floating property were established by In vitro gelling capacity study and In vitro floating study. Additionally, in vitro release study was applied to find the best formulations to delay the release of keto. Then, selected formulations were studied by FTIR and SEM. Lastly, in vivo gelation was performed to examine the gelation in the rat’s stomach. The results showed all formulations were floating after successful gelation as the least amount of sodium alginate to gel oils was 20% w/w. The gels in SO and OO were better than MCT in delaying keto release, and 30% w/w sodium alginate in SO was the best to delay the release of keto within 8 hours of the release study. Selected gels showed interactions between the keto molecules and the molecules of the gel contents by FTIR study, and SEM showed a difference in the internal structure of selected formulations. Lastly, the 30% w/w sodium alginate in SO proved to gel and remain in the rat's stomach in the following periods: 30 min, 1 hour, 2 hours, and after 8 hours. Oily suspension formulations showed floating properties in the stomach and slowed the release of keto and specifically 30% w/w of sodium alginate in SO.

This work targeted studying organogel as a potential floating system. Organgel has an excellent viscoelastic properties, floating system posses a depot property.  Different formulations of 12-hydroxyoctadecanoic acid (HOA) in sesame oil were gelled and selecting F1, F3 and F5 HOA organogels for various examinations: tabletop rheology, optical microscopy, and oscillatory rheology studies. Also, the floating properties studies were conducted at in vitro and in-vivo levels. Lastly, the in-vitro release study using cinnarizine (CN) was to investigate the organogel depot property. Based on the results, the selected concentrations of HOA in sesame oil organogels showed temperature transitions from gel to sol higher than body temperature. These organogels scaffolds inner structures were a star-like shape. The formulation F5 HOA/SO organogels were developing higher storage modulus values, which resulted from the amplitude sweep study. Indeed, all the selected organogels were frequency sweep independent. The organogel’s in vitro floating properties were found positively proven our work’s aim and were buoyant for 24 hours as F5 HOA organogels remained for 12 hours in the rat’s stomach. The depot property showed the slow release of CN from F5 HOA/SO organogel and not more than 65% w/w of CN released after 24 hours.

No abstract

This study aimed to formulate a gastro retentive slow release dosage form based on oral film for metoclopramide hydrochloric acid (HCl), a medication with a narrow absorption window. The gastroretentive film was made using a solvent casting method with varying ratios of primary polymers (HPMC 15000 cps and HPMC K4M), secondary polymer (carbopol 934), and PEG-400 as a plasticizer. The film of hydroxypropyl methylcellulose (HPMC) K4M-3 (50:50) (HPMC K4M: carbopol) was buoyant for 20 minutes. The 52 wt % of metoclopramide HCl (metclo) was released from the HPMC K4M-3 film after 24 hours, and its swelling index was (46.5%). The mucoadhesive strength of the HPMC K4M-3 was 18 gm, and the film showed no effect on the rat’s stomach tissue compared to normal rat tissue histologically. The HPMC K4M-3 produced modest values of percent elongation of 77.6%. To conclude, the optimized film appeared to be a promising mucoadhesive gastro retentive oral film with the ease of administration and controlled release.