Patent US6096338A successfully refreshed from Google Patents.
US6096338A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Delivery systems for hydrophobic drugs
Assignee: Catalent Pharma Solutions LLC
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Filing: 1997-06-27
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Granted: 2000-08-01
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Expires: 2017-06-27
Abstract
Abstract There is provided a carrier for hydrophobic drugs, and pharmaceutical compositions based thereon, which carrier comprises a digestible oil and a pharmaceutically acceptable surfactant component for dispersing the oil in vivo upon administration of the carrier, which comprises a hydrophilic surfactant, said surfactant component being such as not to substantially inhibit the in vivo lipolysis of the digestible oil.
Inventors
- 👤 Jonathan E. Lacy
- 👤 Jonathan K. Embleton
- 👤 Elizabeth A. Perry
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 21:24
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/4841; A61K9/4858; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/12; A61K47/14; A61K47/44
Claims Analysis
Total Claims: 38
Claim 1
Independent Claim
134 words
A carrier system for a hydrophobic drug which comprises: (a) a digestible oil; (b) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said surfactant comprising: (i) a hydrophilic surfactant component which substantially inhibits the in vivo livolysis of said digestible oil, and (ii) a lipophilic surfactant component capable of at least substantially reducing said inhibitory effect of said hydrophilic surfactant component, said lipophilic surfactant component being present in an amount sufficient to achieve the required counteracting of the lipolysis-inhibiting properties of said hydrophilic surfactant, said lipophilic surfactant component comprising one or more of oleic acid, a glyceryl mono-/di-caprylate surfactant and a glyceryl mono-/di-caprylate/caprate surfactant.
Claim 2
Dependent Claim
134 words
A carrier system for a hydrophobic drug which comprises: (a) a digestible oil; (b) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said surfactant comprising: (i) a hydrophilic surfactant component which substantially inhibits the in vivo livolysis of said digestible oil, and (ii) a lipophilic surfactant component capable of at least substantially reducing said inhibitory effect of said hydrophilic surfactant component, said lipophilic surfactant component being present in an amount sufficient to achieve the required counteracting of the lipolysis-inhibiting properties of said hydrophilic surfactant, said lipophilic surfactant component comprising one or more of oleic acid, a glyceryl mono-/di-caprylate surfactant and a glyceryl mono-/di-caprylate/caprate surfactant.
Claim 3
Dependent Claim
27 words
A carrier system according to claim 1 wherein said hydrophilic surfactant component comprises a castor oil or hydrogenated castor ethoxylate having an HLB value greater than 10.
Claim 4
Dependent Claim
18 words
A carrier system according to claim 1, wherein said hydrophilic surfactant component comprises a polyoxy-ethylene hydrogenated castor oil.
Claim 5
Dependent Claim
41 words
A carrier system according to claim 1, which comprises based on the weight thereof: (a) 25-45% by weight of said digestible oil, (b) 30-45% by weight of said hydrophilic surfactant component, and (c) 20-40% by weight of said lipophilic surfactant component.
Claim 6
Dependent Claim
21 words
A carrier system according to claim 1, wherein some or all of the digestible oil is replaced by said lipophilic surfactant.
Claim 7
Dependent Claim
27 words
A carrier system according to claim 1, wherein said hydrophilic surfactant component comprises a transesterification product of polyethylene glycol with glycerol esters of capric and caprylic acids.
Claim 8
Dependent Claim
70 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said pharmaceutical composition being in a liquid oral unit dosage form.
Claim 9
Dependent Claim
70 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said pharmaceutical composition being in a liquid oral unit dosage form.
Claim 10
Dependent Claim
14 words
A hard or soft capsule filled with a pharmaceutical composition according to claim 7.
Claim 11
Independent Claim
64 words
A method of improving the in vivo bioavailability of a hydrophobic drug from a pharmaceutical composition comprising the drug dispersed or dissolved in a digestible oil containing a hydrophilic surfactant which substantially inhibits the in vivo lipolysis of said digestible oil, wherein there is added to the composition a lipophilic surfactant capable of at least substantially reducing said inhibitory effect of said hydrophilic surfactant.
Claim 12
Independent Claim
64 words
A method of improving the in vivo bioavailability of a hydrophobic drug from a pharmaceutical composition comprising the drug dispersed or dissolved in a digestible oil containing a hydrophilic surfactant which substantially inhibits the in vivo lipolysis of said digestible oil, wherein there is added to the composition a lipophilic surfactant capable of at least substantially reducing said inhibitory effect of said hydrophilic surfactant.
Claim 13
Independent Claim
44 words
A method of substantially reducing the inhibitory effect of a hydrophilic surfactant on the in vivo lipolysis of a digestible oil in a drug carrier system comprising the digestible oil and hydrophilic surfactant which comprises adding a lipophilic surfactant to the drug carrier system.
