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Dpp iv inhibitor formulations
专利权人:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人:
KOHLRAUSCH ANJA,ROMER PATRICK,SEIFFERT GERD
申请号:
NZ61342607
公开号:
NZ613426A
申请日:
2007.04.30
申请国别(地区):
NZ
年份:
2015
代理人:
摘要:
Disclosed is a process for the preparation of a solid pharmaceutical composition comprising 0.5 mg to 10 mg of a DPP IV inhibitor active ingredient or a salt thereof, a first diluent, a second diluent, a binder, a disintegrant and a lubricant said process comprising: a) dissolving a binder in a solvent to produce a granulation liquid b) blending a DPP-IV inhibitor, a first and second diluent, and a disintegrant to produce a pre-mix c) moistening the pre-mix with the granulation liquid and subsequently granulating the moistened pre-mix d) optionally sieving the granulated pre-mix through a sieve with a mesh size of at least 1.0 mm e) drying the granulate at about 40-75°C until the desired loss on drying value in the range of 1-5 % is obtained f) delumping the dried granulate and g) adding lubricant to the granulate for final blending wherein the diluents are selected from cellulose powder, dibasic calciumphosphate anhydrous, dibasic calciumphosphate dihydrate, erythritol, low substituted hydroxypropyl cellulose, mannitol, pregelatinized starch and xylitol the binder is selected from copovidone (copolymerisates of vinylpyrrolidon with other vinylderivates), hydroxypropyl methylcellulose (HPMC), hydroxypropylcellulose (HPC), polyvinylpyrrolidon (povidone), pregelatinized starch, or low-substituted hydroxypropylcellulose (L-HPC) the disintegrant is selected from corn starch, crospovidone, low-substituted hydroxypropylcellulose (L-HPC) or pregelatinized starch and the lubricant is selected from talc, polyethyleneglycol, calcium behenate, calcium stearate, hydrogenated castor oil or magnesium stearate and wherein the DPP IV inhibitor is selected from a compound such as 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-aminopiperidin-1-yl)-xanthine (linagliptin).
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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