The article investigated the thickening properties of polyvinylpyrrolidone formulations in eye drops. In the course of research, it was found that kollidon is widely used in pharmaceutical production due to the different properties of soluble and insoluble grades of the group. It also performs the action as a solubilizer, stabilizer and fusion. One of the auxiliary substances used as a thickener in ophthalmic solutions was selected various grades of Kollidon (17, 25, 30, 90 and VA 64) for the study. The condensation property of this drug was determined by calculating various indicators (density, pH value, kinematic and dynamic viscosity, transparency) and by demonstrating the dependence of these parameters on the label and the concentration of the drug. From the studied brands, Kollidon 90 showed the highest concentration result.
According to the statistics of the World Health Organization for 2017, about 285 million people worldwide suffer from eye diseases. About 39 million of them have stopped looking, while
the remaining 246 million suffer from the eye diseases such as human cataracts, glaucoma, conjunctivitis, etc. These ophthalmologic diseases can be cured with the help of drug
Table 1 The table shows the model and concentration of the solution of polyvinylpyrrolidone:
Taken mark, (%) |
Models' numbers |
|||||||||||||||
1 |
2 |
3 |
4 |
5 |
6 |
7 |
8 |
9 |
10 |
11 |
12 |
13 |
14 |
15 |
||
1-3 |
Kollidon 17 |
10 |
- |
|||||||||||||
Kollidon 17 |
20 |
|||||||||||||||
Kollidon 17 |
25 |
|||||||||||||||
4-6 |
Kollidon 25 |
10 |
||||||||||||||
Kollidon 25 |
15 |
|||||||||||||||
Kollidon 25 |
20 |
|||||||||||||||
7-9 |
Kollidon 30 |
15 |
||||||||||||||
Kollidon 30 |
20 |
|||||||||||||||
Коллидон 30 |
25 |
|||||||||||||||
10-12 |
Kollidon VA64 |
- |
10 |
|||||||||||||
Kollidon VA64 |
- |
- |
15 |
|||||||||||||
Kollidon VA64 |
- |
- |
- |
25 |
||||||||||||
13-15 |
Kollidon 90 |
- |
- |
- |
- |
2.5 |
||||||||||
Kollidon 90 |
- |
- |
- |
- |
- |
5 |
||||||||||
Kollidon 90 |
- |
- |
- |
- |
- |
6.5 |
therapy, surgical and laser correction, using modern technologies. In the initial stages of eye diseases, various medications are used. At the subsequent stages can be treated with different eye drops.
The reason why eye drops cannot show the desired result to this time, and the lack of viscosity is a drawback. That is, when the viscosity of the ophthalmic solution is low, its streamlining increases. As a result, after dripping into the eyes, they come out again, without a therapeutic effect. For the effects of the drug, you must re-enter it in large quantities. This property, of course causes the consumer dissatisfaction.
Today, as a result of many experimental studies, there are several ways to solve this problem. One of them is to create a system with high viscosity, which will interact with eye tissues in a short time, and create an array of physical, chemical, biopharmaceutical properties and data thickeners used in ophthalmic solutions.
Purpose of the study:
The study of the thickening properties of the group of polyvinylpyrrolidone used in ophthalmic solutions.
Materials and research methods:
In this study, water-soluble grades of polyvinylpyrrolidone are used: Kollidon 25, Kollidon 30, Kollidon 90, Kollidon VA 64. Viscosity, pH, density and transparency were detected.
Model samples were obtained by dissolving the calculated amount of polyvinylpyrrolidone in distilled water using a magnetic stirrer.
Tools used in the research:
- A viscometer made of a glass capillary “VTZh-2” with a capillary diameter of 1.31 mm was used to determine the viscosity.
- Laboratory ionomer “I-160” was used equipped with a glass electrode and a thermocompressor to measure the pH value.
- Arometer was used to determine density.
Results and their analysis.
Determination of viscosity: according to NSS, the optimal kinematic viscosity of the eye drops is 5-15 cSt, as well as other sources of information cannot exceed the period of 15-30 cSt of viscosity. According to other sources, the viscosity of an aqueous solution of Kollidon increases in accordance with the increase in molecular weight and does not depend on the pH of the solvent.
