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Sugiura T.,University of Shizuoka | Sugiura T.,Towa Pharmaceutical Co. | Uchida S.,University of Shizuoka | Namiki N.,University of Shizuoka
Chemical and Pharmaceutical Bulletin | Year: 2012

Orally disintegrating tablets (ODTs) are useful for improving benefits for patients of various ages. Masking the unpleasant taste of a drug is an important factor in the compliance of patients who take ODTs. We evaluated the taste acceptability effects of various taste-masking methods on bitter famotidine ODTs as a clinical pharmacological study. The following methods were tested to compare taste-masking effects: physical masking by spray-coating famotidine with ethyl cellulose versus organoleptic masking with added sweetener and flavor. The ODT samples were prepared as single or combinations of each taste-masking method using a novel suspension spray-coating method including a placebo. A total of 31 healthy volunteers were enrolled in this randomized, double-blind study and asked to score their bitterness, sweetness and total palate impressions by 100 mm visual analogue scale (VAS). VAS scores were significantly improved by the physical and organoleptic methods as compared to without taste-masked ODTs. Furthermore, the combination of both taste-masking methods was most effective for improving palatability and VAS scores were similar to those of placebo ODTs. The results of this study suggest that different taste-masking mechanisms function cooperatively. © 2012 The Pharmaceutical Society of Japan.

Sasamura S.,Astellas Pharma Inc. | Sasamura S.,Taiho Pharmaceutical Co | Kobayashi M.,Astellas Pharma Inc. | Muramatsu H.,Astellas Research Technologies Co. | And 10 more authors.
Journal of Antibiotics | Year: 2015

FR901459, a product of the fungus Stachybotrys chartarum No. 19392, is a derivative of cyclosporin A (CsA) and a powerful immunosuppressant that binds cyclophilin. Recently, it was reported that CsA was effective against hepatitis C virus (HCV). However, FR901459 lacks active moieties, which are essential for synthesizing more potent and safer derivatives of this anti-HCV agent. Here we identified an actinomycete strain (designated 7887) that was capable of efficient bioconversion of FR901459. Structural elucidation of the isolated bioconversion products (1-7) revealed that compounds 1-4 were mono-hydroxylated at the position of 1-MeBmt or 9-MeLeu, whereas compounds 5-7 were bis-hydroxylated at both positions. The results of morphological and chemical characterization, as well as phylogenetic analysis of 16S ribosomal DNA (rDNA), suggested that strain 7887 belonged to the genus Lentzea. Comparison of the FR901459 conversion activity of strain 7887 with several other Lentzea strains revealed that although all examined strains metabolized FR901459, strain 7887 had a characteristic profile with respect to bioconversion products. Taken together, these findings suggest that strain 7887 can be used to derivative FR901459 to produce a chemical template for further chemical modifications that may provide more effective and safer anti-HCV drugs. © 2015 Japan Antibiotics Research Association All rights reserved.

Sasakura D.,Showa Pharmaceutical University | Nakayama K.,Showa Pharmaceutical University | Chikuma T.,Towa Pharmaceutical Co.
Pharmazie | Year: 2015

Process analytical technology is important for the analysis and control of manufacturing processes. Nearinfrared spectroscopy is widely used in various process analytical technologies for the analysis of the chemical componentsof solid dosage forms. Lubrication is an important process carried out before a tablet is produced. In this process, the concentration of lubricant, such as magnesium stearate (StMg), might change for one of many reasons during powder transport, which would be a critical problem such as variation in tablet compressibility and dissolution failure of compressed tablets. Our group investigated the feasibility of the quantitative monitoring of a change in the concentration of StMg in the feeder tube of tableting equipment employing real-time near-infrared spectroscopy.

Okuda Y.,Towa Pharmaceutical Co. | Okamoto Y.,Towa Pharmaceutical Co. | Irisawa Y.,Towa Pharmaceutical Co. | Okimoto K.,Towa Pharmaceutical Co. | And 2 more authors.
Chemical and Pharmaceutical Bulletin | Year: 2014

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). ODTRAC 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, ODTRAC 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 ODTRAC remained intact and no damage was observed on the surface. ECP-T recovered from ODTRAC 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, ODTRAC 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. © 2014 The Pharmaceutical Society of Japan.

Wakimoto H.,University of Tokyo | Yamasaki R.,Towa Pharmaceutical Co. | Kumano A.,Towa Pharmaceutical Co. | Tsutani K.,University of Tokyo
Japanese Pharmacology and Therapeutics | Year: 2013

An increase in the prescription of generic drugs (GEs) may help to reduce drug expenditure. The Japanese government has promoted the use of GEs and has proposed to expand GE sharing. However, GE sharing is still low. From 2011 to 2012, GE sharing accounted for 23.3% of the total drug volume. Since the number of brand name drugs that may be substituted by GEs has not yet been determined, we calculated the total number of drugs, original drugs, and GEs available in Japan. We searched in three Japanese databases, the master list of medicines by the Various information of Medical Fee (as released on 17 April 2012), the drugs listed on the National Health Insurance Drug Price Standard list by the Ministry of Health, Labour and Welfare (as of 17 April 2012), and the HOT Reference Numbers (as released on 27 April 2012) by the Medical Information System Development Center, and determined that the total number of drugs available in Japan as of 27 April 2012, was 17, 904. Of the 17, 904 drugs found, 786 drugs had an unlisted price. Moreover, 3464 of these drugs were brand name drugs, of which 2711 drugs had expired patents and/or had completed the re-examination period, and 1234 drugs could be substituted by 4098 GEs. This is the first study to determine the exact number of brand name drugs that can be substituted by GEs in Japan, which may be used as a foundation for the development of more rational drug policies and target settings.

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