[EN] ORALLY DELIVERED THERAPEUTICAL COMPOSITION AND USE THEREOF<br/>[FR] COMPOSITION THÉRAPEUTIQUE ADMINISTRÉE PAR VOIE ORALE ET SON UTILISATION
申请人:SHEN HAIFA
公开号:WO2021046497A2
公开(公告)日:2021-03-11
This disclosure is directed to a pharmaceutical composition comprising a bioactive agent (active pharmaceutical ingredient, API) and at least one long chain fatty acid (LCFA), wherein the long chain fatty acid can comprise a carbon chain having at least 10 carbon atoms and can comprise a free carboxylic acid group or a salt thereof. The LCFA-conjugated active pharmaceutical ingredient (API) can be resistant to acid degradation in digestive system and facilitate the delivery of the API across the small intestinal epithelial cell membrane via fatty acid transport protein 4 (FATP4, also known as SLC27A4). The pharmaceutical composition can be formulated in acid- resistant (enteric-release) dosage forms for oral administration in patients. This disclosure is further directed to a process for producing the LCFA-conjugated bioactive agent including protein, polypeptide, small molecule drugs, DNA, RNA, oligonucleotide, or a combination thereof.