Formulation Design for Orally Disintegrating Tablets Containing Enteric-Coated Particles

Abstract

The purpose of this study was to investigate the applicability of our newly developed technology (RACTAB ® technology) for preparing orally disintegrating tablets (ODTs) containing enteric-coated particles. Tamsulosin hydrochloride (TAM) was used as a model drug contained in the enteric-coated particles. Enteric-coated particles containing TAM (ECP-T) were prepared by spray coating a mixture of TAM with controlled-release materials. ECP-T was then mixed with rapidly disintegrating granules (RDGs), which were prepared using the suspension spray-coating method, and was tableted to form ODTs (ODT RAC ). ODT RAC was evaluated for its hardness, thickness, internal structure (X-ray-CT scanning), functional properties (controlled-release profile), and in vivo disintegration time. Since RDGs with micronized ethylcellulose (MEC) increased tablet hardness by increasing the contact frequency between granules, ODT RAC containing ECP-T exhibited high hardness (>50 N) and low friability (<0.5%) with a relatively low compression force. After tableting, the structure of ECP-T in ODT RAC remained intact and no damage was observed on the surface. ECP-T recovered from ODT RAC showed the same dissolution profile of TAM in Japanese Pharmacopoeia (JP) 1st and JP 2nd media as that of intact ECP-T, which indicated that the tableting process did not affect the acid-resistibility of the particle. In addition, ODT RAC rapidly disintegrated in vivo (< 30 s), even at a high compression force (at 9 kN). These findings clearly suggest that RACTAB ® technology is a useful approach to prepare ODTs containing enteric-coated particles.

Examination of Aggregate Formation upon Simultaneous Dissolution of Methacrylic Acid Copolymer LD Enteric Coating Agent, Pharmaceutical Additives, and Zwitterionic Ingredients

“…Methacrylic acid copolymer LD is widely used for enteric coating or sustained release coating. 15,16) To confirm the role of methacrylic acid copolymer LD, we examined other drugs. Aggregates were formed in co-suspensions of levofloxacin with tegafur uracil combination granules and tamsulosin hydrochloride OD tablets, which also contain methacrylic acid copolymer LD.…”

“…The amounts used corresponded to those contained in one tablet of original lansoprazole OD. 15) Aggregate Formation between Levofloxacin and Drugs Containing Methacrylic Acid Copolymer LD Five hundred milligram of levofloxacin was suspended in 30 mL of tap water. After 5 min, a tamsulosin hydrochloride OD tablet or 1 package of tegafur uracil combination granules was added and the mixture was observed.…”

Potential Use of Magnesium Oxide as an Excipient to Maintain the Hardness of Orally Disintegrating Tablets during Unpackaged Storage

“…Several solutions to this problem using additives have been reported to date, but elaborate processing of the additives is required before tablet preparation. 6,7) Further research is required to develop a convenient method of preparing an ODT that exhibits rapid disintegration while maintaining its hardness during storage under high humidity.…”

The prediction of the palatability of orally disintegrating tablets by an electronic gustatory system

“…Recently, based on the requests from 55 patients to enhance their quality of life (QOL),severalpharmaceutical companies have developed various (new) types of ODTs. For example, RACTAB ® technology is one of thenew technologies for the preparation of ODTs, consisting of rapid disintegration granules (RDGs) spray-coated with a suspension of wicking agents using a fluidized-bed granulator.ODTs prepared using the RACTAB ® technology,whichisa simple preparation method, have superior 60 properties, including a comparatively high tablethardness, high physical stability, high resistance against humidity, fast oral disintegration rate, and improved mouth feel (Okuda et al, 2009(Okuda et al, , 2011(Okuda et al, , 2014.…”