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Phenylephrine pharmaceutical formulations and compositions for transmucosal absorption

A technology of phenylephrine and composition, which is applied in the direction of drug combination, drug delivery, medical preparations containing active ingredients, etc., and can solve problems such as difficult to arouse interest and nasal cavity irritation

Inactive Publication Date: 2011-01-05
SCHERING PLOUGH HEALTHCARE PRODUCTS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the nasal, rectal, and ocular mucosa offer some advantages, marginal patient acceptability makes them receptive to topical rather than systemic drug administration
In particular, the potential for irritation and irreversible damage to the nasal cavity with long-term use makes it of little interest as a method of administering several doses when effective systemic administration of phenylephrine is required

Method used

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  • Phenylephrine pharmaceutical formulations and compositions for transmucosal absorption
  • Phenylephrine pharmaceutical formulations and compositions for transmucosal absorption
  • Phenylephrine pharmaceutical formulations and compositions for transmucosal absorption

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0145] Orally disintegrating tablet dosage form

[0146] The following table shows representative formulations of compositions of the invention in the form of orally disintegrating tablets.

[0147] Table 2

[0148] Element

[0149] Magnesium stearate

[0150] The dosage form is prepared by charging Phenylephrine HCl, Avicel PH101 and Povidone into a granulator and mixing. The mixture is then granulated with water and passed through a sieve, eg 8 mesh. The granules are then dried, for example by using a tray drier, and the dried granules are milled through a screen of appropriate size. The granules are then mixed with selected excipients and compressed into tablets.

Embodiment 2

[0152] Softgel capsule dosage form

[0153] The following table shows representative formulations of compositions of the present invention in the form of softgel capsules.

[0154] table 3

[0155] Element

[0156] The formulation was prepared by weighing PEG 400 and water and mixing well with a mixer. Then add phenylephrine HCl and mix until all phenylephrine is dissolved. The composition is then filled into soft gel capsules.

Embodiment 3

[0158] buccal tablet dosage form

[0159] The table below shows representative formulations of compositions of the invention in the form of buccal attach tablets having a diameter of about 7 mm and a hardness of 6-8 kP (kiloPascals).

[0160] Table 4

[0161]

[0162] The tablet is prepared by compressing a tablet containing from about 1 to about 75 mg of phenylephrine or a pharmaceutically acceptable salt thereof and from about 90 to about 400 mg of an excipient such as a bioadhesive polymer using a rotary tablet machine. Magnesium stearate as a lubricant, croscarmellose sodium as a superdisintegrant, granulated sugar (such as dextrose, polydextrin, mannitol, etc.), as an artificial sweetener and artificial flavoring The tablet mixture of sucralose is directly compressed.

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Abstract

Pharmaceutical compositions comprising phenylephrine or a pharmaceutically acceptable salt thereof and methods for administering the pharmaceutical compositions wherein the composition is formulated for systemic absorption of phenylephrine that avoids first pass metabolism. The compositions of the invention are formulated to be applied to oral mucosa of an animal to allow for enhanced systemic delivery of therapeutically active form of phenylephrine.

Description

technical field [0001] The identification or discussion of any reference in this section or any part of this specification shall not be construed as an admission that such reference is available as prior art to the present application. Background technique [0002] Oral administration is the most preferred route of systemic drug administration. However, oral administration of certain drugs can lead to excessive presystemic metabolism of the drug due to hepatic first-pass metabolism and enzymatic metabolism in the intestinal wall. This excessive presystemic metabolism significantly reduces the effective amount of drug that is ultimately absorbed into the bloodstream and exerts its therapeutic effect. The transmucosal route of drug delivery (i.e., the linings of the nose, rectum, eyes, and mouth) offers advantages over oral drug delivery in that it avoids the first-pass effect and presystemic clearance within the intestinal wall, and enables Accelerates absorption into the b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/137
CPCA61K9/006A61K9/2054A61K9/205A61K9/0053A61K9/4866A61K9/2018A61K9/2027A61K9/0056A61K9/0058A61K31/137A61P11/00A61P11/02A61P29/00A61P37/08
Inventor D·蒙泰斯J·奥穆莱恩J·P·雷奥D·奈尔逊J·万X·陈M·A·卡比尔
Owner SCHERING PLOUGH HEALTHCARE PRODUCTS INC
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