CA2391923A1 - Solid carriers for improved delivery of active ingredients in pharmaceutical compositions - Google Patents

Solid carriers for improved delivery of active ingredients in pharmaceutical compositions Download PDF

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Publication number
CA2391923A1
CA2391923A1 CA002391923A CA2391923A CA2391923A1 CA 2391923 A1 CA2391923 A1 CA 2391923A1 CA 002391923 A CA002391923 A CA 002391923A CA 2391923 A CA2391923 A CA 2391923A CA 2391923 A1 CA2391923 A1 CA 2391923A1
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CA
Canada
Prior art keywords
agents
pharmaceutical composition
active ingredient
vaccine
sodium
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CA002391923A
Other languages
French (fr)
Other versions
CA2391923C (en
Inventor
Mahesh V. Patel
Feng-Jing Chen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Lipocine Inc
Original Assignee
Individual
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Publication date
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Application filed by Individual filed Critical Individual
Priority to CA2706113A priority Critical patent/CA2706113A1/en
Publication of CA2391923A1 publication Critical patent/CA2391923A1/en
Application granted granted Critical
Publication of CA2391923C publication Critical patent/CA2391923C/en
Anticipated expiration legal-status Critical
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S977/00—Nanotechnology
    • Y10S977/902—Specified use of nanostructure
    • Y10S977/904—Specified use of nanostructure for medical, immunological, body treatment, or diagnosis
    • Y10S977/906—Drug delivery
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S977/00—Nanotechnology
    • Y10S977/902—Specified use of nanostructure
    • Y10S977/904—Specified use of nanostructure for medical, immunological, body treatment, or diagnosis
    • Y10S977/927—Diagnostic contrast agent

Abstract

The present invention provides solid pharmaceutical compositions for improve d 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 acti ve ingredients, hydrophilic surfactant, lipophilic surfactants and triglyceride s. 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, nutrionals, cosmeceuticals and diagnostic agents.

Claims (38)

