| 摘要 |
Injectable sustained release compositions comprise an emulsion or dispersion of a pharmaceutically active ingredient dispersed in a mixture of a non-toxic film-forming material capable of gelation in the body at the injection site to form a permeable membrane enveloping the active ingredient, with a thixotropic agent, and an ion-exchange material. The active ingredient may be in finely divided solid form or dissolved or dispersed in a carrier liquid, which is preferably aqueous. The film-forming material is a vegetable oil such as castor, safflower, linseed or oiticica oil, preferably together with a proteinaceous material such as oxidised or refined gelatin, white of egg or casein, or hydrolytic or enzymatic degradation products of proteins. Gelation is produced on injection by the effects of in vivo conditions, such as oxidation, temperature, chemical action, or usually by pH change; alternatively a second injection of, for example, dilute acetic acid, may be employed to cause gelation. The thixotropic agent, which is for fluidising the composition during injection, may be finely divided silica, carboxymethyl cellulose, agar or bentonite. Ion exchange materials, which provide for slow permeation of the drug through the membrane, are suitably sulphonated styrene/divinyl benzene resins in cation form. Active ingredients may be antibiotics such as the following tetracyclines: chlor-, oxy-, brom-, 6-demethylchlor-, 6-demethyl-6-deoxy-, and 6-demethyl-6-deoxy-7-brom-tetracycline, or tetracycline itself; and also their magnesium chloride complexes; enzymes such as papain, hormones such as hydrocortisone, or prednisolone; anthelmintics; and tranquilisers such as reserpine and meclizine, salts, e.g. sodium chloride, or injectable iron compounds. Aqueous propylene glycol may be used as a liquid carrier. |
