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Methods for treating early morning pathologies

a pathology and early morning technology, applied in the field of medical treatment, can solve the problems of low patient compliance or undesirable system exposure to therapeutic agents, and achieve the effects of accelerating the disintegration of the core, and improving the rate of release of pharmaceutically active agents

Inactive Publication Date: 2006-08-15
POLICHEM SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]As a second aspect, the present invention provides a pharmaceutical formulation for the time-specific delivery of a pharmaceutically active agent to a subject in need of the therapeutic effects thereof. The formulation comprises: (1) a core comprising the pharmaceutically active agent and a disintegration enhancing agent; and (2) a swellable polymeric coating layer substantially surrounding the core. The swellable polymeric coating layer delays the release of said pharmaceutically active agent from the core for a predetermined period of time dependent upon the thickness of said swellable polymeric coating layer. The disintegration enhancing agent accelerates the disintegration of the core upon disintegration of the swellable polymeric coating layer to improve the rate of release of the pharmaceutically active agent from the core when the desired time for release is reached.
[0007]As a third aspect, the present invention provides a pharmaceutical formulation for the time-specific delivery of a pharmaceutically active agent to a subject in need thereof. The formulation comprises: (1) a first time-specific dosage unit comprising (a) a core containing the pharmaceutically active agent and a disintegration enhancing agent; and (b) a swellable polymeric coating layer substantially surrounding the core; and (2) a second time-specific dosage unit comprising (a) a core containing the pharmaceutically active agent; and (b) a swellable polymeric coating layer substantially surrounding the core. The swellable polymeric coating layer delays the release of the pharmaceutically active agent from the core for a predetermined period of time dependent upon the thickness of the swellable polymeric coating layer. The disintegration enhancing agent accelerates the disintegration of the core upon dissolution of the swellable polymeric coating layer to improve the rate of release of the pharmaceutically active agent from the core. In this embodiment, the core containing the active ingredient may be differently formulated so as to allow the prompt release of the active component or a further controlled or sustained release, after the desired lag-time. For this purpose, either conventional core excipients or excipients which are capable of forming a matrix system may be used.

Problems solved by technology

Unfortunately, the low compliance of patients or the continual exposure of the system to therapeutic agents may be undesirable in some subjects or some situations.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0047]Diclofenac sodium (25 mg), 94.5 mg of dibasic calcium phosphate dihydrate, 113 mg of microcrystalline cellulose, 25 mg of tartaric acid, 25 mg of sodium bicarbonate and 1.5 mg of colloidal silicon dioxide, are mixed thoroughly. Magnesium stearate (1 mg) is added and thoroughly mixed for another 5 min. The granular mixture is formed into tablet cores of 8.7 mm diameter, weighing 285 mg each, using a rotary tablet press. The cores show a disintegration time lower than 1 min. in water, a Schleuninger hardness higher than 10 kp, and a friability lower than 0.1%.

[0048]The swellable polymeric coating layer is applied on to the tablets in an automatic coating pan using the following solution:

[0049]

Hydroxypropylmethylcellulose7.5%w / w(METHOCEL E50 ®)PEG 60001.5%w / wPurified water91.0%w / w

[0050]The solution is applied until a weight gain corresponding to 50% of core weight is achieved. The coated tablets show a dissolution time lag in excess of 300 min., followed by a quick disintegration...

example 2

[0051]Cores (20,000) containing 25 mg diclofenac sodium are prepared according to Example 1.

[0052]The cores are heated to 40° C. and the coating layer is applied onto the cores in a two-step procedure, using an automatic coating pan. In the first step, the cores are wetted with a binder solution including 5% METHOCEL E5®. 10% polyvinylpyrrolidone, and 85% purified water. In the second step, the wetted cores are treated with a dry mixture including 90% METHOCEL K15M®, 9% talc and 1% colloidal silicon dioxide. Steps 1 and 2 are repeated until a weight gain corresponding to 30% of total tablet weight is achieved.

[0053]The coated tablets showed a dissolution time lag in excess of 300 min., followed by a quick disintegration of the tablet.

example 3

[0054]Verapamil HCl (40 mg), 79 mg of dibasic calcium phosphate dehydrate, 18 mg of microcrystalline cellulose, 25 mg of citric acid, 35 mg of sodium bicarbonate, and 2 mg of colloidal silicon dioxide, are mixed thoroughly. Magnesium stearate (1 mg) is added and thoroughly mixed for another 5 min. The granular mixture is formed into tablet cores of 6.8 mm diameter, weighing 200 mg each using a rotary tablet press. The cores show a disintegration time lower than 1 min. in water, a Schleuninger hardness higher than 10 kp and a friability lower than 0.1%.

[0055]The cores are heated to 40° C. and the coating layer is applied onto the cores in a two-step procedure, using an automatic coating pan. In the first step, the cores are wetted with a binder solution including 5% METHOCEL E5®, 10% polyvinylpyrrolidone, and 85% purified water. In the second step, the wetted cores are treated with a dry mixture including 90% METHOCEL K15M®, 9% talc and 1% colloidal silicon dioxide. Steps 1 and 2 are...

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PUM

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Abstract

The present invention provides methods of treating early morning pathologies using a time-specific controlled release dosage formulation which is administered prior to sleep, and which permits or achieves delivery of a pharmaceutically active agent effective for the treatment of the specific early morning pathology to be treated, at about the time of awakening. The time-specific controlled release dosage formulation comprises (1) a core including the pharmaceutically active agent(s) effective for the treatment of the early morning pathology, and (2) a swellable polymeric coating layer substantially surrounding the core. The swellable polymeric coating layer delays the release of the pharmaceutically active agent from the core for a predetermined period of time dependent upon the thickness of the swellable polymeric coating layer, to effect delivery of the pharmaceutically active agent at about the time of awakening.

Description

FIELD OF THE INVENTION[0001]The present invention relates to methods for medical treatment. More particularly, the present invention relates to methods for treating conditions or pathologies, the symptoms of which are more pronounced in early morning.BACKGROUND OF THE INVENTION[0002]It is increasingly recognized that several chronic diseases display rhythmic patterns in the manifestation of symptoms. In this field there is particular interest in those conditions for which symptoms are generally aggravated in the morning. These early morning pathologies are typically treated by either night-time administration of conventional medicines or relatively constant administration of therapeutic agents with the goal of maintaining constant levels of drug in the system of the afflicted subject. By this protocol, the therapeutic benefit of the drag is assured at the time of awakening when the symptoms are generally more pronounced. Unfortunately, the low compliance of patients or the continual...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K9/54A61K9/00A61K9/28A61K9/30A61K9/32A61K9/48A61K31/135A61K31/136A61K31/15A61K31/18A61K31/192A61K31/196A61K31/198A61K31/325A61K31/34A61K31/352A61K31/4365A61K31/4402A61K31/4985A61K31/522A61K31/545A61K31/5513A61K31/573A61K31/60A61K38/00A61K45/08A61K47/32A61K47/38A61P7/02A61P9/10A61P9/12A61P11/06A61P11/08A61P13/00A61P19/02A61P25/16A61P25/20
CPCA61K9/0007A61K9/2866A61K9/2886A61K9/4808A61P11/06A61P11/08A61P13/00A61P19/02A61P25/16A61P25/20A61P7/02A61P9/10A61P9/12
Inventor BUSETTI, CESARECRIMELLA, TIZIANO
Owner POLICHEM SA
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