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. a process for making an electrospun pharmaceutical composition comprising a pharmaceutically acceptable active agent which agent is sparingly water soluble or water insoluble, and a pharmaceutically acceptable polymeric carrier, which process comprises.[0085] in a preferred embodiment of the invention for water insoluble agents, is the active nabumetone, electrospun in w/w % ranges from 0 to 82%, with 200k, 400k, 900k and 2000k polyox, and tween 80, sds, pluronic f68, or tpgs. the mixture was left shaking in a water bath at 37 c.[0089] a stock solution of 30% polyethylene oxide (molecular weight 400k, aldrich) was prepared in milliq™ water by gentle shaking. the mobile phase consisted of acetonitrile/water/acetic acid in the volume ratio of 44/55/1.. the process according to claim 35 wherein the active agent is sparingly water soluble.

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[0043] water solubility of the active agent is defined by the united states pharmacoepia.[0097] accurately weighed out 20 to 50 mg (depending on the expected drug content) of a nanofiber composition, such as described above, into a scintillation vial and dissolved it 5 ml acetonitrile/water (80/20) mixture. different applications have been suggested for these electrospun nanofibers, such as air filters, molecular composites, vascular grafts, and wound dressings. this mixture was left in a shaking water bath at 37 c. the mixture was left in a shaking water bath at 37 c.[0038] the present invention is also directed to a rapidly dissolving dosage form comprising an electrospun water soluble polymer in combination with an active agent, such that the rapid dissolving dosage form disintegrates in a rapid manner, over a short time period, in the mouth or other suitable body cavity.

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. a pharmaceutical composition comprising an electrospun fiber of a pharmaceutically acceptable polymeric carrier integrated with a pharmaceutically acceptable active agent which agent is sparingly water soluble or water insoluble.[0109] one hundred milligrams of paroxetine was dissolved in 20 ml of milliq water. however, it is necessary to use an organic solvent to prepare a homogenous solution of the drug with polymer when the drug is non-water soluble, or sparingly soluble. the mixture was left shaking in a water bath at 37 c.. the process according to claim 35 wherein the active agent is water insoluble.. the process according to claim 24 wherein the active agent is sparingly water soluble.

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20 ul of this solution was injected in waters hplc system equipped with waters 550 pumps, 717plus autosampler, and spectroflow 783 uv detector.. the process according to claim 27 wherein the solvent is a mixture of water and a water miscible solvent.. a process for making an electrospun pharmaceutical composition comprising a pharmaceutically acceptable active agent wherein the agent is sparingly water soluble or water insouble, and a pharmaceutically acceptable polymeric carrier, which process comprises.. the composition according to claim 1 or 2 wherein the polymeric carrier is water insoluble. the solution was quantitatively transferred to a 50 ml volumetric flask using acetonitrile/water (80/20) and made up to volume (50 ml) using acetonitrile/water as diluent.. the composition according to claim 1 wherein the active agent is sparingly water soluble.

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[0108] three hundred fifty milligrams of ropirinole was dissolved in 15 ml of milliq water.[0060] nf grades of sentry polyox, a water soluble resin is available with varying molecular weights as noted above.% solution of polyox wsr n-60k™ (union carbide) was prepared in milliq™ water by gentle mixing in a shaking water bath.[0058] water soluble polymers include but are not limited to, poly(ethylene oxide), polyvinyl alcohol, polyvinyl pyrrolidone, hyaluronic acid, alginates, carragenen, cellulose derivatives such as carboxymethyl cellulose sodium, hydroxyethyl cellulose, hydroxypropylcellulose, hydroxypropylmethyl cellulose, hydroxypropylmethyl cellulose phthalate, cellulose acetate phthalate, starch and its derivatives such as hydroxyethyl starch, sodium starch glycolate, dextrin, chitosan and its derivatives, albumen, zein, gelatin, and collagen.. the process according to claim 24 wherein the active agent is water insoluble. the sample was made up using acetonitrile/water(80:20) as a diluent.

