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78 protocols using cremophor rh40

1

Abuse-Resistant Opioid Formulations

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Example 2

Abuse-resistant formulations are prepared, using the ingredients listed in Table 6 below.

TABLE 6
Abuse-resistant formulations
mg/Capsule
Ingredient2A2B2C
Oxycodone (Pharmaceutically10
Active Agent)
Oxymorphone (Pharmaceutically10
Active Agent)
Hydrocodone (Pharmaceutically10
Active Agent)
α-Tocopherol (Antioxidant)1.51.51.5
PEG-40 hydrogenated castor10-2510-2510-25
oil* (Surfactant)
PEG-14M** (Viscosity-202020
building polymer)
PEG-400 (Co-solvent)505050
Glyceryl monocaprylate†q.s.q.s.q.s. to
(organic vehicle)to 400to 400400
*e.g., CREMOPHOR RH-40, a product of BASF.
**e.g., POLYOX WSR-205, a product of The Dow Chemical Co.
†e.g., CAPMUL MCM C8, a product of ABITEC.

The formulations are prepared by combining PEG-400 and glyceryl monocaprylate with mixing at 50-60° C., dissolving α-tocopherol in the mixture at the same temperature, and then dissolving the drug and PEG-40 hydrogenated castor oil while maintaining the temperature. The mixture is then cooled to ambient temperature, and then PEG-14M is dispersed in the mixture. The final mixture was filled into capsules.

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2

Formulation and Evaluation of Glibenclamide Solid Dosage Forms

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Glibenclamide was obtained from Mahban Chemi Co. (Tehran, Iran). Coarse granular microcrystalline cellulose (Avicel) (Mingtai Chemical, Bah-Dern City, Taiwan), sodium starch glycolate (Yung Zip Chemical, Taichung City, Taiwan), nm-sized amorphous silicon dioxide (Mingtai Chemical, Bah-Der City, Taiwan), Polyoxyethylene (40) Stearate (MYRJ 52) (Croda, Trappes, France), polyvinylpyrrolidone (PVP) and Cremophor® RH 40 (BASF, Germany), polyethylene glycol (PEG 200 and 400), glycerine, propylene glycol (PG), polyoxyethylenlaurylether (Brij35), lactose monohydrate (Pharmaceutical grade), sodium hydroxide and potassium dihydrogen phosphate were obtained from Merck, (Darmstadt, Germany). Diethylene glycol monoethyl ether (transcutol P) was supplied by Gattefosse (Lyon, France).
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3

Cellular Uptake Mechanisms of Pharmaceutical Compounds

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LA and RAN (purity >98%, each) were purchased from Shaanxi Chenguang Pharmaceutical Co., Ltd. (Xi’an, China). AS was purchased from Shaanxi Minsheng Medicine Co., Ltd. (Xi’an, China). Caprylocaproyl macrogol-8 glycerides (Labrasol®) and glyceryl palmitostearate (Precirol® ATO 5) were provided by Gattefossé (Montesquieu, France). Polyoxyl castor oil (Cremophor® RH40) was obtained from BASF (Ludwigshafen, Germany). High-glucose Dulbecco’s modified Eagle medium (DMEM-high) was obtained from Thermo Fisher Scientific (Waltham, MA, USA). Trypsin (0.25%), 0.02% ethylenediaminetetraacetic acid (EDTA), fetal calf serum (FCS), 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT), and phosphate-buffered saline (PBS) were obtained from Shanghai Usen Biotechnology (Shanghai, China). Filipin III, genistein, cytochalasin D, 5-(N,N-dimethyl)-amiloride hydrochloride, monensin sodium, Lyso-Tracker® Red DND-99, and Hoechst33258 stain were purchased from Santa Cruz Biotechnology, Inc. (Santa Cruz, CA, USA). Sodium azide was obtained from Beijing Bei-na Kai-chuang Biotech Co., Ltd (Beijing, China), and chlorpromazine hydrochloride was obtained from Aladdin Industrial Inc. (Shanghai, China). All other chemicals were obtained from Sinopharm Chemical Reagent (Shanghai, China) and were of high-performance liquid chromatography (HPLC) or analytical grade.
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4

Extraction and Formulation of Bioactive Compounds

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Kaempferol (³ 97.0 %) and quercetin (pharmaceutical secondary standard) were purchased from Sigma-Aldrich (Singapore). Crodamol TM PC (propylene glycol dicaprylocaprate) was acquired from Croda (Spain). Tween ® 80 (polysorbate 80, polyoxyethylene sorbitan monooleate) and polyethylene glycol 400 (PEG 400) were purchased from B.L. Hua & Co. Ltd. (Thailand). Cremophor ® RH 40 (PEG-40 hydrogenated castor oil) was purchased from BASF (Germany). Acetonitrile (high-performance liquid chromatography [HPLC] grade) was purchased from RCI Labscan (Thailand). All other chemicals were of analytical grade. M. oleifera leaf powder was purchased from Lopburi province, Thailand.
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5