Claim 14
Independent Claim
44 words
A method of substantially reducing the inhibitory effect of a hydrophilic surfactant on the in vivo lipolysis of a digestible oil in a drug carrier system comprising the digestible oil and hydrophilic surfactant which comprises adding a lipophilic surfactant to the drug carrier system.
Claim 15
Dependent Claim
88 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being selected from the group consisting of clomiphene citrate, danazol, ethinyl estradiol, medroxyprogesterone acetate, mestranol, methyltestosterone, norethisterone, norgestrel, estradiol, conjugated oestrogens, stanozolol, stibestrol, testosterone, and tibolone.
Claim 16
Dependent Claim
88 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being selected from the group consisting of clomiphene citrate, danazol, ethinyl estradiol, medroxyprogesterone acetate, mestranol, methyltestosterone, norethisterone, norgestrel, estradiol, conjugated oestrogens, stanozolol, stibestrol, testosterone, and tibolone.
Claim 17
Dependent Claim
64 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being testosterone.
Claim 18
Dependent Claim
64 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being testosterone.
Claim 19
Dependent Claim
64 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being estradiol.
Claim 20
Dependent Claim
64 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being estradiol.
Claim 21
Dependent Claim
69 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being a combination of progesterone and estradiol.
Claim 22
Dependent Claim
69 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being a combination of progesterone and estradiol.
Claim 23
Independent Claim
138 words
A method of preparing a pharmaceutical composition including a hydrophobic drug and a carrier system for said hydrophobic drug, comprising the steps of forming said carrier system by combining a digestible oil, a hydrophilic surfactant and a lipophilic surfactant, dissolving or dispersing said hydrophobic drug in said carrier system, said hydrophobic drug being rendered more bioavailable, by in vivo lipolysis of said digestible oil, said hydrophilic surfactant substantially inhibiting lipolysis of said digestible oil and said lipophilic surfactant substantially reducing said inhibitory effect of said hydrophilic surfactant, selecting said surfactants by determining in vitro the relative lipolysis of (a) said digestible oil, (b) said digestible oil and hydrophilic surfactant in combination, and (c) said digestible oil, hydrophilic surfactant and lipophilic surfactant in combination, so that (b) is substantially less than (a) and (c) is substantially more than (b).
Claim 24
Independent Claim
138 words
A method of preparing a pharmaceutical composition including a hydrophobic drug and a carrier system for said hydrophobic drug, comprising the steps of forming said carrier system by combining a digestible oil, a hydrophilic surfactant and a lipophilic surfactant, dissolving or dispersing said hydrophobic drug in said carrier system, said hydrophobic drug being rendered more bioavailable, by in vivo lipolysis of said digestible oil, said hydrophilic surfactant substantially inhibiting lipolysis of said digestible oil and said lipophilic surfactant substantially reducing said inhibitory effect of said hydrophilic surfactant, selecting said surfactants by determining in vitro the relative lipolysis of (a) said digestible oil, (b) said digestible oil and hydrophilic surfactant in combination, and (c) said digestible oil, hydrophilic surfactant and lipophilic surfactant in combination, so that (b) is substantially less than (a) and (c) is substantially more than (b).
Claim 25
Independent Claim
97 words
A method of preparing a pharmaceutical composition including a hydrophobic drug dissolved or dispersed in a carrier system, comprising the steps of forming said carrier system by combining a digestible oil and a hydrophilic surfactant component, dissolving or dispersing said hydrophobic drug in said carrier system, said hydrophobic drug being rendered more bioavailable, by in vivo lipolysis of said digestible oil, selecting said carrier system by determining in vitro the relative lipolysis of (a) said digestible oil and (c) said digestible oil and hydrophilic surfactant component in combination so that (c) is 50% or more of (a).
Claim 26
Independent Claim
97 words
A method of preparing a pharmaceutical composition including a hydrophobic drug dissolved or dispersed in a carrier system, comprising the steps of forming said carrier system by combining a digestible oil and a hydrophilic surfactant component, dissolving or dispersing said hydrophobic drug in said carrier system, said hydrophobic drug being rendered more bioavailable, by in vivo lipolysis of said digestible oil, selecting said carrier system by determining in vitro the relative lipolysis of (a) said digestible oil and (c) said digestible oil and hydrophilic surfactant component in combination so that (c) is 50% or more of (a).
Claim 27
Dependent Claim
34 words
A method according to claim 16, wherein said step of selecting said carrier system includes determining the relative lipolysis of (a) and (c) by comparing the acidity of pancreatin solutions of (a) and (c).
Claim 28
Dependent Claim
46 words
A method according to claim 17, wherein said pancreatin solutions comprise simulated intestinal fluids, each containing the same weight of said digestible oil and said hydrophilic surfactant component being present in (c) in the same ratio with said digestible oil as used in said carrier system.
