Natural rubber blends for floating theophylline beads.

Natural rubber (NR)'s value has become increasingly important for human applications. This study prepared NR beads as floating drug delivery system by dripping NR latex into hardening solution to obtain spherical beads. Theophylline was loaded as a model drug. NR latex formed into harden beads suddenly after dripping droplets in acidic medium. These NR beads floated instantly and buoyant in HCl buffer for over 8 h with prolonged theophylline release. Their morphologies, crystallinity and thermal properties were observed using microscope, X-ray diffractometer, and thermogravimetry, respectively. Addition of 100 phr sodium bicarbonate increased drug release owing to liberation of carbon dioxide promoting porous NR matrix. Composite of 50 and 200 phr shellac in NR beads floated in HCl buffer for over 12 h. Moreover, 200 phr shellac efficiently retarded release of theophylline from NR composite beads (lower than 10 % in 8 h), whereby promoting theophylline release in phosphate buffer (pH 6.8) (approximately 80 % in 8 h). NR-shellac beads had greater water sorption (2.5 times) and erosion (4.9 times) in phosphate buffer than in HCl buffer. Thus, NR beads exhibited desirable attributes as floating drug delivery system. Both sodium bicarbonate and shellac modified matrix properties and drug release of NR beads.

New Insight into the Impact of Effervescence on Gel Layer Microstructure and Drug Release of Effervescent Matrices Using Combined Mechanical and Imaging Characterisation Techniques.

Gel layer characteristics play a crucial role in hydrophilic hydroxypropyl methylcellulose (HPMC) matrix development. Effervescent agents have the potential to affect the gel layer microstructures. This study aimed to investigate the influence of effervescence on the microstructure of the gel layer around HPMC matrices using a combination of texture analysis and imaging techniques. The relationship with drug release profile and release mechanisms were also examined. The high amounts of effervescent agents promoted a rapid carbonation reaction, resulting in a high gel layer formation with a low gel strength through texture analysis. This finding was ascribed to the enhanced surface roughness and porosity observed under digital microscopy and microporous structure of the gel layer under scanning electron microscopy. The reconstructed three-dimensional images from synchrotron radiation X-ray tomographic microscopy notably exhibited the interconnected pores of various sizes from the carbonation reaction of effervescent and microporous networks, indicating the gel layer on the tablet surface. Notably, effervescence promoted the increase in interconnected porosities, which directly influenced the strength of the gel layer microstructure, drug release patterns and release mechanism of the effervescent matrix tablet. Therefore, combined mechanical characterisation and imaging techniques can provide new insights into the role of effervescent agents on the gel layer microstructure, and describe the relationship of drug release patterns and release mechanism of matrix tablets.

Stereomicroscope with Imaging Analysis: A Versatile Tool for Wetting, Gel Formation and Erosion Rate Determinations of Eutectic Effervescent Tablet.

Wettability, gel formation and erosion behaviors could influence the drug release pattern of solid dosage forms. Typically, these parameters are evaluated using a variety of techniques. Nonetheless, there has been no previous research on versatile tool development for evaluating several tablet characteristics with a single tool. The aim of this study was to develop the versatile tool for measuring various physical properties of eutectic effervescent tablets and also investigate the relationship between these parameters with parameters from drug dissolution. Ibuprofen (IBU)-poloxamer 407 (P407) eutectic effervescent tablets were fabricated with a direct compression method. Their wetting properties, gel formation and erosion behaviors were investigated using a stereomicroscope with imaging analysis in terms of the liquid penetration distance, gel thickness and erosion boundary diameter, respectively. In addition, the dissolution rate (k) and disintegration time of eutectic effervescent tablets in 0.1 N HCl buffer pH 1.2 were also determined. Incorporation of P407 into the IBU tablet improved the tablet wetting properties with increasing liquid penetration distance under stereoscope. CO2 liberation from effervescent agents promoted tablet surface roughness from matrix erosion. The relationship between observed physical properties and disintegration and dissolution parameters suggested that the combination of erosion by effervescent agents and gel formation by P407 had a potential influence on dissolution enhancement of the formulation. Therefore, a developed stereomicroscope with an imaging analysis technique was exhibited as an alternative versatile tool for determining the wetting properties, gel formation and erosion behaviors of pharmaceutical solid dosage forms.