For in vivo pharmacokinetic studies, mice were fasted overnight and i.p. injected with 5 mg/kg ACY-1083 dissolved in 10% dimethylacetamide (DMAC, Sigma-Aldrich, St. Louis, MO) + 10% Solutol HS 15 (BASF, Houston, TX) in saline, or 30 mg/kg ACY-1215 dissolved in 10% DMAC+ 15% Solutol HS 15 in saline. Blood and brain were collected at 5 min, 15 min, 30 min, 1 h, 4 h and 8 h post injection. Plasma was obtained by centrifugation at 2000×g for 5 min at 4 °C. Brain homogenates were obtained by homogenizing the brain in 3 volumes of PBS. Plasma and brain compound level was analyzed using liquid chromatography-tandem mass spectrometry (Waters Corporation, Milford, MA) and was calculated from standard curves of ACY-1083 and ACY-1215 in mouse plasma and brain, respectively. Pharmacokinetic parameters were calculated using WinNonlin software (Certara USA, Inc., Princeton, NJ).
Solutol hs 15
Manufactured by BASF
Sourced in Germany, United States, India, United Kingdom, China
Solutol HS 15 is a non-ionic solubilizer and emulsifier manufactured by BASF. It is a polyethylene glycol 660 12-hydroxystearate that can be used in various pharmaceutical and cosmetic applications to improve the solubility and stability of active ingredients.
Automatically generated - may contain errors
Lab products found in correlation
Labrasol, by Gattefosse (8 mentions)
Tween 80, by Merck Group (6 mentions)
Labrafil m 1944 cs, by Gattefosse (5 mentions)
Capryol 90, by Gattefosse (4 mentions)
Peceol, by Gattefosse (4 mentions)
Poloxamer 188, by BASF (4 mentions)
Transcutol hp, by Gattefosse (4 mentions)
Precirol ato 5, by Gattefosse (4 mentions)
Gelucire 44 14, by Gattefosse (4 mentions)
Cremophor rh40, by BASF (4 mentions)
Compritol 888 ato, by Gattefosse (4 mentions)
Osi 906, by BASF (3 mentions)
Poloxamer 407, by BASF (3 mentions)
Lauroglycol fcc, by Gattefosse (3 mentions)
Dspe peg2000 mal, by NOF corporation (3 mentions)
Lauroglycol 90, by Gattefosse (2 mentions)
Cremophor el, by BASF (2 mentions)
3 4 5 dimethylthiazol 2 yl 2 5 diphenyltetrazolium bromide mtt, by Merck Group (2 mentions)
Udpga, by Merck Group (2 mentions)
Alamethicin, by Merck Group (2 mentions)
66 protocols using solutol hs 15
1
Pharmacokinetic Analysis of ACY Compounds
2
OSI-906 Administration in Mice
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OSI-906 (linsitinib) was purchased from Selleck Chemicals (München, Deutschland), Chemscene (NJ, USA), and MedChem Express (NJ, USA). For the administration experiments, 8-week-old mice were orally treated with 10 μL/g of either the vehicle (30% Solutol HS-15; BASF, Ludwigshafen am Rhein, Germany) or OSI-906 (45 mg/kg) for 7 days between 7:00 P.M. and 8:00 P.M. Solutol HS-15 was dissolved in water at 30% w/v. The powder of OSI-906 was dissolved in 30% Solutol at a concentration of 4.5 mg/mL. The mice were sacrificed after 7 days of daily administration (OSI-906 or vehicle, oral gavage) or after a 7-day or 21-day withdrawal period following 7 days of administration. For the leptin injection experiments, 8-week-old mice treated with or without OSI-906 (45 mg/kg) were subcutaneously injected with PBS or leptin (Peprotech, NJ, USA) (0.5 mg/kg) twice a day for 7 days.
