Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Wearing apparel – fabric – or cloth
Reexamination Certificate
1998-04-14
2001-05-08
Dees, Jose' G. (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Wearing apparel, fabric, or cloth
C424S078020, C424S078040, C424S443000, C424S445000, C424S447000, C424S449000
Reexamination Certificate
active
06228381
ABSTRACT:
The invention relates to a presentation form for the application of pharmaceutical active compounds, pharmaceutical auxiliaries, pharmaceuticals and/or diagnostics, comprising a carrier and a preparation attached to the carrier, which is detachable from the carrier on contact with a liquid during the application and a [lacuna] for the production thereof.
EP 0064 841 A1 discloses a presentation form for bringing pharmaceutical agents into contact with body moisture, in which the pharmaceutical agent is contained in a soluble matrix, comprising, for example, a water-soluble polymer, and is applied to a strip as a film and dried.
The dried film comprising the pharmaceutical agent is relatively rigid and does not always dissolve sufficiently rapidly on contact with body moisture. When used in the eye, the dried hard film can also lead to injuries.
The embedding of pharmaceuticals in polymers of hydrophilic monomers in the form of polymer solutions and emulsions as a presentation form has been known for a long time, reference being made, by way of example, to German Patent Specification 26 36 559, Swiss Patent Specification 625 704 or, for use in the eye, German Offenlegungschrift 24 48 737.
By way of example, reference is made to EP 0507 224 A2, in which eye drops are prepared from an ophthalmic substance and a swellable polysaccharide and instilled into the eye, and swell after instillation.
EP 224 987 A discloses eye drops which contain a polymeric component in the form of soluble or insoluble hyaluronan or hylan and a medicament. The eye drops are present in an aqueous to viscoelastic solution and are instilled into the eye.
DE 24 41 191 A1 discloses a presentation form in which a dried active compound-containing individual dose is applied to a carrier, the carrier employed being plastic or glass, which do not absorb liquids.
WO 91/19480 discloses an active compound dose in the presentation form of a compressed, pressed and lyophilized shaped part, such as a tablet. Compression does improve the strength of the presentation form, but rapid rehydration is prevented by the high density. In addition, there is the danger of further contamination of the product by microorganisms during preparation due to the additional pressing of the active compound.
The manner of application of pharmaceuticals such as ophthalmological preparations in drop form and drop solutions of this type have a number of disadvantages, such as, in particular, inaccurate application due to the person applying them and the tolerability of the active compounds, pharmaceutical auxiliaries, pharmaceuticals and/or diagnostics according to the generic term is proposed, wherein the carrier is hydrophobic or hydrophobized and the preparation contains the pharmaceutical active compound, pharmaceutical auxiliary, pharmaceutical and/or diagnostic and a swellable hydrophilic or water-soluble hydrophilic polymer and is formed as a lyophilizate, the preparation being detachable from the carrier for the purpose of application by means of hydration of the preparation. Advantageous embodiments of the invention can be inferred from the characterizing features of subclaims
2
to
16
. To prepare the presentation form according to the invention, a process as claimed in claim
17
is proposed.
The application system developed according to the invention is preservative-free. As a presentation form, it is advantageously suitable for topical application. The hydrophilized preparation contains the pharmaceutical, auxiliary or the diagnostic embedded in a swellable or water-soluble polymer structure, which after wetting with liquid, in particular body fluid, such as mucus, blood, lacrimal fluid or a suitable medium, forms a gel which is automatically detached from the carrier and enters into active combination with the body as a viscous substance solution or substance suspension. For application, the carrier is held at the gripping end and the flexible end, to which the active compound is applied, is brought into contact with the desired body part. It is possible to apply the carrier containing the lyophilized preparation—virtually in the form of “dry drops”—in various ways, for example:
application of medication intra-, pre- and post-operatively
local application to mucous membranes
therapy of bacterial and viral infections and mycoses predetermined individual dose.
Compared with conventional methods of application of active compounds and auxiliaries and diagnostics, the presentation form according to the invention has the following advantages:
The dosage, for example, of ophthalmological preparations is more precise, because in each case only the amount of active compound for one application is accommodated on a carrier, and the deposition of the hydrated dispersion in the conjunctival sac can be controlled better by the user than instillation and counting of the drops from eye drop bottles.
Preservatives are not necessary, because the carriers are individually sterile-packed, and the packing is only opened immediately before use. Thus possible disadvantageous effects of preservatives, for example damage to the cornea, conjunctiva and Tenon's capsule, which is unavoidable in the case of addition of preservative to ophthalmological preparations, do not apply.
Because the lyophilizate is anhydrous during storage, the stability, especially of active compounds sensitive to hydrolysis, improves.
At the same time, the necessity of adjusting the pharmaceutical solutions to a pH optimal for stability, which as a rule is not physiologically optimal, does not apply. Thus the tolerability of the application of pharmaceuticals and other substances by means of the presentation form according to the invention is further improved.
The duration of release can be prolonged so that the frequency of use can be decreased under certain circumstances compared with conventional drops.
Due to the softness and flexibility of the carrier, the danger of injuries on contact of the presentation form with body parts, such as mucous membranes or the conjunctiva or cornea, which can occur as a result of applicatiors [sic] of conventional methods, such as, for example, pipette tips which consist of relatively solid material, is decreased. This is especially of importance in the case of older patients with an impaired fine motor system, who use the medication themselves.
According to the invention, by choice of the hydrophilic polymer it is possible to control the release of active compound within certain limits.
The invention is seen as the combination of three elements, namely the application of a drop of the solution of a hydrophilic polymer, which can contain pharmacologically active substances, to a hydrophobic carrier, and the preparation of an anhydrous lyophilizate in situ.
Only when these three subaspects are fulfilled at the same time are the aims and advantages according to the invention realized.
The following properties are uppermost here:
1. Rapid rehydration on contact with a liquid, in particular body fluid, such as lacrimal fluid, which is achieved by the hydrophilic polymer in which one or more pharmacologically active substances can be dissolved being present in the form of a highly porous lyophilizate.
2. The detachment of the carrier during rehydration and adhesion to a body part, for example to the conjunctiva, which is achieved by the combination of the hydrophilic polymer with the hydrophobic carrier.
3. The absence of preservatives and the stability of pharmaceuticals sensitive to hydrolysis, whose mutual requirement is freedom from water.
4. The decrease in the danger of injury on contact with this soft flexible carrier.
5. The precise dosage [lacuna] the possibility of dose reduction in comparison with the application of liquid drops from individual and multi-dose containers.
According to the invention, the presentation form for the topical application of pharmaceutical and other substances is designed such that a solid, compact, but flexible optionally soft carrier is available for the preparation, and th
Diestelhorst Michael
Grunthal Sabine
Suverkrup Richard
Antonelli Terry Stout & Kraus LLP
Dees Jose' G.
Shelborne Kathryne E.
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