摘要:
A lipid represented by formula (I), wherein each of R?1 and R2¿ is an alkyl or alkenyl chain having between about 8 to about 24 carbon atoms; n = 1-20; L is selected from the group consisting of (i) -X-(C=O)-Y-CH¿2?-, (ii) -X-(C=O)-, and (iii) -X-CH2-, wherein X and Y are independently selected from oxygen, NH and a direct bond; and Z is a weakly basic moiety that has a pK of less than about 7.4 and greater than about 4.0 is described.
摘要:
Injectable depot compositions are provided that include a bioerodible, biocompatible polymer, an aromatic alcohol having miscibility in water of less than or equal to 7 wt.% at 25°C, in an amount effective to plasticize the polymer and form a gel therewith, and a beneficial agent. The composition may additionally contain an ester of an aromatic acid, or an aromatic ketone. The compositions are readily implanted beneath a patient's body surface by injection, as the aromatic alcohol not only facilitates solubilization of the polymer, but also acts as a thixotropic agent, substantially increasing the shear thinning behavior of the composition.
摘要:
A method of preparing liposomes to a selected particle size is described. In the method, a vesicle-forming lipid dissolved in a lipid solvent is hydrated with a second solvent to form a hydration mixture having greater than 10 and less than 50 weight percent of the lipid solvent. The target amount of lipid solvent in the lipid solvent is selected to obtain a desired particle size.
摘要:
A device for the transdermal administration of fluoxetine (10) at a therapeutically effective rate comprises: (a) a reservoir (12) containing a composition comprising an amount of a pharmaceutically acceptable salt of fluoxetine; (b) a backing (14) behind the body contacting-distal surface of the reservoir; and (c) means (16) for maintaining the reservoir in fluoxetine transmitting relation with a body surface or membrane.
摘要:
A device for the transdermal administration of fluoxetine (10) at a therapeutically effective rate comprises:
(a) a reservoir (12) containing a composition comprising an amount of a pharmaceutically acceptable salt of fluoxetine; (b) a backing (14) behind the body contacting-distal surface of the reservoir; and (c) means (16) for maintaining the reservoir in fluoxetine transmitting relation with a body surface or membrane.
摘要:
An electrotransport agent delivery device (10) for delivering a therapeutic agent through intact skin, and a method of operating same, is provided. The device applies a pulsing electrotransport current wherein current pulses have a magnitude above a critical level (Ic) at which the skin is transformed into a higher electrotransport delivery efficiency (E) state. Most preferably the length of the applied current pulses is at least 5 msec and preferably at least 10 msec.
摘要:
A liposomal composition and a method of using the same for achieving intracellular delivery of a liposome-entrapped agent is described. The liposomes are composed of a pH sensitive lipid and include a targeting ligand to direct the liposomes to a target cell. The liposomes also include a stabilizing component, such a polymer-derivatized lipid, where the polymer is attached to the lipid by a releasable linkage. Administration of the liposomes results in cellular internalization and destabilization of the liposome for intracellular delivery of the entrapped agent.
摘要:
Skin patches (20) having a microprojection array (10), a reservoir (18) containing an antigenic agent and an immune response augmenting adjuvant, and methods of using same to vaccinate animals (e.g., humans) is disclosed. In a preferred embodiment, the microprojection arrays (10) are composed of a photoetched and micro-punched titanium foil (14). The microprojections (12) are coated with a liquid formulation containing a vaccine antigen and an adjuvant such as glucosaminyl muramyl dipeptide, dried, and applied to skin of the animal to be vaccinated using an impact applicator. The microprojections (12) create superficial pathways through the stratum corneum to facilitate permeation of antigenic agent and adjuvant. Antigen dose and depth of penetration can be controlled. This technology has broad applicability for a wide variety of therapeutic vaccines to improve efficacy, and convenience of use.