1. A pharmaceutical composition comprising a solid carrier, the solid carrier comprising a substrate and an encapsulation coat on the substrate, wherein the encapsulation coat comprises at least one pharmaceutical active ingredient and at least one hydrophilic surfactant.
2. 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.
3. The pharmaceutical composition of claim 1, wherein the active ingredient is hydrophobic and has an intrinsic aqueous solubility of less than about 1 mg/mL.
4. The pharmaceutical composition of claim 3, wherein the active ingredient is selected from the hydrophobic members of the group consisting of analgesics, anti-inflammatory agents, anthelmintics, 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, ~-Blockers, cardiac inotropic agents, corticosteroids, diuretics, anti-parkinsonian agents, gastro-intestinal agents, histamine receptor antagonists, keratolytics, lipid regulating agents, anti-anginal agents, cox-2 inhibitors, leucotriene inhibitors, macrolides, muscle relaxants, nutritional agents, opioid 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.
5. The pharmaceutical composition of claim 3, wherein the active ingredient is selected from the group consisting of acutretin, albendazole, albuterol, aminogluthemide, amiodarone, amlodipine, amphetamine, amphotericin B, atorvastatin, atovaquone, azithromycin, baclofen, beclomethsone, benezepril, benzonatate, betamethasone, bicalutanide, budesonide, bupropion, busulphan, butenafine, calcifediol, calciprotiene, calcitriol, camptothecan, candesartan, capsaicin, carbamezepine, carotenes, celecoxib, cerivistatin, cetrizine, chlorpheniramine, cholecalciferol, cilostazol, cimetidine, cinnarizine, ciprofloxacin, cisapride, clarithromycin, clemastine, clomiphene, clomipramine, clopidrogel, codeine, coenzyme Q10, cyclobenzaprine, cyclosporine, danazol, dantrolene, dexchlopheniramine, diclofenac, dicoumarol, digoxin, dihydro epiandrosterone, dihydroergotamine, dihydrotachysterol, dirithromycin, donepezil, efavirenz, eposartan, ergocalciferol, ergotamine, essential fatty acid sources, etodolac, etoposide, famotidine, fenofibrate, fentanyl, fexofenadine, finasteride, flucanazole, flurbiprofen, fluvastatin, fosphenytion, frovatriptan, furazolidone, gabapentin, gemfibrozil, glibenclamide, glipizide, glyburide, glymepride, griseofulvin, halofantrine, ibuprofen, irbesartan, irinotecan, isosorbide dinitrate, isotreinoin, itraconazole, ivermectin, ketoconazole, ketorolac, lamotrigine, lanosprazole, leflunomide, lisinopril, loperamide, loratadine, lovastatin, L-thryroxine, lutein, lycopene, medroxyprogesterone, mefepristone, mefloquine, megesterol acetate, methadone, methoxsalen, metronidazole, metronidazole, miconazole, midazolam, miglitol, minoxidil, mitoxantrone, montelukast, nabumetone, nalbuphine, naratiptan, nelfinavir, nifedipine, nilsolidipine, nilutanide, nitrofurantoin, nizatidine, omeprazole, oprevelkin, osteradiol, oxaprozin, paclitaxel, paricalcitol, paroxetine, pentazocine, pioglitazone, pizofetin, pravastatin, prednisolone, probucol, progesterone, pseudo-ephedrine, pyridostigmine, rabeprazole, raloxifene, refocoxib, repaglinide, rifabutine, rifapentine, rimexolone, ritanovir, rizatriptan, rosigiltazone, saquinavir, sertraline, sibutramine, sildenafil citrate, simvastatin, sirolimus, spironolactone, sumatriptan, tacrine, tacrolimus, tamoxifen, tamsulosin, targretin, tazarotene, telmisartan, teniposide, terbinafine, terzosin, tetrahydrocannabinol, tiagabine, ticlidopine, tirofibran, tizanidine, topiramate, topotecan, toremifene, tramadol, tretinoin, troglitazone, trovafloxacin, ubidecarenone, valsartan, venlafaxine, vertoporfin, vigabatrin, vitamin A, vitamin D, vitamin E, vitamin K, zafirlukast, zileuton, zolmitriptan, zolpidem, zopiclone, pharmaceutically acceptable salts, isomers, and derivatives thereof, and mixtures thereof.
6. The pharmaceutical composition of claim 1, wherein the active ingredient is a hydrophilic active ingredient having an apparent water solubility of at least about 1 mg/mL.
7. The pharmaceutical composition of claim 6, wherein the active ingredient is a hydrophilic drug, a cytokine, a peptidomimetic, a peptide, a protein, a toxoid, a serum, an antibody, a vaccine, a nucleoside, a nucleotide, a portion of genetic material, a nucleic acid, or a mixture thereof.
8. The pharmaceutical composition of claim 6, wherein the active ingredient is selected from the hydrophilic members of the group consisting of analgesics, anti-inflammatory agents, anthelmintics, 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, keratolytics, lipid regulating agents, anti-anginal agents, cox-2 inhibitors, leucotriene inhibitors, macrolides, muscle relaxants, nutritional agents, opioid 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.
9. The pharmaceutical composition of claim 8, wherein the active ingredient is selected from the group consisting of acarbose; acyclovir; acetyl cysteine;

