Orally disintegrating tablet of dehydroepiandrosterone and/or combination of dehydroepiandrosterone and l-theanine

FIELD: medicine.

SUBSTANCE: invention represents a biologically active composition in the form of an orally disintegrating tablet characterised by the fact that it contains dehydroepiandrosterone (DHEA) as an active component, or its combination with theanine, and inert filling agents: mannitol, sorbitol, maltitol, crospovidone, copovidone, a lubricant, an intensive sweetening agent and a flavouring agent in certain mixture ratio.

EFFECT: composition is stable and has high bioavailability.

4 cl, 3 ex

 

The invention relates to the field of pharmaceutical and food industry.

Dehydroepiandrosterone (DHEA, DHEA) is a multifunctional steroid hormone, secreted by the adrenal glands the adrenal glands and affect androgen receptors.

L-Theanine (L-Theanine, L-Theanine) is an amino acid derived from tea leaves, natural antioxidant, actively penetrates into the brain through the blood-brain barrier and exerts psychoactive properties: reduces stress, improves cognitive abilities and improves mood, has anticonvulsant activity; reduces blood sugar, lowers blood pressure (Nathan P, Lu K, Gray M, Oliver S (2006). "The neuropharmacology of L-theanine(N-ethyl-L-glutamine): a possible neuroprotective and cognitive enhancing agent. J Herb Pharmacother 6 (2): 21-30)

In the late 80-ies of the last century it was found that this little-known at the time the hormone is directly associated with the aging process. DHEA has been found in large numbers in people under the age of puberty, and over the years, its level decreased. It is proved that DHEA prevents lipid peroxidation of cell membranes, normalizes the function of the immune system, cellular activity restores, rejuvenates the body, prevents the development of malignant tumors, improving strength and endurance of muscles, improves memory, speed Rea�tion, normalizes sexual activity, stimulates weight loss. About it, there are quite extensive clinical and experimental information.

As in women, and men DHEA plays an important role in the prevention of premature aging. It is known that over the years reduced its production, at the same time in the embryonic period it regulates energy metabolism during the growth and development of the immune system and the brain. In women, DHEA plays a crucial role in the synthesis of androgens, which decreases during menopause, which leads to the decrease of sexuality and libido.

Using the collected data about the hormone was suggested that the control of the level of DHEA at different ages and its timely adjustments can slow the onset of various disease conditions associated with old age, and to mitigate the violations associated with reduced function of the adrenal glands in men and women.

Kasson and colleagues were the first who confirmed therapeutic benefits from supplementation with dehydroepiandrosterone (DHEA) in women with reduced ovarian reserve (DOR) [Casson PR, MS Lindsay, Pisarska MD, Carson SA, Buster JE. Dehydroepiandrosterone supplementation augments ovarian stimulation in poor responders: a case series. Hum Reprod. 2000; 15:2129-2132. dot: 10.1093/humrep/15.10.2129. PubMed]. They also suggested that androgen offers the potential to replace steroids postmenopausal women, in addition to estrogens [Buster JE, Cason PR Straughn AB, Dale D, Umstot ES, Chiamori N, Abraham GE. Postmenopausal steroid replacement with micronized dehydroepiandrosterone: preliminary oral bioavailability and dose proportionality studies. Am J Obstet Gynecol. 1992; 66:1163-1168-PubMed] that DHEA has immunomodulatory actions [Casson PR, Andersen RN, Herrod HG, Stentz FB, Straughn AB, Abraham GE, Buster JE. Oral dehydroepiandrosterone in physiologic doses modulates immune function in postmenopausal women. Am J Obstet Gynecol. 1993;169:1536-1539. PubMed].

Currently dehydroepiandrosterone available in the form of dietary supplements, such as Biolife, SciFit DHEA 200, Swanson DHEA 50mg, etc.

The main difficulty of creating effective forms for the introduction connected with the fact that DHEA is poorly soluble in water.

Known sublingual form for receiving DHEA representing the solutions or suspensions (US5407927 (A) - (1995-04-18).

A composition comprising a dehydroepiandrosterone and methods of its manufacture and application (Patent RU 2220727). In particular, discloses capsules containing 50 mg of DHEA, lactose, starch and magnesium stearate. The stability of the known compounds is achieved by a special polymorphic form of the active principle. However, such forms do not solve the problem of its rapid absorption.

