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EP0179583A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

A system for enhancing the water dissolution rate and solubility of poorly soluble drugs

Assignee: Merck and Co Inc
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Filing: 1985-10-01
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Granted: —
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Expires: 2005-10-01
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Abstract

Abstract Novel anhydrous compositions comprise a poorly water-soluble drug and a surfactant having enhanced dissolution rate and solubility. The drug-surfactant ratio in the composition is such that dissolution and solubility of the drug are enhanced. The compositions disclosed herein are useful in the treatment of patients (human and veterinary) as well as domestically and in agriculture.

Inventors

  • 👤 David G. Pope
  • 👤 Paul K. Wilkinson

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-24 19:17
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/107; A61K9/1075; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/14; A61K47/16; A61K47/18; A61K47/186; A61K47/20; A61K47/22; A61K47/26; A61K47/28; A61K47/44; A61K9/14; A61K9/141; A61K9/145; A61K9/146

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 11 words
An anhydrous composition comprising a poorly water-soluble drug and a surfactant.
Claim 2
Dependent Claim 11 words
An anhydrous composition comprising a poorly water-soluble drug and a surfactant.
Claim 3
Dependent Claim 97 words
A composition as claimed in Claim 1 in which the drug is a B-blocker, antimicrobial agent, anti-inflammatory agent, non-steroidal anti-inflammatory agent, antihypertensive agent, sex hormone, muscle relaxant, antiasthma agent, antiemetic agent, antidepressant, diuretic, vasodilator or antiparasitic agent and the surfactant is a polysorbate, a polyoxyethylene polyol, sodium lauryl sulphate, sodium desoxycholate, a sorbitan, a polyoxyalkylated isostearyl alcohol, a polyoxyethylene alkyl ether, a polyoxyethylene polyol fatty acid ester, a polyoxyethylene fatty glyceride, a cocoamido alkyl betaine, a dioctyl sodium sulphosuccinate, an ethoxylated tallowate, a C-cetyl or C-decyl betaine, stearyl dimethyl benzyl ammonium chloride or an ether amine salt.
Claim 4
Dependent Claim 63 words
A composition as claimed in Claim 2 in which the drug is timolol, propanolol, bupranolol, cefoxitin, erythromycin, lincomycin, hydrocortisone, betamethasone, prednisolone, indomethacin, sulindac, diflunisal, methyldopa, clonidine, estrogen, androgen, progestin, cyclobenzaprine, baclofen, diazepan, theophyline, dyphyline, pipamazine, chlorpromazine, protriptyline, amitriptyline, aldactone, diuril, hydrochlorothiazide, ivermectin, thiabendazole, avermectin, abamectin, nitroglycerin or papaverine, and the surfactant is polysorbate 80, a polyoxyethylene polyol, sodium lauryl sulphate or sodium desoxycholate.
Claim 5
Dependent Claim 41 words
A composition as claimed in any preceding claim in which the ratio of the weight of drug to that of surfactant ranges from 1:0.05 to 1:20 and the drug-surfactant combination constitutes from 10 to 100% by weight of the total formulation.
Claim 6
Dependent Claim 30 words
A composition as claimed in Claim 4 in which the said ratio ranges from 1:1 to 1:10 and the said combination constitutes from 40 to 98% of the total formulation.
Claim 7
Dependent Claim 17 words
A composition as claimed in any preceding claim, for use in the treatment of a medical disorder.
Claim 8
Dependent Claim 29 words
The use of a composition as claimed in any one of Claims 1 to 5 in domestic or agricultural applications where the drug component is known for such use.
Claim 9
Dependent Claim 49 words
A process for preparing a composition as claimed in any one of Claims 1 to 5 comprising appropriately dissolving the drug into the surfactant at a temperature in the range from room temperature for liquid surfactants to temperatures no greater than 10°C above the melting point of solid surfactants.
Claim 10
Dependent Claim 38 words
The process as claimed in Claim 8 including the further step of dissolving the solution obtained in an aqueous or aqueous alkanolic solvent and evaporating to a dry product at a temperature in the range -30°C to +60°C.

References Cited (Backward Citations)

EP0012523A1 Cited

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