A sample kit of Hypromellose having different viscosity levels, hydroxypropoxy (HPO) content and particle size was applied to a robustness study of a hydrophylic matrix tablet of dipyridamole. There was a difference in dissolution between the different viscosity grades of Hypromellose. However, there was no significant difference in the release profile when parameters were carried over the upper and lower limit of each specification. The only exception was a difference in release profile with the lowest viscosity grade containing lower end of HPO. Overall the data suggested that the formulation used in this study was highly robust with respect to the properties of Hypromellose.
Hypromellose Acetate Succinate (HPMCAS) is known as an enteric polymer and used in coating for the last 30 years. HPMCAS also has excellent properties to use as a carrier in "solid dispersion, a method to improve the solubility of poorly water-soluble drugs, due to its high solubilizing capability and high performance to maintain super-saturation. As a method to prepare solid dispersion, "Hot Melt Extrusion (HME)" is becoming attractive because of freedom from organic-solvents and high productivity. In HME, the polymer should be extruded at relatively low temperature as it can decompose at high temperature. In this study, Shin-Etsu has developed a new grade of HPMCAS that has better workability in the HME process. This new grade can be easily extruded at lower temperature than the conventional grades, while it keeps the original performance of heat stability, water adsorption and maintaining super saturation of APIs.
The development of bioavailable solid dispersions requires the use of secondary materials for stabilizing the amorphous dispersion while also enhancing dissolution and solubility of the new chemical entity. With the increased use of amorphous dispersions, HPMCAS (Hypromellose Acetate Succinate) has emerged as a commonly used excipient for formulary design. This white paper details the properties of HPMCAS that make it a beneficial material for use in solid dispersion formulation, with a specific focus on relevant properties for melt extrusion.
Presented at AAPS 2014
Orally-disintegrating tablets (ODT) are becoming a popular dosage form, especially for geriatric patients. A new co-processed excipient SmartEx, has been developed for immediate release tablets or ODT. This excipient contains DMannitol, Low-substituted Hydroxypropylcellulose and Polyvinyl Alcohol. In this study, its compressibility, disintegration, and stability were evaluated.
L-HPC (Low-substituted Hydroxypropyl Cellulose) was first approved in 1987 as a disintegrant/binder for pharmaceutical solid dosage forms in Japan. A recent survey shows that L-HPC is ranked as the first choice for tablet disintegrant by Japanese pharmaceutical companies. Not only a disintegrant, L-HPC also functions as binder due to its good compressibility. There are many cases that L-HPC solved problems of interactions with APIs other issues such as capping.