Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF2 Cites 14 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a pharmaceutical composition that can deliver drugs, particularly poly(amino acids) such as peptides and proteins, orally in a fast and effective way. The composition has a rapid disintegration time and a rapid dissolution rate, which allows the active ingredient to be absorbed quickly and achieve the desired therapeutic effect. The composition can be made without the need for an enteric coating or peptidase inhibitor, and can be used to treat disorders related to abnormal bone resorption or arthritic conditions. The composition can be in the form of a tablet or capsule with a hardness of between 3 Kp and 20 Kp. The invention also provides a method for manufacturing the pharmaceutical composition with a disintegration time of no more than 10 minutes and a dissolution time of no more than 20 minutes.

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pharmaceutical composition
  • Pharmaceutical composition
  • Pharmaceutical composition

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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
concentrationaaaaaaaaaa
weightaaaaaaaaaa
concentrationaaaaaaaaaa
Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com