Acid-treated yeast cell wall as a binder displaying function of disintegrant.
This investigation examined the application of acid-treated yeast cell wall (AYC) as a binder functioning as a disintegrant. Acetylsalicylic acid (ASA) was granulated with AYC, hydroxypropylcellulose (HPC), polyvinylpyrrolidone (PVP), or pullulan (PUL) and compressed into a tablet in the absence of disintegrant. Particle size and angle of repose of the granules, tensile strength, disintegration time, and water absorption behavior of the tablets and ASA release profiles from the tablets were measured. The surface of AYC-granules was observed with a scanning electron microscope. As was the case with the granules of HPC, PVP, or PUL, D50 of the granules of AYC increased with increasing AYC addition percentage, indicating that it is possible to granulate ASA with AYC. Tablets incorporating HPC, PVP, and PUL failed to disintegrate within 30 minutes at all percentages of binder addition because in the case of the HPC, PVP, or PUL tablets in the dissolution medium, water scarcely penetrated into the inner region of the tablet, causing no disintegration. In the case of the AYC tablets, disintegration was not detected at 3% or less of AYC. When AYC was equal to or greater than 5%, AYC tablets disintegrated in approximately 4 minutes and rapid ASA release from the tablets was observed. These results may have been caused by the following. In the case of the AYC 3% granules, ungranulated aspirin powder remained, but in the case of the AYC 5% granules, ASA powder was granulated and covered with AYC. Water absorption was observed initially; however, a plateau was reached in the case of the AYC 3%-tablet. In contrast, in the cases of the AYC 5% and more tablets, water absorption was greater and increased with time. The angle of repose of the AYC 5% granules was 25.7 degrees, which represented high fluidity. The tablets produced by compressing the granules demonstrated sufficient tensile strength greater than 0.8 MPa. The tablets rapidly disintegrated and rapid ASA release was obtained. AYC functioned as a binder at granulation; additionally, AYC served as a disintegrant in the dissolution of drug from the tablets. These results indicate that AYC affords high utility as a unique pharmaceutical additive possessing contrary functions such as binding and disintegration.
Ozeki
Tetsuya
T
Department of Pharmaceutics and Drug Delivery, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Tokyo, Japan. ozekit@ps.toyaku.ac.jp
Katsuyama
Hideyo
H
Yasuzawa
Yuriko
Y
Takashima
Yuuki
Y
Kasai
Takahide
T
Eguchi
Takahiro
T
Kakiuchi
Hisaya
H
Yuasa
Hiroshi
H
Okada
Hiroaki
H
D000143:Acids / Q000737:chemistry*; D001241:Aspirin / Q000378:metabolism; D002473:Cell Wall / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry; D005079:Excipients / Q000737:chemistry*; D010316:Particle Size; D010592:Pharmaceutic Aids / Q000737:chemistry; D011208:Powders / Q000737:chemistry / Q000378:metabolism; D012441:Saccharomyces cerevisiae / Q000737:chemistry*; D013607:Tablets / Q000737:chemistry / Q000378:metabolism; D013718:Tensile Strength; D013997:Time Factors; D014867:Water / Q000378:metabolism
D000143:Acids; D003692:Delayed-Action Preparations; D005079:Excipients; D010592:Pharmaceutic Aids; D011208:Powders; D013607:Tablets; D014867:Water; D001241:Aspirin