[EN] HIGH DRUG LOADING LIQUID ORAL PHARMACEUTICAL COMPOSITIONS<br/>[FR] COMPOSITIONS PHARMACEUTIQUES LIQUIDES À FORTE CHARGE POUR ADMINISTRATION PAR VOIE ORALE
申请人:ZYWIE LLC
公开号:WO2016154313A1
公开(公告)日:2016-09-29
A high drug loading liquid oral pharmaceutical composition comprises (i) an active pharmaceutical ingredient selected from the group consisting of a BCS Class 1 drag, a BCS Class II drug, a small molecule chaperone, and combinations thereof; (ii) at least one pharmaceutically acceptable excipient; and (iii) a diluent, wherein the active pharmaceutical ingredient is in the form, of granules having a granular core comprising from about 60 to about 97 weight percent of an active pharmaceutical ingredient and from about 3 to about 40 weight percent of the excipient, wherein the weight percent is based on the total weight of the granular core; wherein the granule core is coated with (iv) a water-soluble seal coating in an amount to provide from about 0.5 to about 5 percent weight gain, and (v) an enteric coating in an amount to provide from about 0.5 to about 50 percent weight gain. Unexpected advantages of the high drug loading oral suspension composition according to the invention include at least the following: (1) improved adsorption in the gastrointestinal tract; (2) maintain effective blood concentration over a 24 hour period; (3) reduce undesirable side effects of excipients as compared to solid dosage forms; (4) reduce the number of doses required; and (5) provide an improved taste and mouthfeel qualities.