| 摘要 |
The invention comprises O-acetyl-N-3, 5-dimethyl benzheparide, or the O-acetyl derivative of the N-3, 5-dimethylbenzoate of heparamine (Specification 863,235). The compound is preferably at least 70% acetylated and may be in the form of a non-toxic salt e.g. sodium or potassium salt. The compound is made by reaction of the N-3, 5-dimethylbenzoate of heparamine (N-3, 5-dimethyl-benzheparide) with acetic anhydride, e.g. at 10 DEG C.-25 DEG C. in a pyridine-formamide medium. In examples, the sodium salt of N-3, 5 dimethylbenzheparide is O-acetylated, the product is converted to free acid form by treatment with cation exchange resin and thence to the potassium salt by neutralisation with potassium hydroxide. O-acetyl-N-3, 5-dimethylbenzheparide possesses anticoagulant and antilipaemic activity and may be used in pharmaceutical compositions in conjunction with a carrier.ALSO:Pharmaceutical compositions having anticoagulant and antilipaemic activity contain a carrier and O - acetyl - N - 3,5 - dimethylbenz heparide (the O-acetyl derivative of the N-3,5-dimethylbnezoate of heparamine, see Specification 863,235), or non-toxic salts thereof. The compositions may be formed as powders, granules or tablets for oral administration in suspension in water, syrup, or oil or oil/water emulsion. The compound may also be administered parenterally in a sterile aqueous or non-aqueous injection solution or suspension. |
