Solid dosage form of preparations of memantine and its salts

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to solid fast-disintegrating dosage form of medication with antiparkinsonian action, which contains as active pharmaceutical ingredient memantine and/or memantine hydrochloride and cellulose II with the following ingredient ratio, wt %: memantine and/or memantine hydrochloride - 5-10, cellulose II - 90-95. Dosage form can represent pellet, created by method of direct pelletting.

EFFECT: obtaining fast-disintegrating in oral cavity dosage form, its distribution throughout oral cavity and delay of its transport to stomach, in order to provide medication delivery, not entering gastrointestinal tract and eliminating metabolism of medication in liver.

2 cl, 2 ex

 

The invention relates to medicine, in particular to pharmaceutical production technology of medicinal products, and relates to solid dosage forms means antiparkinsonian actions, which contains as an active pharmaceutical ingredient memantine and/or memantine hydrochloride.

Memantine (structural formula shown below) is, from a pharmacological point of view, miscoupling noncompetitive antagonist glutamatergic the NMDA-receptor. The disorder of the system glutamatergic neurotransmission, manifested in the form of neuronal excitoxicity, seen as the most important component in the etiology parkinsonism disorders and, in particular, Alzheimer's disease.

The structural formula of memantine

Memantine has a higher affinity to proteins of the NMDA receptor than Mg2+, therefore, provides an extension of influx of Ca2+ions, which are responsible for the manifestations of neuronal excitoxicity. By possessing low affinity of memantine to the NMDA receptor allows for rapid restoration of the physiological function of the receptor.

Memantine and its salts are white or white with metallic shades of powders, crystals are needle-shaped and other shapes with the experimental the nd solubility in water of about 26 mg/ml, density of about 1,365 g/cm3and a bitter metallic taste.

Dosage forms on the basis of memantine today presents under the trademarks of Namenda, Akatinol, Abixa. Drugs are presented in the dose of 10 mg and have the following composition (INSTRUCTION for medical use of the drug Akatinol Memantine (Akatinol Memantine), see http://www.medkrug.ru/medicament/show/5229):

Of memantine hydrochloride 10 mg

Excipients:

Lactose 174,75 mg;

Microcrystalline cellulose to 52.1 mg;

Colloidal silicon dioxide 1.25 mg;

Talc of 11.15 mg;

Magnesium stearate is 0.75 mg

Besides the famous patented pharmaceutical form antiparkinsonian actions containing memantine.

So, from the description to the patent of Russian Federation №2326660 (IPC A61K 31/13 (2006.01)published 20.06.2008) known oral medication in the form of a solid dosage form containing memantine as active substances and auxiliary components in the following ratios, wt.%:

Memantine 0,5-10,0

Disintegrant 2,0-40,0

anti-friction substance 0,2-10,0

physiologically neutral filler - rest.

The filler may contain microcellulose.

In addition, from the Eurasian patent №011446 (published 27.02.2009) known drug, which are solid oral medicament is built form with modified-release comprising memantine or memantine hydrochloride, and pharmaceutically acceptable polymeric carrier, with a major impact on modified release of active ingredient, and a filler, the polymeric carrier is selected from cellulose polymers and their derivatives (hydroxymethylcellulose, hydroxyethyl cellulose, carboxymethyl cellulose, microcrystalline cellulose polysaccharides and their derivatives), as filler contains lactose monohydrate, microcrystalline cellulose, silicon dioxide, or a mixture thereof, a lubricating agent. The active ingredient is contained in an amount up to 35 wt.%, media - 20-70 wt.%, filler - 5-80 wt.%, lubricating agent is 0.8 to 1.2 wt.%.

A disadvantage of the known pharmaceutical forms is the presence of a large number of ingredients, which leads to higher drug, and complexity of the technology of its production and reduce shelf life. The presence of microcrystalline cellulose in the amount of more than 20% wt. will lead to a significant slow release of the active substance and the binder absence will not allow to achieve the desired hardness of the tablets.

The closest analogue of the proposed solution is a dosage form containing memantine in the amount of 0.5-10% and microcrystalline cellulose in an amount of 90-99,5% (RF patent No. 2326660, is published 20.06.2008).

The disadvantages of the known pharmaceutical forms is used as a dosage form capsule contains granular drug, because it results in slow release of the active substance and intensive metabolism of the active substance in the liver.

In addition, the use of tablets and capsules of memantine in pediatric purposes is not always possible due to, for example, an undeveloped nervous system in infants, as well as due to disorders of swallowing reflex. The same persons older observed tremor, dysphagia, inability to take fluids and other disorders that restrict reception of tablets of drugs.