acetylcholine chloride; alatrofloxacin; alendronate; alglucerase; amantadine hydrochloride; ambenomium; amifostine; amiloride hydrochloride; aminocaproic acid;
amphotericin B; antihemophilic factor (human); antihemophilic factor (porcine);
antihemophilic factor (recombinant); aprotinin; asparaginase; atenolol;
atracurium besylate; atropine; azithromycin; aztreonam; BCG vaccine; bacitracin;
becalermin;
belladona; bepridil hydrochloride; bleomycin sulfate; calcitonin human;
calcitonin salmon; carboplatin; capecitabine; capreomycin sulfate; cefamandole nafate;
cefazolin sodium; cefepime hydrochloride; cefixime; cefonicid sodium; cefoperazone;
cefotetan disodium; cefotoxime; cefoxitin sodium; ceftizoxime; ceftriaxone; cefuroxime axetil;
cephalexin; cephapirin sodium; cholera vaccine; chrionic gonadotropin;
cidofovir;
cisplatin; cladribine; clidinium bromide; clindamycin and clindamycin derivatives;
ciprofloxacin; clondronate; colistimethate sodium; colistin sulfate;
cortocotropin;
cosyntropin; cromalyn sodium; cytarabine; daltaperin sodium; danaproid;
deforoxamine;
denileukin diftitox; desmopressin; diatrizoate megluamine and diatrizoate sodium;
dicyclomine; didanosine; dirithromycin; dopamine hydrochloride; dornase alpha;
doxacurium chloride; doxorubicin; editronate disodium; elanaprilat;
enkephalin;
enoxacin; enoxaprin sodium; ephedrine; epinephrine; epoetin alpha;
erythromycin; esmol hydrochloride; factor IX; famiciclovir; fludarabine; fluoxetine; foscarnet sodium;
ganciclovir; granulocyte colony stimulating factor; granulocyte-macrophage stimulating factor; growth hormones- recombinant human; growth hormone- bovine;
gentamycin;
glucagon; glycopyrolate; gonadotropin releasing hormone and synthetic analogs thereof;
GnRH; gonadorelin; grepafloxacin; hemophilus B conjugate vaccine; Hepatitis A
virus vaccine inactivated; Hepatitis B virus vaccine inactivated; heparin sodium;
indinavir sulfate; influenza virus vaccine; interleukin-2; interleukin-3; insulin-human;
insulin lispro; insulin procine; insulin NPH; insulin aspart; insulin glargine;
insulin detemir;
interferon alpha; interferon beta; ipratropium bromide; isofosfamide; japanese encephalitis virus vaccine; lamivudine; leucovorin calcium; leuprolide acetate;
levofloxacin; lincomycin and lincomycin derivatives; lobucavir; lomefloxacin;
loracarbef; mannitol; measles virus vaccine; meningococcal vaccine;
menotropins;
mephenzolate bromide; mesalmine; methanamine; methotrexate; methscopolamine;
metformin hydrochloride; metroprolol; mezocillin sodium; mivacurium chloride;
mumps viral vaccine; nedocromil sodium; neostigmine bromide; neostigmine methyl sulfate;
neutontin; norfloxacin; octreotide acetate; ofloxacin; olpadronate; oxytocin;
pamidronate disodium; pancuronium bromide; paroxetine; pefloxacin; pentamindine isethionate;
pentostatin; pentoxifylline; periciclovir; pentagastrin; phentolamine mesylate;
phenylalanine; physostigmine salicylate; plague vaccine; piperacillin sodium;
platelet derived growth factor-human; pneumococcal vaccine polyvalent; poliovirus vaccine inactivated; poliovirus vaccine live (OPV); polymixin B sulfate; pralidoxine chloride;
pramlintide; pregabalin; propofenone; propenthaline bromide; pyridostigmine bromide;
rabies vaccine; residronate; ribavarin; rimantadine hydrochloride; rotavirus vaccine;
salmetrol xinafoate; sincalide; small pox vaccine; solatol; somatostatin;
sparfloxacin;
spectinomycin; stavudine; streptokinase; streptozocin; suxamethonium chloride;
tacrine hydrochloride; terbutaline sulfate; thiopeta; ticarcillin; tiludronate;
timolol; tissue type plasminogen activator; TNFR:Fc; TNK-tPA; trandolapril; trimetrexate gluconate;
trospectinomycin; trovafloxacin; tubocurarine chloride; tumor necrosis factor;
typhoid vaccine live; urea; urokinase; vancomycin; valaciclovir; valsartan; varicella virus vaccine live; vasopressin and vasopressin derivatives; vecoronium bromide; vinblastin;
vincristine; vinorelbine; vitamin B12; warfarin sodium; yellow fever vaccine;
zalcitabine; zanamavir; zolandronate; zidovudine; pharmaceutically acceptable salts, isomers and derivatives thereof; and mixtures thereof.
10. The pharmaceutical composition of claim 1, wherein the at least one hydrophilic surfactant comprises a non-ionic hydrophilic surfactant having an HLB value of at least about 10.
11. The pharmaceutical composition of claim 10, 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;
tocopherol polyethylene glycol succinates; sugar esters; sugar ethers; sucroglycerides;
and mixtures thereof.
12. The pharmaceutical composition of claim 1, wherein the at least one hydrophilic surfactant comprises an ionic surfactant.
13. The pharmaceutical composition of claim 12, 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, carnitines, oligopeptides, and polypeptides; glyceride derivatives of amino acids, oligopeptides, and polypeptides; acyl lactylates; mono-,diacetylated tartaric acid esters of mono-,diglycerides; succinylated monoglycerides; citric acid esters of mono-,diglycerides;
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.
14. The pharmaceutical composition of claim 1, wherein the substrate is a powder or a multiparticulate.