Known agent having anti-hangover effect, containing as active ingredients L-serine and fructose and additionally theanine (EN 2358723 C1, 20.06.2009). The tool can be made in the form of tablets and is used as a dietary Supplement. The decision does not relate to the PR�dispersed biologically active compounds.

Known sublingual form for receiving DHEA representing the solutions or suspensions (US5407927 (A) - (1995-04-18). The liquid form does not provide acceptable organoleptic characteristics.

International patent application WO 2013012326 (A1) - 2013-01-24 describes a tablet comprising granules containing DHEA, and granules containing microcrystalline cellulose. Pills make the release of 50% of the hormone within 30 minutes.

Known tablet for buccal administration LINGUE containing 17-(1-estradiol) (0.5 mg), progesterone (200 mg), testosterone (2.0 mg) and DHEA (10.0 mg) as the active principle and excipients: silica, magnesium stearate, acacia, stevia and polyethylene glycol, flavor, wildberry. Tablets may be biologically active, nutraceutical or nutritional supplements. Buccal form requires dissolution in the mouth for 5-10 minutes (WO/2006/105615, publ. 12.10.2006). This source can be specified as the closest analogue.

The object of the invention is the creation of a new form of biologically active additives on the basis of DHEA or its combination with L-theanine.

The problem is solved solid form - orodispersible the tablet quickly disintegrating in the mouth.

A distinctive feature orodispersible form is that at the time of her appointment is not required nor drink water, nor Beriev�VAT. It decomposes in the presence of saliva, usually in a few minutes, preferably in less than one minute.

New biologically active composition in the form orodispersible tablets contains one biologically active ingredient dehydroepiandrosterone (DHEA) and the following excipients: mannitol, sorbitol, maltitol, polyplasdone, copovidone, moving substance. Intense sweetener and flavoring in the following ratio of components, wt.%:

Dehydroepiandrosterone (DHEA) 8-12%

Mannitol 69-72%

Sorbitol 1.4% to 1.8%

Maltitol of 1.0-1.4%

Polyplasdone 10-14%

Copovidone is 0.1-0.2%

Moving substance 0,5-1%

Intense sweetener 1,4-1,8%

Flavor 1-2%.

Another option of the invention is a biologically active composition in the form orodispersible tablets containing as active principle a combination of L-theanine with Dehydroepiandrosterone (DHEA) and excipients: mannitol, sorbitol, maltitol, polyplasdone, copovidone, a moving substance, intense sweetener and flavoring in the following ratio of components, wt.%:

Dehydroepiandrosterone (DHEA)3-35%
L-theanine2-30%
Mannitol 39-75%
Sorbitol0.4 to 5.8%
Maltitol0,1-4,4%
Polyplasdone1.0-20%
CopovidoneOf 0.1-0.2%
Moving substanceOf 0.1-5%
Intense sweetenerOf 0.4% to 3.8%
FlavoringOf 0.1-5%

The inclusion of theanine in the composition provides a potentiation of energy and hormone potential Dehydroepiandrosterone.

As a sliding agent may be selected starch, talc, kaolin, bentonites, silica. Most preferably, the use of silicon dioxide, colloidal anhydrous.

As the Intense sweetener may be selected from aspartame, Acesulfame potassium, saccharin, stevioside and the like, and mixtures thereof. Most preferably, the use of aspartame.

The flavoring is selected from the acceptable food flavorings type "forest fruits" or "tropical blend".

The invention is illustrated by the following examples.

Example 1

Each Town�sperna Tablet (Dehydroepiandrosterone (DHEA) - 25 mg) contains:

Dehydroepiandrosterone (DHEA)10%The active substance

Inert fillers

Mannitol177.8 mg71.12%Solvent, sweetener
Sorbitol4.0 mg1.6%The binder component
Maltitol2.9 mg1.16%Sweetener
Polyplasdone30.8 mg12.32%Dezintegriruetsja component
Copovidone0.4 mg0.16%The binder component
Silica, colloidal anhydrous2.1 mg0.84%Moving substance
Aspartame4.0 mg 1.6%Sweetener
Flavor "forest fruits"3.0 mg1.2%Flavoring
The total number of250.0 mg100%

Example 2 a Method of manufacturing

The manufacturing process consists of seven main steps: (1) control of starting materials and primary packaging (2) weighing, (3) filtration, (4) mixing, (5) pressing, (6) packing and (7) control of the final product. Lot size: (360.000 kg=1440000 tablets (250 mg each).

