Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes
Patent
1985-02-25
1988-04-26
Griffin, Ronald W.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Liposomes
424456, 424460, 514801, 514963, 514965, A61K 950
Patent
active
047403756
ABSTRACT:
This disclosure recognizes the fact that the technology of making vesicles from lecithin and lecithin-like molecules, although well known and highly developed, is associated with problems of instability. It is known that vesicles coalesce, rupture and spill their contents long before the vesicle is used for its intended purpose.
It has been discovered and disclosed herein that the deterioration of the vesicle delivery system is due in part to the rupture of the bipolar lipid vesicle membrane by the contents of the core volume or by an external agent. For example, the more detergent-like the properties of the pharmacological agent within the vesicle core volume, the more pronounced will be the attack on the vesicle wall interior. These events in turn will lead to vesicle membrane rupture.
This disclosure sets forth the proper manufacturing techniques to achieve vesicle stability following the discovery and also discloses a large-scale experiment which fully establishes the function taking place microscopically in the true vesicle. The experiment designed to substantiate the discovery is one using visible sized dialysis bags to show that gelatinized pharmacological agents are capable of existing without disruption in the appropriate solutions. The dialysis bag could not be used in the administration of a pharmacological agent to a person but illustrates on a large-scale what takes place microscopically in the actual vesicle environment.
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Geho W. Blair
Lau John R.
Griffin Ronald W.
Technology Unlimited Inc.
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