In connection with this important is the creation of a solid bistrotdepierrerue dosage form means antiparkinsonian actions on the basis of memantine and/or its salts using cellulose second crystalline modification (hydrocellulose, cellulose II) as the only component that replaces the filler, the disintegrator and the binder.

Object of the invention is the creation of innovative, sustainable, solid preformed bistrotdepierrerue dosage forms of memantine or memantine hydrochloride with raspadaemost to 60 seconds, release more than 80% within the first 60 minutes after administration and hardness of more than 80 N with universal buccal or enteral introduction in relation to the chosen physician therapy and capabilities of the patient, as well as simplifying the dosage form. This dosage form must meet all the requirements of the pharmaceutical agent within the shelf-life of the drug, respectively, receiving bystrousvaivaemyh dosage forms should provide a therapeutic concentration of the active substance in the blood plasma in accordance with the values obtained from clinical studies.

Dosage form should be coated with a polymer shell, easy release of the active substance, to provide high bioavailability, to be safe for health.

The technical result of the invention is to ensure the delivery of drugs, bypassing the gastrointestinal tract, and the exclusion of drug metabolism in the liver.

In addition, the technical result is the possibility of taking the drug without water, providing a partial absorption of the drug before getting into the stomach, which will result in the release of the active substance directly into the upper Vena cava, which avoids primary metabolism in the liver.

The claimed technical result is achieved due to the use of solid bistrotdepierrerue dosage form means antiparkinsonian actions, containing as an asset of the CSOs pharmaceutical ingredient memantine and/or memantine hydrochloride and targeted supplements. According to the present invention as additives target dosage form contains cellulose II in the following ratio of ingredients, wt.%:

memantine and/or memantine hydrochloride - 5-10;

cellulose II is 90-95.

As is well known, cellulose exists in four types of crystalline modification I, II, III, IV. The transition from one crystalline modification of (polymorphic state to another occurs as a result of chemical and/or thermal effects.

Below figure in the form of a block diagram, which schematically shows the shape modifications microcellulose and methods of conversion of polymorphs of cellulose among themselves.

The most common are forms I and II. Natural cellulose is composed mainly of two modifications of the I-th shape: 1α and 1β. Data allomorphy are present in different proportions depending on the origin (e.g., bacterial or plant).

Modified cellulose forms II (cellulose II) is derived from forms I through regeneration or mercerization. Regeneration consists in the dissolution of crystalline cellulose in the solvent followed by recrystallization in water.

The process of mercerization, first proposed 150 years ago by Mercer, is a steeping cellulose I-th form in a concentrated sodium hydroxide solution followed what kristallizatsiei in the water.

As shown by tests, cellulose II is better described properties superdisintegrants, at the same time has a high plasticity, which allows you to use it as a filler in the creation of new effective drugs. The relatively high content of cellulose-2 as filler will significantly reduce the impact of factors such as segregation, when mixed with the active substance and/or pelletizing, which, in turn, leads to significant fluctuations of the active substance per unit.

Currently, as substances, disintegrators, that is, substances that enhance the penetration of the water environment in the medical form and bring it to a rapid swelling and disintegration, which leads to faster release of the active substance, usually used pregelatinized starch, hypromellose (HPMC), crosscarmelose, crospovidone, alginic acid in the form of its salts or mixtures of salts. The innovativeness of the proposed dosage form is the introduction of the modified cellulose II as a universal ingredient that replaces the disintegrator and the filler, which, as shown by the tests, allows to reduce the time raspadaemosti, to increase the plastic properties of the composition for obleceni the pressing and accordingly, to increase the stability of the above pharmaceutical composition to changes in the process that leads to lower production costs and a significant increase in product quality in comparison with existing analogues.

At the same time properties superdisintegrants shown cellulose-2, allow you to create a pill or palette with high speed raspadaemosti.

Due to the fact that cellulose II has lower crystallinity than microcrystalline cellulose, can be used as a binder.

In addition, the density of cellulose II is lower than that of microcrystalline cellulose, and 1.5 g/cm3that is close to the density of the active substance of memantine (1,365 g/cm3). This property will reduce the segregation and to achieve an exact match of dose per unit without the use of additional auxiliary ingredients. A higher value of the specific gravity of cellulose-2 compared with cellulose-1 in combination with memantine leads to higher hardness of the tablets (more than 80 M).

Despite the fact that the properties of cellulose II differ substantially from the properties of microcrystalline cellulose (cellulose I), its composition is identical to the structure of cellulose I, which will replace the modification of the first modification II b the C the risk of degradation of the active substance. At the same time reducing components in the solid dosage form leads to increased stability of the active component and, accordingly, to increase the shelf life of the drug.