Determination of pH value: pH values determined during sample examination:
The results show a weaker environment. Therefore, samples require a buffer solution to prepare an ophthalmic solution. Definition of transparency: the study was conducted by comparing the reference solution. As a result, all samples were transparent.
Determination of density: the density of the sample varies slightly (from 1.012 to 1.079 g/cm3).
Table 2 Values of 15 samples under the study by density, viscosity, pH and transparency
Model № |
Density, g/sm3 |
Kinematic viscosity, sSt |
Dynamic viscosity, sPz |
рН value |
Transparency |
1 |
1.012 |
2.23 |
2.57 |
4.13 |
Yellow |
2 |
1.071 |
7.03 |
7.53 |
4.20 |
Yellow |
3 |
1.093 |
7.78 |
8.50 |
4.21 |
Yellow |
4 |
1.017 |
3.73 |
3.79 |
3.52 |
Light yellow |
5 |
1.027 |
6.53 |
6.70 |
3.65 |
Light yellow |
6 |
1.040 |
12.77 |
13.29 |
3.67 |
Light yellow |
7 |
1.026 |
8.55 |
8.78 |
3.71 |
Light yellow |
8 |
1.037 |
14.36 |
14.89 |
3.73 |
Light yellow |
9 |
1.047 |
50.61 |
52.99 |
3.74 |
Light yellow |
10 |
1.016 |
3.91 |
3.97 |
4.02 |
Light yellow |
11 |
1.026 |
7.36 |
7.55 |
3.96 |
Light yellow |
12 |
1.031 |
23.41 |
24.14 |
3.74 |
Light yellow |
13 |
1.053 |
6.33 |
6.67 |
4.18 |
Colorless |
14 |
1.062 |
16.01 |
17.00 |
4.42 |
Colorles |
15 |
1.079 |
30.02 |
32.39 |
4.31 |
Colorles |
тығыздық
= 1.062
г/см3
Kinematic
colorless viscosity =
16.01 сСт
Kollidon 90
Dynamic
pH =4.42 viscosity =
17.00 сПз
Diagram 1 Indicators of Kollidon 90, denoting optimal thickening results for ophthalmic solution
The table shows the physico-chemical properties of soluble in collagen brands obtained during the study. Received brand Kollidon (17, 25, 30, 90 and VA 64) (Manufacturing company BASF, Germany). Aqueous solutions of Kollidon are colorless, transparent, indicate a weak pH value (3.52-4.42), the kinematic viscosity is concentrated and ranges from 2.23 to 50.61 sSt, and the density varies from 1.012 to 1.079 g/sm3.
Among the few samples that can be used as the most capable of preparing ophthalmic solution, sample 14 is the most suitable (Kollidon 90). Since this sample can be a thickening factor even at low concentrations. The diagram shows the values obtained in the study of the brand Kollidon 90.
Conclusion. Polyvinylpyrrolidone is an organic substance that is included in the composition of additional substances, resulting from the polarization of vinylpyrrolidone. Nowadays, it is widely used in the pharmaceutical industry. Soluble brands are found in solubilizers and stabilizers. And soluble brands are used as a density binder, a solubilizer and a stabilizer.
The models were selected that can be used as the thickeners for the preparation of ophthalmic solution: models 8, 9, 12, 14. From them, the sample 14 is the most effective (Kollidon 90 (5%)). This sample can show the desired concentrated effect even at low concentrations.
REFERENCES
- Georgievsky V.P., Konaev F.A. Technology and standardization of drugs. Kharkov: 2000. 784 р.
- E.A. Yegorova Glaucoma // National leadership. 2013. №2. Р. 41-46.
- Egoshina Yu.A., Kiselueva L.A. 2009. Modern excipients in tablet production // Successes of modern science. 2009. №10. Р. 11-14.
- Zhilyakova E.T., Baskakova A.V., Novikova M.Yu. Development of technological methods to increase the solubility of acyclovir // Basic research. 2013. №4. Р. 91-96.