Pharmaceutical composition

a technology of pharmaceutical compositions and compositions, applied in the field of pharmaceutical compositions, can solve problems such as insufficient protection

Inactive Publication Date: 2011-09-08
AZRIA MOISE +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0028]The present invention therefore provides a pharmaceutical composition that enables the successful delivery of drugs in a pharmaceutically effective amount, particularly poly(amino acids) such as peptides, peptidomimetics and proteins, e.g. hormones to a subject via oral administration to accomplish the desired therapeutic effect.
[0032]In particular, the present invention provides pharmaceutical compositions comprising a calcitonin as the active ingredient together with the delivery agent 5-CNAC, where the pharmaceutical composition is manufactured in such a way so as to provide improved oral bioavailability, e.g. satisfactory or optimal oral bioavailability for the calcitonin active ingredient.
[0035]It was within the scope of the present invention that it has surprisingly been found that faster disintegration of the pharmaceutical compositions of the present invention in a subject, e.g. the stomach, provides the best absorption characteristics for the active peptides and proteins, where major peptide or protein degradation occurs by pepsin or other enzymes. The present invention thus further provides a pharmaceutical composition capable of delivering a peptide or protein via oral administration without the need for an enteric coating or a peptidase inhibitor. In embodiments, therefore, the compositions of the invention are free of enteric coating or peptidase inhibitors, or both.
[0043]In another embodiment, the composition according to the invention additionally comprises a disintegrant, particularly a disintegrant selected from any superdisintegrant, such as a crospovidone or a povidone and / or another agent that decreases disintegration time, for example by effervescent and / or other means.

Problems solved by technology

However, because the compositions may deliver the active agent more efficiently than prior compositions, less amounts of active agent than those used in prior dosage unit forms or delivery systems can be administered to a subject while still achieving the same blood levels and / or therapeutic effects.
However, those approaches alone do not offer sufficient protection to achieve a satisfactory plasma level of the peptide and proteins, there still remains a need to provide alternative means for successfully delivering peptide and protein medicaments to a patient, whilst protecting them from chemical and enzymatic degradation in order to enable them to provide a therapeutic effect.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Pharmaceutical Composition 1

[0243]

IngredientAmount (mg)PercentSalmon calcitonin0.80.16Micronized 5-CNAC22845.6Avicel PH 102(E)24147.94Crospovidone, NF255Magnesium stearate50.3Total500

[0244]Salmon calcitonin, 5-CNAC and crospovidone were blended together in a first blending step. Avicel PH 102 was screened and added to the mixture and blended in a second blending step. Magnesium stearate was then added and the mixture was blended further in a final blending step. The final blend was compressed into a 500 mg tablet and evaluated in a Rhesus monkey. The results are shown in FIG. 5.

example 2

Alternative Pharmaceutical Composition (3 BATCHES)

[0245]The same composition as in Example 1 was made, i.e. a composition comprising:

IngredientAmount (mg)PercentSalmon calcitonin0.80.16Micronized 5-CNAC22845.6Avicel PH 102(E)24147.94Crospovidone, NF255Magnesium stearate50.3

[0246]However, in contrast to Example 1 Salmon calcitonin and Avicel PH 102 were blended in a first blending step. 5-CNAC and crospovidone were then added to the first blend in a second blending step. Finally, Magnesium Stearate was added in a final blending step.

[0247]The final blend was then compressed at 3 different compression levels to obtain 3 different batches of tablets each having a different hardness, in order to provide 3 different disintegration times:

[0248](i) 1 min 10 secs DT

[0249](ii) 5 mins 40 secs DT

[0250](iii) 8 mins 51 secs DT

example 3

Alternative Pharmaceutical Composition

[0251]A similar blend was made to that of Example 1, except that an amount of Cab-o-sil was added to form a composition comprising:

IngredientAmount (mg)PercentSalmon calcitonin0.60.12Micronized 5-CNAC22845.6Avicel PH 102(E)24147.94Crospovidone, NF255Cab-o-sil1.50.3Magnesium stearate51Total500

[0252]Salmon calcitonin, 5-CNAC and crospovidone were blended in a first blending step. Avicel and Cab-o-sil were screened and added in a second blending step. Finally, Magnesium stearate was added in a final blending step. The final blend was compressed into a 500 mg tablet. The incorporation of Cab-o-sil improved the compression profile of the tablet.

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Abstract

The present invention provides oral pharmaceutical compositions that enable the successful delivery of drugs in a pharmaceutically effective amount, particularly poly(amino acids) such as peptides, peptidomimetics and proteins, e.g. hormones to a subject via oral administration to accomplish the desired therapeutic effect. The oral pharmaceutical composition comprising a poly(amino acid) as the active ingredient, e.g. a peptide or protein, shows a rapid disintegration and / or dissolution such that the active ingredient is able to attain a therapeutic effect.

Description

[0001]This application is a 371 of PCT / US06 / 44642 filed Nov. 16, 2006 which claims benefit of U.S. Provisional Application No. 60 / 737,631, filed Nov. 17, 2005, which in its entirety is herein incorporated by reference.[0002]The present invention relates to a novel pharmaceutical composition for the oral delivery of pharmaceutical compounds, in particular poly(amino acids) including peptides or, alternatively, peptidomimetics.[0003]In particular, the present invention relates in an embodiment to a novel oral pharmaceutical composition containing a poly(amino acid), for the treatment of a disorder caused by abnormal bone resorption and / or to the treatment of an arthritic condition and to other subject matter.BACKGROUND TO THE INVENTION[0004]Hormones[0005]Poly(amino acids) which have been used or proposed to be used for pharmaceutical or veterinary purposes include, but are not limited to the following, including synthetic, natural or recombinant sources thereof: polypeptide hormones s...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/23A61K38/22A61P19/02A61P19/10G01N33/00
CPCA61K9/2027A61K38/23A61K31/198A61K9/2054A61K38/29A61P5/06A61P19/00A61P19/02A61P19/08A61P19/10A61K9/20A61K9/28A61K9/2013A61K9/2095
Inventor AZRIA, MOISEBATEMAN, SIMON DAVIDGHOSH, ANASUYA ASHOKLI, SHOUFENGROYCE, ALAN EDWARD
Owner AZRIA MOISE
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