Pharmaceutical composition with sustained-release of gliclazide

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition made mainly as solid medicinal formulations and comprising therapeutically effective amount of gliclazide and the special additive in the amount 4.65-6.70 mass. p. per mass unit of active substance. The additive comprises hydroxypropylmethylcellulose, microcrystalline cellulose, aerosil and stearate taken in the following ratio of components, mass. p. per 1 m. p. of active substance: hydroxypropylmethylcellulose, 2.50-3.50; microcrystalline cellulose, 2.12-3.00; aerosil, 0.01-0.05, and stearate, 0.02-0.15. Proposed pharmaceutical composition provides the sustained-release of gliclazide and high bioavailability of active substance, a simple method for its preparing as compared with solid medicinal formulation of gliclazide known from the prior art.

EFFECT: improved and valuable properties of composition.

3 cl, 2 tbl, 3 ex

 

The invention relates to the field of medicine, specifically a drug with anti-diabetic action.

Along with insulin - injection drug in the treatment of diabetes is widely used derivatives, sulfonylureas, which are used in the form of tablets. Among sulfonylureas created two generations of drugs. Butamid, Balaban, etc. belong to the first-generation drugs and can be used more often in the early stages of diabetes mellitus type II. In case of progressive type II diabetes is more effective drugs of the second generation, which include glibenclamide, glipizide and one of the most promising antidiabetic - gliclazide (Mashkovsky PPM, "Drugs", M, "Medicine", 1993, 1 o'clock, s-661).

Renowned pharmaceutical composition with anti-diabetic action, based on gliklazida (RF patent No. 2177318, 2001)that meets all the requirements of Gosfarmakapei XI edition with high bioavailability. However, to obtain therapeutic effect of this drug should be taken at least 2 times a day, which is not always convenient, especially for working people.

Just in recent years appeared patents protecting prolongirovanie form gliklazida. In the Eurasian patent №003751, 2003 proposed solid pharmaceutical compositions with controlled release, is received by thermal molding. Mixture for thermal molding is selected from the group polymethylacrylate type Eudragit different brands and one of the active ingredients, among which is mentioned and gliclazide. The temperature of the heat molding is from 60 to 150°C. the Disadvantages of this invention are quite complicated way to obtain and, especially, high temperature, which is exposed to the mixture of ingredients upon receipt of the specified composition.

The closest technical solution is a Eurasian patent # 002625, 2002, which describes a matrix tablet for prolonged release gliklazida, which includes a combination of polymeric compounds of cellulose and glucose syrup in the range from 10 to 40% of the total weight of these tablets. The composition of matrix tablets composed of different types of hydroxypropylmethylcellulose, maltodextrin, dehydrate secondary acidic calcium phosphate, magnesium stearate and colloidal silica. Prepare a matrix tablet complicated way in several stages, consisting of thorough mixing gliklazida, maltodextrine and dihydrate secondary acid phosphate of calcium, moistening the mixture with water followed by moist granulation of the mixture, drying and sorting the dried granulate. This granulate is mixed with hydroxyprop-politicallegal, a mixture of grease colloidal Cremonese the om and magnesium stearate and compressed on a rotary press machine.

Thus, known from literary sources of the dosage form gliklazida slow release characterized by a complex, multistage methods for their production, which determines, apparently, a small Arsenal of long-acting preparations gliklazida on the market antidiabetic medicines.

Therefore, it is highly important problem of creating anti-diabetic drug prolonged action on the basis of gliklazida.

The objective of this invention is to provide prolonged drug-based gliklazida for long, at least 12 hours, the release of active substance from the dosage form that meets all regulatory requirements Gosfarmakapei XI edition, and with high bioavailability (see table 1).

The problem is solved by a pharmaceutical composition with a slow release of the active substance, which is used therapeutically effective amount gliklazida containing the target additive, composition and proportion which provides a prolonged release gliklazida and its lasting effect in the patient with diabetes. Prolonged dosage form of the drug provides maximum therapeutic effect, reducing p and that minimize any adverse impact on the patient's body. This is achieved by controlling the speed of release of the active substance, which allows, on the one hand, to reduce the total content of gliklazida in the blood, and on the other hand, maintain in the blood constant, a therapeutically effective concentration.

