摘要:
Prodrugs containing an active drug molecule linked to a polyethylene glycol group, and a method of use thereof are described. Exemplary soluble ester prodrugs contain naproxen, triamcinolone acetonide, gancyclovir, taxol, cyclosporin, dideoxyinosine, trihydroxy steroids, and flurbiprofen molecules linked to polyethylene glycol (PEG) groups. Pharmaceutical compositions containing these prodrugs, and a method of using these esters for treating disease states or symptoms are also described.
摘要:
The invention relates to codrugs having improved properties, methods for preparing and administering them, and methods of formulating and administering the codrugs as pharmaceutical preparations. In certain embodiments, the codrugs can be locally administered to deliver the constituent biologically active compound in a sustained-release fashion, reducing systemic concentrations of the biologically active compound.
摘要:
Compositions for controlled release of one or more therapeutic agents where the composition is essentially free of excipients are disclosed. In particular, compositions comprising a HMG-CoA reductase inhibitor, particularly simvastatin, and a NSAID, such as a COX-2 inhibitor, particularly celecoxib, in which greater than 90% of the weight of the composition is made up of the HMG-CoA reductase inhibitor and NSAID are provided.
摘要:
The invention relates to codrugs having improved properties, methods for preparing and administering them, and methods of formulating and administering the codrugs as pharmaceutical preparations. In certain embodiments, the codrugs can be locally administered to deliver the constituent biologically active compound in a sustained-release fashion, reducing systemic concentrations of the biologically active compound.
摘要:
A codrug composition of at least two drug compounds covalently linked to one another via a labile bond to form a single codrug composition, or ionically linked to one another to form a single workings composition, and methods of use of the codrug for the treatment of various medical conditions. The codrug may be administered by itself or in the form of a bioerodible or nonbioerodible substance.
摘要:
The present invention provides pharmaceutical compositions for topical delivery comprising a suitable carrier and a codrug capable of penetrating, or being transported across, the dermis. The codrug according to the invention comprises a first constituent moiety linked to a second constituent moiety, wherein the second constituent moiety is the same as, or different from, the first constituent moiety. The first and second constituent moieties are so linked that they are easily transported into or across the dermis, into the skin, or into the blood or lymphatic system, and are reconstituted in vivo to form the first and second constituent moieties.
摘要:
The present invention provides pharmaceutical compositions for topical delivery comprising a suitable carrier and a codrug capable of penetrating, or being transported across, the dermis. The codrug according to the invention comprises a first constituent moiety linked to a second constituent moiety, wherein the second constituent moiety is the same as, or different from, the first constituent moiety. The first and second constituent moieties are so linked that they are easily transported into or across the dermis, into the skin, or into the blood or lymphatic system, and are reconstituted in vivo to form the first and second constituent moieties.
摘要:
The invention provides a compound comprising a first pharmacological moiety connected to at least a second pharmacological moiety through a physiologically labile linker, or a salt thereof. The invention also provides a method of reducing cardiovascular disease or cardiovascular disease-related conditions in an individual. The method involves administering to an individual with cardiovascular disease an effective amount of a compound, in which the compound has a first pharmacological moiety linked to a second pharmacological moiety, and the compound or either or both of the constituent pharmacological moieties acts to reduce, treat, or prevent cardiovascular disease. The compounds of the invention can be delivered in a drug delivery device.