Method for obtaining membrane for intestinally soluble polymeric capsules

FIELD: medicine.

SUBSTANCE: the [present innovation deals with manufacturing intestinally soluble capsular forms of medicinal preparations, particularly, to the technology for creating capsular membranes of improved protective properties. The innovation deals with the method for obtaining capsular membrane out of calcium alginate due to successive keeping capsular nuclei in solutions of sodium alginate and calcium chloride, in which sodium alginate solution at concentration of 1.5-2.0% (weight/volume) should be pre-treated with ultrasound for about 8-10 at the power of 400-450 W/sq. cm. Calcium chloride solution should be applied at concentration of 2.0-2.5%, moreover, the terms for keeping capsular nuclei in solutions of sodium alginate and calcium chloride corresponds to 5 min in every solution.

EFFECT: higher efficiency.

1 dwg, 3 ex, 1 tbl

 

This invention relates to the production of enteric capsule forms of medicines, in particular to the technology of creating shells of capsules with superior protective properties.

For enteric capsules the most important quality criterion is the ability to protect contained within them the drug substance from the aggressive environment of the stomach. Highly meet this requirement coatings of calcium alginate, which is not soluble in acidic media.

A method of obtaining coatings for tablets (capsules) on the basis of sodium alginate. Sodium alginate (concentration of 5.0-10.0%) in pure form or mixed with gum and/or glycerol sprayed on the surface of the tablets (capsules) before formation of the protective sheath (US 06326028, "Alginate and gellan gum as tablet coating, 2001).

The disadvantage of this method is the complexity of the hardware design process, the use of plasticizers (glycerol). In addition, the resulting shell tablets (capsules) is dissolved in conditions of the stomach and cannot serve as a reliable protection for the encapsulant.

A method of obtaining a shell of calcium alginate for biological tissues. Tissue samples repeatedly covered by layers of calcium alginate by alternately keeping the samples in 1.0% solution of sodium alginate and 1.7% solution of calcium chloride (S 05578314, "Multiple layer alginate coatings of biological tissue for transplantation", 1996).

The disadvantages of this process are small thickness of 0.02-0.2 mm) and the strength of the resulting membrane.

Closest to the claimed is a method of obtaining a shell of calcium alginate for capsules with immobilized cells of Nicotiana tabacum by successive extracts of nuclei capsules in solutions of sodium alginate and calcium chloride. Kernel capsules initially formed from drops of 2.3% (weight/volume) solution of sodium alginate in at 0.7-1.4% solution of calcium chloride for 20 minutes. The hardened pellets saturated with ions of CA2+separated from the solution, washed with distilled water and immersed in a 1% solution of sodium alginate for 20 minutes. Free ions of CA2+react with the alginate molecules, forming a shell around the nucleus. To cure capsules incubated for 20 minutes in a 0.7% solution of calcium chloride and washed with distilled water. Depending on the concentration of the solution of calcium chloride (at 0.7-1.4%) thickness of the resulting membrane is 0.22-0,86 mm (Shibasaki-Kitakava N., Y. lizuka, T. Yonemoto Cultures of Nicotiana tabacum Cells Immobilized in Calcium Alginate Gel Beads Coated with Cell - Free Gel Film. Journal of Chemical Engineering of Japan, Vol.34, No.11, pp.1431-1438, 2001).

The disadvantages of this method are the low density shell, its low protective properties, as well as a significant duration of time (1.5 to 2.0 h).

The basis for this is th of the invention is the creation of the technological process, which allows you to get a shell made of calcium alginate with superior protective properties.

The technical result is to increase the density of the shell due to the treatment ultrasound source solution of sodium alginate.

The task and the specified technical result is achieved by the fact that in the method of obtaining shell capsules of calcium alginate by successive extracts of nuclei capsules in solutions of sodium alginate and calcium chloride according to the invention the solution of sodium alginate concentration of 1.5-2.0% (weight/volume) pre-treated with ultrasound for 8-10 minutes, with a capacity of 400-450 watts/cm2solution of calcium chloride is used in a concentration of 2.0-2.5%, and the extract cores capsules in solutions of sodium alginate and calcium chloride spend five minutes in each solution.

Under the influence of ultrasound decreases the viscosity of the polymer solution, there is a break intermolecular bonds alginic acid. As a result, in the process of formation of alginate gel number of links "calcium - alginate increases, thereby causing the formation of more dense structure of the shell.

The optimal value of the concentration of the solution of sodium alginate used to obtain the shell, it was recognized value in the range of 1.5-2.0% (weight/volume). The smaller the concentration of which does not provide the necessary density of the shell. Use in the process of working solutions with concentrations above 2.0% (weight/volume) is difficult due to the large viscosity values.

