Cyclosporin-containing soft capsule compositions

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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A61K 3700

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active

055894550

ABSTRACT:
The present invention relates to a soft capsule composition containing a stable microemulsion concentrate which is more stable and suitable for the preparation of cyclosporin-containing soft capsules. More specifically, the present invention relates to a microemulsion concentrate containing cyclosporin as an active ingredient, polyethylene glycol as a cosurfactant, one component or a mixture of two or more selected from the group consisting of an esterified compound of fatty acid and primary alcohol, medium chain fatty acid triglyceride and monoglyceride as an oil component, and a surfactant having HLB value of 10 to 17 such as Nikkol HCO-50 or Tween 20, which is suitable for formulation into soft capsules and to a soft capsule composition containing said microemulsion concentrate. In the microemulsion concentrate according to the present invention, cyclosporin, polyethylene glycol, the oil component and the surfactant are present in the ratio of 1:0.1-10:1-10:1-10, preferably 1:0.5-8:2-6:2-8, by weight. The soft capsule preparation containing polyethylene glycol, ethyl linoleate, caprylic/capric acid triglyceride, oleic acid monoglyceride, Nikkol HCO-50 or Tween 20 according to the present invention is highly stable during storage in comparison with the prior soft capsules containing ethanol, propylene glycol, transcutol, glycofurol, etc., as a cosurfactant, and provides an advantage in that the appearance and composition content of the soft capsule are not changed, and further that since the bioavailability of cyclosporin is about 4 times or more as high as that of the prior commercial products and pharmacokinetic properties of cyclosporin including difference between bioavailabilities in respective subjects are improved, the administration dosage, side effects and costs of the drugs are reduced.

REFERENCES:
patent: 4388307 (1983-06-01), Cavanak
patent: 4996193 (1991-02-01), Hewitt et al.
patent: 5051402 (1991-09-01), Kurihara et al.
patent: 5338761 (1994-08-01), Nakajima et al.
patent: 5342625 (1994-08-01), Haver et al.
patent: 5350741 (1994-09-01), Takada

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