15. The pharmaceutical composition of claim 1, wherein the substrate is an additive, an active ingredient or a mixture thereof.
16. The pharmaceutical composition of claim 15, wherein the substrate is an additive comprising a solubilizer, an enzyme inhibitor, an anti-adherent, an anticoagulant, an antifoaming agent, an antioxidant, a binder, a bufferant, a chelating agent, a coagulant, a colorants or opaquants, a coolant, a cryoprotectant, a diluent or filler, a disintegrant or super disintegrant, a hydrogen bonding agent, a flavorant or desensitizer, an ion-exchange resin, a plasticizer, a preservative, a solvent, a sweetener, a thickener, or a mixture thereof.
17. The pharmaceutical composition of claim 15, wherein the substrate is a multiparticulate comprised of a granule, a pellet, a bead, a spherule, a beadlet, a microcapsule, a millisphere, a nanocapsule, a nanosphere, a microsphere, a platelet, a tablet or a capsule.
18. The pharmaceutical composition of claim 1, wherein the solid carrier is 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.
19. The pharmaceutical composition of claim 1, wherein the encapsulation coat further comprises at least one lipophilic additive selected from the group consisting of lipophilic surfactants and triglycerides.
20. The pharmaceutical composition of claim 19, wherein the lipophilic additive is selected from the group consisting of alcohols; polyoxyethylene alkylethers;
fatty acids; bile acids; glycerol fatty acid esters; acetylated glycerol fatty acid esters;
lower alcohol fatty acids esters; polyethylene glycol fatty acids esters;
polyethylene glycol glycerol fatty acid esters; polypropylene glycol fatty acid esters;
polyoxyethylene glycerides; lactic acid derivatives of mono/diglycerides; propylene glycol diglycerides;
sorbitan fatty acid esters; polyoxyethylene sorbitan fatty acid esters;
polyoxyethylene-polyoxypropylene block copolymers; transesterified vegetable oils; sterols;
sterol derivatives; sugar esters; sugar ethers; sucroglycerides; 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; and mixtures thereof.
21. The pharmaceutical composition of claim 19, wherein the lipophilic additive is a triglyceride selected from the group consisting of vegetable oils, fish oils, animal fats, hydrogenated vegetable oils, partially hydrogenated vegetable oils, synthetic triglycerides, modified triglycerides, fractionated triglycerides, and mixtures thereof.
22. 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.
23. The pharmaceutical composition of claim 1, wherein the composition is encapsulated, extruded, compressed, pelletized, coated, mixed, granulated, crystallized, lyophilized or molded.
24. 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 sub-lingual 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.
25. The pharmaceutical composition of claim 1, wherein the composition is formulated for immediate release, pulsatile release, controlled release, extended release, delayed release, targeted release, or targeted delayed release.
26. The pharmaceutical composition of claim 1, wherein the composition is formulated for oral, nasal, ocular, urethral, buccal, transmucosal, vaginal, topical or rectal delivery.
27. A method of administering an active ingredient to a mammal, the method comprising administering to the mammal a dosage form of the pharmaceutical composition of claim 1.
28. The method of claim 27, wherein the mammal is a human.
29. A pharmaceutical composition comprising a solid carrier, the solid carrier comprising at least one pharmaceutical active ingredient and at least one hydrophilic surfactant.
30. The pharmaceutical composition of claim 29, wherein the active ingredient is hydrophobic and has an intrinsic aqueous solubility of less than about 1 mg/mL.
31. The pharmaceutical composition of claim 29, wherein the active ingredient is a hydrophilic active ingredient having an apparent water solubility of at least about 1 mg/mL.
32. The pharmaceutical composition of claim 29, wherein the at least one hydrophilic surfactant comprises a non-ionic hydrophilic surfactant having an HLB value of at least about 10.
33. The pharmaceutical composition of claim 29, wherein the at least one hydrophilic surfactant comprises an ionic surfactant.
34. A method of administering an active ingredient to a mammal, the method comprising administering to the mammal a dosage form of the pharmaceutical composition of claim 29.
35. The method of claim 34, wherein the mammal is a human.
36. A pharmaceutical composition comprising a solid carrier, the solid carrier comprising at least one pharmaceutical active ingredient, at least one hydrophilic surfactant, and at least one lipophilic additive selected from the group consisting of lipophilic surfactants and triglycerides.
37. A method of administering an active ingredient to a mammal, the method comprising administering to the mammal a dosage form of the pharmaceutical composition of claim 36.
38. The method of claim 37, wherein the mammal is a human.
CA2391923A 1999-11-23 2000-11-22 Solid carriers for improved delivery of active ingredients in pharmaceutical compositions Expired - Lifetime CA2391923C (en)

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