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Use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant for the manufacture of a medicament for treating female genital disorders

A technology of polyacrylic acid and cellulose ether, which is applied in diseases, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of inability to achieve solid-gel transition, tablet retention, etc., and achieve improved chemical and physical properties. Effects of stability, pH reduction, and low production cost

Inactive Publication Date: 2013-05-01
POLICHEM SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In these cases, low shear forces from body motions fail to achieve the solid-gel transition, resulting in prolonged tablet retention in the vaginal cavity without performing any drug release

Method used

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  • Use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant for the manufacture of a medicament for treating female genital disorders
  • Use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant for the manufacture of a medicament for treating female genital disorders
  • Use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant for the manufacture of a medicament for treating female genital disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Embodiment 1 (comparative example)

[0086] Ciclopirox olamine 100 mg controlled-release bioadhesive vaginal tablets with lot number P06-037 were produced according to conditions known in the art.

[0087] Qualitative-quantitative formulations are shown in Table I.

[0088] Table I

[0089]

[0090] The method consisted of blending ingredients 1-8 followed by direct compression using a rotary tablet press (Officine Ronchi). A tablet weighing 760 mg with a hardness of 201N is obtained. Components No. 2 and No. 3 are components in the hydrophilic matrix (i).

Embodiment 2

[0092] Ciclopirox olamine 100 mg controlled release bioadhesive vaginal tablets with lot number P06-038 were produced according to the teachings of the present invention.

[0093] Tablets were prepared as described in Example 1.

[0094] Qualitative-quantitative formulations are shown in Table II.

[0095] Table II

[0096]

[0097] Components No. 2, No. 3 and No. 4 are components in the hydrophilic matrix (i).

[0098] A tablet weighing 760 mg with a hardness of 248N is obtained.

Embodiment 3

[0100] Structural analysis measurements were carried out on the tablets described in Example 1 (Lot No. P-06-037) and Example 2 (Lot No. P-06-038) in order to evaluate their bioadhesive properties and their degree of swelling. Tests for significant differences between means were performed by one-way ANOVA. Differences at the P<0.05 level were considered significant.

[0101] The bioadhesive properties were evaluated by a structure analyzer [1] and porcine vaginal mucosa was used as biosubstrate in order to simulate vaginal application.

[0102] A software-controlled dynamometer (AG / MC Acquati) with a 5 daN force cell was used to measure the separation force.

[0103] Sample Preparation

[0104] vaginal mucosa

[0105] The connective tissue was stripped from the vaginal mucosa obtained from the slaughterhouse using surgical scissors and stored at -20°C until use. The mucous membrane was thawed and carefully inspected visually for any defects prior to experimental applicati...

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Abstract

The invention relates to use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant for the manufacture of a medicament for treating female genital disorders. A hydrophilic matrix is disclosed which comprises: a) at least one polyacrylic acid derivative in preferred amounts of 0.5-40%, b) at least one cellulose ether in preferred amounts of 30-90% and c) at least one disintegrant in preferred amounts of 2-50%, with respect to the weight of the matrix. This matrix is used in combination with at least one pharmaceutically acceptable active principle for manufacturing solid bioadhesive controlled release formulations for the treatment of vaginal disorders, such as vulvovaginal candidiasis, bacterial vaginosis or trichomoniasis. The matrix is used in amounts of about 5-60%, preferably 20-40%, and the active principle in amounts of about 2-70%, preferably 5-50%, with respect to the weight of the formulation.

Description

[0001] The present invention is a divisional application of Chinese patent application 200780023985.8 filed on June 21, 2007. The title of the original application is "preparation of a hydrophilic matrix comprising polyacrylic acid derivatives, cellulose ether and a disintegrating agent for Use of drugs for the treatment of disorders of the female reproductive tract". field of invention [0002] The present invention relates to bioadhesive controlled release tablets for vaginal delivery for the treatment of female genital disorders. Background of the invention [0003] Vaginal delivery is an important route of drug delivery for local and systemic diseases. However, despite the many advantages of this route of administration, such as self-insertion and avoidance of the first-pass effect, there is a wide inter-individual variability and has not been widely exploited. [0004] Furthermore, commercial forms such as creams, foams, gels, douches, and tablets are believed to resi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K47/32A61P15/00A61P31/10A61P31/04A61P33/02A61P31/12A61P15/02A61P31/02
CPCA61K9/0039A61K31/496A61K9/2054A61P15/00A61P15/02A61P31/00A61P31/02A61P31/04A61P31/10A61P31/12A61P33/00A61P33/02A61K47/34A61K47/38A61K9/20
Inventor S·德路易吉布鲁斯基F·马兰德
Owner POLICHEM SA
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