1. A pharmaceutical composition in the form of a solid carrier comprising an admixture of: (a) a pharmaceutical active ingredient selected from the group consisting of: analgesics, anti-inflammatory agents, antihelminthics, anti-arrhythmic agents, anti-bacterial agents, anti-viral agents, anti-coagulants, anti-depressants, anti-diabetics, anti-epileptics, anti-fungal agents, anti-gout agents, anti-hypertensive agents, anti-malarials, anti-migraine agents, anti-muscarinic agents, anti-neoplastic agents, erectile dysfunction improvement agents, immunosuppressants, anti-protozoal agents, anti-thyroid agents, anxiolytic agents, sedatives, hypnotics, neuroleptics, \u03b2-blockers, cardiac inotropic agents, corticosteroids, diuretics, anti-parkinsonian agents, gastro-intestinal agents, histamine receptor antagonists, keratolyptics, lipid regulating agents, anti-anginal agents, Cox-2 inhibitors, leukotriene inhibitors, macrolides, muscle relaxants, nutritional agents, opiod analgesics, protease inhibitors, sex hormones, stimulants, muscle relaxants, anti-osteoporosis agents, anti-obesity agents, cognition enhancers, anti-urinary incontinence agents, nutritional oils, anti-benign prostate hypertrophy agents, essential fatty acids, non-essential fatty acids, and mixtures thereof, (b) an effective solubilizing amount of at least one hydrophiliac surfactant, which is effective to partially or fully solubilize the pharmaceutically active ingredient in the solid carrier, and optionally (c) an additive, wherein the at least one hydrophilic surfactant is selected from: (i) a hydrophilic surfactant that solidifies at ambient room temperature; (ii) a mixture of hydrophilic surfactants that in combination solidify at ambient room temperature; (iii) a hydrophilic surfactant that solidifies at ambient room temperature in the presence of the additive; and (iv) a combination of two or more of (i), (ii), and (iii), wherein the effective solubilizing amount of the at least one hydrophilic surfactant is an amount effective to facilitate sustained solubilization of the active ingredient upon administration, with the proviso that when the at least one hydrophilic surfactant includes (iii), the composition then includes the optional additive.
2. A pharmaceutical composition in the form of a solid carrier comprising an admixture of: (a) a pharmaceutical active ingredient; (b) an effective solubilizing amount of at least one hydrophilic surfactant selected from the group consisting of (i) polyoxyethylene sorbitan fatty acid esters, (ii) polyoxyethylene-polyoxypropylene block copolymers, (iii) polyglycerol fatty acid esters, (iv) polyoxyethylene glycerides, (v) polyoxyehtylene sterols, deriviatives, and analogues thereof, (vi) polyoxyehtylene vegetable oils, (vii) polyoxyethylene hydrogenated vegetable oils, (viii) reaction mixtures of polyols and at least one member of the group consisting of fatty acids, glycerides, vegetable oils, hydrogenated vegetable oils, and sterols (ix) tocopheryl polyethylene glycol succinates, (x) sugar esters, (xi) sugar ethers, (xii) sucroglycerides, and (xiii) mixtures thereof; and (c) an additive to provide for controlled release of the active ingredient following administration to a patient, said additive selected from the group consisting of polyvinylpyrrolidone, polyethylene glycol, hydroxypropyl methylcellulose, hyrosypropyl cellulose and other cellulose derivatives and mixtures thereof.
3. The pharmaceutical composition of claim 1, wherein the effective solubilizing amount of the hydrophilic surfactant is an amount effective to facilitate rapid dispersion of the active ingredient upon administration.
4. The pharmaceutical composition of claim 3, wherein the rapid dispersion comprises micellization andor emulsification.
5. The pharmaceutical composition of claim 1, wherein the carrier further comprises a substrate and wherein the admixture is in the form of an encapsulation coat on the substrate.
6. The pharmaceutical composition of claim 5, wherein the substrate is a powder or a multiparticulate.
7. The pharmaceutical composition of claim 6, wherein the substrate is a multiparticulate selected from the group consisting of granules, pellets, beads, spherules, beadlets, microcapsules, millispheres, nonocapsules, microspheres, platelets, tablets, and capsules.
8. The pharmaceutical composition of claim 1, wherein the composition includes the additive.
9. The pharmaceutical composition of claim 8, wherein the additive is selected from the group consisting of solubilizers, enzyme inhibitors, anti-adherents, anticoagulants, antifoaming agents, antioxidants, binders, bufferants, chelating agents, coagulants, colorants, opaquants, coolants, cryoprotectants, diluents, fillers, disintegrants, super disintegrants, hydrogen bonding agents, flavorants, desensitizers, ion-exchange resins, plasticizers, preservatives, solvents, sweeteners, thickeners, and mixtures thereof.
10. The pharmaceutical composition of claim 9, wherein the additive is selected from the group consisting of anti-adherents, binders, and disintegrants.
11. The pharmaceutical composition of claim 10, wherein the additive is an anti-adherent selected from the group consisting of talc, magnesium stearate, fumed silica, micronized silica, polyethylene glycols, surfactants, waxes, stearic acid, stearic acid salts, stearic acid derivatives, starch, hydrogenated vegetable oils, sodium benzoate, sodium acetate, leucine, PEG-4000 and magnesium lauryl sulfate.
12. The pharmaceutical composition of claim 10, wherein the additive is a binder selected from the group consisting of matrix binders, film binders, and chemical binders.
13. The pharmaceutical composition of claim 10, wherein the additive is a disintegrant selected from the group consisting of croscarmellose sodium, starch, starch derivatives, clays, gums, cellulose, cellulose derivates, alginates, crosslinked polyvinylpyrrolidone, sodium starch glycolate and microcrystalline cellulose.