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[0111] eight hundred and fifty milligrams of polyox wsr-1105 (900k) was dissolved in 20 ml acetonitrile by shaking overnight in a water bath at 35 c.[0057] preferably, the polymeric carriers are divided into three categories: (1)water soluble polymers useful for rapid dissolve and immediate release of active agents, (2) water insoluble polymers useful for controlled release of the active agents; and (3) ph sensitive polymers for pulsatile or targeted release of active agents. g polyox wsr-1105 (900k) was added 1 ml milliq water and 12 ml acetonitrile.  the state would also see deep cuts to education, public health and funding for clean air and water. 4,946,684; 5,298,261; 5,466,464; 5,501,861; 5,762,961; 5,866,163 disclose taste masked rapidly dissolving dosage forms having organoleptically acceptable properties disintegrate rapidly in patients mouth without chewing or with minimum amount of water.[0039] a rapid dissolve dosage form may include a drug which is either water soluble or water insoluble.

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. the composition according to claim 1 or 2 wherein the polymeric carrier is water soluble.[0059] preferably, a water soluble polymer for use herein is polyethylene oxide, such as the brand name polyox. (for nabumetone this can be prepared by 10 fold dilution of a solution containing 25 mg nabumetone in 100 mls of 50/50 methanol/water). this mixture was left in a shaking water bath at 37 c.[0100] the equipment used for this procedure is a modified usp4, the major differences being: 1) low volume cell; 2)stirred cell; 3) retaining filters which are adequate at retaining sub micron material. all of the disclosed water insoluble polymers are not pharmaceutically acceptable for use herein, however the water soluble polymers disclosed are believed to be pharmaceutically acceptable.

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. the process according to claim 24 wherein the solvent is water immisicible. suitably, water is the best solvent for a water soluble active agent, and a water soluble polymer like polyox.. the process according to claim 24 wherein the solvent is water miscible. the mixture was left shaking in a water bath at 37 c.[0112] seven hundred and fifty milligrams of polyox wsr-1105 (900k) was dissolved in 20 ml acetonitrile by shaking overnight in a water bath at 35 c.) discloses a solid drug pulverized in an aqueous solution of a water-soluble high molecular substance using a wet grinding machine.

Patent US20030017208 - Electrospun pharmaceutical compositions

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  the state would also see deep cuts to education, public health and funding for clean air and water. one use of the increased surface area of drug is improved bioavailability in the case of a poorly water soluble drug. 400k, union carbide) in milliq™ water/acetonitrile was prepared by mixing 15 g of peo in 50 ml water and 150 ml acetonitrile. as such it is unlikely with poorly soluble drugs and with water as the dissolution medium that 100% of the drug will dissolve in the 20 minute duration of the test.[0037] the present invention is therefore directed to use in any form of a nanofibrous drug either alone, or in combination with a pharmaceutically acceptable polymer (or combination thereof) for enhancing the bioavailability of a drug, preferably a poorly water soluble drug. the dissolution medium is water at a flow rate of 5 ml/min.

