COMPACTED SOLID DOSAGE FORM

Abstract

The present invention relates to dosage forms comprising a compressed blend of a biologically active ingredient, one or more polymers like a poly(a-hydroxy carboxylic acid) in which optionally is incorporated a glass transition modifying agent, and optional further ingredients, wherein the polymer or polymeric mixture has a specific glass transition temperature which causes the system to be in the glassy state at ambient conditions before administration and to be in the rubbery state under the physiological conditions to which the system is exposed after administration, resulting in pulsed release of said biologically active ingredient.

Claims

1. A compacted composition comprising one or more biologically active ingredients and one or more polymers wherein the polymer or polymeric mixture has a specific glass transition temperature at ambient conditions before administration and at physiological conditions after administration, resulting in pulsed release of said one or more biologically active ingredient(s).

2. A composition according to claim 1 further comprising a glass transition modifying agent.

3. A composition according to claim 2 wherein the glass transition modifying agent is a plasticizer or an anti-plasticizer.

4. A composition according to claim 1 wherein the composition is a compacted solid composition.

5. A composition according to claim 4 wherein the one or more polymers is poly(α-hydroxy carboxylic acid).

6. A composition according to claim 1 further comprising a water-soluble filler.

7. A composition according to claim 1 wherein the one or more biologically active ingredients is a vaccine or vaccine component.

8. A method of immunizing a patient against a disease comprising administering to said patient a therapeutically effective composition according to claim 1.

9. A composition according to claim 1 for the use as a medicine or for the use as a means for delivering a medicament to a patient.

Description

DESCRIPTION OF THE DRAWINGS

[0063] FIG. 1 shows a compact wherein the release of theophylline from non-heated mixed implants compressed at 7.9*10.sup.7 and 2.0*10.sup.8 Pa. All implants consisted of PLA (IV 0.2) and contained mannitol.

[0064] In more detail it is an example of a compact wherein the release of theophylline from mixed implants compressed at 7.9*10.sup.7 (O) and 2.0*10.sup.8 (Δ) Pa is shown. All implants consisted of 90.9% PLA (IV 0.2), 5.1% mannitol, 3.6% inulin, and 0.4% theophylline. The inulin and theophylline was a freeze-dried powder mixture. Compressed implants were oblong 6×2×2 mm and were submerged in 37° C., 100 mM PBS release medium in a shaking water bath.

[0065] FIG. 2 shows a compact wherein the release of theophylline from implants with freeze dried inulin/theophylline, mixed with mannitol and implants with physically mixed inulin/theophylline, without mannitol compressed at 2.0*10.sup.8 Pa. All implants consisted of PLA (IV 0.2).

[0066] In more detail it is an example of a compact wherein the release of theophylline from implants with freeze dried inulin/theophylline, mixed with mannitol (Δ) and implants with physically mixed inulin/theophylline, without mannitol (◯) compressed at 2.0*10.sup.8 Pa is shown.

[0067] All implants contained 90.9% PLA (IV 0.2). For one implant the polymer was mixed with 5.1% mannitol, 3.6% inulin, and 0.4% theophylline, where the inulin and theophylline was a freeze-dried powder mixture. For a second implant the polymer was mixed with 8.3% inulin and 0.8% theophylline, where the inulin and theophylline was a physically mixed powder. Compressed implants were oblong 6×2×2 mm and were submerged in 37° C., 100 mM PBS release medium in a shaking water bath.

[0068] FIG. 3 shows a compact wherein the release of dextran with an average molar mass of 1000, 12000, 150000, and 1100000 Da from non-heated mixed implants with freeze dried polyvinylpyrrolidone (K12)/dextran, mixed with mannitol compressed at 2.0*10.sup.8 Pa. All implants consisted of PLGA (50:50 lactic:glycolic acid, IV 0.2).

[0069] More detailed it is an example of a compact wherein the release of dextran from implants with freeze dried polyvinylpyrrolidone/dextran (average molar mass 1000 (◯), 12000 (Δ), 150000 (□), and 1100000 (⋄) Da), mixed with mannitol compressed at 2.0*10.sup.8 Pa is shown. All implants contained 90.9% PLGA (50:50 lactic:glycolic acid, IV 0.2). For all implants the polymer was mixed with 5.1% mannitol, 3.6%polyvinylpyrrolidone, and 0.4% dextran, where the dextran and polyvinylpyrrolidone was a freeze-dried powder mixture. Compressed implants were oblong 6×2×2 mm and were submerged in 37° C., 100 mM PBS release medium in a shaking water bath.