14. The pharmaceutical composition of claim 8, wherein the additive is polyvinylpyrrolidone.
15. The pharmaceutical composition of claim 8, wherein the additive is cyclodextrin.
16. The pharmaceutical composition of claim 8, wherein the additive is polyethylene glycol.
17. The pharmaceutical composition of claim 16, wherein the additive is a cellulosic polymer.
18. The pharmaceutical composition of claim 17, wherein the cellulosic polymer is selected from the group consisting of sodium carboxymethyl cellulose, hydroxypropyl cellulose, and hydroxypropylmethyl cellulose.
19. The pharmaceutical composition of claim 18, wherein the cellulosic polymer is hydroxypropylmethyl cellulose.
20. The pharmaceutical composition of claim 1, wherein the active ingredient is a drug, a nutrient, a cosmeceutical, a diagnostic agent, a salt thereof, an isomer thereof, a derivative thereof, or a mixture thereof.
21. The pharmaceutical composition of claim 1, wherein the active ingredient has an intrinsic aqueous solubility of less than about 1 mgmL.
22. A pharmaceutical composition in the form of a solid carrier comprising a substrate and an encapsulation coat on the substrate, wherein the encapsulation coat comprises a therapeutically effective amount of a hydrophobic pharmaceutical active ingredient and an effective solubilizing amount of at least one hydrophilic surfactant, wherein the effective solubilizing amount of the at least one hydrophilic surfactant is an amount effective to facilitate sustained solubilization of the active ingredient upon administration.
23. The pharmaceutical composition of claim 1, wherein the active ingredient is selected from the group consisting of analgesics, anti-bacterial agents, anti-viral agents, anti-inflammatory agents, anti-depressants, anti-diabetics, anti-epileptics, anti-hypertensive agents, anti-migraine agents, immunosuppressants, anxiolytic agents, sedatives, hypnotics, neuroleptics, \u03b2-blockers, gastro-intestinal agents, lipid regulating agents, anti-anginal agents, Cox-2 inhibitors, leukotriene inhibitors, macrolides, muscle relaxants, opioid analgesics, protease inhibitors, sex hormones, cognition enhancers, anti-urinary incontinence agents, and mixtures thereof.
24. The pharmaceutical composition of claim 1, wherein the active ingredient is selected from the group consisting of acetretin, albendazole, albuterol, aminoglutethimide, amiodarone, amlodipine, amphetamine, amphotericin B, atorvastatin, atovaquone, azithromycin, baclofen, beclomethasone, benezepril, benzonatate, betamethasone, bicalutanide, budesonide, bupropion, busulfan, butenafine, calcifediol, calcipotriene, calcitriol, camptothecin, candesartan, capsaicin, carbamezepine, carotenes, celecoxib, cerivastatin, cetirizine, chlorpheniramine, cholecalciferol, cilostazol, cimetidine, cinnarizine, ciprofloxacin, cisapride, clarithromycin, clemastine, clomiphene, clomipramine, clopidogrel, codeine, coenzyme Q10, cyclobenzaprine, cyclosporin, danazol, dantrolene, dexchlorpheniramine, diclofenac, dicoumarol, digoxin, dehydroepiandrosterone, dihydroergotamine, dihydrotachysterol, dirithromycin, donezepil, efavirenz, eprosartan, ergocalciferol, ergotamine, essential fatty acid sources, etodolac, etoposide, famotidine, fenofibrate, fentanyl, fexofenadine, finasteride, fluconazole, flurbiprofen, fluvastatin, fosphenytoin, frovatriptan, furazolidone, gabapentin, gemfibrozil, glibenclamide, glipizide, glyburide, glimepiride, griseofulvin, halofantrine, ibuprofen, irbesartan, irinotecan, isosorbide dinitrate, isotretinoin, itraconazole, ivermectin, ketoconazole, ketorolac, lamotrigine, lansoprazole, leflunomide, lisinopril, loperamide, loratadine, lovastatin, L-thryroxine, lutein, lycopene, medroxyprogesterone, mifepristone, mefloquine, megestrol acetate, methadone, methoxsalen, metronidazole, miconazole, midazolam, miglitol, minoxidil, mitoxantrone, montelukast, nabumetone, nalbuphine, naratriptan, nelfinavir, nifedipine, nilsolidipine, nilutanide, nitrofurantoin, nizatidine, omeprazole, oprevelkin, oestradiol, oxaprozin, paclitaxel, paracalcitol, paroxetine, pentazocine, pioglitazone, pizofetin, pravastatin, prednisolone, probucol, progesterone, pseudoephedrine, pyridostigmine, rabeprazole, raloxifene, rofecoxib, repaglinide, rifabutine, rifapentine, rimexolone, ritanovir, rizatriptan, rosiglitazone, saquinavir, sertraline, sibutramine, sildenafil citrate, simvastatin, sirolimus, spironolactone, sumatriptan, tacrine, tacrolimus, tamoxifen, tamsulosin, targretin, tazarotene, telmisartan, teniposide, terbinafine, terazosin, tetrahydrocannabinol, tiagabine, ticlopidine, tirofibran, tizanidine, topiramate, topotecan, toremitfene, tramadol, tretinoin, troglitazone, trovafloxacin, ubidecarenone, valsartan, venlafaxine, verteporfin, vigabatrin, vitamin A, vitamin D, vitamin E, vitamin K, zafirlukast, zileuton, zolmitriptan, zolpidem, zopiclone, pharmaceutically acceptable salts, isomers, and derivatives thereof, and mixtures thereof.
