Biconvex rapidly disintegrating dosage forms

Details Biconvex rapidly disintegrating dosage forms Biconvex rapidly disintegrating dosage forms

1998-12-03

2001-05-01

Spear, James M. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

C424S465000, C424S485000, C424S486000, C424S488000, C424S439000, C424S441000, C514S770000, C514S772300, C514S773000, C514S774000, C514S776000, C514S777000, C514S779000, C514S780000, C514S781000, C514S782000, C514S783000

Reexamination Certificate

active

06224905

ABSTRACT:

The present invention relates to a process of preparing solid rapidly disintegrating dosage forms shaped as a biconvex tablets having symmetrical top and bottom surfaces, and to dosage forms obtainable thereby.
Solid rapidly disintegrating dosage forms loaded with a predetermined quantity of an active ingredient are known from GB-A-1,548,022 (U.S. Pat. No. 4,305,502). These solid dosage forms comprise a porous network of a matrix material carrying an active ingredient, the matrix material consisting of a water-soluble or a water-dispersable carrier material. The solid dosage forms are prepared by freeze-drying or lyophilization of the solvent from a frozen solution or suspension of the matrix material and the active ingredient.
Various improvements for preparing dosage forms by lyophilization have been developed. GB-A-2,111,423 and U.S. Pat. No. 4,371,516 disclose such methods of preparing solid dosage forms which are rapidly disintegrated by water and in which a network of matrix material carries a predetermined amount of an active ingredient, particularly a pharmaceutical substance. Such dosage forms find many applications, particularly where it is desired to administer, dispense or otherwise utilise an active ingredient in predetermined unit quantities. For example, certain active ingredients which are used in solution or suspension form, but which are difficult or hazardous to transport or store in such form, may be converted into a solid form which can be added by the user to an aqueous medium to produce the desired solution or dispersion containing a predetermined amount of the active ingredient. Further, the active ingredient may be a reagent which can be added to a known amount of aqueous liquid to produce a standardised liquid composition which then can be used, for example, in chemical analysis. Further, the active ingredient may be a diagnostic compound which has to be added to a biological sample (e.g. blood, urine) and thus allows one to determine the amount of a particular constituent present in the sample. Preferably, however, the active ingredient is a drug substance for human or veterinary use. Rapidly dissolving solid drug dosage forms are particularly suitable for oral administration. When orally administered they generally disintegrate rapidly in the mouth (e.g. within one or two seconds) and thus the dosage form is a particularly advantageous means for administering drugs to humans and animals. Such dosage forms can be used as alternatives to conventional tablets, pills or capsules, particularly for patients—humans and animals alike—who have difficulty in swallowing these conventional dosage forms. U.S. Pat. No. 4,642,903 teaches a procedure for preparing a freeze-dried foam dosage form using conventional lyophilization techniques which results in rapidly dissolving pharmaceutical dosage forms.
WO-93/23017 addresses a problem intrinsic to conventional lyophilization methods, namely the lack of uniform porosity in the lyophilized product. Uniform porosity in a lyophilized product is critical for post-loading a placebo or unloaded dosage form with an active ingredient. WO-93123017 concerns a method of producing a dosage form that will avoid cracking and meltback, has adequate strength, and porosity and exhibits a fast speed of dissolution.
Other methods for the preparation of solid dosage forms which rapidly disintegrate in the mouth, namely solid state dissolution techniques are disclosed in U.S. Pat. No. 5,039,540, U.S. Pat. No. 5,215,756, U.S. Pat. No. 5,330,764. and U.S. Pat. No. 5.298,261.
GB-2,119,246 concerns a process of preparing solid dosage forms using molds having a side wall or walls diverging outwardly from the base and making an angle of at least 5° at the surface of the composition. When lyophilizing under-filled molds of this type, one obtains solid shaped articles which have a more even thickness and thus are flatter than articles obtained from underfilled molds with side walls perpendicular to the base.
Solid dosage forms as provided by the prior art are used to deliver predetermined amounts of active ingredients. Since the administration of such products is associated with many risks, there is a need to package them adequately, e.g. in blister packs, and to bestow an identity on them.
The packaging of solid rapidly disintegrating dosage forms prepared according to prior art methods, especially on a large industrial scale, is associated with a number of particular problems. First, the friability of such dosage forms seriously constrains the methods by which they can be transported and handled. Consequently, any reduction in the friability of solid rapidly disintegrating dosage forms will greatly enhance their industrial utility by relaxing the production constraints. A second problem which directly relates to the shape of solid rapidly disintegrating dosage forms prepared according to prior art methods concerns the fact that the top and bottom surfaces of the dosage forms often are not symmetrical. Usually the bottom will be a flat surface more or less perpendicular to the side wall or walls of the dosage form, whereas the top surface may be concave or flat, depending upon the extent to which the molds are filled. Dosage forms in which top and bottom are distinct have the disadvantage that they may call for process steps to orient the dosage forms prior to filling them in blister packs (the process involves detecting each individual form's orientation, and selecting and reversing those forms that have the undesired orientation).
The present invention provides a single solution to all these problems, consisting of imparting a symmetrical convex top and bottom surface to solid rapidly disintegrating dosage forms. First, this results in dosage forms with less acute angles between side wall or walls and top or bottom surfaces which reduces the friability of the dosage forms. The symmetry further means that there is not any longer a distinction between bottom and top of a dosage form once it is removed from its mold. The biconvex shape has the further advantage that the dosage forms can easily be arranged to lie on one of their convex surfaces by gently shaking them. In addition, they can easily be picked up, either during production and packaging, or later by the patient or the person administering the dosage form.
The biconvex shape of the solid dosage forms prepared according to the present invention also serves to distinguish them from other prior art dosage forms and thus may assist in preventing errors by physicians, pharmacists or by the end-users, the patients in the administration of medicines loaded onto biconvex-shaped dosage forms.


REFERENCES:
patent: 4758598 (1988-07-01), Gregory
patent: 4792448 (1988-12-01), Ranade
patent: 5516530 (1996-05-01), Lo et al.
patent: 2 111 423 (1983-07-01), None
patent: 93/23017 (1993-11-01), None
patent: 95/09608 (1995-04-01), None

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