Pharmaceutical antidiabetic composition and method of obtaining antidiabetic composition

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of medicine, namely, to antidiabetic composition. Method of obtaining antidiabetic pharmaceutical composition includes preparation of trituracio mixture of active substance repaglinide, taken in therapeutically efficient quantity, with complex-forming substance, solubiliser and colloid silicon dioxide, further addition of filling agent, disintegrant and lubricant, and tabletting by method of direct pressing.

EFFECT: pharmaceutical composition in form of tablet, obtained by claimed method, is characterised by high degree of active substance release, satisfactory strength and has storage term longer than 2 years.

10 cl, 1 tbl

 

The invention relates to the field of medicine, particularly, to a tool that can be used for the treatment of diabetes.

Repaglinide widely used in medical practice as hypoglycemic agents.

In the international application WO 2007/111933 described pharmaceutical composition containing as active ingredient Repaglinide and as excipients - a filler/diluent, solvent/solubilizer and, optionally, other excipients. Famous composition is intended for nasal administration and cannot be performed in solid form.

In patent document CN 101695491 described composition of Repaglinide, which contains as excipients filler, binder, such as oksipropilmetiltselljuloza, lubricant, such as stearic acid, and other excipients, which prolong the release of Repaglinide. The composition is characterized by a slow release of the active substance, which is not always acceptable.

In patent application US 2009/0209587 described pharmaceutical composition, comprising Repaglinide and complexing agent, such as meglumine. In a preferred embodiment, the composition includes a binder (polyvinylpyrrolidone), a solubilizer/solvent (poloxamer 188, glycerin), napolnitel the (microcrystalline cellulose, starch, anhydrous dicalcium phosphate), disintegrant (polacrilin potassium), lubricant (magnesium stearate). The disadvantages of the known compositions should include the need to use contraception Repaglinide to achieve acceptable performance release Repaglinide and excessively large variation of their values (83-100%). Also known composition can be obtained in tablet form only wet granulation.

The objective of the invention is the creation of antidiabetic drug on the basis of Repaglinide in the form of a solid dosage form that has a shelf life of 2 years, with a high degree of release of the active substance and the method of obtaining antidiabetic composition.

To solve the stated problem, the proposed method for antidiabetic composition includes a preliminary preparation of a mixture of the active substance - Repaglinide with a complexing agent, a solubilizer and silicon dioxide, then add other ingredients such as filler, disintegrant and lube and tableting by direct pressing, with ingredients taken in the following ratio, parts by weight:

Repaglinide- 0,50-2,00
kompleksoobrazuyushchie
substance- 1,50-30,00
The solubilizer- 0,50-10,00
Silicon dioxide colloidal- 0,05-2,00

and tableting. Preferably the mixture of Repaglinide with a complexing agent, a solubilizer and a silicon dioxide wipe through a sieve, more preferably through a sieve with a cell diameter of not more than 450 μm.

In another aspect of the invention features antidiabetic pharmaceutical composition in tablet form comprising the active substance Repaglinide in therapeutically effective amounts as trituration mixture of complexing agent, solubilizer and silicon dioxide colloidal, and filler, disintegrant and lubricant in the following ratio of ingredients, parts by weight:

Repaglinide- 0,50-2,00
Complexing
substance- 1,50-30,00
The solubilizer- 0,50-10,00
Silicon dioxide is kolloidnyi - 0,05-2,00,

and obtained by the claimed method.

The active ingredient in the proposed composition is Repaglinide. Repaglinide - hypoglycemic agent, quickly lowers blood glucose by stimulating release of insulin from functioning β-cells of the pancreas. Used in the treatment of diabetes mellitus type 2 (insulin-independent). The inventive composition may also contain a dye.

The preferred ratio of ingredients of the inventive compositions is, parts by weight:

Repaglinide- 0,50-2,00
Complexing
substance- 1,50-30,00
The solubilizer- 0,50-10,00
Filler- 13,50-330,00
Disintegrant- 0,50-15,00
Lubricant- 0,05-2,00
Silicon dioxide- 0,05-2,00
Dye- 0-0,15

Savlon what I composition characterized by a high degree and uniformity of the values of the release of the active substance, stability indicators during storage at satisfactory strength without the use of the method of wet granulation. Thus, the composition releases 99-100% of the active substance in the environment dissolution buffer solution Mac-Elvina with pH 5.0 after 30 minutes (HPLC).

In the comparative example, the composition in the absence of complexing agents and a solubilizer release of Repaglinide was 20% for the same time interval.

The introduction of the tablets Repaglinide obtained by the method of direct compression of complexing agents and a solubilizer (Repaglinide is present in the form of a mechanical mixture with excipients), increased the rate of release of 20%, and for tablets, in which Repaglinide present in the form of triturate with a solubilizer and a complexing agent and silicon dioxide, the rate of release increased 2.7 times compared to the last comparative example (or 3.25 times with regard to the composition, where the complexing agent and a solubilizer missing).

In the process of development of the drug was able to apply the technology of direct extrusion technology instead of wet granulation, used in the preparation of the prototype. Receiving tablets by direct pressing is scientifically sound, as it eliminates the use of SWL is genitalia and subsequent drying, which have an adverse impact on the active substance and are critical factors in the production of tablets, affecting the stability of the dosage form.

In a preferred embodiment, the composition includes as a filler combination of lactose monohydrate and microcrystalline cellulose, more preferably in a ratio of 0.05 to about 30.0 parts by weight of lactose monohydrate per 1 parts by weight of microcrystalline cellulose, which allows to achieve high strength of the resulting tablets without the use of wet granulation.

