The aerosolization of salbutamol sulfate, measured as fine particle dose (FPD LD) and fine particle fraction (FPF LD) (<6.4 microm mass median aerodynamic diameter), from two sieved (63-90 microm) lactose monohydrate carriers, one as supplied, one smoothed by controlled surface dissolution, was studied. In general, no significant variation in FPD LD was observed at drug loadings between 10 and 63.5 microg and 10 and 135 microg for the surface dissolved and as supplied lactose monohydrates, respectively. Increasing the drug load above these levels resulted in linear increases in FPD LD with increasing drug load with the surface dissolved lactose monohydrate exhibiting higher FPD LD and FPF LD. This suggests that, at lower drug loadings, areas of the carrier exhibiting higher adhesion, so-called active sites, were being preferentially occupied and filled. Since there was no evidence of drug agglomeration using scanning electron microscopy, the observations suggest that the number and range of such higher energy "active sites" can be reduced by modifying the surface roughness, that is, energies, of the carrier.
The surface of lactose monohydrate was modified by solution phase variable temperature dissolution. Lactose monohydrate crystals were added to a known volume of a saturated solution of lactose monohydrate at 25 degrees C. The temperature of the mixture was then ramped to either 30, 35, 40, or 50 degrees C to produce lactose monohydrate batches with reduced levels of fines and lower surface roughness. A dramatic decrease in surface roughness with increasing dissolution temperature was visually observed using scanning electron microscopy. Particle size analysis suggested that the level of lactose fines was reduced after treatment at the lowest dissolution temperature, 30 degrees C. Evaluation of the samples' drug aerosolization using a twin stage impinger, after blending with salbutamol sulphate, suggested that even though there were dramatic changes in roughness and particle size distribution after surface dissolution at 30 degrees C, there was no significant difference in aerosolization as measured by fine particle fraction. However, after surface dissolution at 35 degrees C, there was an increase in fine particle fraction. Surface dissolution at even higher temperatures did not result in any further increase in fine particle fraction. These observations suggest that surface roughness and fines play an important role in the aerosolization of salbutamol sulphate, but the inter-relationships are not straightforward.
Gliclazide is a hypoglycemic agent exhibiting to some extent inadequate and variable absorption as a consequence of poor aqueous solubility and slow dissolution rates. A sodium salt of gliclazide was prepared and investigated for solubility and dissolution properties in comparison to untreated gliclazide. The salt was formed by adding equimolar amounts of gliclazide and sodium hydroxide in an aqueous-ethanolic phase. To confirm salt formation, sodium gliclazide was fully characterized by spectroscopy, differential scanning calorimetry, and potentiometric titration. Furthermore, solubility and in vitro dissolution studies of formulated tablets were performed at pH values of 1.2, 4.5, and 6.8. Sodium gliclazide demonstrated a significant increase in solubility at pH values of 4.5 and 6.8. The most apparent increase was achieved in unbuffered distilled water with a 235-fold higher solubility. Moreover, sodium gliclazide showed an enhancement in the dissolution rate in all tested media, but most significantly at pH 4.5 and 6.8. The highest difference (60%) in dissolution rate between gliclazide and its sodium salt was obtained at pH 6.8 at 30 min.The sodium salt of gliclazide presents improved solubility and drug dissolution, therefore limiting the possibility of variable absorption and improving the onset of action with potential enhancement in its overall bioavailability.
Purpose – The current status of nanotechnology research and development in Jordan is analyzed. In recent years, Jordanian institutions demonstrated considerable interest in the development and production of nanotechnology. Here the purpose of this paper is to provide detailed information about the status of nanotechnology in Jordan in terms of several factors that influence selectivity in nanotechnology and the number of published peer-reviewed research articles. Design/methodology/approach – Several factors that influence selectivity in nanotechnology and the number of published peer-reviewed research articles were analyzed. A detailed analysis of the collected data reveals that the number of publications, citations, and patents is highly dependent on the amount of research fund. Findings – The development in nanotechnology is associated with presence and accessibility of sensitive laboratory equipment. The nanotechnology research output in Jordan is still lower than it should be due to the lack of necessary laboratory infrastructure. This is due to the insufficient funds allocated to scientific research, the restrictive access to available instruments and the bureaucracy of some governmental departments. Compared to some developed countries, Jordan is noticeably behind in developing a nanotechnology system of research and industry. It will take time as well as technical and financial resources in order to achieve an advanced level in the field of nanotechnology in Jordan. Nevertheless, many Jordanian researchers are doing their best and are producing some good research articles. Research limitations/implications – The many applications to the same approach. Practical implications – Time and publications’ resources. Social implications – Peer cooperation. Originality/value – First comprehensive review ever. A base for researchers and decision makers.
Complexes of diclofenac sodium (DF-Na) with hydroxypropyl betacyclodextrin (HPβCD) were prepared by co-evaporation in a 1:1 ratio and characterized in light of previously reported data. Phase solubility diagrams were obtained for DF-Na with HPβCD in the presence and absence of zinc ions. Dissolution profiles were obtained for DF-Na and its HPβCD complex at acidic (pH 1.2) as well as in phosphate buffer (pH 6.8), in the presence and absence of zinc. HPβCD, as expected, was shown to improve the dissolution of DF-Na in acidic medium but not in phosphate buffer (pH 6.8). The presence of zinc ions decreased the in vitro dissolution of DF-HPβCD complex in acidic medium (pH 1.2) but not in phosphate buffer (pH 6.8). It was confirmed that the precipitate that was formed by zinc ions in the presence of HPβCD and DF-Na contained no cyclodextrin and most likely it was a mixture of the complexes: DF-Zn and DF-Zn with some molecules of water. In vivo experiments on rats have shown that HPβCD has no statistically significant effect on absorption or bioavailability of DF-Na in spite of the observed improvement of its in vitro dissolution by HPβCD. Moreover, zinc ions were shown to decrease the absorption rate of DF-Na in rats model but did neither significantly alter the absorption nor bioavailability of DF-HPβCD complex. The zinc induced precipitates of DF were shown to have significantly different crystalline properties when HPβCD was present. Therefore, the pharmaceutical details of a DF-Na preparation should be considered when designing the formulation and predicting possible interaction between DF-Na (or other potential NSAIDs) and zinc metal.
The pharmaceutical quality of five generics of glibenclamide that are available in the Jordanian market was assessed according to the British Pharmacopoeia (BP) monograph (2009). Similarly, the originator glibenclamide (Daonil ® ) which was obtained from the Saudi market was subjected to analysis and used as a reference product. All products were found satisfactory in terms of identification and related substances as per the BP requirements. However, the assay results showed that only two products, in addition to the reference (Daonil ® ) satisfied the BP specifications which required glibenclamide content to be within the range: 95 to 105% of the labeled content. All products, in spite of marginal deviations for two of them, were found to pass the United States Pharmacopoeia (USP) assay specifications (90 to 110%). Significant differences in dissolution behavior were observed between the different generics and the originator (Daonil ® ). Daonil ® exhibited the lowest dissolution profile while some products showed dissolution profiles that were almost twice that of Daonil ® .
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
334 Leonard St
Brooklyn, NY 11211
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.