3
Formulation and Evaluation of Transwell Assay
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VIN was obtained from Harbin Sanlian Pharmaceutical Factory (Heilongjiang, China). Dulbecco’s Modified Eagle’s medium and Nonessential amino acids (DMEM) were purchased from GIBCO (USA). Solutol HS 15 was supplied by BASF (Ludwigshafen, Germany). Transcutol P was obtioned from Castris (Gattefosse, France). Ethyl oleate was purchased from Beijing Changcheng Chemical Ltd. (Beijing, China). Fetal bovine serum (FBS) was gained from Hycolone (USA). Penicillin, streptomycin, trysin and ethylenediaminetertraacetic acid (EDTA) were purchased from Sigma (USA). Transwell® nunclone™ was supplied by COSTAR (Camgridge, MA, USA). Eudragit L30D55 and Eudragit FS30D were obtioned from Evonik Degussa. HPMC was gained from Colorcon. Sucrose, mannitol and sodium bicarbonate?were purchased from Bodi chemical co, LTD (Tianjin, China).
Other materials were Solutol HS 15 (BASF, Ludwigshafen, Germany), Transcutol P (Castris, Gattefosse, France), ethyl oleate (Beijing Changcheng Chemical Ltd., Beijing, China), fetal bovine serum (FBS) (Hyclone, USA), Penicillin, streptomycin, trypsin, ethylenediaminetetraacetic acid (EDTA) (Sigma, USA), Transwell® nunclon™(COSTAR, Cambridge, MA, USA), Eudragit L30D55 and Eudragit FS30D (Evonik Degussa), HPMC (Colorcon), sucrose, mannitol, sodium bicarbonate (Bodi chemical co., LTD, Tianjin, China), All other reagents were of analytical grade.
Other materials were Solutol HS 15 (BASF, Ludwigshafen, Germany), Transcutol P (Castris, Gattefosse, France), ethyl oleate (Beijing Changcheng Chemical Ltd., Beijing, China), fetal bovine serum (FBS) (Hyclone, USA), Penicillin, streptomycin, trypsin, ethylenediaminetetraacetic acid (EDTA) (Sigma, USA), Transwell® nunclon™(COSTAR, Cambridge, MA, USA), Eudragit L30D55 and Eudragit FS30D (Evonik Degussa), HPMC (Colorcon), sucrose, mannitol, sodium bicarbonate (Bodi chemical co., LTD, Tianjin, China), All other reagents were of analytical grade.
4
Formulation and Evaluation of Enzalutamide Soft Capsules
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ENZ was purchased from MSN Labratories Private Ltd. (Telangana, India). The Xtandi® soft capsule, TPGS and MCT oil were supplied by Boryung Corporation (Seoul, Republic of Korea). Labrafac PG, Peceol, Labrasol, Capryol 90, Transcutol P, and Lauroglycol 90 were obtained from Gattefosse (St. Priest, France). Cremophor EL, Cremophor RH60, and Solutol HS15 were supplied by BASF (Ludwigshafen, Germany). Castor oil, coconut oil, olive oil, sesame oil, sunflower oil, corn oil, soybean oil, cotton seed oil, peanut oil, polysorbate 80, ammonium acetate, acetone, and acetonitrile were purchased from Daejung Co. Ltd. (Siheung, Republic of Korea). Sodium carboxymethyl cellulose was purchased from Duksan Pure Chemical (Ansan, Republic of Korea). All other chemicals used were of analytical grade.
5
Development of DOX·HCl Nanoformulation
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DOX·HCl was purchased from Dalian Meilun Biological Technology Co., Ltd. (Dalian, China). TPGS2000 was synthesized in our laboratory using Vitamin E succinate (VES) and polyethylene glycol (PEG) 2000 and 1-ethyl-3-(3-dimethyl aminopropyl)-1-carbodiimide hydrochloride (EDCI), 4-dimethylpyridine (DMAP), and N-hydroxysuccinimide (NHS) were purchased from Shanghai Covalent Chemistry (Shanghai, China). Succinic anhydride (SA) was procured from Aladdin Reagent Co., Ltd. (Shanghai, China). Solutol HS15 was purchased from BASF Corporation (Ludwigshafen, Germany). Triethylamine (TEA), methylene chloride, chloroform, 1,4-dioxane, and anhydrous ethers were procured from Shanghai Ling Feng Chemical Reagent Co., Ltd. (Shanghai, China). RPMI 1640 medium (with penicillin-streptomycin), trypsin, and phosphate-buffered saline (PBS) buffer were purchased from Genome Biomedical Technology Co., Ltd. (Hangzhou, China). Fetal bovine serum (FBS) was procured from Gibco (NY, USA) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) was purchased from Sigma (USA). All other reagents were of analytical grade or higher purity.
