Issue link: https://www.e-digitaleditions.com/i/238663
c-Kheurart_10-15_Masters 12/30/13 1:55 PM Page 12 Tablets & Capsules 12 January 2014 sidered a key ingredient for emulsification and potential bioavailability enhancement. Two SELF preparations (27F and 27H) were also selected to assess in vitro dissolution. Stage 4: Manufacture of prototype batches. Four excipient combinations (lots 1 through 4) were used to formulate LFHC prototypes (Table 3). These prototypes were manufactured with the required target dose in batches of 1,500 capsules, but the capsules were not banded and thus not completely sealed. The butylated hydroxyanisole (BHA) and butylated hydroxytoluene Table 1 Excipients evaluated at elevated temperature Gelucire 44/14 Cremophor RH 4 PEG 8000 Schercemol TN Transcutol Captex 200P Lauroglycol 90 Miglyol 812 Softigen 701 Akomed R S.E.L.F. 27D** Crillet 1 HP Propylene glycol Labrafil M2125 Labrafac CC Soybean oil Capmul MCM Labrafac Hydro WL 1219 Miglyol 840 Imwitor 742 Myvacet 9-45K S.E.L.F. 27E** Labrasol PEG 400 Vitamin E TPGS Polysorbate 80 Glycerin Capmul PG-8 Labrafac PG Capryol 90 Imwitor 988 S.E.L.F. 27A* S.E.L.F. 27F** Plurol Oleique CC 497 Peppermint oil Cremophor ELP Macol LA 4 Sunflower oil Bio-Soft N25-7 Miglyol 829 Cottonseed oil Imwitor 491 S.E.L.F. 27B* S.E.L.F. 27G* Solutol HS 15 Miglyol 810 Medium-chain triglycerides Gelucire 50/13 Captex 355 Neobee M-5 Softisan 645 Imwitor 308 Hexylene glycol S.E.L.F. 27C** S.E.L.F. 27H** * Semisolid at room temperature ** Liquid at room temperature Table 2 Excipient mixtures used to evaluate solubility at elevated temperature Serial number Excipients Proportion 1 2 3 4 5 6 7 8 9 10 1 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 Citric acid (1.0%) + HPBCD* (20% solution in water) Propylene glycol + HPBCD Propylene glycol + citric acid + HPBCD Glycerin + HPBCD Glycerin + citric acid + HPBCD Transcutol HP + HPBCD Transcutol HP + citric acid + HPBCD Cremophor ELP + Transcutol HP Cremophor ELP + propylene glycol Transcutol HP + propylene glycol Propylene glycol + polyethylene glycol 8000 + Transcutol HP Propylene glycol + glycerin + Transcutol HP Transcutol HP + hexylene glycol Gelucire 44/14 + Transcutol HP + propylene glycol Cremophor ELP + PEG 8000 Cremophor ELP + propylene glycol + HPBCD Capmul MCM + Cremophor ELP Capmul MCM + Cremophor RH 40 Captisol + Cremophor ELP + PEG 8000 Captisol + Cremophor ELP + propylene glycol Cremophor ELP + propylene glycol + Imwitor 308 Cremophor ELP + Transcutol HP + Imwitor 308 Cremophor ELP + propylene glycol + Imwitor 308 Propylene glycol + Transcutol + Imwitor 308 Gelucire 44/14 + propylene glycol + Imwitor 308 Gelucire 44/14 + Cremophor ELP Myvacet 9-45K + Lauroglycol + Labrasol 1.0 ml + 3.5 ml 2.250 g + 2.250 g 3.000 g + 0.045 g + 1.455 g 3.500 g + 1.000 g 3.455 g + 0.045 g + 1.000 g 3.500 g + 1.000 g 3.455 g + 0.04 5g + 1.000 g 1.000 g + 3.500 g 1.000 g + 3.500 g 2.250 g + 2.250 g 2.000g + 0.450 g + 2.000 g 2.000 g + 0.750 g + 1.750 g 3.000 g + 1.500 g 1.500 g + 1.500 g + 1.500 g 2.750 g + 1.750 g 2.000 g + 1.000 g+ 1.500 g 1.000 g + 3.500 g 1.500 g + 3.000 g 1.000 g + 2.750 g + 0.750 g 1.000 g + 2.000 g + 1.5000 g 1.350 g + 0.900 g + 2.250 g 0.900 g + 0.450 g + 3.150 g 1.125 g + 0.675 g + 2.250 g 0.900 g + 0.900 g + 2.700 g 0.675 g + 0.675 g + 3.150 g 2.250 g + 2.250 g 2.250 g + 0.450 g + 1.800 g * HPBCD = hydroxypropyl-beta-cyclodextrin