Sustained release pharmaceutical formulation comprising phenylephrine

A phenylephrine, pharmaceutical technology, applied in the field of salt pharmaceutical composition, can solve the problem of unsatisfied continuous availability

Active Publication Date: 2009-07-29
BAYER CONSUMER CARE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Accordingly, the need for infrequent release of phenylephrine for the convenience of the patient and for the continued availability of therapeutically active phenylephrine to subjects in need of such administration is not met

Method used

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  • Sustained release pharmaceutical formulation comprising phenylephrine
  • Sustained release pharmaceutical formulation comprising phenylephrine
  • Sustained release pharmaceutical formulation comprising phenylephrine

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0140] The preferred method of manufacture is direct compression using a two-layer rotary tablet press. A preferred composition is a bilayer tablet having two distinct layers: a sustained release layer and an immediate release layer. For extended-release tablets, first mill phenylephrine HCl through a laboratory-size conical mill using a 20-mesh screen. Hydroxypropylcellulose Klucel EXF, Hydroxypropylcellulose Klucel GXF, sodium carboxymethylcellulose and one-third of microcrystalline cellulose were passed through the same conical mill. The ground material was then mixed in an appropriately sized PK blender for 5 minutes. The remaining microcrystalline cellulose was added to the blender and blended for an additional 5 minutes. Magnesium stearate was manually screened through a 30 mesh screen, added to the blend and blended for an additional 3 minutes and discharged into a suitably labeled container.

[0141] For immediate-release tablets, phenylephrine hydrochloride and lor...

Embodiment 1

[0153] Example 1. Bioavailability of Phenylephrine

[0154] The following study was performed to examine the absorption behavior of phenylephrine in the GI tract. Administration to healthy male and nonpregnant, nonlactating healthy female subjects: via Enterion TM Capsules (Protocol A - 9 subjects) 10 mg phenylephrine hydrochloride, 10 mg Sudafed PE delivered to the colon TM (Protocol B - 8 subjects) or via Enterion TM Capsules (Schedule C - 8 subjects) delivered 30 mg of phenylephrine hydrochloride to the colon, all regimens administered orally after an overnight fast. enter TM Capsules (Pharmaceutical Profiles Ltd, UK) allow for the orchestration of drug release at desired locations within the GI tract. To determine that the capsules have reached the desired location, the formulations of regimens A and C are administered orally with 210 mL of water followed by a radiolabeled drink containing 4 MBq 99m-Tc-diethylenetriaminepentaacetic acid (DTPA) in 30 mL of water so that...

Embodiment 2

[0194] Example 2. Preparation of Exemplary Formulations A-G and Determination of Dissolution Profiles

[0195] The dissolution profiles of exemplary formulations A-G (detailed in Table 2) were tested using a USP I dissolution apparatus set at 75 rpm over a period of 14 hours. Dissolution studies were performed at 37°C ± 0.5°C with 900ml of water buffered with 0.5mM phosphate buffer, pH 7.4. At each time interval, samples of the solution were analyzed by HPLC at 215 nm to determine the percent phenylephrine dissolved. Table 15 shows the three average dissolution results. and, image 3 Dissolution profiles are shown.

[0196] Table 15.

[0197]

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Abstract

The invention discloses a pharmaceutical composition comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is for oral administration wherein the composition delivers phenylephrine or a pharmaceutically acceptable salt thereof via absorption in the colon. The pharmaceutical composition comprises a core comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is in a time-dependent, pH-dependent, or colon-specific enzyme-dependent erodible layer that degrades to expose the core to release phenylephrine in the colon. In one preferred embodiment, the erodible layer encases the core. The composition optionally further comprises phenylephrine in the erodible layer or other additional layer(s). The pharmaceutical composition can further comprise one or more additional therapeutically active agents selected from one or more of the group consisting of antihistamines, analgesics, anti-pyretics, and non-steroidal anti-inflammatory agents. The invention also discloses methods of administering phenylephrine via the colon, thereby increasing the bioavailable amount of therapeutically active unconjugated phenylephrine relative to the total phenylephrine in the plasma.

Description

Background of the invention [0001] Phenylephrine and its pharmaceutically acceptable salts have been recognized by those skilled in the art as safe and effective nasal decongestants for use in humans when administered at frequent intervals. Commercially available formulations include nasal gels, nasal drops, and nasal sprays (i.e. Nasal Drops or Nasal Jelly) and immediate-release oral tablets or gelatin capsules (i.e. Sudafed PE TM or LiquiCaps). Due to the short plasma half-life of the active phenylephrine species in the body, currently formulated phenylephrine and its pharmaceutically acceptable salts are usually administered every four hours to relieve nasal congestion. Thus, the need for infrequent release of phenylephrine for the convenience of the patient and for the continued availability of therapeutically active phenylephrine to subjects in need of such administration is not met. [0002] Infrequent dosing results in improved patient compliance and appropriate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/36A61K31/137
CPCA61K9/2054A61K9/209A61P27/16A61K9/20A61K31/137
Inventor D·蒙泰斯J·奥穆莱恩J·P·雷奥R·T·诺沃克J·万M·A·凯比尔M·A·阿布塔里夫G·E·弗里茨
Owner BAYER CONSUMER CARE
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