Coated drug delivery formulations

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Coated drug delivery formulations
Agent: Knobbe Martens Olson & Bear LLP - Irvine, CA, US
Inventor: Guru V. Betageri
Class: 424451000 (USPTO), A61K009/48 (Intl Class)
#20050152965
07/14/05
The invention relates generally to methods of making formulations for delivering biological agents to a patient. In one aspect, proliposomal drug-delivery systems for medicaments are provided. In another aspect, coated proliposomal formulations for poorly water soluble drugs, and methods for making the same, are provided. Certain embodiments of the present invention provide enhanced stability and bioavailability for pharmaceutical formulations.
[0002] 1. Field of the Invention
[0003] This invention relates generally to delivery systems for formulations comprising biologically active agents. In one embodiment, the invention relates to coated proliposomal formulations for poorly water soluble drugs.
SUMMARY OF THE INVENTION
[0008] Although the use of proliposomes and the use of enteric and non-enteric coatings are independently known in the art, the combination of a coating with a proliposomal formulation has not been disclosed. Surprisingly, when a coating of some embodiments of the current invention is combined with a proliposomal formulation of some embodiments of the current invention, drug delivery is enhanced. In many embodiments of the present invention, this novel and unexpected enhancement, which results from the unique combination of a coating and a proliposomal formulation, relates to increased drug absorption, stability and bioavailability.
[0009] In many embodiments of the current invention, the combination of a coating and a proliposomal formulation overcomes the disadvantages of drug delivery systems known in the prior art. For example, the utility of previous systems for orally administering labile pharmacological substances has been limited by the need to use toxic amounts of delivery agents, the instability of the systems, the inability to protect the active ingredient, the inability to effectively deliver drugs that are poorly water soluble or labile, the inadequate shelf life of the systems, the failure of the drug delivery systems to promote absorption of the active agent and the difficulties inherent to manufacturing the systems. Several embodiments of the present invention overcome one or more of these disadvantages.
[0010] In some embodiments, a formulation comprising a biologically active agent is produced by application of one or more enteric coatings. In other embodiments, a formulation comprising a biologically active agent is produced by application of one or more non-enteric coatings.
[0011] The term "enteric coating," as used herein, shall be given its ordinary meaning and shall also include materials that permit acid-labile drugs to remain active in the stomach upon oral ingestion such that the active ingredient is released and absorbed in the intestine. Enteric coatings materials are well known in the pharmaceutical art and include alginates, alkali-soluble acrylic resins, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, and the like. Enteric coatings may be used for oral routes of administration. Enteric coatings may be used for non-oral routes of administration. For example, enteric coatings may be useful for transdermal applications, as well as for other non-oral routes.
[0012] The term "acid-labile," as used herein, shall be given its ordinary meaning and shall also include drugs, compositions, or materials (e.g., coating materials) that degrade in acidic environments, dissolve in acidic environments, are unstable in acidic environments, and/or are inactivated in acidic environments.
[0013] The term "non-enteric coating," as used herein, shall be given its ordinary meaning, and as such, includes acid-labile materials and/or materials that degrade in the stomach, or other acidic environments. Non-enteric coatings are useful for both oral and non-oral routes of administration.
[0014] Several embodiments of the current invention are particularly advantageous because they offer a simple and inexpensive system to facilitate the administration of medicaments and other agents. In many embodiments, a drug delivery system according to some embodiments of the invention enhances the stability and bioavailability of biologically active agents.
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