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Medicament with a delayed release of active ingredient
| Details |
Inventors: Seth, Pawan;
Assignee: Mepha AG Dornacherstrasse 114 (Aesch, CH)
Primary Examiner: Page; Thurman K.
Assistant Examiner:
Attorney, Agent or Firm: Birch, Stewart, Kolasch & Birch
In addition to the active ingredient, the capsules contain a nonionic surfactant consisting of a polyglycol ester or ether having hydrophilic and lipophilic portions, and an organic polymer which is capable of forming a free-flowing composition with the active ingredient and the surfactant. The essential point for the delay in release is the matching of the water-solubility of the active ingredient and the hydrophilic/lipophilic character (HLB value) of the surfactant as follows: PRETEXTREPLACED |
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DETAILED DESCRIPTION I claim: 1. A medicament exhibiting a delayed release of active ingredient in the form of hard gelatin capsules which comprises: an active ingredient; a surfactant ingredient which comprises polyglycol ethers, esters of mixtures thereof, which has both hydrophilic and lipophilic portions and is chosen based on the relative water solubility or water insolubility of said active ingredient, wherein said solubility or insolubility is defined as follows:
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water-insoluble
HLB value above 16;
sparingly soluble
HLB value between 10 and 16; and
water-soluble HLB value below 10.
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said surfactant ingredient having the following hydrophilipophilic balance (HLB) value, above 16 for an active ingredient which is insoluble or slightly soluble in water, between 16 and 10 for an active ingredient which is sparingly soluble in water, and less than 10 for an active ingredient which is soluble in water; and an organic polymer or polymers which form a homogeneous solution or suspension with said active ingredient and said surfactant ingredient, the solution or suspension being in free-flowing form below about 70. degree. C. , wherein said active ingredient is in an amount of about 1 to 60%, said surfactant ingredient is in an amount of about 30 to 90% and said organic polymer is in an amount of about 1 to 45% of the weight of the contents of the capsule. 2. A medicament as claimed in claim 1, wherein said surfactant ingredient is a polyoxyethylene glycol fatty acid ester a polyoxyethylene glycol fatty alcohol ether or a fatty acid ester of sorbitan etherified by polyoxyethylene glycol. 3. A medicament as claimed in claim 2, wherein said surfactant ingredient is the palmitostearate of a polyoxyethylene glycol having the following molecular weight: 4000, for an HLB value above 19; 1500, for an HLB value of 17; or 400, for an HLB value of 11 to 12; polyoxyethylene glycol 300-distearate for an HLB value of 9 to 10; the laurate, palmitate, stearate or oleate of sorbitan etherified by 4 mol of polyoxyethyene glycol, or a mixture of two or more of these compounds
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