The use of cellulose II, as shown by tests, allows for the delivery of medicinal substance (memantine and/or memantine hydrochloride), bypassing the gastrointestinal tract, i.e. by absorption in the oral cavity and upper thirds of esophagus. This method will bypass the intensive metabolism of medicinal substances in the liver, since the buccal region and the region of the upper third of esophagus not served by the portal vein and the permeate enters the systemic circulation.

In the organoleptic tests of tablets produced using cellulose II, it was observed that the particles of this component is quickly distributed in the oral cavity without causing discomfort, at the same time having mucoadhesive properties, slowing the transport of dissolved particles of medicinal substances in the digestive tract, providing a more complete absorption through membranes of the oral cavity and esophagus.

The cumulative effect of increasing the bioavailability is not concentrated on a simple reduction of the time decomposition (as discussed in these sources), but consists of three main phases: rapid Vara is the response of the tablet in the oral cavity (or in the stomach and subsequent intestine, as discussed in the cited thesis), the distribution of the oral cavity and slow transport in the stomach by mucoadhesive properties, which is especially important when using the drug in pediatric patients, the elderly, patients with tremor, dysphagia, and other disorders that restrict the reception of tablets of drugs.

Thus, in addition to these advantages, the proposed structure is bistrotdepierrerue generic dosage form, allowing you to use it as a normal tablet fast action, and as oral-despergiruemaya form, as well as to simplify the production technology of medicinal product by optimizing the composition and technological parameters, strength characteristics, stability in time, reduce the cost of the finished product while providing assurance to the patient's values assessment indicators of bioavailability.

Dosage form may be in the form of solid pellets, created by way of direct pelletierine.

In addition, pharmaceutical form as the target additives may optionally contain lactose monohydrate, hypromellose (HPMC), polyvinylpyrrolidone (PVP), lubricants in the following ratio of ingredients, wt.%:

ComponentConcentration, mass. %
Memantineor5-10
Of memantine
Hydrochloride
Cellulose-290-95%
HPMC and/or PVP0-4%
Lactose monohydrate0-5%
Lubricant0-2%

Innovative patented pharmaceutical composition is in the introduction cellulose-2 as a universal ingredient to replace the substance of the cage and substance-filler that reduces the number of ingredients in the composition and significantly increase the bioavailability of the active substance (memantine), to increase the plastic properties of the composition to facilitate pressing and, accordingly, increase the sustainability of this pharmaceutical is the result of the composition to changes in the production process, that, in turn, leads to lower production costs and a significant increase in product quality in comparison with analogues.

Further, the invention is confirmed by the examples.

Example 1

Dosage form as tablets were manufactured by direct compression and contained, wt.%:

Memantine - 5 and cellulose-2 - 95.

A mixture of powders of memantine and cellulose-2 is mixed for 15 minutes in a powder mixer and tabletroute at pressures sufficient to achieve a porosity of not more than 10 volume percent. The resulting tablets have the necessary hardness, resistance to abrasion and release of the active ingredient.

It was further determined characteristics of the obtained tablets - raspadaemost, release and hardness. The hardness of the resulting tablets memantine with a diameter of 9 mm was in the range of 80-100 N. Raspadaemost received the tablets ranged from 1 to 3 minutes. The release of the active substance was determined in the apparatus with a stirrer, a speed which was 50 rpm Speed of release was more than 80% of the active ingredient in 15 minutes.

Also the resulting tablets were coated with a polymer shell containing HPMC, talc and dye. After determining the release profile was found that the application of a cosmetic coating obtained is tabletki of memantine does not affect the release profile.

Example # 2

Dosage form in the form of pellets was made by a method of direct pelletierine contained, wt.%:

Memantine - 5 and cellulose-2 - 95.

A mixture of powders of memantine and cellulose-2 pelletized in pelletization with a smooth rotating disk and a spray of distilled water. The obtained pellets are sieved with the Department of faction 250-800 μm and dried.

It was further determined characteristics of the obtained pellets - raspadaemost and release. Raspadaemost pellets was determined visually after placing the pellets in distilled water. Time raspadaemosti pellets ranged within 1 minute. The profile definition release was performed identically to the method described in example 1. The rate of release of the memantine of pellets amounted to more than 80% of the active substance in 15 minutes.

1. Solid bystrodeistviya dosage form means antiparkinsonian actions, containing as the active pharmaceutical ingredient memantine and/or memantine hydrochloride and additives target, wherein the target contains additives cellulose II in the following ratio of ingredients, wt.%:

memantine and/or memantine hydrochloride5-10
cellulose II90-95

2. Dosage form according to claim 1, characterized in that it represents the pellets are created by way of direct pelletierine.



 

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