Propolis Extract Formulation with Surfactants

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Propolis extract diluted in water was solubilized in hydrogenated castor oil (Cremophor-RH 40, Basf Latin America, São Paulo, Brazil). Subsequently, the anionic surfactant sodium PEG-7 olive oil carboxylate (5%-Olivem 400, The Hallstar, Chicago, IL, USA) was added to the formulation. Finally, a 5% EDTA solution was added to the final formulation.
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6

Huperzine A Formulation Development and Characterization

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Huperzine A (purity 99%) was purchased from Wanbangde Pharmaceutical Group Co., Ltd. (Zhejiang, China). Diphenhydramine hydrochloride (Lot No. 100066–200807) was purchased from the National Institutes for Food and Drug Control (Beijing, China). Propylene glycol was obtained from Tianjin Damao Chemical Reagent Factory (Tianjin, China). Polyoxyl 40 hydrogenated castor oil (Cremophor RH40®) was purchased from BASF, Germany. Castor oil was obtained from Sinopharm Group Chemical Reagent Co., Ltd. (Shanghai, China). Cycloheximide was purchased from Sigma Chemical Co. (St. Louis, MO, USA). Acetonitrile and methanol were HPLC grade and were supplied by the Oceanpak Alexative Chemical Co., Ltd. (Gothenburg, Sweden). Pure water was prepared by the Milli-Q Ultrapure water purification system (Millipore, Bedford, MA, USA). All other chemicals used in this study were analytical grade.
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7

Lipid-Based Nanocarrier Formulation

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JIB-04 was a generous gift from Assoc. Prof. PhD Elisabeth Martinez from Department of Pharmacology, University of Texas Southwestern Medical Center, USA. Solid lipids -Precirol ATO 5 and Compritol 888 ATO were gifts from Gattefossé (France). Surfactants -Kolliphor RH 40 (Cremophor RH 40, KRH40) was a gift from BASF (Germany) and Span 80 (S80) was purchased from Sigma-Aldrich (Germany). Propylene glycol (PG) was used as a co-surfactant and acquired from Merck (Germany). Cationic lipids -1,2-di-O-octadecenyl-3-trimethylammonium propane (chloride salt) (DOTMA) was purchased from Avanti Polar Lipids (USA) and dimethyldioctadecylammonium bromide (DDAB) from Tokyo Chemical Industry (Japan).
Standard ultra-pure water (upH2O) was used in all formulations.
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8

Curcumin and Thymoquinone Formulation

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Curcumin (CUR, 99.5% pure) was purchased from Enzo life Sciences, (Lausen, Switzerland) and THQ (purity >99.8%) from Sigma Aldrich Company St Louis, MO, USA. Sodium chloride (NaCl), and Hydrochloric acid (HCl) were obtained from (BDH laboratories Ltd. UK). The high purity water was obtained through a Milli-Q Integral Water Purification System (Millipore, Bedford, MA). Imwitor 988 (I988, medium chain mono- and diglycerides), and HCO40 (PEG-40-hydrogenated castor oil) were obtained as gift from Nikko Chemicals Co. (Tokyo, Japan). Black seed oil (BSO) was collected directly from naturally obtained Nigella Sativa seeds by cold pressing (100% pure, no added solvents). The amount of thymoquinone was available in the BSO depending on the ratio used in the formulations. CrEL (Cremophor EL), and CrRH40 (Cremophor RH40) were purchased from BASF, Germany. Transcutol P (TcP) was kindly supplied by Gattefossé, France. Neusilin® US2 grade substance as adsorbent (fine powder of Magnesium Alumino Metasilicate) was obtained from Fuji Chemical Industry, Japan. Another adsorbent Syloid® 244 FP silica material was purchased from W. R. Grace & Co., USA. All other chemicals and solvents used in the studies were analytically pure and or HPLC grade, respectively.
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9

Cycloheximide and STA-9090 in vivo study

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Cycloheximide (CHX) and STA-9090 were obtained from Selleck Chemicals. Stock solutions of CHX (10mmol/L) and STA-9090 (10mmol/L) were stored at −20°C. For in vivo studies, STA-9090 (5mg/mL) was diluted with 10% DMSO, 18% Cremophor RH 40 (BASF), 3.6% dextrose (Sigma, St. Louis, MO, USA) and 68.4% water. STA-9090 treatments of mice with STA-9090 were carried out by intraperitoneal injection at the dose of 25mg/kg/d every 3 days, totaling 7 injections.
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10

Optimization of Cholesterol-Based Nanoparticles

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DCN was a kind gift from EVA Pharmaceutical Industries (Cairo, Egypt). Cholesterol (CH), Span 60 (sorbitan monostearate), Brij S2 (polyoxyethylene (2) stearyl ether), Brij C10 (polyoxyethylene (10) cetyl ether), and acetonitrile (HPLC grade) were purchased from Sigma Chemical Co. (St. Louis, MO). Sodium taurocholate (STC), Cremophor EL, and Cremophor RH 40 were acquired from BASF Co. (Florham Park, NJ). Methanol, chloroform, disodium hydrogen phosphate, potassium dihydrogen phosphate, and sodium chloride were purchased from El-Nasr Pharmaceutical Chemicals Co. (Abu-Zaabal, Cairo, Egypt). All other reagents were of analytical grade and were used as received.
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