Claim 29
Dependent Claim
40 words
A method according to claim 18, wherein said hydrophilic surfactant component includes a hydrophilic surfactant that substantially inhibits the in vivo lipolysis of said digestible oil, and a lipophilic surfactant that substantially reduces said inhibitory effect of said hydrophilic surfactant.
Claim 30
Dependent Claim
130 words
A pharmaceutical composition comprising a hydrophobic drug and a carrier system for said hydrophobic drug, said carrier system comprising a digestible oil, a hydrophilic surfactant and a lipophilic surfactant, said hydrophobic drug being dissolved or dispersed in said carrier system, said hydrophobic drug being rendered more bioavailable, by in vivo lipolysis of said digestible oil, said hydrophilic surfactant substantially inhibiting lipolysis of said digestible oil and said lipophilic surfactant substantially reducing said inhibitory effect of said hydrophilic surfactant said surfactants being selected by determining in vitro the relative lipolysis of (a) said digestible oil, (b) said digestible oil and hydrophilic surfactant in combination, and (c) said digestible oil, hydrophilic surfactant and lipophilic surfactant in combination, so that (b) is substantially less than (a) and (c) is substantially more than (b).
Claim 31
Dependent Claim
130 words
A pharmaceutical composition comprising a hydrophobic drug and a carrier system for said hydrophobic drug, said carrier system comprising a digestible oil, a hydrophilic surfactant and a lipophilic surfactant, said hydrophobic drug being dissolved or dispersed in said carrier system, said hydrophobic drug being rendered more bioavailable, by in vivo lipolysis of said digestible oil, said hydrophilic surfactant substantially inhibiting lipolysis of said digestible oil and said lipophilic surfactant substantially reducing said inhibitory effect of said hydrophilic surfactant said surfactants being selected by determining in vitro the relative lipolysis of (a) said digestible oil, (b) said digestible oil and hydrophilic surfactant in combination, and (c) said digestible oil, hydrophilic surfactant and lipophilic surfactant in combination, so that (b) is substantially less than (a) and (c) is substantially more than (b).
Claim 32
Dependent Claim
89 words
A pharmaceutical composition including a hydrophobic drug dissolved or dispersed in a carrier system, said carrier system comprising a digestible oil and a hydrophilic surfactant component, said hydrophobic drug being dissolved or dispersed in said carrier system, said hydrophobic drug being rendered more bioavailable, by in vivo lipolysis of said digestible oil, said carrier system being selected by determining in vitro the relative lipolysis of (a) said digestible oil and (c) said digestible oil and hydrophilic surfactant component in combination so that (c) is 50% or more of (a).
Claim 33
Dependent Claim
89 words
A pharmaceutical composition including a hydrophobic drug dissolved or dispersed in a carrier system, said carrier system comprising a digestible oil and a hydrophilic surfactant component, said hydrophobic drug being dissolved or dispersed in said carrier system, said hydrophobic drug being rendered more bioavailable, by in vivo lipolysis of said digestible oil, said carrier system being selected by determining in vitro the relative lipolysis of (a) said digestible oil and (c) said digestible oil and hydrophilic surfactant component in combination so that (c) is 50% or more of (a).
Claim 34
Dependent Claim
66 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being a sex hormone.
Claim 35
Dependent Claim
66 words
A pharmaceutical composition comprising: (a) a hydrophobic drug, and (b) a drug carrier system comprising: (i) a digestible oil, and (ii) a pharmaceutically acceptable surfactant for dispersing the oil in vivo upon administration of the carrier system, said surfactant comprising a hydrophilic surfactant component, and being such that it does not substantially inhibit the lipolysis of the digestible oil, said hydrophobic drug being a sex hormone.
Claim 36
Dependent Claim
31 words
A method as set forth in claim 9 or claim 10, wherein the lipophilic surfactant is selected from the group consisting of fatty acids and mono- and/or di-glycerides of fatty acids.
Claim 37
Dependent Claim
33 words
A method as set forth in claim 9 or claim 10, wherein the lipophilic surfactant is selected from the group consisting of oleic acid, a glyceryl mono-/di-caprylate surfactant and a glyceryl mono-/di-caprylate/caprate surfactant.
Claim 38
Dependent Claim
41 words
A pharmaceutical composition according to any one of claims 11, 12, 13, 14 or 22, wherein said pharmaceutical composition comprises from 0.1% to 50% by weight of said hydrophobic drug and from 50% to 99.9% by weight of said carrier system.
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 2003-08-01 | 2004-01-31 | 2004-08-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2007-08-01 | 2008-01-31 | 2008-08-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2011-08-01 | 2012-01-31 | 2012-08-01 | $7700.00 | Window Closed / Lapsed |