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Patent
Ohara Pharmaceutical Co. | Date: 2016-11-18

The present invention relates to a novel compound represented by formula (1), or salt thereof, wherein R is hydroxy group or hydrogen atom; R^(1 )and R^(2 )are the same or different, and are each independently benzyl group which may have a substituent. The present invention provides therapeutically agents, which have remarkable stability against cytidine deaminase, a metabolic enzyme, can be absorbed in vivo by oral administration and inhibit protein synthesis by being incorporated easily into nucleic acid bio-synthesis in vivo for replacing injection agent (5-azacytidine or 2-deoxy-5-azacytidine) used in clinic for treating myeloma.


Sakuma S.,Setsunan University | Tachiki H.,Towa Pharmaceutical Co. | Uchiyama H.,Towa Pharmaceutical Co. | Fukui Y.,Kyowa Pharmaceutical Industry Co. | And 9 more authors.
Molecular Pharmaceutics | Year: 2011

The ratio of AUC to the dose (AUC/dose) was previously found as a parameter that predicts a risk of bioinequivalence of oral drug products. On the basis of the combination of this parameter and the biopharmaceutics classification system (BCS), a perspective for biowaivers of human bioequivalence studies is discussed. Databases of bioequivalence studies using immediate-release solid oral dosage forms were disclosed by 6 Japanese generic pharmaceutical companies, and the number of subjects required for demonstrating bioequivalence between generic and reference products was plotted as a function of AUC/dose for each BCS category. A small variation in the number of subjects was constantly observed in bioequivalence studies using dosage forms containing an identical BCS class 1 or class 3 drug, even though formulations of the generic product differ between companies. The variation was extremely enlarged when the drugs were substituted with BCS class 2 drugs. Rate-determining steps in oral absorption of highly water-soluble BCS class 1 and class 3 drugs are independent of formulations when there is no significant difference in the in vitro dissolution profiles between formulations. The small variation observed for both BCS categories indicates that the number of subjects converges into one value for each drug. Our analysis indicates the appropriateness of biowaiver of bioequivalence studies for immediate-release solid oral dosage forms containing not only BCS class 1 drugs but also class 3 drugs. © 2011 American Chemical Society.


Nakata Y.,OHARA Pharmaceutical Co. | Kiyosawa Y.,OHARA Pharmaceutical Co. | Kagara K.,OHARA Pharmaceutical Co. | Matsuoka M.,Tokyo University of Agriculture and Technology
Journal of Chemical Engineering of Japan | Year: 2010

To obtain a desired polymorphic composition of MPPO (4-(1-(2-(3-methoxyphenethyl)phenoxy)-3-(dimethylamino)propan-2-yloxy)-4-oxobutanoic acid), operation conditions were sought for seeded and drowning-out batch crystallization. Polymorphic mixtures having the same composition with the seed were obtained by controlling the seeding temperature, because it determined the supersaturations for the crystallization of both polymorphs.Analyzing the changes in the solution concentration and monitoring the particle behavior with FBRM, different crystallization behaviors between the polymorphs were made clear. © 2010 The Society of Chemical Engineers, Japan.


Nakata Y.,OHARA Pharmaceutical Co. | Kiyosawa Y.,OHARA Pharmaceutical Co. | Kagara K.,OHARA Pharmaceutical Co. | Matsuoka M.,Tokyo University of Agriculture and Technology
Organic Process Research and Development | Year: 2010

Based on our recent study on the batch crystallization of polymorphic mixture of 4-(1-(2-(3-methoxyphenethyl)phenoxy)-3-(dimethylamino) propan-2-yloxy)-4-oxobutanoic acid (MPPO), in which the polymorphic composition was found to vary with the seed composition and with the seeding temperature, and sizedependent compositions were also observed, particle size and composition distributions were measured to clarify these phenomena. The polymorphic composition of the product varied with seed size, and it was always lower than the seed composition. From the size and polymorphic distributions, as well as volume shape factors, the crystallization behaviors of the two polymorphs (Form A and Form B) were discussed, and we concluded that Form B grows faster and nucleates more easily than Form A. © 2010 American Chemical Society.


Patent
Ohara Pharmaceutical Co. | Date: 2010-08-04

It has been desired to provide a method for producing a granulated preparation capable of maintaining a stability of a chemically unstable substance in a neutral or acidic region for a long period of time with a simple and safe method in a preparation procedure, and a tablet produced by using the method.The invention provides a granulation method in which an unstable substance is successively subjected to aqueous stabilization treatment and granulation procedure. Further, it became possible to provide a tablet which is absorbed in the intestine without losing the potency in a gastric region by forming an intermediate layer on a surface of the thus obtained granule and subsequently subjecting the granule to enteric coating.

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