25. The pharmaceutical composition of claim 24, wherein the active ingredient is selected from the group consisting of acetretin, albendazole, albuterol, aminoglutethimide, amiodarone, amlodipine, amphetamine, amphotericin B, atorvastatin, atovaquone, azithromycin, baclofen, benzonatate, bicalutanide, busulfan, butenafine, calcifediol, calcipotriene, calcitriol, camptothecin, capsaicin, carbamezepine, carotenes, celecoxib, cerivastatin, chlorpheniramine, cholecaliferol, cimetidine, cinnarizine, ciprofloxacin, cisapride, cetirizine, clarithromycin, clemastine, clomiphene, codeine, coenzyme Q10, cyclosporin, danazol, dantrolene, dexchlorpheniramine, diclofenac, digoxin, dehydrepiandrosterone, dihydroergotamine, dihyrotachysterol, dirithromycin, donepezil, efavirenz, ergocalciferol, ergotamine, essential fatty acid sources, etodolac, etoposide, famotidine, fenofibrate, fentanyl, fexofenadine, finasteride, fluconazole, flurbiprofen, fluvastatin, fosphenytoin, frovatriptan, furazolidone, gabapentin, gemfibrozil, glibenclamide, glipizide, glyburide, glimepiride, griseofulvin, halofantrine, ibuprofen, irinotecan, isotretinoin, itraconazole, ivermectin, ketoconazole, ketorolac, lamotrigine, lansoprazole, leflunomide, loperamide, loratadine, lovastatin, L-thryroxine, lutein, lycopene, mifepristone, mefloquine, megestrol acetate, methdone, methoxsalen, metronidazole, miconazole, midazolam, miglitol, mitoxantrone, medroxyprogesterone, montelukast, nabumetone, nalbuphine, naratriptan, nelfinavir, nilutanide, nitrofurantoin, nizatidine, omeprazole, oestradiol, oxaprozin, paclitaxel, paracalcitol, pentazocine, pioglitazone, pizofetin, pravastatin, probucol, progesterone, pseudoephedrine, pyridostigmine, rabeprazole, raloxifene, rofecoxib, repaglinide, rifabutine, rifapentine, rimexolone, ritanovir, rizatriptan, rosiglitazone, saquinavir, sibutramine, sildenafil citrate, simvastatin, sirolimus, spironolactone, sumatriptan, tacrine, tacrolimus, tamoxifen, tamsulosin, targretin, tazarotene, teniposide, terbinafine, tetrahydrocannabinol, tiagabine, tizanidine, topiramate, topotecan, toremifene, tramadol, tretinoin, troglitazone, trovafloxacin, verteporfin, vigabatrin, vitamin A, vitamin D, vitamin E, vitamin K, zafirlukast, zileuton, zolmitriptan, zolpidem, zopiclone, pharmaceutically acceptable salts, isomers and derivatives thereof, and mixtures thereof.
26. The pharmaceutical composition of claim 25, wherein the active ingredient is selected from the group consisting of acetretin, albuterol, aminoglutethimide, amiodarone, amlodipine, amprenavir, atorvastatin, atovaquone, baclofen, benzonatate, bicalutanide, busulfan, calcifediol, calcipotriene, calcitriol, camptothecin, capsaicin, carbamezepine, carotenes, celecoxib, chlorpheniramine, cholecaliferol, cimetidine, cinnarizine, cisapride, citrizine, clemastine, coenzyme Q10, cyclosporin, danazol, dantrolene, dexchlorpheniramine, diclofenac, dehydroepiandrosterone, dihydroergotamine, dihyrotachysterol, efavirenz, ergocalciferol, ergotamine, essential fatty acid sources, etodolac, etoposide, famotidine, fenofibrate, fexofenadine, finasteride, fluconazole, flurbiprofen, fosphenytoin, frovatriptan, furzolidone, glibenclamide, glipizide, glyburide, glymepride, ibuprofen, irinotecan, isotretinoin, itraconazole, ivermectin, ketoconazole, ketorolac, lamotrigine, lansoprazole, leflunomide, loperamide, loratadine, lovastatin, L-thryroxine, lutein, lycopene, medroxyprogesterone, mifepristone, megestrol acetate, methoxsalen, metronidazole, miconazole, miglitol, mitoxantrone, montelukast, nabumetone, naratriptan, nelfinavir, nilutanide, nitrofurantoin, nizatidine, omeprazole, oestradiol, oxaprozin, paclitaxel, paracalcitol, pioglitazone, pizofetin, pranlukast, probucol, progesterone, pseudoephedrine, rabeprazole, raloxifene, rofecoxib, repaglinide, rifabutine, rifapentine, rimexolone, ritanovir, rizatriptan, rosiglitazone, saquinavir, sildenafil citrate, simvastatin, sirolimus, tramadol, tacrolimus, tamoxifen, tamsulosin, targretin, tazarotene, teniposide, terbenafine, tetrahydrocannabinol, tiagabine, tizanidine, topiramate, topotecan, toremifene, tramadol, tretinoin, troglitazone, trovafloxacin, ubidecarenone, vigabatrin, vitamin A, vitamin D, vitamin E, vitamin K, zafirlukast, zileuton, zolmitriptan, pharmaceutically acceptable salts, isomers and derivative thereof, and mixtures thereof.