6
Pharmacokinetic Evaluation of Novel Compounds
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Example 18
Male SD rats were fasted overnight. Compounds of the invention were dissolved in dimethyl acetamide at 10 times the final concentration, then Solutol HS 15 (BASF) was added to a final concentration of 10%. Finally 80% saline was added and vortexed to achieve a clear solution. For the IV dosing three animals were injected via the foot dorsal vein with 1 mg/kg compound. For the PO dosing 5 mg/kg of compound was delivered by oral gavage. Blood was collected via the tail vein into K2EDTA tubes at 5 minutes, 15 minutes, 30 minutes, 1 hour, 2 hours, 4 hours, 8 hours and 24 hours after dosing. The blood was centrifuged at 2000 g for 5 minutes at 4° C. to obtain plasma. The plasma was extracted with acetonitrile and the level of compound was analyzed by LC/MS/MS. The level of compound in plasma was calculated from a standard curve in rat plasma. The IV clearance and area under the curve were calculated using WinNonLin software. The dose adjusted area under the curve for the IV and oral dosing were used to calculate the oral bioavailability. A summary of results is presented in Table 3.
7
Lipid-based Nanocarrier Formulation Development
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Capmul MCM was a kind gift from Abitec Corporation, USA. Miglyol 812 and Miglyol 840 were obtained from Sasol, Germany. Capryol 90 and Labrafac FCC were kind gifts from Gattefosse Pvt. Ltd., Mumbai, India. Phospholipids were obtained as kind gift samples from Lipoid, Germany. Tween 20, Tween 80 and stearylamine were obtained from S.D. Fine Chem. Ltd., Mumbai, India. Solutol HS 15 and Poloxamer 188 were obtained from BASF, Mumbai, India. MYS 40 was obtained from Nikko Chemicals Co. Ltd., Tokyo, Japan. Didodecyldimethylammonium bromide (DDAB) and Cetyltrimethylammonium bromide (CTAB) were purchased from Fluka Chemicals (New Jersey, USA). Ethanol was purchased from S.D.Fine Chem. Ltd., Mumbai, India and Glycerol from Qualigens, Mumbai, India.
8
Pharmacokinetic Evaluation of Compounds
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Example 18
Male SD rats were fasted overnight. Compounds of the invention were dissolved in dimethyl acetamide at 10 times the final concentration, then Solutol HS 15 (BASF) was added to a final concentration of 10%. Finally 80% saline was added and vortexed to achieve a clear solution. For the IV dosing three animals were injected via the foot dorsal vein with 1 mg/kg compound. For the PO dosing 5 mg/kg of compound was delivered by oral gavage. Blood was collected via the tail vein into K2EDTA tubes at 5 minutes, 15 minutes, 30 minutes, 1 hour, 2 hours, 4 hours, 8 hours and 24 hours after dosing. The blood was centrifuged at 2000 g for 5 minutes at 4° C. to obtain plasma. The plasma was extracted with acetonitrile and the level of compound was analyzed by LC/MS/MS. The level of compound in plasma was calculated from a standard curve in rat plasma. The IV clearance and area under the curve were calculated using WinNonLin software. The dose adjusted area under the curve for the IV and oral dosing were used to calculate the oral bioavailability. A summary of results is presented in Table 3.
9
Adora2b Deficiency and DSS-Induced Colitis
10
Synthesis and Characterization of Potential Bioactive Compounds
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