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Enteric solid oral dosage form of bisphosphonate containing a chelating agent

A bisphosphonate oral agent and bisphosphonate technology, applied in the field of bisphosphonate oral dosage forms, can solve problems such as abnormal deposition of calcium and phosphate, poor patient compliance, and complicated patients, and achieve relief of upper gastrointestinal effects of tract stimulation, increased compliance, simplified treatment

Inactive Publication Date: 2007-05-02
THE PROCTER & GAMBLE COMPANY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 2. Conditions that cause or lead to abnormal deposition of calcium and phosphate in the body
These dosing instructions can be complicated and inconvenient for the patient, which can lead to poor patient compliance

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment I

[0131] Enteric-coated tablets containing risedronate and EDTA

[0132] Preparation of tablets comprising risedronate and ethylenediamine by preparing a coating composition together with compressed tablets comprising risedronate and ethylenediaminetetraacetic acid and then applying the coating composition to the tablets Enteric-coated tablets of tetraacetic acid.

[0133] An enteric coating composition in the form of a coating is prepared, each tablet comprising the following excipients:

[0134] A. Enteric coating suspension

[0135] Element:

[0136] Eudragit L 30 D-55  (wet basis) 143.3mg

[0137] (manufactured by Rhm Pharma GmbH and Co.KG, Darmstadt, Germany)

[0138] Triethyl citrate 6.45mg

[0139] Talc 21.5mg

[0140] Red Iron Oxide 0.22mg

[0141] Simethicone emulsion (30%) 0.43mg

[0142] Polysorbate 80 0.43mg

[0143] Purified water 307.7mg

[0144] Enteric coatings were prepared as follows:

[0145] Pigment suspensions were prepared by adding polysorbat...

Embodiment II

[0162] Enteric-coated tablet containing risedronate and EDTA

[0163] Enteric-coated tablets containing risedronate sodium were prepared using a method similar to that described in Example I as follows.

[0164] A coating composition in the form of a coating is prepared, each tablet comprising the following excipients:

[0165] Element:

[0166] Acryl-EZE (manufactured by Colorcon, Inc., West Point, Pa.) dry solid 200mg

[0167] Purified water 950mg

[0168] A coating weight of 40% weight gain was obtained for the tablets by conventional pan coating methods, the tablets contained 150 mg risedronate and 75 mg EDTA, resulting in a final oval tablet weight of 500 mg. The composition of each tablet is as follows:

[0169] Active ingredient:

[0170] Risedronate Sodium 150mg*

[0171] Chelating agent:

[0172] Disodium edetate 75mg

[0173] excipient

[0174] Mannitol 100mg

[0175] Starch 1500 159mg

[0176] Silica 1mg

[0177] Stearic acid 15mg

[0178] *This amount is...

Embodiment III

[0180] Enteric-coated tablet containing risedronate and EDTA

[0181] Preparation of tablets comprising risedronate and ethylenediamine by preparing a coating composition together with compressed tablets comprising risedronate and edetate and then applying said coating composition to said tablets Enteric-coated tablets of tetraacetic acid.

[0182] An enteric coating composition in the form of a coating is prepared, each tablet comprising the following excipients:

[0183] A. Enteric coating suspension

[0184] Element:

[0185] Eudragit L 30 D-55  (wet basis) 47.8mg

[0186] (manufactured by Rhm Pharma GmbH and Co.KG, Darmstadt, Germany)

[0187] Triethyl citrate 2.15mg

[0188] Talc 7.17mg

[0189] Red Iron Oxide 0.07mg

[0190] Simethicone emulsion (30%) 0.14mg

[0191] Polysorbate 80 0.14mg

[0192] Purified water 102.6mg

[0193] Enteric coatings were prepared as follows:

[0194] Pigment suspensions were prepared by adding polysorbate 80, ground iron oxide ...

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PUM

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Abstract

Oral dosage forms of a bisphosphonate comprised of a safe and effective amount of a pharmaceutical composition comprising a bisphosphonate, a chelating agent, and, means for effecting delayed release of the bisphosphonate and the chelating agent in the lower gastrointestinal tract provide delivery of the pharmaceutical composition to the lower gastrointestinal tract of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between bisphosphonates and food or beverages, which interaction results in the bisphosphonate active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, the present invention effects delivery of the bisphosphonate and the chelating agent to the lower GI tract, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.

Description

field of invention [0001] The present invention relates to an oral dosage form of a bisphosphonate consisting of a safe and effective amount of a pharmaceutical composition comprising a bisphosphonate, a chelating agent for administering the bisphosphonate active ingredient with food or drink, a A method for affecting the delayed release of bisphosphonates and chelating agents in the lower gastrointestinal tract, and one or more pharmaceutically acceptable excipients. The oral dosage forms of the present invention provide delivery of the pharmaceutical composition into the lower gastrointestinal tract of a mammalian subject and provide drug-effective absorption of the bisphosphonate with or without administration with food or beverage. The invention also relates to methods of treatment or prevention of disorders characterized by abnormal calcium and phosphate metabolism comprising administering an oral dosage form as described herein to a human or other mammal in need thereof....

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/675A61K31/00A61K9/28A61K9/00
CPCA61K9/2013A61K9/2086A61K9/2846A61K9/2009A61P19/00A61P19/02A61P19/08A61P19/10A61P3/14A61P35/00A61P35/04A61P5/18A61P5/20A61P5/22A61K9/20
Inventor R·J·当塞罗D·E·小布吉奥
Owner THE PROCTER & GAMBLE COMPANY
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