Step 1. Control of starting materials and primary packaging

All released raw materials and primary packaging double-checked using quality Control of Chemicals.

Step 2. Weighing of raw materials

Step 3. Sifting through a strainer (0.5±0.05 mm)

All weighted material is sifted through a strainer to ensure no clumps, which are formed during storage.

Step 4. Mixing

Equipment: mixer Servolift MC (capacity maximum mixing drum 500 kg) - diffusion mixer

The order of addition to the mixing drum:

1. DHEA - 36.000 kg

2. Aspartame - 5.760 kg

3. Aromatized�R forest fruits Of 4,320 kg

4. Copovidone - 0.576 kg

5. Silica, colloidal anhydrous - 3.024 kg

6. Maltitol - 4.176 kg

7. Sorbitol - 5.760 kg

8. Polyplasdone - 44.352 kg

9. Mannitol - 256.032 kg.

The mixing process was conducted at a mixing speed of 11 rpm for 50 minutes.

Step 5. Pressing

Equipment: rotationy tablet press for pressing tablets KILIAN S250 SMART

The method used for the manufacture of tablets is direct compression using a rotary tablet press.

The parameters are the following:

Appearance - white round tablet with a flat upper surface with beveled edges

Weight - 20 tablets 5.0 g ± 5%

The average weight of tablets - 250 mg ± 5%

Height tablets - 3.4±0.5 mm

Hardness is not more than 50 N

Step 6. Packaging

1. The bottle of pills marked in primary packaging: plastic containers and caps, 30 tablets each.

2. Packaging is one of the primary packaging leaflets with packaging in cardboard boxes.

Step 7. End-product control

The disintegration timeNot more than 2 minutes

Example 3

Dehydroepiandrosterone (DHEA)3%
L-theanine30%
Mannitol39,2%
Sorbitol5,8%
Maltitol14%
Polyplasdone5%
Copovidone0,1%
Starch1%
Aspartame1,8%
The raspberry flavoring0,1%

The disintegration time is not more than 3 minutes.

The composition is prepared in the sequence of example 2, where theanine mixed with DHEA.

Indications for use of trains:

- Stress and depression (increases stress resistance of the organism).

- Obesity (DHEA normalizes the fat content in muscles occurs weight loss without loss of appetite).

- Prevention of tumors (including cancer).

- Cardiovascular disease (halve the death rate from cardiovascular disease).

- Memory loss and Alzheimer's disease (protects brain cells from a number of degenerative diseases).

- Sports nutrition.

- Osteoporosis (increases bone density and prevents osteoporosis � women and men).

Diabetes.

Is multiple sclerosis.

- AIDS.

- Normalization of hormonal levels in men, increases sexual activity and the Genesis of sperm) and women (delays the onset of menopause).

- Prevents premature aging.

- Involution and any signs of involutional disorders, including immune system and diseases associated with involution of the organism.

1. Biologically active composition in the form orodispersible tablet, which contains dehydroepiandrosterone (DHEA) as an active ingredient and excipients: mannitol, sorbitol, maltitol, polyplasdone, copovidone, a moving substance, intense sweetener and flavoring in the following ratio of components, wt.%:

Dehydroepiandrosterone (DHEA)8-12
Mannitol69-72
Sorbitol1,4-1,8
MaltitolOf 1.0-1.4
Polyplasdone10-14
Copovidone0,1-0,2
Moving substance0,5-1
Intense sweetener1,4-1,8
Flavoring1-2

2. Biologically active composition in the form orodispersible tablets, characterized in that it contains a combination of dehydroepiandrosterone (DHEA) with L-theanine as an active ingredient and excipients: mannitol, sorbitol, maltitol, polyplasdone, copovidone, a moving substance, intense sweetener and flavoring in the following ratio of components, wt.%:

Dehydroepiandrosterone (DHEA)3-35
L-theanine2-30
Mannitol39-75
Sorbitol0.4-5,8
Maltitol0,1-4,4
Polyplasdone1,0-20
Copovidone0,1-0,2
Moving substanceOf 0.1-5
Intense sweetener0,4-3,8
Flavoring Of 0.1-5

3. The composition according to claim 1, characterized in that it contains as a moving substance silica colloidal anhydrous.

4. The composition according to claim 1, characterized in that it contains as an intense sweetener aspartame.



 

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