Pourable liquid vehicles

Details Pourable liquid vehicles Pourable liquid vehicles

2000-09-11

2003-01-07

Page, Thurman K. (Department: 1615)

Drug, bio-affecting and body treating compositions

Designated organic nonactive ingredient containing other...

Solid synthetic organic polymer

C424S485000, C424S486000

Reexamination Certificate

active

06503955

ABSTRACT:

TECHNICAL FIELD
Concentrated levels of polyoxyalkylene block copolymers are useful in vehicles incorporated into products that are designed to deliver compositions, materials and substances to moistened surfaces and aqueous environment. Acquiring moisture during use, the vehicle becomes sufficiently transformed from a liquid to a gel-like form that provides a benefit to the user. For example, mucosal surfaces of the body contain sufficient water to allow the pourable liquid vehicle comprising concentrated polyoxyalkylene block copolymers to be effectively delivered to the desired site wherein the accompanying compositions, materials and substances tenaciously adhere to the moistened surfaces and resist dissolution or erosion by water or biological fluid. Such uses include, but are not limited to the delivery of personal health care compositions, formulations and compounds including, but not limited to, pharmaceuticals (OTC and prescription), nutrients and the like.
In the discipline of pharmaceutical compositions there are a wide variety of dosage forms. Examples include tablets, capsules, elixirs, syrups, liquid-filled capsules, suspensions, coated tablets or capsules for administration by mouth; gels, rinses, dentifrices, lozenges, sprays, medicated lollipops, liquid filled capsules for intra-oral administration; gels, suspensions or solutions for intra-ocular or intra-aural administration; suppositories and douches or enemas for intra-rectal or vaginal administration; and creams, ointments, gels, lotions and patches for topical application on the skin and scalp; and liquid suspension or solutions for injection by syringe, nasal gels, solutions, or suspensions for application into the nose with special applications or sprayers.
The majority of these compositions are in the physical form of a fluid having a viscosity ranging from pourable liquids to stiff gels. Pourable liquids are often preferred since they are in the best form to be administered. For example, only liquids, or perhaps low viscosity gels, can be injected through a syringe, or poured from a bottle into a medicine cup, or drawn up into a syringe or medicine dropper, or squeezed from a dropper bottle into the eye or ear, or atomized into the nasal cavities. In addition to the compatibility with pharmaceutical administration devices and with the mode of introduction into the body, it is often desirable for the composition to easily spread after application without the aid of manual action or devices. The eye drop compositions, for example, need to spread over the surface of the eye, as do swallowed liquids intended to coat the throat, esophagus, or stomach. This is similarly true of rectal enemas or vaginal douche compositions.
In many cases, however, pharmaceutical dosage forms in form of pourable liquids are not necessarily desirable since once administered, such pourable liquids are easily removed from the intended treatment site. In such circumstances the therapeutic advantage of the composition may be significantly diminished or even lost completely. It is appropriate, therefore, to surmise that for the purpose of being retained at the targeted site, it may be desirable for a particular pharmaceutical composition to be more viscous, even in the form of a gel that is not readily flowable. It is, however, difficult or even impossible to administer such a viscous composition to its intended site to do the most good. For example, serious injury could occur when attempting to spread a gel on the surface of one's eye using a finger or more elaborate applicators. More problematic is coating the stomach lining, as this site is simply not accessible using simple self-administer applicators.
There is, therefore, a need for pharmaceutical compositions that are “smart”; that is, capable of being administered in a pourable liquid that are converted or transformed after administration into a vehicle having sufficient viscosity to essentially remain at the targeted site. Such compositions require a built-in chemical or physical triggering mechanism(s) that respond to conditions after application in or on a surface including the body.
BACKGROUND OF THE INVENTION
Attempts to develop such compositions have been ongoing for a significant period of time. Examples of such compositions include intra-ocular dosage forms as disclosed in Edsman, K., Carlfors, J., Petersson, R.,
Rheological Evaluation of Poloxamer as an In Situ Gel for Ophthalmic Use
, European Journal of Pharmaceutics Vol. 6 pp.105-112 (1998) herein incorporated by reference. Compositions such as these are broadly described as primarily aqueous solutions of block co-polymer surfactants, other wise referred to as “poloxamers”, that are commonly known in the art. When formulated in water as somewhat concentrated solutions, or with water and co-solvents, the poloxamer solution remains as a pourable liquid. The most commonly reported example of this type of system consists of poloxamer 407 at concentrations ranging from about 10% to 35% by weight of the composition in water. These compositions are administered at room temperature as liquids. They form a gel upon reaching body temperature. The trigger for converting these compositions to a gel, therefore, is body heat.
In situ gelation of pharmaceutical compositions based on poloxamer that are biologically triggered are known in the art. For example Kim, C. K., Lee, S. W., Choi, H. G., Lee, M. K., Gao, Z. G., Kim, I. S., and Park, K. M.:
Trials of In Situ Gelling and Mucoadhesive Acetaminophen Liquid Suppository in Human Subjects
, International Journal of Pharmaceutics vol. 174, pp. 201-207 (1998) incorporated herein by reference. Kim et al. discloses liquid suppositories for enhancing absorption of the pain and fever relieving drug acetaminophen.
U.S. Pat. No. 5,256,396, issued Oct. 26, 1993, to Colgate Palmolive Company, incorporated herein by reference, describes similar compositions containing poloxamer 407 and water at specified concentrations. Other products utilizing bio-triggers include those comprising poloxamer 407 at ranges preferably 12% to 17%. When combined with pharmaceutically active agents, these compositions are injected into the gingival space between the root of a tooth and the gum.
Poloxamers represent a large family of polymers that vary in molecular weight as well as in the percentage or portion of the block copolymer that is considered hydrophobic. Compositions comprising other poloxamers from this family having similar liquid/gelling characteristics are somewhat predictable, lacking only in the understanding of the required concentration of poloxamer. While there is a large number of uses for such compositions, they all rely on the same general mechanism of temperature-induced gelation of aqueous poloxamer dispersions. Compositions known in the art are found to be inadequate, however, as the gel structure readily dissolves in aqueous environments.
SUMMARY OF THE INVENTION
The present invention covers pourable liquid vehicles used to deliver compositions, materials and substances to moistened surfaces and aqueous environments. The benefits of compositions formulated with such pourable liquid vehicles include retention of the compositions, materials and substances on the moistened surface. This in turn allow for effective delivery of a desired composition, material and substance in the vehicle that acts on targeted surface, resisting erosion or run-off even in an aqueous environment. Such pourable liquid vehicles have a number of utilities for delivery of all kinds of materials including but not limited to cleaning and treating surfaces of objects as well as biological or living organisms, including living creatures.
Another object of this invention is to utilize such pourable liquid vehicles to deliver health care compositions and materials and substances to living creatures, particularly mammals, and most particularly humans. Even another object of the present invention is to develop a method for effective delivery of health care compositions, materials and substances.
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