PC-SOD

Modified biologically active protein.（EP0406804）

A modified biologically active protein consisting essentially of a biologically active protein bonded to lecithin via a chemical linkage.

LECITHINIZED SUPEROXIDE DISMUTASE AND THE DRUG CONTAINING IT AS AN ACTIVE INGREDIENT（JP3857338）

DRUG COMPOSITION CONTAINING LECITHIN-MODIFIED SUPEROXIDE DISMUTASE （EP1188445）

A drug composition comprising a lecithin-modified superoxide dismutase (PC-SOD) represented by the general formula (I)SOD'(Q-B)m and a drug carrier and exhibiting specific properties, stability and so on: (I)(wherein SOD' is a superoxide dismutase residue; Q is a chemical crosslinkage; B is a residue obtained by freeing a lysolecithin having hydroxyl at the 2-position of glycerol from the hydroxyl hydrogen; and m is a positive number of 1 or above). This composition is little lowered in the activity of PC-SOD even after long-term storage by virtue of the action of sucrose in the composition, gives freeze-dried products having good properties, and is suppressed in the appearance of peaks assignable to analogues in column chromatography, thus being useful as the ingredient of drugs.

LECITHINIZED SUPEROXIDE DISMUTASE COMPOSITION AND PROCESS FOR PRODUCING THE SAME（WO2006040980）

A lecithinized superoxide dismutase (PC-SOD) composition useful as a base for medicines. The composition comprises PC-SOD's which are obtained by replacing one or more of the amino groups of a specific SOD with a lecithin residue represented by the following general formula (I) and which comprise, as main components, PC-SOD's(A) in which m amino groups [m is an integer of 1-4 and the average of m is 1.5-2.4] have been replaced with the lecithin residue, the PC-SOD's(A) comprising PC-SOD(a1) in which m=1, PC-SOD(a2) in which m=2, PC-SOD(a3) in which m=3, and PC-SOD(a4) in which m=4.

THERAPEUTIC AGENT FOR INTERSTITIAL PNEUMONIA（WO2008075706）

Disclosed is a therapeutic agent for interstitial pneumonia, which ensures to exert the effect of superoxide dismutase (SOD) contained therein. Specifically disclosed is a therapeutic agent for interstitial pneumonia, which comprises 10 to 100 mg of lecithin-conjugated superoxide dismutase represented by the general formula (I), which further comprises sucrose for the purpose of increasing its stability, and which has a dosage form suitable for intravenous administration. SOD'(Q-B)m (I) wherein SOD' represents a residue of superoxide dismutase; Q represents a chemical crosslink; B represents a residue produced by removing a hydrogen atom from a hydroxy group in lysolecithin which has the hydroxy group at position-2 of a glycerol moiety therein; and m represents an average number of lysolecithin molecules bound to one superoxide dismutase molecule and is an integer of 1 or greater.

AS-013

Emulsion of lipid containing a prostaglandin analogue.（EP0423697）

An emulsion of lipid containing a prostaglandin analogue of the formula (1): <CHEM> wherein R<1> is an alkanoyl group, R<2> is a hydrogen atom or an alkyl group, each of R<3> and R<4> is a hydrogen atom or a protective group for an alcohol, R<5> is an alkyl group which may have a substituent, and ---- is a single bond or a double bond.

Prostaglandin analogue（JP2849608）

Process for producing a purified prostaglandin derivative（US6632958）

An alkene (1) is added to cyclopentenone (2) under the action of an alkyl lithium and an organic copper reagent to form an adduct, said adduct is reacted with e.g. a carboxylic anhydride (4) to obtain a prostaglandin derivative (6), which is then treated with a nitrogen-containing compound such as 2,2'-bipyridyl to efficiently remove the organic copper reagent used in the synthesis and by-products derived from said reagent, to obtain a purified prostaglandin derivative (6) having a high purity:

Nano steroid・Nano PGE1

NANOPARTICLE CONTAINING WATER-SOLUBLE NON-PEPTIDIC LOW MOLECULAR WEIGHT SUBSTANCE（WO2007074604）

Disclosed is a nanoparticle containing a water-soluble non-peptidic low molecular weight substance, which is excellent in targeting of the substance to an affected part and sustained release of the substance and shows a reduced accumulation of the substance in the liver. The nanoparticle can be prepared by hydrophobizing a water-soluble non-peptidic low molecular weight substance with a metal ion and then reacting the hydrophobized substance with a polylactic acid-polyethylene glycol block copolymer or a poly(lactic acid/glycolic acid)-polyethylene glycol block copolymer.

G-CSF

ZINC-CONTAINING SUSTAINED-RELEASE COMPOSITION, ITS PREPARATION, AND METHOD FOR PRODUCING THE SAME（WO2004096179）

With a simple and high-yield production method, a zinc-containing sustained-release composition capable of stabilizing a physiologically active protein or peptide, typically G-CSF by precipitation and retaining drug efficacy for several days in a living body owing to its sustained releasability is provided.
Concretely, a zinc-containing sustained-release composition produced by forming a precipitate by mixing a physiologically active protein or peptide, a water-soluble zinc salt, a water-soluble carbonate and/or a water soluble phosphate aqueous solution.
The zinc-containing sustained-release composition may be administered as a zinc-containing sustained preparation by adding a pharmaceutically acceptable additive as is necessary.

