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6 protocols using pharmacoat 603

1

Glimepiride Nanosuspension Stabilization

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Glimepiride (Actavis, Leskovac, Serbia, chemical structure shown in Figure 1), was used as a poorly soluble drug. Two grades of hydroxypropyl cellulose-HPC-SL and HPC-L (Nisso HPC, Nippon Soda Co., Tokyo, Japan) and hypromellose (HPMC)-Pharmacoat® 603 and Pharmacoat® 615 (Shin-Etsu Chemical Co., Ltd., Tokyo, Japan), differing in viscosity, poloxamer 188 (Kolliphor™ P 188 micro, BASF, Ludwigshafen, Germany), polyvinylpyrrolidone K25 (PVP K25-Kollidon® 25, BASF, Ludwigshafen, Germany) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®, BASF, Ludwigshafen, Germany) were tested as potential nanosuspension stabilizers. Mannitol (Pearlitol® 160 C, Roquette Frères, Lestrem, France) was used as a matrix former for spray drying of the nanosuspension in order to prevent aggregation of glimepiride nanocrystals during solidification process.
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2

Bisacodyl Formulation Development

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Bisacodyl (0.999 in mass fraction purity) was kindly provided by Dong-A ST Co., Ltd. (Seoul, Republic of Korea). Hydroxypropyl cellulose (HPC, SSL grade) was obtained from Nippon Soda Co., Ltd. (Tokyo, Japan). Hydroxypropyl methylcellulose (HPMC, Pharmacoat® 603), hydroxypropyl methylcellulose acetate succinate (HPMCAS, AQOAT® MG), and hydroxypropyl methylcellulose phthalate (HPMCP, HP-50) were acquired from Shin-Etsu Chemical Co., Ltd. (Tokyo, Japan). Polyvinylpyrrolidone K12 (PVP K12, Kollidon® K12), polyvinylpyrrolidone vinyl acetate copolymer (PVP VA64, Kollidon® VA64), and polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer (Soluplus®) were supplied by BASF Co., Ltd. (Ludwigshafen, Germany). Ultrapure water was obtained using the Milli-Q purification system (Millipore, Molsheim, France). Other chemicals and solvents used in this study were of high-performance liquid chromatography (HPLC) or reagent grade.
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3

Film-Forming Polymer Characterization

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SA (AppliChem GmbH, Darmstadt, Germany) (10,000–600,000 g/mol) and HPMC (Pharmacoat® 603, Shin Etsu Chemical Co., Ltd., Tokyo, Japan) were used as a film-forming agent in the polymer film. GLY 85% (w/w %) was added to the film as a plasticizer [Ph. Eur. 8.], CTZ [Ph. Eur. 8.], which was a gift from ExtractumPharma Pharmaceutical Manufacturing, Marketing and Consulting Inc, Kunfehértó, Hungary was the API in the polymer film. Mucin (Carl Roth GmbH + Co. KG, Karlsruhe, Germany) (10 w/w %) dispersion was used in the in vitro mucoadhesion test. Diiodomethane was used in the surface free energy measurement.
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4

Metformin Quasi-Emulsion Tablet Formulation

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Metformin hydrochloride (MF, Auro Laboratories Ltd., Mumbai, India) was dissolved in demineralized water and crystallized in technical-grade acetone (density used for calculations: 0.784 g/mL at 25 °C [14 (link)]). Two types of hypromellose (HPMC, Pharmacoat® 603, Shin-Etsu Chemical Co., Ltd., Tokyo, Japan, and Methocel™ K4M, Colorcon, Dartford, UK) were used as polymeric stabilizers of the quasi-emulsion.
For tableting, hyprolose (HPC SSL SFP, Nippon Soda, Tokyo, Japan) was used as a dry binder, and magnesium stearate (Parteck® LUB MST, Merck KGaA, Darmstadt, Germany) as a lubricant.
Caffeine (BASF, Ludwigshafen, Germany) was used as a tracer, to determine the residence time distribution.
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5

Formulation and Characterization of Losartan Potassium Tablets

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Losartan potassium (Form I, Dr. Reddy’s Laboratories, Jinnaram Mandal, Telangana, India), silicified microcrystalline cellulose (PROSOLV® SMCC 50, JRS Pharma, Rosenberg, Germany), copovidone (Kollidon® VA 64 (Fine), BASF Pharma, Ludwigshafen, Germany), crospovidone (Kollidon® CL, BASF, Ludwigshafen, Germany), dicalciumphosphate anhydrous (DI-CAFOS® A 150, Chemische Fabrik Budenheim, Budenheim, Germany), lactose (Tablettose® 80, Flowlac® 100, MEGGLE, Wasserburg am Inn, Germany), isomalt (galenIQTM 721, BENEO-Palatinit, Mannheim, Germany), microcrystalline cellulose (VIVAPUR® 102, JRS Pharma, Rosenberg, Germany), Ludipress® (BASF Pharma, Ludwigshafen, Germany), magnesium stearate (Parteck® LUB MST, Merck, Darmstadt, Germany), sodium stearyl fumarate (PRUV®, JRS Pharma, Rosenberg, Germany), talc (Talkum® Pharma G, C.H. Erbslöh, Krefeld, Germany), HPMC (PHARMACOAT® 603, Shin-Etsu Chemical, Tokyo, Japan), macrogol (PEG 6000, BASF Pharma, Ludwigshafen, Germany), methanol (HPLC grade, VWR Chemicals, Radnor, PA, USA), acetonitrile (HPLC grade, Honeywell, Charlotte, NC, USA), phosphoric acid (Merck, Darmstadt, Germany), monobasic potassium phosphate (Fisher Scientific, Waltham, MA, USA), disodium hydrogen phosphate anhydrous (AppliChem, Darmstadt, Germany), and sodium hydroxide solution 1 N (Merck, Darmstadt, Germany) were used.
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6

Polymer Film for Enhanced Mucoadhesion and Permeation

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Sodium alginate (SA) (Biochemica GmbH, Darmstadt, Germany) (10,000–600,000 g/mol) and hydroxy methylcellulose (HPMC) (Pharmacoat® 603, Shin Etsu Chemical Co., Ltd., Tokyo, Japan) were used as film-forming agents in the polymer film. Glycerol (GLY) 85% (w/w %) was added to the film as a plasticizer (Ph. Eur.8.). Citric acid (CA) (Ph. Eur. 8.) was incorporated in the polymer film system as a permeation enhancer. Cetirizine dihydrochloride (CTZ) (Ph. Eur. 8.) was the API, which was a gift from ExtractumPharma Pharmaceutical Manufacturing, Marketing and Consulting Inc., Kunfehértó, Hungary. Mucin (Carl Roth GmbH + Co. KG, Karlsruhe, Germany) (10 w/w %) dispersion was used in the in vitro mucoadhesion test.
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