The processing of the original solution of sodium alginate ultrasound hold for 8-10 minutes at power ultrasound 400-450 watts/cm2. For a specified period of time, the viscosity of the solution reaches a constant value. Reducing the processing time does not lead to the desired technical result, but the increase was not feasible due to power consumption. The reduction of power ultrasound also does not lead to the desired technical result is the density of the resulting membrane increases insignificantly. Increasing capacity in excess of 450 W/cm2does not lead to a noticeable increase in the density of the shell. The quality of the shell measured in terms of the specific density, and the percentage output of model substances (metronidazole) of the capsules in conditions that mimic the conditions of the human stomach (temperature 37°C, 0.1 N. hydrochloric acid, pH≈1).

While holding the nuclei of the capsules in a solution of sodium alginate, is 5 minutes was deemed optimal in the case of use as the cores of the granules of calcium alginate. For a specified period of time on the surface of the cores is formed of a homogeneous, without breaks, a layer of alginate. When using other materials time remove the CI is determined experimentally. Time capsules in a solution of calcium chloride should be at least 5 minutes at least, experimentally obtained and is needed for the final formation of the shell. A further increase in the exposure time is impractical, as it does not improve the result.

The optimal concentration of calcium chloride is 2.0 - 2.5%. The use of solutions of lower concentrations increases the solidification shell, and a further increase does not affect the speed of the process.

Example 1.

Preparation of nuclei capsules.

For the preparation of nuclei capsules used the 1.5% (weight/volume) solution of sodium alginate containing metronidazole (model substance) 5 mg/ml

To obtain a 2.0% solution of calcium chloride hitch weight 10.0 g was dissolved in 490 ml of distilled water.

10 ml of a solution of sodium alginate with metronidazole used for making cores capsules. The solution dropwise, at a rate of 10 ml/min) was added into a solution of calcium chloride. The process ionotropic gelation continued for 25-30 minutes under stirring on a magnetic stirrer at a speed of not more than about 50./minutes of the Obtained granules were separated from the solution of calcium chloride on the grid and washed with 30 ml of distilled water.

The formation of the shell of the capsules.

100 ml of 1.5% (weight/volume) solution of sodium alginate for 9 the minutes were treated with ultrasound at a power of 450 W/cm 2.

The obtained kernel capsules immersed in the announced solution of sodium alginate for 5 minutes. The capsules were separated on the grid and was placed in a 2.0% solution of calcium chloride for 5 min to strengthen formed around the nucleus of the shell.

The finished capsules were separated on the sieve and washed with 30 ml of distilled water.

According to microscopic examination is the thickness of the formed shell is in the range of 0,3-0,5 mm the length of the process of manufacturing the shell of 40-50 minutes.

The quality of the membranes was evaluated by the value of its specific density and the percentage yield of metronidazole capsules in an environment that simulates the environment of the human stomach (or 0.1 n hydrochloric acid, pH≈1, temperature 37°). The value of the specific gravity 1,275 g/cm3the output of metronidazole is 14.6%.

Example 2.

The experiment was carried out analogously to example 1 except that ultrasonic treatment of the starting solution of sodium alginate was not conducted. The density of the membrane amounted to 1,073 g/cm3the output of metronidazole capsules of 24.5%.

Example 3.

The experiment was carried out analogously to example 1 except that ultrasonic treatment of the starting solution of sodium alginate was carried out at ultrasonic power 500 W/cm2. The density of the shell was 1,278 g/cm3the output of metronidazole capsules 14,55%.

The number e is sperimental is not limited to these examples. The results of all experiments are given in the table and on the graph of dependence of the solution viscosity of sodium alginate from time to time (see drawing).

Treatment of sodium alginate ultrasound for 8-10 minutes with the power of 400-450 watts/cm allowed to increase the density of the resulting shell 1.12 times and reduce the output of a model substance of capsules 1.68 times. In addition, the timing of the process was reduced from 1.5 to 2 hours up to a maximum of 40-50 minutes.

Industrial applicability.

This method of obtaining shell capsules suitable for implementation in laboratory and pilot-scale conditions on the existing equipment for the production of capsular forms of drugs. Currently, way is at the stage of laboratory experiments.

Table 1

Comparative data of the shells of the capsules obtained at different values of the power-U3-processing.
Power ultrasound, W/cm2(processing time is 9 min)The viscosity of a solution of sodium alginate, PA·The density of the resulting membrane, g/cm3The output of the model substance %
Without treatment UZ0,1531,07324,5
1500,1401,116
2500,1211,17020,5
3500,0921,26017,1
4000,0861,27115,5
4500,0831,27514,6
5000,0801,27814,55

The method of obtaining shell capsules of calcium alginate by successive extracts of nuclei capsules in solutions of sodium alginate and calcium chloride, wherein the solution of sodium alginate concentration of 1.5-2.0% (weight/volume) pre-treated with ultrasound for 8-10 min, capacity of 400-450 watts/cm2solution of calcium chloride is used in a concentration of 2.0-2.5%, and the extract cores capsules in solutions of sodium alginate and calcium chloride spend five minutes in each solution.



 

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