27. The pharmaceutical composition of claim 26, wherein the active ingredient is selected from the group consisting of amlodipine, amprenavir, atorvastatin, atovaquone, celecoxib, cisapride, coenzyme Q10, cyclosporin, famotidine, fenofibrate, fexofenadine, finasteride, ibuprofen, itraconazole, lansoprazole, loratadine, lovastatin, megestrol acetate, montelukast, nabumetone, nizatidine, omeprazole, oxaprozin, paclitaxel, paracalcitol, pioglitazone, pranlukast, progesterone, pseudoephedrine, rabeprazole, rapamycin, rofecoxib, repaglinide, rimexolone, ritanovir, rosiglitazone, saquinavir, sildenafil citrate, simvastatin, sirolimus, tramadol, tacrolimus, tamsulosin, teniposide, terbenafine, tetrahydrocannabinol, tiagabine, tizanidine, tramadol, troglitazone, vitamin A, vitamin D, vitamin E, zafirlukast, zileuton, pharmaceutically acceptable salts, isomers and derivatives thereof, and mixtures thereof.
28. The pharmaceutical composition of claim 1, wherein the active ingredient is selected from the group consisting of progesterone, dehydroepiandrosterone, amiodarone, spironolactone and mixtures thereof.
29. The pharmaceutical composition of claim 1, wherein the active ingredient is selected from the group consisting of clopidogrel, pioglitazone, zafirlukast, sertraline, tramadol, and fentanyl.
30. The pharmaceutical composition of claim 1, wherein the active ingredient is selected from the group consisting of tacrolimus, sirolimus, cilostazol, bicalutaminde, simvastatin, and lovastatin.
31. The pharmaceutical composition of claim 1, wherein the at least one hydrophilic surfactant comprises a non-ionic hydrophilic surfactant.
32. The pharmaceutical composition of claim 31, wherein the non-ionic hydrophilic surfactant has an HLB value of at least about 10.
33. The pharmaceutical composition of claim 31, wherein the non-ionic hydrophilic surfactant is selected from the group consisting of alkylglucosides; alkylmaltosides; alkylthioglucosides; lauryl macrogolglycerides; polyoxyethylene alkyl ethers; polyoxyethylene alkylphenols; polyethylene glycol fatty acids esters; polyethylene glycol glycerol fatty acid esters; polyoxyethylene sorbitan fatty acid esters; polyoxyethylene-polyoxypropylene block copolymers; polyglycerol fatty acid esters; polyoxyethylene glycerides; polyoxyethylene sterols, derivatives, and analogues thereof; polyoxyethylene vegetable oils; polyoxyethylene hydrogenated vegetable oils; reaction mixtures of polyols and at least one member of the group consisting of fatty acids, glycerides, vegetable oils, hydrogenated vegetable oils, and sterols; tocopheryl polyethylene glycol succinates; sugar esters; sugar ethers; sucroglycerides; and mixtures thereof.
34. The pharmaceutical composition of claim 33, wherein the non-ionic hydrophilic surfactant is a polyoxyethylene sorbitan fatty acid esters.
35. The pharmaceutical composition of claim 34, wherein the polyoxyethylene sorbitan fatty acid ester is PEG-20 sorbitan monooleate.
36. The pharmaceutical composition of claim 33, wherein the non-ionic hydrophilic surfactant is a polyoxyethylene vegetable oil.
37. The pharmaceutical composition of claim 36, wherein the polyoxyethylene vegetable oil is polyethoxylated caster oil.
38. The pharmaceutical composition of claim 37, wherein the polyethoxylated caster oil is PEG-35 caster oil.
39. The pharmaceutical composition of claim 33, wherein the non-ionic hydrophilic surfactant is a polyoxyethylene hydrogenated vegetable oil.
40. The pharmaceutical composition of claim 39, wherein the polyoxyethylene hydrogenated vegetable oil is polyethoxylated hydrogenated caster oil.
41. The pharmaceutical composition of claim 40, wherein the polyethoxylated hydrogenated caster oil is PEG-40 hydrogenated castor oil.
42. The pharmaceutical composition of claim 33, wherein the non-ionic hydrophilic surfactant is a tocopheryl polyethylene glycol succinate.
43. The pharmaceutical composition of claim 42, wherein the tocopheryl polyethylene glycol succinate is tocopheryl PEG-1000 succinate.
44. The pharmaceutical composition of claim 33, wherein the non-ionic hydrophilic surfactant is a polyoxyethylene glyceride.
45. The pharmaceutical composition of claim 44, wherein the polyoxyethylene glyceride is a PEG-8 capryliccapric glyceride.
46. The pharmaceutical composition of claim 31, wherein the non-ionic hydrophilic surfactant is selected from the group consisting of lauryl macrogol glycerides and stearoyl macrogol glycerides.
47. The pharmaceutical composition of claim 46, wherein the non-ionic hydrophilic surfactant is a lauryl macrogol glyceride.
48. The pharmaceutical composition of claim 47, wherein the lauryl macrogol glyceride is lauryl macrogol-32 glyceride.
49. The pharmaceutical composition of claim 46, wherein the non-ionic hydrophilic surfactant is a stearoyl macrogol glyceride.
50. The pharmaceutical composition of claim 1, wherein the at least one hydrophilic surfactant comprises an ionic surfactant.
51. The pharmaceutical composition of claim 50, wherein the ionic surfactant is selected from the group consisting of alkyl ammonium salts; bile acids and salts, analogues, and derivatives thereof; fatty acid derivatives of amino acids, camitines, oligopeptides, and polypeptides; glyceride derivatives of amino acids, oligopeptides, and polypeptides; acyl lactylates; mono- and di-acetylated tartaric acid esters of mono- and di-glycerides; succinylated monoglycerides; citric acid esters of mono- and di-glycerides; alginate salts; propylene glycol alginate; lecithins and hydrogenated lecithins; lysolecithin and hydrogenated lysolecithins, lysophospholipids and derivatives thereof; phospholipids and derivatives thereof; salts of alkylsulfates; salts of fatty acids; sodium docusate; and mixtures thereof.
