Delivery systems for hydrophobic drugs
First Claim
Patent Images
1. 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.
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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.
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Citations
25 Claims
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1. A carrier system for a hydrophobic drug which comprises:
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(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. - View Dependent Claims (2, 3, 4, 5, 6)
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7. A pharmaceutical composition comprising:
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(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. - View Dependent Claims (8)
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9. 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.
- 10. 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.
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11. A pharmaceutical composition comprising:
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(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. - View Dependent Claims (25)
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12. A pharmaceutical composition comprising:
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(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.
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13. A pharmaceutical composition comprising:
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(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.
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14. A pharmaceutical composition comprising:
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(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.
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15. 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).
- 16. 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).
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20. 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).
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21. 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).
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22. A pharmaceutical composition comprising:
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(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.
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Specification