Sanwa Kagaku Kenkyusho Co., Ltd.

Toshiyuki Kouzaki

Makoto Sato

Masayasu Kurono

Kiichi Sawai

Yasuaki Kondo

Takahiko Mitani

Yoshiro Ishiwata

Takahito Jomori

Yuji Hayashi

Shigeaki Yoshina

Masahiro Nakajima

Hideaki Ninomiya

Syoji Yokochi

Motohiro Takeda

Mitsuhiro Makino

Tatsushi Maeda

Masaki Ando

Masanao Nakoshi

Yoko Ishihara

Fumio Higuchi

A GLP-1 derivative is provided including an amino acid sequence of GLP-1 (7-35) having deletion, substitution and/or addition of one or more amino acids and having Waa-(Xaa)n-Yaa (in which Waa is Arg or Lys, Xaa is Arg or Lys, n is an integer of 0 to 14, and Yaa is Arg, Arg-NH, Lys, Lys-NHor Hse) added to the C-terminus of the peptide having a GLP-1 activity. These derivatives are highly absorbable via a mucous membrane. The GLP-1 derivative can be conferred with resistance to dipeptidyl peptidase IV by substituting amino acid 8 in its GLP-1 amino acid sequence with Ser, or with resistance to trypsin by substituting amino acids 26 and 34 with Gln and Asn, respectively. The absorption efficiency of the GLP-1 derivatives via mucous membranes can be further improved by preparing a composition using a charge-regulated fat emulsion regulated to be negatively charged thereon.

GLP-1 derivative and preparation thereof absorbable via mucous membrane

The invention relates to a polystyrene sulfonate-containing gel preparation for therapy of hyperpotassemia, wherein the particle size of polystyrene sulfonate is controlled within the range of at least 5-100 &mgr;m, the viscosity of its solution before gelation is adjusted depending on the particle size by adding a thickening agent, and the polystyrene sulfonate particles after gelation is uniformly dispersed therein. More preferably, a water-displacing agent is contained, whereby the amount of water in the preparation is reduced. This gel preparation does not cause a sense of foreign matter or a sense of roughness in the oral cavity upon ingestion and intake, thus making it unnecessary to drink water for ingestion, and further its water content is low, so that control of water intake is made easy, even in the case of a patient with renal insufficiency who is subjecting to restriction in intake of water to significant improve the quality of life of the patient.

Polystyrene sulfonate-containing gel preparation

A pharmaceutical composition is disclosed comprising a fat emulsion containing microspheres and having its electric charge adjusted to a negative value and a biologically active substance selected from the group consisting of a basic peptide and a basic protein, which biologically active substance is adsorbed to the microspheres in the fat emulsion. An acidic phospholipid, a fatty acid, a bilic acid and a salt of such substances is preferred as an agent for adjusting the electric charge of the fat emulsion. Motilin derivatives, vasoactive intestinal polypeptide derivatives and calcitonin are preferred biologically active substances.

Pharmaceutical composition containing biologically active peptide or

There is disclosed a pharmaceutical composition of stabilized [Leu.sup.13 ]-motilin-Hse. The composition comprises at least one of organic acids and salts thereof, as a first stabilizer, and pH thereof is adjusted in a range of 5.5-8.0. The composition may contain at least one of substances selected from saccharides, amino acids, proteins and salts thereof, as a second stabilizer. Conversion of [Leu.sup.13 ]-motilin-Hse into [Leu.sup.13 ]-motilin-Hse-lactone is suppressed by increasing pH value and deamidization in asparagine residue at 19-position is suppressed by the presence of the organic acid or salt thereof.

Pharmaceutical composition of stabilized [Leu.sup.13 ]-motilin-Hse

A 3-oxygermylpropionic acid preparation is provided, which activates the action of 3-oxygermylpropionic acid having the general formula: [(O.sub.1/2).sub.3 GeCH.sub.2 CH.sub.2 COOH]n wherein n=an integer of at least 1 and is readily solubilized and disintegrated in vivo. The present preparation is manufactured by compression-molding at high pressure a composition comprising 3-oxygermylpropionic acid and two or more low-molecular substance of high solubility in water. The low-molecular substances are selected from the group consisting of white sugar, sorbitol, fructose, sucrose, glucose, lactose, mannitol and sodium chloride.

Binder-free orally administrable tablet containing 3-oxygermylpropionic

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Nagoya, Japan

Toshiyuki Kouzaki