52. The pharmaceutical composition of claim 1, wherein the solid carrier comprises a bead, a beadlet, a granule, a spherule, a pellet, a microcapsule, a microsphere, a nanosphere, a film, a wafer, a sprinkle, an implant, a troche, a lozenge, a platelet, a nanocapsule or a strip.
53. The pharmaceutical composition of claim 1, wherein the solid carrier is enteric coated, coated for fast disintegration, seal coated, film coated, barrier coated, compress coated, or coated with an enzyme-degradable coating.
54. The pharmaceutical composition of claim 1, wherein the composition is encapsulated, extruded, compressed, pelletized, coated, mixed, granulated, crystallized, lyophilized or molded.
55. The pharmaceutical composition of claim 1, wherein the composition is prepared by spheronization.
56. The pharmaceutical composition of claim 1, wherein the composition is prepared by compression.
57. The pharmaceutical composition of claim 1, wherein the composition is prepared by extrusion.
58. The pharmaceutical composition of claim 1, in the form of a capsule, a tablet, an ovule, a suppository, a wafer, a chewable tablet, a buccal tablet, a sublingual tablet, a quick-dissolve tablet, an effervescent tablet, a granule, a pellet, a bead, a pill, a sachet, a sprinkle, a film, a dry syrup, a reconstitutable solid, a suspension, a lozenge, a troche, an implant, a powder, a triturate, a platelet, or a strip.
59. The pharmaceutical composition of claim 1, wherein the composition is formulated for controlled release.
60. The pharmaceutical composition of claim 59, wherein the controlled release is immediate release, pulsatile release, extended release, delayed release, targeted release, targeted delayed release, or mixtures thereof.
61. The pharmaceutical composition of claim 1, wherein the composition is formulated for oral, nasal, ocular, urethral, buccal, transmucosal, vaginal, topical or rectal delivery.
62. A method of administering an active ingredient to a mammalian patient, the method comprising administering the pharmaceutical composition of claim 1 to the patient.
63. The method of claim 62, wherein the mammal is a human.
64. The pharmaceutical composition of claim 2, wherein the active ingredient is selected from the group consisting of analgesics, anti-inflammatory agents, antihelminthics, anti-arrhythmic agents, anti-bacterial agents, anti-viral agents, anti-coagulants, anti-depressants, anti-diabetics, anti-epileptics, anti-fungal agents, anti-gout agents, anti-hypertensive agents, anti-malarials, anti-migraine agents, anti-muscarinic agents, anti-neoplastic agents, erectile dysfunction improvement agents, immunosuppressants, anti-protozoal agents, anti-thyroid agents, anxioytic agents, sedatives, hypnotics, neuroleptics, \u03b2-blockers, cardiac inotropic agents, corticosteroids, diuretics, anti-parkinsonian agents, gastro-intestinal agents, histamine receptor antagonists, kerarolytics, lipid regulating agents, anti-anginal agents, Cox-2 inhibitors, leukotriene inhibitors, macrolides, muscle relaxants, nutritional agents, opioid analgesics, protease inhibitors, sex hormones, stimulants, muscle relaxants, anti-osteoperosis agents, anti-obesity agents, cognition enhancers, anti-urinary incontinence agents, nutritional oils, anti-benign prostate hypertrophy agents, essential fatty acids, non-essential fatty acids, and mixtures thereof.
65. The pharmaceutical composition of claim 64, wherein the effective solubilizing amount of the hydrophilic surfactant is an amount effective to facilitate sustained solubilization of the active ingredient upon administration.
66. The pharmaceutical composition of claim 64, wherein the effective solubilizing amount of the hydrophilic surfactant is an amount effective to partially or fully solubilize the active ingredient in the solid carrier.
67. The pharmaceutical composition of claim 64, wherein the effective solubilizing amount of the hydrophilic surfactant is an amount effective to facilitate rapid dispersion of the active ingredient upon administration.
68. The pharmaceutical composition of claim 67, wherein the rapid dispersion comprises micellization andor emulsification.
69. The pharmaceutical composition of claim 64, wherein the hydrophilic surfactant is PEG-20 sorbitan monooleate.
70. The pharmaceutical composition of claim 64, wherein the hydrophilic surfactant is selected from the group consisting of PEG-35 caster oil, PEG-40 hydrogenated castor oil, and mixtures thereof.
71. The pharmaceutical composition of claim 64, wherein the hydrophilic surfactant is tocopheryl PEG-1000 succinate.
72. The pharmaceutical composition of claim 64, wherein the hydrophilic surfactant is selected from the group consisting of lauryl macrogols-32 glyceride, stearoyl macrogols glyceride and mixtures thereof.
73. The pharmaceutical composition of claim 64, wherein the hydrophilic surfactant is PEG-8 capryliccapric glyceride.
74. The pharmaceutical composition of claim 64, wherein the hydrophilic surfactant is a poloxamer.
75. The pharmaceutical composition of claim 64, wherein the controlled release is immediate release, extended release, delayed release, pulsatile release, targeted release or mixtures thereof.
76. The pharmaceutical composition of claim 64, wherein the solid carrier is provided with one or more coatings.
77. The pharmaceutical composition of claim 61, wherein the composition is prepared by spheronization, pelletization, coating, balling, extrusion, spray congealing, nanoencapsulation, super critical fluid processes, cryopelletization, mixing, molding, compression, granulation, lyophilization, chilling, agglomeration, congealing, drying, melt extrusion, crystallization, coacervation, and combinations thereof.