As the target additives used hydroxypropylmethylcellulose (HPMC), microcrystalline cellulose (MCC), Aerosil and salt of stearic acid in the following ratio of components, parts by weight of 1 wt. hours of active ingredient:

GPMC2,50-3,50
MCC2,12-3,00
Aerosil0,01-0,05
Salt of stearic acid0,02-0,15

The total number of target components is 4.65-6,70 parts by weight of 1 wt h of the active substance.

Included with the tablet HPMC and MCC creates a hydrophilic matrix, providing a modified, controlled release gliklazida and its prolonged action.

As a salt of stearic acid it contains magnesium and/or calcium salts.

A new pharmaceutical composition is made in the form of a solid dosage form, preferably in the form of tablets. Tablets gliklazida slow release of the active substance get know who Tim way by tabletting on a tablet machine homogeneous mixture of the ingredients of the composition.

The proposed ratio of the active substance and the target additives found experimentally and is optimal, providing prolonged drug gliclazide compliance with all requirements of Gosfarmakapei XI ed. and high bioavailability. Long release gliklazida from the dosage form is confirmed by the indicator of the quality of the tablets Dissolve. The number gliklazida, passed on Wednesday dissolution in 2 hours, is from 24 to 30%, after 4 hours from 42 to 44%, and after 12 hours - from 78 to 87% (see table 1). At the same time for neprolongirovannymi tablets gliklazida rate of dissolution is not less than 75% in 45 min (Gasparikova XI ed., part 1, PP 156).

Table 2 shows the quantitative ratio of the components of the inventive pharmaceutical composition for the treatment of diabetes mellitus type II slow release gliklazida.

The following examples illustrate the invention (see table 2).

Example 1. (Trust supplements - 5,67 parts by weight to 1 parts by weight of gliklazida).

Mix the powders gliklazida in the amount of 15.0 g, Aerosil in the amount of 0,5g, MCC in the amount of 38.5 g and HPMC in the number of 45.0 g, mix thoroughly, then add 1.0 g of calcium stearate, again thoroughly mixed and tabletirujut n the tabletting machine. Get tablets gliklazida with an average weight 0,201 g and the content in one tablet 0,0299 g gliklazida. The resulting tablets have a high bioavailability and meet all the requirements of Gosfarmakapei XI publications (see table 1).

Example 2. (Trust supplements with 4.65 parts by weight to 1 parts by weight of gliklazida). Obtaining tablets gliklazida carried out as in example 1, on the basis of 15.0 g gliklazida, 37,50 g HPMC, 31,80 g MCC, 0.15 g of Aerosil and 0.30 g of magnesium stearate. Get tablets gliklazida with an average weight 0,190 g and with an average content in each tablet 0,0317 g gliklazida. The obtained tablets meet all the requirements of Gosfarmakapei XI ed. and have high bioavailability (see table 1).

Example 3. (Trust supplements - 6,70 parts by weight to 1 parts by weight of gliklazida). Obtaining tablets gliklazida carried out as in example 1, on the basis of 15.0 g gliklazida, 52,5 g HPMC, 45,0 g MCC, 0.75 g of Aerosil and 2.25 g of magnesium stearate. Get tablets gliklazida with an average weight of 0.2 to 10 g and the average content in one tablet 0,0285 g gliklazida. The obtained tablets meet all regulatory requirements (see table 1).

A comparative study of General toxic effect of the claimed pharmaceutical compositions gliklazida prolonged action and a standard (neprolongirovannymi drug gliklazida) rangareddy rats-males at doses of 14 mg/kg and 75 mg/kg (therap viteska). Experimental results showed that the integral indicators of the state of peripheral blood biochemical parameters, functional status excretory, cardiovascular, nervous systems identical to the Comparators. The drugs tested doses did not cause structural abnormalities in organs and tissues. Thus, confirmed bioequivalence actions and claimed the standard drug.

