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Pharmaceutical compositions with hydrating and lubricating activity

a technology of lubricating activity and pharmaceutical compositions, applied in the field of pharmaceutical compositions, can solve the problems of restrictive diet, intense physical activity, dry vaginal area,

Inactive Publication Date: 2017-01-26
FIDIA FARM SPA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides pharmaceutical compositions containing ester derivatives of hyaluronic acid for the treatment of vaginal dryness and atrophic vaginitis. These compositions have been found to be effective in restoring the hydration and turgidity of the vaginal mucosa, which is the surface of the vagina facing the lumen. The use of these compositions as lubricants for the genital mucosa has also been found to be beneficial in preventing opportunistic infections and promoting a healthy vaginal environment. The patent text also describes the causes of vaginal dryness and the current treatments available, including lubricants.

Problems solved by technology

It will easily be deduced from this complex picture that any variation in the vaginal equilibrium leads to alterations of the mucosa, which tends to lose its hydration and turgidity, giving rise to vaginal dryness.
There are also mental and physical causes such as stress, particularly restrictive diets, intense physical activity, and serious social problems.
Finally, dryness can be caused by mental or relationship problems that prevent regular mucus production during the stages of sexual arousal.
They have a long-lasting effect, because they do not dry on contact with air and do not interact unfavourably with bodily fluids, but are not very lubricant (they produce friction) and above all dissolve latex, which means that they cannot be used with a condom, as they would reduce its contraceptive efficacy and its efficacy against sexually transmitted diseases;
They are easily spread and dry slowly, but can attack silicone-based products;
water-based: gels with a high water content which are easily spreadable, compatible with biological fluids and have no effect on the latex of which condoms are made; however, although they give an excellent sensation of well-being after application, they dry very easily, and consequently require frequent application.
However, the high water content causes them to dry quite quickly.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0020]preparation of hyaluronic acid benzyl ester wherein 50% of the HA carboxyl groups are esterified with benzyl alcohol (Hyafflp50).

[0021]10.6 g of HA tetrabutylammonium salt (weight-average molecular weight 200,000 Da), corresponding to 17 milliequivalents of monomer units, is solubilised in 530 ml of dimethyl sulphoxide at 25° C., 7.8 milliequivalents of benzyl bromide are added, and the resulting solution is maintained at 30° C. for 12 hours. A solution of 62 ml of water containing 9 g of sodium chloride is then added, and the resulting mixture is poured slowly into 3000 ml of acetone under constant stirring. The precipitate that forms is filtered, washed three times with 500 ml of acetone / water 5:1, and finally dried under vacuum at 30° C. for eight hours. The precipitation stage is repeated; the precipitate is washed twice with acetone / water 5:1 and then three times with acetone alone, followed by drying under vacuum at 30° C. for 24 hours.

[0022]The end product thus obtained...

example 2

[0030]evaluation of the hydrating effect of a preparation of HA (Formulation A) and a preparation of Hyaff11p50 (Formulation B) wherein the average MW of HA is 180,000-230,000 Da.

[0031]The formulations were prepared simply by hydrating HA powders “as is” or Hyaff11p50 with an isotonic saline solution (NaCl 0.9% w / v in water) to obtain a final concentration of 0.2%.

[0032]The study was conducted ex-vivo on porcine vaginal mucosa obtained by surgical removal and devoid of pathological diseases.

[0033]Samples of vaginal mucosa with an area of 2 cm2 were placed on Petri dishes and treated with 1 ml of Formulation A or Formulation B, or with an equal volume of saline solution (Control).

[0034]The samples were then moistened with 1 ml of saline solution to simulate the vaginal environment, and stored in an incubator at 37° C. with constant humidity. After one hour, the strips of mucosa were transferred to dry Petri dishes and, taking this as Time 0 and the maximum level of hydration, their d...

example 3

[0038]Evaluation of release of benzyl alcohol from Hyaff11p50 in an aqueous environment.

[0039]Hyaff11p50 was dissolved in water and incubated in isotonic saline solution (NaCl 0.9% w / v in water) at the concentration of 1 mg / ml at 37° for 3 days. The presence of benzyl alcohol in the incubation medium was detected by HPLC using a C18 column and a UV detector, and measured after 24, 48 and 72 hours (T1, T2 and T3 respectively). The results, calculated as the percentage of benzyl alcohol compared with the initial content, are set out in Table 2 below. The release of benzyl alcohol, in the total absence of enzymes, is clearly substantial, consistent and linear.

TABLE 2Evaluation of release of benzyl alcohol into the mediumT1T2T3Benzyl alcohol in34%57%79%medium(% of initialcontent)

[0040]This means that after application to the vaginal mucosa, the benzyl alcohol released can combat any bacteria and fungi present, which find a fertile medium in vaginal mucosa altered by dryness.

[0041]In vie...

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Abstract

The present invention discloses pharmaceutical compositions comprising ester derivatives of hyaluronic acid for use as a topical treatment in disorders of the vaginal mucosa characterised by loss of elasticity and hydration, such as vaginal dryness and / or atrophic vaginitis; said compositions can also be used successfully to lubricate the genital mucosa.

Description

FIELD OF THE INVENTION[0001]The present invention discloses pharmaceutical compositions comprising ester derivatives of hyaluronic acid for use as a topical treatment in disorders of the vaginal mucosa characterised by loss of elasticity and hydration, such as vaginal dryness and / or atrophic vaginitis, and as lubricants for the genital mucosa.BACKGROUND OF THE INVENTION[0002]The vaginal mucosa is the surface of the vagina facing the lumen. It consists of a thick multi-layered lining epithelium without keratin but protected by mucus, which is rich in mucopolysaccharides secreted by muciparous cells. The cells of the vaginal mucosa, especially those of the outermost layers, are hormone-correlated, and play an important part in maintaining the metabolic balance of the vaginal environment. Said cells are therefore stimulated by oestrogens to synthesise and store large quantities of glycogen (sugar reserve), which is introduced into the vaginal lumen when said cells are shed. The glycoge...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/728A61K9/12A61K9/02A61K9/00A61K9/06
CPCA61K31/728A61K9/0034A61K9/122A61K9/02A61K9/06A61K9/08A61K47/36A61P15/00A61P15/02
Inventor PILOTTO, LAURAGENNARI, GIOVANNIZANELLATO, ANNA MARIA
Owner FIDIA FARM SPA
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