As a solubilizer composition may contain nutriceuticals, dioctylsulfosuccinate, dextran, polyoxyethylenesorbitan, twins, poloxamer, poloxamine, polietilenglikolmonostearat and other similar substances, preferably poloxamer 188, as complexing substances, the composition may contain meglumin, diethanolamine, lysine, arginine, trometamol and other, preferably N-methyl-D-glucamine.

As disintegrant the composition may contain calcium carmellose, carboximetilkrahmal sodium, croscarmellose sodium, crospovidone, potassium, polacrilin, preferably potassium, polacrilin, as the lubricant is stearic acid and its derivatives, such as salts of stearic acid, calcium stearate, magnesium stearate, zinc stearate, and that the same nutritionalvalue, it is preferable to use calcium stearate and/or magnesium, as dye preferably used iron oxide yellow.

A new pharmaceutical composition are in the form of solid dosage forms, preferably in the form of tablets.

Examples of carrying out the invention is presented in the table.

A typical example (example 1). To achieve homogeneity of mixing and ensure release of the active substance from the tablets sifted substance Repaglinide mixed with silicon dioxide colloidal, complexing agent and solubilizer. After mixing, the mixture is forced through a sieve with a mesh size of 450 microns.

If necessary, the use of dye in tablet dosage of 1 mg to achieve a uniform coloring of the tablets separately prepare a mixture of parts of a filler, such as lactose monohydrate and colorant iron oxide yellow. For this dye yellow ferric oxide pound in a mortar with a small amount of lactose monohydrate.

To a mixture of substance Repaglinide with silicon dioxide, a complexing agent and a solubilizer is added a filler, disintegrant and salt of stearic acid (stearate) and ready weight tabletirujut. Get tablets with an average weight 0,100 g (0.5 mg and 1 mg) and 0,130 g (dose 2 mg), strength 70÷90 N (Dosi the set of 0.5 mg and 1 mg) and 110÷140 N (dose 2 mg).

The obtained tablets satisfy regulatory requirements in the pharmaceutical agent. Dissolution, % release Repaglinide on Wednesday dissolution buffer solution Mac-Elvina with a pH of 5.0 - 30 minutes (HPLC) - 99, the content of Repaglinide in one tablet (HPLC) 0.5 mg (dosage 0.5 mg), 1.0 mg (dosage 1 mg) and 2.0 mg (dosage 2 mg). The resulting tablets have a shelf life of over 2 years.

Table
IngredientsContent parts by weight
Dosage 0.5 mgDosage 1 mgDosage 2 mg
Examples
123123123
Repaglinide1,001,001,001,00 1,001,001,001,0001,00
Poloxamer 1886,001,0020,003,000,5010,001,500,2505,00
N-methyl-D-glucamine20,003,0060,0010,001,5030,006,500,75015,00
Lactose monohydrate95,60280,0016,0047,50140,008,0030,8595,0005,00
Microcrystalline cellulose67,4011,20220,0033,455,50 100,0022,503,50070,00
Potassium, polacrilin8,001,0030,004,000,5015,002,000,2507,50
Colloidal silicon dioxide1,000,104,000,500,052,000,350,0251,00
Salt of stearic acid1,000,104,000,500,052,000,300,0251,00
The colorant iron oxide yellow---0,050,010,15 ---

1. The method of obtaining antidiabetic pharmaceutical composition, which includes a preliminary preparation trituration mixture of the active substance (Repaglinide taken in therapeutically effective amounts, with a complexing agent, a solubilizer and silicon dioxide colloidal, then add filler, disintegrant and lube and tableting by direct pressing, with ingredients taken in the following ratio, parts by weight:

Repaglinide0,50-2,00
Complexing substance1,50-30,00
The solubilizer0,50-10,00
Silicon dioxide colloidal0,05-2,00

2. The method according to claim 1, in which the mixture of Repaglinide with a complexing agent, a solubilizer and a silicon dioxide colloidal rubbed through a sieve.

3. The method according to claim 2, in which the sieve has a cell diameter of not more than 450 μm.

4. The method according to any one of claims 1 to 3, characterized in that additionally use the dye.

5. The method according to any one of claims 1 to 3, characterized in that the COI is lsout as filler combination of lactose monohydrate and microcrystalline cellulose.

6. The method according to any one of claims 1 to 3, characterized in that you take lactose monohydrate and microcrystalline cellulose in the following ratio, parts by weight:

Lactose0.05 to about 30.0
Microcrystalline cellulose1

7. Antidiabetic pharmaceutical composition in the form of a tablet that contains the active substance Repaglinide in therapeutically effective amounts as trituration mixture with kompleksoobrazuyushchim agent, solubilizer and silicon dioxide colloidal, and filler, disintegrant and lubricant in the following ratio of ingredients, parts by weight:

Repaglinide0,50-2,00
Complexing substance1,50-30,00
The solubilizer0,50-10,00
Silicon dioxide colloidal0,05-2,00,

and obtained by the method according to any one of claims 1 to 6.

8. Antidiabetic pharmaceutical composition according to claim 7, characterized in that it contains one tablet Repaglinide in the amount of 0.5 mg.

9 Antidiabetic pharmaceutical composition according to claim 7, characterized in that it contains one tablet Repaglinide in the amount of 1 mg

10. Antidiabetic pharmaceutical composition according to claim 7, characterized in that it contains one tablet Repaglinide at 2 mg



 

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