RU2582290C2 - Dental gel having niosomes for treatment of inflammatory and dystrophic periodontal diseases - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to drugs for dental purposes. Disclosed is a dental gel prepared using a suspension of niosom, made based on PEG-12 dimethicone, containing dihydroquercetin and dry extract of oak bark, in amount of 10 wt% suspension of niosom, 1 wt% of dihydroquercetin and 0.5 wt% of dry oak bark extract in gel, containing, wt%: triethanolamine - 2, gelling agent - 2.5, fragrant - 0.15, preserving agent - 0.05, distilled water - up to 100. Use of niosoma provides high percentage of delivery of active substances. Transdermal delivery of dihydroquercetin stops sclerotic processes, normalises microcirculation in tissues. Tannins of oak bark have antiseptic and wound healing action without violation of oral microflora.

EFFECT: dental gel is used for treatment and prevention of periodontal diseases.

1 cl, 1 tbl

Description

 The invention relates to medicine, namely to dentistry, in particular to transdermal therapeutic systems - gels, designed for targeted delivery of active substances (AS) through the alveolar mucosa.

Periodontal diseases include a large group of pathological processes, the main of which are gingivitis, periodontitis and periodontal disease proper. It is believed that the cause of periodontal disease is the lack of blood supply to the gum tissue, which in severe advanced cases leads to its atrophy and, as a consequence, to tooth loss. Gingivitis - gum disease - is caused by bacteria in food debris, plaque, and other consequences of poor oral hygiene. And finally, periodontitis - the most common periodontal disease, are the result of an unfavorable course of gingivitis, characterized by a violation of the gingival attachment, the formation of gingival and periodontal pockets.

Traditional methods of prevention and treatment of periodontal diseases due to a rather complicated etiology and limited penetration of active substances are not effective enough (RF 2179841, RF 2078559). The combination of the use of therapeutic systems with high-tech devices in the field of dentistry and dental equipment is possible only in stationary conditions (RF 2372949), which seriously limits the consumer both in time and price. In this context, the science-based development of nanocapsulated dosage forms suitable for use both in the hospital and at home deserve attention.

The invention (RF 2146137) is considered as a liposome source of hydroxylated proline or lysine for activation of collagen synthesis in the gums, however, parenteral administration of the emulsion casts doubt on the localization of the drug in the focus of periodontosis.

The concept of using heavy metal ions to provide tanning and antimicrobial effects is not new (RF 2139036). However, the high concentration of hydrogen sulfide during putrefactive processes in the oral cavity casts doubt on the aesthetic appearance of the teeth, since when using such a composition, the appearance of hard-to-remove black plaque of silver sulfide will be observed.

The closest prototype of the invention we have developed is a dental transdermal elixir (RF 2327445). However, having the recipe for this drug, one can call into question the claimed mechanism of action, since the abundance of plant extracts: large plantain, sweet clover, pharmaceutical marigold, St. John's wort, chamomile, medicinal sage, dioecious nettle, as well as aloe juice and tree-buckthorn oil, taken in a ratio of 1: 1: 1: 2: 2: 1: 1: 1: 2, in combination with a biocomplex of a natural antioxidant - extract of fruits and flowers of hawthorn in a ratio of 1: 2; diverse in action and can not have any pronounced therapeutic effect. The use in the manufacture of the volatile, toxic precursor - chloroform can significantly limit the serial production of the product.

SUMMARY OF THE INVENTION

It is proposed to use a gel containing niosomes for the treatment and prevention of periodontal disease. The multidirectional effect of the gel allows not only to remove the external manifestations of periodontal disease, but also to combat the causes that caused this disease. The niosomes obtained from PEG-12 dimethicone with dihydroquercetin and an extract of oak bark included in the internal volume, subsequently dispersed with an ARA homogenizer, are complete multilamellar vesicles of standard size from 20 to 100 nm, including a high percentage of immobilized active substances, which are stable during storage . The use of organosilicon nanocontainers - niosomes allows you to deliver active substances into the deep layers of the periodontium, and not work locally on the surface of the damaged oral mucosa, reduce inflammation, improve microcirculation, and stop sclerotic processes. It has been experimentally proved that the highest therapeutic activity is observed in a gel with 10% niosomes containing 1% dihydroquercetin and 0.5% oak bark extract. A further increase in the percentage of niosomes and active substances did not lead to an increase in therapeutic activity.

The implementation of the invention

For the formation of niosomes, a surface-active compound containing PEG-12 dimethicone was used.

Due to the fact that active substances occupy a small volume relative to other components of the gel, its incorporation into niosomes is carried out by adding 5% PEG-12 dimethicone to an aqueous solution of dihydroquercetin (10% by weight) and dry oak bark extract (5% by weight) in a separate container. The process is carried out at room temperature and intensive mechanical homogenization of the reclosure by a homogenizer for 5 minutes. After the inclusion of AS in niosomes, a suspension of niosomes is introduced to other components of the gel at room temperature. The final stage of the formation of vesicles occurs with intensive mechanical stirring of the mixture.

Phase A is prepared at room temperature by homogenizing the components in a recycle homogenizer. Phases B and C containing suspensions of niosomes are made separately according to the technology described above and are introduced into phase A with stirring. To stabilize the concentration of hydrogen ions (pH) to 6.6-7.0 and form a gel structure, phase D is introduced. The preparation phases and gel formulations are presented in Table 1.

The gel in an amount of 1 cm for adults and 0.5 cm for children from 1 year old is squeezed onto a clean finger and rubbed with light massaging movements into the affected area of the mucosa. In case of periodontal disease, the gel is introduced into the pockets or applied in the form of compresses, or gently rubbed 1-2 times a day.

Indications for the use of the drug are inflammatory, ulcerative, necrotic, infectious, trophic lesions of the oral mucosa, gingivitis, periodontitis, teething pain in children. The drug is rapidly absorbed, which due to the transdermal basis provides a high percentage of AC delivery.

The designed gel passed clinical trials at the Department of Therapeutic Dentistry of the Stavropol State Medical University (protocol No. 4 of March 11, 2012). As a result of the studies, the optimal percentage ratio of niosomes and active substances was selected, which allows to obtain the maximum therapeutic effect.

Claims (1)

Dental gel, characterized in that for its preparation using a suspension of niosomes made on the basis of PEG-12 dimethicone containing dihydroquercetin and dry oak bark extract, in an amount of 10 wt. % suspension of niosomes, 1 wt. % dihydroquercetin and 0.5 wt. % dry extract of oak bark in a gel composition containing wt. %:
triethanolamine 2 gelling agent 2,5 perfume 0.15 preservative 0.05 distilled water up to 100