78. The pharmaceutical composition of claim 64, wherein the active ingredient is selected from the group consisting of analgesics, anti-bacterial agents, anti-viral agents, anti-inflammatory agents, anti-depressants, anti-diabetics, anti-epileptics, anti-hypertensive agents, anti-migraine agents, immunosupressants, anxiolytic agents, sedatives, hypnotics, neuroleptics, \u03b2-blockers, gastro-intestinal agents, lipid regulating agents, anti-anginal agents, Cox-2 inhibitors, leukotriene inhibitors, macrolides, muscle relaxants, opioid analgesics, protease inhibitors, sex hormones, cognition enhancers, anti-urinary incontinence agents, and mixtures thereof.
79. The pharmaceutical composition of claim 78, wherein the effective solubilizing amount of the hydrophilic surfactant is an amount effective to partially or fully solubilize the active ingredient in the solid carrier.
80. The pharmaceutical composition of claim 78, wherein the effective solubilizing amount of the hydrophilic surfactant is an amount effective to facilitate rapid dispersion of the active ingredient upon administration.
81. The pharmaceutical composition of claim 80, wherein the rapid dispersion comprises micellization andor emulsification.
82. The pharmaceutical composition of claim 2, wherein the active ingredient is selected from the group consisting of acetretin, albendazole, albuterol, aminoglutethimide, amiodarone, amlodipine, amphetamine, amphotericin B, atorvastatin, atovaquone, azithromycin, baclofen, beclomethasone, benezepril, benzonatate, betamethasone, bicalutanide, budesonide, bupropion, busulfan, butenafine, calcifediol, calcipotriene, calcitriol, camptothecin, candesartan, capsaicin, carbamezepine, carotenes, celecoxib, cerivastatin, cetirizine, chlorpheniramine, cholecalciferol, cilostazol, cimetidine, cinnarizine, ciprofloxacin, cisapride, clarithromycin, clemastine, clomiphene, clomipramine, clopidogrel, codeine, coenzyme Q10, cyclobenzaprine, cyclosporin, danazol, dantrolene, dexchlorpheniramine, diclofenac, dicoumarol, digoxin, dehydroepiandrosterone, dihydroergotamine, dihydotachysterol, dirithromycin, donezepil, efavirenz, eprosartan, ergocalciferol, ergotamine, essential fatty acid sources, etodolac, etoposide, famotidine, fenofibrate, fentanyl, fexofenadine, finasteride, fluconazole, flurbiprofen, fluvastatin, fosphenytoin, frovatriptan, furazolidone, gabapentin, gemfibrozil, glibenclamide, glipizide, glyburide, glimepiride, griseofulvin, halofantrine, ibuprofen, irbesartan, irinotecan, isosorbide dinitrate, isotretinoin, itraconazole, ivermectin, ketoconazole, ketorolac, lamotrigine, lansoprazole, leflunomide, lisinopril, loperamide, loratadine, lovastatin, L-thyroxine, lutein, lycopene, medroxyprogesterone, mifepristone, mefloquine, megestrol acetate, methadone, methoxsalen, metronidazole, miconazole, midazolam, miglitol, minoxidil, mitoxantrone, montelukast, nabumetone, nalbuphine, naratriptan, nelfinavir, nifedipine, nilsolidipine, nilutanide, nitrofurantoin, nizatidine, omeprazole, oprevelkin, oestradiol, oxaprozin, paclitaxel, paracalcitol, paroxetine, pentazocine, pioglitazone, pizofetin, pravastatin, prednisolone, probucol, progesterone, pseudoephedrine, pyridostigmine, rabeprazole, raloxifene, rofecoxib, repaglinide, rifabutine, rifapentine, rimexolone, ritanovir, rizatriptan, rosiglitazone, saquinavir, sertraline, sibutramine, sildenafil citrate, simvastatin, sirolimus, spironolactone, sumatriptan, tacrine, tacrolimus, tamoxifen, tamsulosin, targretin, tazarotene, telmisartan, teniposide, terbinafine, terazosin, tetrahydrocannabinol, tiagabine, ticlopidine, tirofibran, tizanidine, topiramate, topotecan, toremifene, tramadol, tretinoin, troglitazone, trovafloxacin, ubidecarenone, valsartan, venlafaxine, verteporfin, vigabatrin, vitamin A, vitamin D, vitamin E, vitamin K, zafirlukast, zileuton, zolmitriptan, zolpidem, zopiclone, pharmaceutically acceptable salts, isomers, and derivatives thereof, and mixtures thereof.