It is shown that the claimed gliclazide completely absorbed from the gastrointestinal tract, and With amaxachieved in 6-12 hours, while the standard drugmaxachieved through 2-6 hours, which confirms the prolonged nature of the proposed drug gliclazide.

Clinical testing of the proposed drug gliclazide were conducted in 4 hospitals in Russia. In accordance with the approved by the ethical Committee of the clinical trial Protocol were conducted on 80 patients with diabetes mellitus P-type (43 women and 37 men) aged from 33 to 76 years for three months. Dose of drug was administered individually and ranged from 1 to 3 tablets at one time during Breakfast.

Clinical efficacy was evaluated according to the well-being of patients, their objective status, the degree of compensation of carbohydrate metabolism, the biochemical indicators anal is for blood.

All patients underwent a baseline examination in the hospital, then was seen in the outpatient setting.

Against the backdrop of ongoing treatment of a single patient were observed deterioration in General health. Severe hypoglycemic events, phenomena ketoacidosis not recorded a single patient. Most of the patients weight remained stable, at the same time, some patients with high body mass was celebrated for its reduction.

12 weeks after start of treatment was observed statistically significant decrease in the level of glycated hemoglobin (8.7±1,1% to 7.3±0,8; p<0.05), and reduced levels of fasting glucose (on average, from 8.3±1.3 mmol/l to 6.8±0.9 mmol/l) and 2 hours after a meal (from 10.6±of 1.7 to 8.5±0.6 mmol/l).

None of the patients were observed clinically significant changes in blood counts, General urine analysis, biochemical parameters (krankina, cholesterol, urea, ACT, ALT, and others). If the drug is not a single documented case of allergic reactions and other side effects.

Clinical studies of the proposed drug gliclazide showed that he has a prolonged blood glucose-lowering effect in patients with diabetes mellitus P-type, and its long-term use was not accompanied by any unwanted side effects and Allergy is a mini reactions.

According to the results of clinical trials approved the instruction on medical application of the proposed drug gliclazide.

Table 1
№№ p/pName quality scoreStandards of quality requirementsThe actual indicators
Example 1Example 2Example 3
1.The average weight of the tablets, g0,2 ±7,5%, i.e. from 0,185 to 0,2150,2010,1900,210
2.Content gliklazida, g0,03±7,5%, i.e. from 0,0277-0,03230,02990,03170,0285
3.Impuritieseach all - not more than 0.2%;0,110,150,10
the amount of the impurities is not more than 1.0 %0,210,370,24
4.Dissolution, %2 hours - 15-35252718,6
4 o'clock - 30-55434437,5
12 o'clock - at least 758890 81,3
5.Bioavailability, %75-125107100110

Table 2
IngredientsContent parts by weight to 1 parts by weight of gliklazida
Examples
123
The hypromellose3,002,503,50
Microcrystalline celluloseto 2.572,123,00
Aerosil0,030,010,05
Salt of stearic acid0,070,020,14

1. Pharmaceutical composition for treating diabetes mellitus type II with prolonged visualidentity gliklazida, characterized in that it contains a therapeutically effective amount gliklazida and special additive in the amount of the 4.65-6,70 parts by weight to 1 parts by weight of active substance which it contains hypromellose, microcrystalline cellulose, Aerosil and salt of stearic acid in the following ratio of components, parts by weight to 1 parts by weight of active ingredient:

The hypromellose2,50-3,50Microcrystalline cellulose2,12-3,00Aerosil0,01-0,05Salt of stearic acid0,02-0,15

2. The pharmaceutical composition according to claim 1, characterized in that salts of stearic acid it contains magnesium and/or calcium salts.

3. The pharmaceutical composition according to claim 1, characterized in that it is made in the form of a solid lekarstvennoi forms, mainly in the form of tablets.



 

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