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in the oral context this would produce small particulate matter, which could be ingested without needing water.[0092] to 10 ml of the stock solution of water/acetonitrile from example 3 above was added 0. this extremely high surface area has profound influence on the bioavailability of a poorly water soluble drug, since it is known that increased surface can lead to increased dissolution rate.[0070] a preferred solvent is a mixture of water and acetonitrile, or water and acetone.[0110] three hundred milligrams of kytril was dissolved in 15 ml of milliq water.[0049] other suitable active agents are amprenavir (agenerase), lamivudine (epivir), epoprostenol (flolan), zanamivir (relenza), alosetron (lotronex), alelometasone (aclovate), beclomethasone (beclovent and beconase), malphalan (aleran), naratriptan (amerge), succinylcholine, cefuroxiime (ceftin), ceftazidime (ceptaz), cefuroxime (zinacef), zidovudine (retrovir), fluticasone (flonase or cutivate), pyrimethamine (daraprim), colfosceril, sumatriptan (imitrex), lamotrigine (lamictal), chlorambucil (leukeran), atovaquone (malaron or mepron), mivacurium (mivacron), busulfan (myleran), vinorelbine (navelbine), cisatracurium (nimbex), doxacurium (nuromax), atacurium (tracrium), oxiconazole (oxistat), mercaptopurine (purinethol) and thioguanine (tabloid), grepafloxacin (raxar), salmeterol (serevent), clobetasol (temovate), ranitidine, famotidine, omeprazole (r and s isomers), remifentanil (ultiva), valacyclovir (valtrex), acyclovir (zovirax), famciclovir (famvir), penciclovir (denavir), albuterol (ventolin), bupropion (wellbutrin or zyban), or abacavir (ziagen), 4-(3,4-dihydro-1-methyl-2(1h)-isoquinolinyl)-n-(4-fluorophenyl)-5,6-dimethyl-2-pyrimidinamine, (n-(2,6-dichlorobenzoyl)-4-(2,6-dimethoxyphenyl)-l-phenylalanine); telmisartan, lacidipine, eniluracil, amoxicillin (amoxcil), clavulanate, mupirocin, ticarcillin, cerivastatin (baycol), carvedilol (coreg), topotecan (hycamtin)), factive, locilex, novastan, tranilast, lotrifiban, 8-[(4-amino-1-methylbutyl)amino]-2,6-dimethoxy-4-methyl-5-(3-trifluoromethylphenoxy)quinoline succinate, (1s,2r,3s)-1-(1,3-benzodioxol-5-yl)-2,3-dihydro-3-[2-(2-hydroxyethoxy)-4-methoxyphenyl]-5-propoxy-1h-indene-2-carboxylic acid, nelarabine, dutasteride, maribavir, 3-(3-{1-[(isopropyl-phenyl-carbamoyl)-methyl]-2,4-dioxo-5-phenyl -2,3,4,5-tetrahydro-1h-benzo[b][1,4]diazepin-3-yl}-ureido)-benzoic acid; 6-amino -3-(2,3,5-trichlorophenyl)pyrazin-2-ylamine; (2r,3r,4s,5r)-2-[6-amino-2-(1s-hydroxymethyl -2-phenyl-ethylamino)-purin-9-yl]-5-(2-ethyl-2h-tetrazol-5-yl)-tetrahydro-furan -3,4-diol; (6α,11β,16α,17α)-6,9-difluoro-11-hydroxy-16-methyl-3-oxo-17-({[(3s)-2-oxotetrahydrofuran-3-yl]thio}carbonyl)androsta-1,4-dien-17-yl propionate; (3s)-tetrahydrofuran-3-yl (1s,2r)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propylcarbamate; (3r,5r)-3-butyl-3-ethyl-7,8-dimethoxy-5-phenyl-2,3,4,5-tetrahydro-1,4-benzothiazepine 1,1-dioxide; (1s,3s,4s,8r)-3-(3,4-dichlorophenyl)-7-azatricyclo[5.

[0062] water insoluble polymers include but are not limited to, polyvinyl acetate, methyl cellulose, ethylcellulose, noncrystalline cellulose, polyacrylates and its derivatives such as the eudragit family of polymers available from rohm pharma (germany), poly(alpha-hydroxy acids) and its copolymers such as poly(ε-caprolactone), poly(lactide-co-glycolide), poly(alpha-aminoacids) and its copolymers, poly(orthoesters), polyphosphazenes, poly(phosphoesters), and polyanhydrides.[0107] two hundred milligrams of ropirinole was dissolved in 15 ml of milliq water. this being the case, electrospun polymer (water-soluble) nanofibers may suitably be premixed with drug during spinning or post mixed during fabrication of the rapid dissolve dosage form.[0101] flow cell description: swinnex filter assemblies obtained from millipore, having 0. sentry polyox is a water soluble resin which is listed in the nf and have approximate molecular weights from 100k to 900k and 1000k to 7000k. the mixture was left in a shaking water bath at 37 c.

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