.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 6,923,988

« Back to Dashboard

Details for Patent: 6,923,988

Title: Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
Abstract:The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutritional agents, cosmeceuticals and diagnostic agents.
Inventor(s): Patel; Mahesh V. (Salt Lake City, UT), Chen; Feng-Jing (Salt Lake City, UT)
Assignee: Lipocine, Inc. (Salt Lake City, UT)
Filing Date:May 01, 2003
Application Number:10/428,341
Claims: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, .beta.-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 and/or 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 mg/mL.

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, .beta.-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 caprylic/capric 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, .beta.-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 and/or 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 caprylic/capric 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, .beta.-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 and/or 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.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc