摘要:
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.
摘要:
An optically active form of mepenzolate bromide is provided. An agent for ameliorating chronic obstructive pulmonary disease that contains the optically active form as an active ingredient and is based on a bronchodilator effect and an anti-inflammatory effect is also provided. (3R)- or (3S)-3-[(hydroxy)(diphenyl)acetoxy]-1,1-dimethylpiperidinium bromide (hereinafter referred to as "(R)- or (S)-mepenzolate bromide") is provided. An agent for ameliorating chronic obstructive pulmonary disease that contains the (R)- or (S)-mepenzolate bromide as an active ingredient is provided. Furthermore, an agent for ameliorating chronic obstructive pulmonary disease whose mode of administration is airway administration or inhalation administration is provided.
摘要:
There is provided a beraprost sodium-containing nanoparticle that contains beraprost sodium among other prostaglandin I 2 (prostacyclin) derivatives, which are therapeutic agents for pulmonary hypertension. The beraprost sodium-containing nanoparticle is obtained by making beraprost sodium hydrophobic using a metal ion and allowing the hydrophobic beraprost sodium to react with poly-L-lactic acid or a poly(L-lactic acid/glycolic acid) copolymer, and a poly-DL- or L-lactic acid-polyethylene glycol block copolymer or a poly(DL- or L-lactic acid/glycolic acid)-polyethylene glycol block copolymer. The beraprost sodium-containing nanoparticle excels in sustained release of an active ingredient, reduces a side effect, and furthermore, has an excellent drug retention in the blood. Therefore, the beraprost sodium-containing nanoparticle is quite outstanding particularly regarding the sustainability of the medicinal effect.
摘要:
An ameliorating agent for chronic obstructive pulmonary disease (COPD) containing as an active ingredient a lecithinized superoxide dismutase represented by the following general formula (I): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒSOD'(Q-B) m €ƒ€ƒ€ƒ€ƒ€ƒ(I) (in the formula SOD' represents a residue of the superoxide dismutase; Q represents a chemical crosslinking; B represents a residue without a hydrogen atom of a hydroxyl group of lysolecithin having the hydroxyl group at the 2-position of glycerol; m is the average number of bonds of lysolecithin to one molecule of superoxide dismutase and represents an integer of 1 or more). The ameliorating agent for COPD is intravenously administered or inhalation-administrated.
摘要:
This invention provides a safe and effective agent for ameliorating chronic obstructive pulmonary disease (COPD) that has both a bronchodilator effect and an anti-inflammatory effect. The agent for ameliorating chronic obstructive pulmonary disease contains mepenzolate bromide as an active ingredient. More preferably the mode of administration of the agent for ameliorating chronic obstructive pulmonary disease is airway administration or inhalation administration, and furthermore the mode of administration thereof is oral administration or rectal administration. This invention is a safe and effective agent for ameliorating chronic obstructive pulmonary disease (COPD) that has both a bronchodilator effect and an anti-inflammatory effect of mepenzolate bromide.