An investigation into the digestibility of chitosan by human colonic bacteria.

The suitability of chitosan (non-crosslinked and crosslinked by glutaraldehyde) for colonic drug delivery was assessed by incubation of chitosan films in human faecal slurry and assessment of the film’s disappearance with time. It was found that non-crosslinked chitosan, was digested by colonic bacteria, but crosslinked chitosan was not

In vivo evaluation of pH-sensitive polymeric microparticles for site specific drug delivery to the small intestine and colon

A novel emulsification/solvent evaporation process was developed to formulate prednisolone-loaded Eudragit L and S microparticles as drug delivery vehicles to target different regions of the gastrointestinal tract. Microparticles were characterised in vitro and in vivo. This is the first report of drug absorption form orally administered Eudragit L and S microparticles

A New Method for Producing Pharmaceutical Co-crystals: Laser Irradiation of Powder Blends

In this work, a high-power CO2 laser was used to irradiate powder blends of co-crystal formers, with the specific aim of trying to cause recrystallization to a co-crystal structure. By varying the power and raster speed of the laser, it was found that sufficient thermal energy could be imparted to the powder to cause molecular rearrangement. It was possible to form co-crystals of caffeine with oxalic acid and caffeine with malonic acid. Interestingly, it was found that, to form co-crystals successfully, the coformers needed to sublime to an appreciable extent, which indicates that the mechanism of rearrangement involves interaction and nucleation in the vapor phase. Laser irradiation thus offers a new route to creation of pharmaceutical co-crystals and a potentially rapid screen for likely co-crystal formation between coforming pairs

Advanced machine-learning techniques in drug discovery

The popularity of machine learning (ML) across drug discovery continues to grow, yielding impressive results. As their use increases, so do their limitations become apparent. Such limitations include their need for big data, sparsity in data, and their lack of interpretability. It has also become apparent that the techniques are not truly autonomous, requiring retraining even post deployment. In this review, we detail the use of advanced techniques to circumvent these challenges, with examples drawn from drug discovery and allied disciplines. In addition, we present emerging techniques and their potential role in drug discovery. The techniques presented herein are anticipated to expand the applicability of ML in drug discovery

Energy consumption and carbon footprint of 3D printing in pharmaceutical manufacture

Achieving carbon neutrality is seen as an important goal in order to mitigate the effects of climate change, as carbon dioxide is a major greenhouse gas that contributes to global warming. Many countries, cities and organizations have set targets to become carbon neutral. The pharmaceutical sector is no exception, being a major contributor of carbon emissions (emitting approximately 55% more than the automotive sector for instance) and hence is in need of strategies to reduce its environmental impact. Three-dimensional (3D) printing is an advanced pharmaceutical fabrication technology that has the potential to replace traditional manufacturing tools. Being a new technology, the environmental impact of 3D printed medicines has not been investigated, which is a barrier to its uptake by the pharmaceutical industry. Here, the energy consumption (and carbon emission) of 3D printers is considered, focusing on technologies that have successfully been demonstrated to produce solid dosage forms. The energy consumption of 6 benchtop 3D printers was measured during standby mode and printing. On standby, energy consumption ranged from 0.03 to 0.17 kWh. The energy required for producing 10 printlets ranged from 0.06 to 3.08 kWh, with printers using high temperatures consuming more energy. Carbon emissions ranged between 11.60 and 112.16 g CO2 (eq) per 10 printlets, comparable with traditional tableting. Further analyses revealed that decreasing printing temperature was found to reduce the energy demand considerably, suggesting that developing formulations that are printable at lower temperatures can reduce CO2 emissions. The study delivers key initial insights into the environmental impact of a potentially transformative manufacturing technology and provides encouraging results in demonstrating that 3D printing can deliver quality medicines without being environmentally detrimental

Sediment Distribution Based on Grain Size Analyses in Weda Bay, Northern Maluku

An integrated study of sediment distribution was conducted in Weda Bay, Northern Maluku to provide general information on transportation and deposition process based on sediment grain size distribution. The study was conducted during the Weda Bay Expedition using the “Baruna Jaya VII” research vessel in March 13th –22th 2013. Sieving method (granulometric) was used to analyze the grain size. The results indicated that in general the pattern of sea floor sediment distribution was dominated by clay – sand grain-sized. The current speed influenced the sediment transport, deposition, and distribution. Larger fractions of sediment were quickly settled on the sea floor due to stronger currents around Southern area (Widi islands), meanwhile the lesser fractions of the transported away into other places with weaker currents conditions

The Milky Way: Paediatric milk-based dispersible tablets prepared by direct compression - a proof-of-concept study

Objectives: Dispersible tabletsare proposed by the World Health Organisation as the preferred paediatric formulation. It was hypothesised that tablets made from a powdered milk-base that disperse in water to form suspensions resembling milk might be a useful platform to improve acceptability in children. Methods: Milk-based dispersible tablets containing various types of powdered milk and infant formulae were formulated. The influence of milk type and content on placebo tablet properties was investigated using a design-of-experiments approach. Responses measured included friability, crushing strength, and disintegration time. Additionally, the influence of compression force on the tablet properties of a model formulation was studied by compaction simulation. Key findings: Disintegration times increased as milk content increased. Compaction simulation studies showed that compression force influenced disintegration time. These results suggest that the milk content, rather than type, and compression force were the most important determinants of disintegration. Conclusion: Up to 30% milk could be incorporated to produce 200 mg 10 mm flat-faced placebo tablets by direct compression disintegrating within 3 minutes in 5-10 ml of water, which is a realistic administration volume in children. The platform could accommodate 30% of a model API (caffeine citrate)