Compositions and methods for mucosal delivery

A polymer, mucosal surface technology, used in drug combinations, inactive components of polymer compounds, drug delivery, etc., can solve problems such as solubility and poor bioavailability without consideration

Inactive Publication Date: 2008-05-28
LAVIPHARM LABORATORIES INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

While the above references consider release routes, they do not consider bioavailability issues due to poor solubility or low dissolution rates

Method used

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  • Compositions and methods for mucosal delivery
  • Compositions and methods for mucosal delivery
  • Compositions and methods for mucosal delivery

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 9

[0068] Example 9 illustrates how the properties of the dosage unit vary when different hydroxymethylcellulose polymers are used. Example 10 demonstrates how the use of accelerators (exemplified by starch graft copolymers) can increase mucoadhesion up to at least 84%. In vivo studies of the dosage unit showed that it was well tolerated by patients (Example 12) and that bioavailability was improved (Example 13).

Embodiment 1-3

[0070] Embodiment 1-3: Instant Films, Composition and Related Properties

[0071] Films were prepared as follows: A homogeneous mixture of the components in the amounts given in Table 1 was prepared as a coating solution. Amounts are given in weight percent of the coating solution. The mixture was degassed in a vacuum chamber and coated on the non-siliconized side of a polyester film and dried in a hot air circulating oven to form a free-standing, non-stick flexible film. The film is then cut into dosage units for packaging.

[0072] Table 1: Formulations of instant films using several different hydrocolloids

[0073] Composition: coating solution%

Example 1

Example 2

Example 3

Pullalan (P-20)

%(weight)

17.5

Methocel E5% (by weight)

21.06

POLYOX WSR N-10% (by weight)

1.8

PVA(Vinol 125)%(weight)

1.5

Cellulose gum % (weight)

8.1

Propylene glycol % (weigh...

Embodiment 4-8

[0081] Embodiment 4-8: Hydroxypropyl methylcellulose-based fast-dissolving oral lining containing therapeutic agent

[0082] Membranes were prepared according to Examples 1-3. The therapeutic agent is added to the homogeneous mixture (coating solution) prior to film formation.

[0083] table 5

[0084] Composition (coating solution)

Example 4

Example 5

Example 6

Example 7

Example 8

nicotine

1.4

Hydromorphone

2.92

Oxybutynin

3.71

Estradiol

1.49

Mint

1.0

1.0

1.0

1.0

1.0

Methocel E5 (HPMC)

21.06

21.06

21.06

21.06

21.06

Propylene Glycol

1.0

1.0

1.01

1.0

1.0

Aspartame

0.8

0.8

0.8

0.8

0.8

citric acid

0.7

0.7

0.7

0.7

0.7

polyoxyethylene castor oil

40

1.0

1.0

...

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Abstract

The present invention relates to a dosage unit comprising a water-soluble hydrocolloid and a mucosal surface-coat-forming film, such film including an effective dose of active agent. In the dosage unit slidenafil citrate, nicotine, hydromorphone, oxybutynine or estradiol are used as active agents.

Description

field of invention [0001] The present invention relates to a device and a method for drug delivery with a dissolving membrane structure. Background of the invention [0002] Many pharmaceutical dosage forms are administered orally in the form of solid shaped preparations such as tablets, pills, caplets and capsules, which retain their shape under moderate pressure. These dosage forms are usually designed to release the drug by swallowing whole or chewing with sufficient liquid. Some patients, especially pediatric and elderly patients, have difficulty swallowing or chewing solid dosage forms. Some patients, such as children or animals who refuse to take the medicine, may try to hide the solid pill to spit it out later. Additionally, many pediatric and geriatric patients are reluctant to take solid dosage forms because the active drug can be difficult to swallow or remain in the throat or esophagus even when liquid is administered with the dosage unit. In addition, fluid av...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K9/00A61P15/10A61KA61K9/14A61K9/16A61K9/46A61K9/48A61K31/216A61K31/465A61K31/485A61K31/495A61K31/505A61K31/519A61K31/565A61K47/10A61K47/30A61K47/36A61K47/38A61K47/42A61P1/02A61P15/18A61P31/04A61P31/10A61P31/12
CPCA61K9/006A61K9/145A61K9/0007A61K31/495A61K31/505A61K9/7015A61K9/0043A61K9/0031A61K9/1623A61K9/0056A61K9/0034A61K9/7007A61P1/02A61P15/10A61P15/18A61P31/04A61P31/10A61P31/12A61P43/00A61K9/70
Inventor L·-L·H·陈W·R·普菲斯特D·W·伦T·布拉纳乔派桑J·奥斯博尼H·S·谭L·陶
Owner LAVIPHARM LABORATORIES INC
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