83. The pharmaceutical composition of claim 82, wherein the active ingredient is selected from the group consisiting of acetretin, albendazole, albuterol, aminoglutethimide, amiodarone, amlodipine, amphetamine, amphotericin B, atorvastatin, atovaquone, azithromycin, baclofen, benzonatate, bicalutanide, busulfan, butenafine, calcifediol, calcipotriene, calcitriol, camptothecin, capsaicin, carbamezepine, carotenes, celecoxib, cerivastatin, chlorpheniramine, cholecaliferol, cimetidine, cinnarizine, ciprofloxacin, cisapride, cetirizine, clarithromycin, clemastine, clomiphene, codeine, coenzyme Q10, cyclosporin, danazol, dantrolene, dexchlorpheniramine, diclofenac, digoxin, dehydrepiandrosterone, dihydroergotamine, dihyrotachysterol, dirithromycin, donepezil, efavirenz, ergocalciferol, ergotamine, essential fatty acid sources, etodolac, etoposide, famotidine, fenofibrate, fentanyl, fexofenadine, finasteride, fluconazole, flurbiprofen, fluvastatin, fosphenytoin, frovatriptan, furazolidone, gabapentin, gemifibrozil, glibenclamide, glipizide, glyburide, glimepiride, griseofulvin, halofantrine, ibuprofen, irinotecan, isotretinoin, itraconazole, ivermectin, ketoconazole, ketorolac, lamotrigine, lansoprazole, leflunomide, loperamide, loratadine, lovastatin, L-thryroxine, lutein, lycopene, mifepristone, mefloquine, megestrol acetate, methdone, methoxsalen, metronidazole, miconazole, midazolam, miglitol, mitoxantrone, medroxyprogesterone, montelukast, nabumetone, nalbuphine, naratriptan, nelfinavir, nilutanide, nitrofurantoin, nizatidine, omeprazole, oestradiol, oxaprozin, paclitaxel, paracalcitol, pentazocine, pioglitazone, pizofetin, pravastatin, probucol, progesterone, pseudoephedrine, pyridostigmine, rabeprazole, raloxifine, rofecoxib, repaglinide, rifabutine, rifapentine, rimexolone, ritanovir, rizatriptan, rosiglitazone, saquinavir, sibutramine, sildenafil citrate, simvastatin, siroliumus, spironolactone, sumatriptan, tacrine, tacrolimus, tamoxifen, tamsulosin, targretin, tazarotene, teniposide, terbinafine, tetrahydrocannabinol, tiagabine, tizanidine, topiramate, topotecan, toremifene, tramadol, tretinoin, troglitazone, trovafloxacin, verteporfin, vigabatrin, vitamin A, vitamin D, vitamin E, vitamin K, zafirlukast, zileuton, zolmitriptan, zolpidem, zopiclone, pharmaceutically acceptable salts, isomers and derivatives thereof, and mixtures thereof.
84. The pharmaceutical composition of claim 83, wherein the active ingredient is selected from the group consisting of acetretin, albuterol, aminoglutethimide, amiodarone, amlodipine, amprenavir, atorvastatin, atovaquone, baclofen, benzonatate, bicalutanide, busulfan, calcifediol, calcipotriene, calcitrol, camptothecin, capsaicin, carbamezepine, carotenes, celecoxib, chlorpheniramine, cholecaliferol, cimitidine, cinnarizine, cisapride, citrizine, clemastine, coenzyme Q10, cyclosporin, danazol, dantrolene, dexchlorpheniramine, diclofenac, dehydroepiandrosterone, dihydroergotamine, dihyrotachysterol, efavirenz, ergocalciferol, ergotamine, essential fatty acid sources, etodolac, etoposide, famotidine, fenofibrate, fexofenadine, finasteride, fluconazole, flurbiprofen, fosphenytoin, frovatriptan, flurzolidone, glibenclamide, glipizide, glyburide, glymepride, ibuprofen, ironotecan, isotretinoin, itraconazole, ivermectin, ketoconazole, ketorolac, lamotrigine, lansoprazole, leflunomide, loperamide, loratadine, lovastatin, L-thyroxine, lutien, lycopene, medroxyprogesterone, mifepristone, megestrol acetate, methoxsalen, metronidazole, miconazole, miglitol, mitoxantrone, montelukast, nabumetone, naratriptan, nelfinavir, nilutanide, nitrofurantoin, nizatidine, omeprazole, oestradiol, oxaprozin, paclitaxel, paracalcitol, pioglitazone, pizofetin, pranlukast, probucol, progesterone, pseudophedrine, raberprazole, raloxifene, rofecoxib, repaglinide, rifabutine, rifapentine, rimexolone, ritanovir, rizatriptan, rosiglitazone, saquinavir, sildenafil citrate, simvastatin, sirolimus, tramadol, tacrolimus, tamoxifen, tamsulosin, targretin, tazarotene, teniposide, terbenafine, tetrahydrocannabinol, tiagabine, tizanidine, topiramate, topotecan, toremifine, tramadol, tretinoin, troglitazone, trovafloxacin, ubidecarenone, vigabatrin, vitamin A, vitamin D, vitamin E, vitamin K, zafirlukast, zileuton, zolmitriptan, pharmaceutically acceptable salts, isomers and derivative thereof, and mixtures thereof.
85. The pharmaceutical composition of claim 84, wherein the active ingredient is selected from the group consisting of amlodipine, amprenavir, atorvastatin, atovaquone, celecoxib, cisapride, coenzyme Q10, cyclosporin, famotidine, fenofibrate, fexofenadine, finasteride, ibuprofen, itraconazole, lansoprazole, loratadine, lovastatin, megestrol acetate, montelukast, nebumetone, nizatidine, omeprazole, oxaprozin, paclitaxel, paracalcitol, pioglitazone, pranlukast, progesterone, pseudoephedrine, rabeprazole, rapamycin, rofecoxib, repaglinide, rimexolone, ritanovir, rosiglitazone, saquinavir, sildenafil citrate, simvastatin, sirolimus, tramadol, tacrolimus, tamsulosin, teniposide, terbenafine, tetrahydrocannabinol, tiagabine, tizanidine, tramadol, trogliazone, vitamin A, vitamin D, vitamin E, zafirlukast, zileuton, pharmaceutically acceptable salts, isomers and derivatives thereof, and mixtures thereof.
86. The pharmaceutical composition of claim 2, wherein the active ingredient is selected from the group consisting of progesterone, dehydroepiandrosterone, amiodarone, spironolactone and mixtures thereof.
87. The pharmaceutical composition of claim 2, wherein the active ingredient is selected from the group consisting of clopidogrel, pioglitazone, zafirlukast, sertraline, tramadol, and fentanyl.