Nano particle technology

SUSTAINED-RELEASE COMPOSITION, PROCESS FOR PRODUCING THE SAME AND PREPARATION THEREOF（EP1514538）

The present invention provides a sustained-release composition by which a sustained-release effect can be obtained for a long time when injecting microparticles of the composition in an amount that can be subcutaneously or intramuscularly injected to a human with ease and without pain. The composition comprises porous hydroxyapatite microparticles having pores embolized by filling the pores in the microparticles with a biologically active drug, a human serum protein, and a mucopolysaccharide, and adding a divalent metal ion. Alternatively, the composition comprises porous hydroxyapatite microparticles having pores embolized in the outer layer by filling the pores in the microparticles with a biologically active drug, a human serum protein, and a water-soluble calcium salt one after another or at one time, and then adding sodium carbonate, sodium hydrogen carbonate, or an aqueous carbonate ion solution.

DRUG-CONTAINING SUSTAINED RELEASE MICROPARTICLE, PROCESS FOR PRODUCING THE SAME AND PREPARATION CONTAINING THE MICROPARTICLE （WO2004112751）

Sustained release microparticles suitable for various types of drugs, or drug-containing sustained release microparticles capable of sustained release of drugs over a period of three days or more and capable of, with respect to highly water-soluble drugs as well, inhibiting initial burst release; a process for producing the same; and preparations containing the microparticles. In particular, the drug-containing sustained release microparticles comprise a drug other than human growth hormone and a porous apatite derivative, or comprise a drug other than human growth hormone, a porous apatite derivative and a water-soluble bivalent metal compound. The drug-containing sustained release microparticles can be produced by dispersing under agitation microparticles of a porous apatite derivative in an aqueous solution containing a drug so that the aqueous solution infiltrates in the porous apatite derivative; adding thereto an aqueous solution containing a water-soluble bivalent metal compound so that the water-soluble bivalent metal compound infiltrates in the porous apatite derivative; further adding additives such as a stabilizer to the mixture; and effecting lyophilization or vacuum drying.

DRUG-CONTAINING NANOPARTICLE, PROCESS FOR PRODUCING THE SAME AND PARENTERALLY ADMINISTERED PREPARATION FROM THE NANOPARTICLE（WO2005060935）

An external preparation or injectable solution that exerts the effect of enabling percutaneous or transmucous in vivo absorption of fat-soluble drugs and water-soluble drugs not having been satisfactorily attained hitherto and that contains a highly absorbable fat-soluble/water-soluble drug. The injectable solution especially aims at sustained release and target effects. In particular, drug-containing nanoparticles (secondary nanoparticles) are provided by causing primary nanoparticles containing a fat-soluble drug or fat-solubilized water-soluble drug to act with a divalent or trivalent metal salt. Further, drug-containing nanoparticles (tertiary nanoparticles) are provided by first causing primary nanoparticles containing a fat-soluble drug or fat-solubilized water-soluble drug to act with a divalent or trivalent metal salt to thereby obtain secondary nanoparticles and thereafter causing a monovalent to trivalent basic salt to act on the secondary nanoparticles. Still further, there are provided a process for producing these nanoparticles, and a percutaneous or transmucous external preparation or injectable solution in which these nanoparticles are contained.

Others

METHOD OF SCREENING COMPOUND SAFE TO GASTRIC MUCOSA（WO2005073718）

A screening method for selecting a compound being safe to gastric mucosa and having less side effect of gastrointestinal tract lesion or a salt thereof, especially a nonsteroidal antiinflammatory compound or a salt thereof. There is provided a method of screening a compound safe to gastric mucosa, especially a nonsteroidal antiinflammatory compound, characterized in that using a liposome having a fluorescent dye, especially calcein, sealed therein and having a cell membrane model constituted of a phospholipid, such as phosphatidylcholine, phosphatidylglycerol, phosphatidylserine or phosphatidylinositol, the liposome is reacted with a test compound and thereafter the degree of leakage of fluorescent dye from the liposome is estimated.

TABLET MAKING MORTAR OR PESTLE（EP1882468）

An object of the invention is to provide a punch or die for tabletting to be excellent durability and releasability. When a coating layer is provided on a surface, the coating layer is yet securely prevented from detachment. In the punch or die for tabletting, the tablet-forming surface layer 5 contains a base metal and a hardening metal in a fused state which is different from the base metal, and a hardening metal content is incremental from the base metal toward the tablet-forming surface layer 5. The hardening metal contains at least any one of W, C, B, Ti, N, and Cr. Furthermore, in the punch or die for tabletting, the tablet-forming surface layer 5 ranges between 0.1 [mu]m and 5 [mu]m in terms of arithmetical mean roughness Ra of the surface.

METAL SURFACE TREATMENT METHOD（WO2008090662）

[PROBLEMS] To reliably bond various metals onto a surface of various parent metals in an alloyed state in a simple, easy and efficient manner. [MEANS FOR SOLVING PROBLEMS] A metal surface treatment method comprising a shot peening step of shot peening dissimilar metal particles (2), which are different from a parent metal (1), on the surface of the parent metal (1) to provide a dissimilar metal film (3) on the surface of the parent metal (1), and an electron beam irradiation step of applying electron beams (4) to the surface of the parent metal (1) with the dissimilar metal film (3) provided thereon by the shot peening step to bond the dissimilar metal film (3) and the parent metal (1).

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