Abstract:
PURPOSE: Provided is a process for preparing amorphous form of cefuroxime axetil, thereby producing amorphous form of cefuroxime axetil, which is excellent in elution in a living body and has stability, in high yield and purity. CONSTITUTION: The amorphous cefuroxime axetil represented by the formula(1) is manufactured by the steps of: dissolving cefuroxime axetil in a polar organic solvent; passing CO2 gas therethrough; and adding a water soluble solution containing inorganic salts to precipitate amorphous cefuroxime axetil.
Abstract:
PURPOSE: Provided is a pharmaceutical composition for intramuscular injection containing loxoprofen having excellent anti-inflammatory effects, as an active ingredient, and its pharmaceutically acceptable salts. CONSTITUTION: The pharmaceutical composition for intramuscular injection contains loxoprofen represented by the formula(1) or its pharmaceutically acceptable salts. It is manufactured by dissolving loxoprofen or its pharmaceutically acceptable salt, a stabilizing agent or solution adjuvant in water for injection then sterilizing it.
Abstract:
A method for preparing a dibenzothiepin derivative is provided to obtain the pharmaceutically active dibenzothiepin derivative with high purity and high yield through a simple process. The method for preparing a dibenzothiepin derivative represented by the formula(I) comprises the steps of: (a) reacting a propiophenone represented by the formula(II) with a halogenating agent to obtain a halo-ketone compound represented by the formula(III); (b) reacting the compound(III) with a condensing agent to obtain a cyclized halo-ketone compound represented by the formula(IV); (c) reacting the compound(IV) with an alkylorthoformate to obtain a cyclized haloacetal represented by the formula(V); (d) reacting the compound(V) with a zinc halide to obtain an ester compound represented by the formula(VI); and (e) hydrolyzing the compound(VI) to prepare the compound(I). In the formulae, X is halogen, and R1 is C1-6 alkyl, phenyl or phenyl having a substituent selected from the group consisting of H, halogen, C1-6 alkyl, and hydroxy.
Abstract:
The present invention relates to an orally administrable antimalarial combined preparation containing artemisinine or its derivatives, and pyronaridine or its salts, as active ingredients, with pharmaceutically acceptable carriers, and to preparation process thereof.
Abstract:
Disclosed is a formulation for intramuscular injection containingloxoprofen or a pharmaceutically acceptable salt thereof, having an excellent anti-inflammatory analgesic effect, as an active ingredient.
Abstract:
PURPOSE: An intermediate for preparing £2-(2,6-dichloroanilino)phenyl| acetoxyacetic acid (referred as "aceclofenac") used as an anti-inflammatory and analgesic agent, and methods for preparing aceclofenac are provided to improve production yield and purity without a process of waste heavy metal. CONSTITUTION: The intermediate which is used for preparing aceclofenac represented by the formula 1, is represented by the formula 2, wherein R1 and R2 are independent of each other and are an alkyl group of C1-C4. Aceclofenac is prepared by selectively hydrolyzing the intermediate of the formula 2 by using an acid in organic solvent. Preferably, the acid is HCl, H2SO4 or methanesulfonic acid; the solvent is alkyl acetate of C1-C5; and the reaction temperature is 20-40 deg.C. The intermediate of the formula 2 is prepared by reacting the alkali metal salt of compound of the formula 3 with the compound of the formula 4(X-CH2-COO-CH2OR¬1OR¬2) in solvent, wherein R1 and R2 are independent each other and are an alkyl group of C1-C4, and X is a halogen atom. Preferably X is Cl or Br; and the solvent is DMF or DMSO.
Abstract translation:目的:制备2-(2,6-二氯苯胺基)苯基的中间体 用作抗炎和止痛剂的乙酰氧基乙酸(称为“醋氯芬酸”),以及制备醋氯芬酸的方法,以提高生产产率和纯度,而无需重金属废物。 构成:用于制备由式1表示的醋氯芬酸的中间体由式2表示,其中R 1和R 2彼此独立并且是C 1 -C 4的烷基。 通过在有机溶剂中使用酸选择性水解式2的中间体来制备醋氯芬酸。 优选地,酸是HCl,H 2 SO 4或甲磺酸; 溶剂是C1-C5的烷基乙酸酯; 反应温度为20-40℃。 式2的中间体通过使式3的化合物的碱金属盐与式4的化合物(X-CH 2 -COO-CH 2 OR 1 OR 2)在溶剂中反应制备,其中R 1和R 2各自独立地 另外是C1-C4的烷基,X是卤素原子。 优选地,X是Cl或Br; 溶剂为DMF或DMSO。