88. The pharmaceutical composition of claim 2, wherein the active ingredient is selected from the group consisting of tacrolimus, sirolimus, cilostazol, bicalutaminde, simvastatin, and lovastatin.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
What is claimed is:
1. A process comprising solution grafting a hydrocarbon polymer prepared from at least one C2 to C28 polymerizable hydrocarbon, said polymer having a number average molecular weight in the range of from about 5,000 to about 500,000, with an ethylenically unsaturated C3 to C10 carboxylic acid material, using a free radical initiator, in the presence of an aromatic ester oil of the formula
4
wherein R1, R2, R3, R4, R5, and R6 are independently selected from the group consisting of hydrogen, COOR7, COOR8, COOR9, COOR10, COOR11, and COOR12, provided that no more than 5 of R1, R2, R3, R4, R5, and R6 are hydrogen, and R7, R8, R9, R10, R11, and R12 are independently selected from the group consisting of alkyl and alkylesters.
2. The process of claim 1, wherein the hydrocarbon polymer is a copolymer of ethylene with a C3 to C28 alpha olefin.
3. The process of claim 2 wherein the copolymer comprises from about 15 to about 90 weight percent ethylene and, correspondingly, from about 85 to about 10 weight percent of the alpha olefin.
4. The process of claim 2 wherein the C3 to C28 alpha olefin is propylene.
5. The process of claim 3 wherein the C3 to C28 alpha olefin is propylene.
6. The process of claim 1, wherein the copolymer is grafted with the unsaturated material by dissolving the copolymer in the aromatic ester and adding the unsaturated material and free radical initiator over about 0.1 to about 12 hours at a temperature of from about 25 C. to about 250 C.
7. The process of claim 6 wherein about 5 to 95% of the copolymer is dissolved in 95 to 5 wt. % of the aromatic ester to form a solution, the amount of the unsaturated material is about 0.05 to 10 wt. % based upon the weight of the solution, and the amount of the initiator is about 0.005 to 10 wt. % based on the weight of the solution.
8. The process of claim 7 further comprising, after the grafting step, the steps of adding about 40 to 500 wt. %, based upon the weight of the solution, of mineral or synthetic lubricating oil and then adding an amine sufficient to neutralize the acid and heating at 100 C. to 250 C. for 0.5 to 10 hours.
9. The process of claim 8, wherein the unsaturated material is maleic anhydride and the amine is N-(4-anilinophenyl)-3-aminobutanamide.
10. The process of claim 7, wherein the unsaturated material is a nitrogen-containing ethylenically unsaturated monomer.
11. The process of claim 10, wherein the nitrogen-containing monomer is selected from the group consisting of vinyl pyridines, vinyl pyrrolidones, vinyl imidazoles, and amine group-contining acrylates and methacrylates.
12. A dispersant-viscosity index improver prepared by a process comprising solution grafting a hydrocarbon polymer prepared from at least one C2 to C28 polymerizable hydrocarbon, said polymer having a number average molecular weight in the range of from about 5,000 to about 500,000, with an ethylenically unsaturated C3 to C10 carboxylic acid material, using a free radical initiator, in the presence of an aromatic ester oil of the formula
5
wherein R1, R2, R3, R4, R5, and R6 are independently selected from the group consisting of hydrogen, COOR7, COOR8, COOR9, COOR10, COOR11, and COOR12, provided that no more than 5 of R1, R2, R3, R4, R5, and R6 are hydrogen, and R7, R8, R9, R10, R11, and R12 are independently selected from the group consisting of alkyl and alkylesters.
13. The dispersant-viscosity index improver of claim 12, wherein the hydrocarbon polymer is a copolymer of ethylene with a C3 to C28 alpha olefin.
14. The dispersant-viscosity index improver of claim 13 wherein the copolymer comprises from about 15 to about 90 weight percent ethylene and, correspondingly, from about 85 to about 10 weight percent of the alpha olefin.
15. The dispersant-viscosity index improver of claim 13 wherein the C3 to C28 alpha olefin is propylene.
16. The dispersant-viscosity index improver of claim 14 wherein the C3 to C28 alpha olefin is propylene.
17. The dispersant-viscosity index improver of claim 12, wherein the copolymer is grafted with the unsaturated material by dissolving the copolymer in the aromatic ester and adding the unsaturated material and free radical initiator over about 0.1 to about 12 hours at a temperature of from about 25 C. to about 250 C.
18. The dispersant-viscosity index improver of claim 17 wherein about 5 to 95% of the copolymer is dissolved in 95 to 5 wt. % of the aromatic ester to form a solution, the amount of the unsaturated material is about 0.05 to 10 wt. % based upon the weight of the solution, and the amount of the initiator is about 0.005 to 10 wt. % based on the weight of the solution.
19. The dispersant-viscosity index improver of claim 18 wherein the process further comprises, after the grafting step, the steps of adding about 40 to 500 wt. %, based upon the weight of the solution, of mineral or synthetic lubricating oil and then adding an amine sufficient to neutralize the acid and heating at 100 C. to 250 C. for 0.5 to 1 hours.
20. The dispersant-viscosity index improver of claim 19, wherein the unsaturated material is maleic anhydride and the amine is N-(4-anilinophenyl)-3-aminobutanamide.
21. The dispersant-viscosity index improver of claim 18, wherein the unsaturated material is a nitrogen-containing ethylenically unsaturated monomer.
22. The dispersant-viscosity index improver of claim 21, wherein the nitrogen-containing monomer is selected from the group consisting of vinyl pyridines, vinyl pyrrolidones, vinyl imidazoles, and amine group-contining acrylates and methacrylates.