Solid Dispersions of Fenbendazole with Polymers and Succinic Acid Obtained via Methods of Mechanochemistry: Their Chemical Stability and Anthelmintic Efficiency
Abstract
:1. Introduction
2. Materials and Methods
2.1. Raw Materials
2.2. Mechanochemical Modification of Fenbendazole Substance
2.3. Mechanochemical Interaction of Substance of FBZ with SA
2.4. Analysis of Products after Mechanochemical Modification of FBZ
2.5. Anthelmintic Efficiency of Products of Mechanochemical Modification of FBZ
3. Results and Discussion
3.1. The Analysis of Physical and Chemical Properties of Products, Obtained via Mechanochemical Modification of FBZ
3.2. Analysis of Products of Mechanochemical Modification of FBZ with SA
3.3. Results of Testing of Anthelmintic Efficiancy of Products of Mechanochemical Modification of FBZ
- –
- The most active forms of application of FBZ are its two-component solid dispersions with PVP and AG (Composition 1, Composition 2);
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- Three-component solid dispersions with the addition of SA (Composition 3, Composition 4) were not so active.
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- Product II and product III had insufficient weak activity, despite the high content of FBZ (75% and 95%, respectively), which can be explained by the low content of OFZ (up to 3%). It is known that OFZ, as a metabolite of FBZ, has a higher anthelmintic activity [17].
4. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Data Availability Statement
Conflicts of Interest
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Sample and Conditions for Its Production | Sample Solubility | |
---|---|---|
Absolute, mg/L | Increase | |
FBZ—initial substance | 0.33 | - |
SD composition FBZ:PVP (1:9), 5 h m.p. * | 7.9 | 24 ** |
SD composition FBZ:SA:PVP (1:1:3), 5 h m.p. | 12.2 | 37 |
SD composition FBZ:AG (1:9), 5 h m.p. | 7.0 | 21 ** |
SD composition FBZ:SA:AG (1:1:3), 5 h m.p. | 9.6 | 29 |
Samples of Solid Dispersions, Reaction Products, Conditions, and Date of Their Receipt | The Content of Fenbendazole, % | |
---|---|---|
Estimated | Found | |
FBZ:AG (1:9), mechanical processing 7 h, prod. date 27 February 2015—Composition No. 1 | 10 | 15 |
FBZ:PVP (1:9), mechanical processing 5 h, prod. date 30 June 2020—Composition No. 2 | 10 | 14 |
FBZ:SA:PVP (1:1:3), mechanical processing 5 h, prod. date 7 April 2022—Composition No. 3 | 20 | 23 |
FBZ:SA:AG (1:1:3), mechanical processing 5 h, prod. date 7 April 2022—Composition No. 4 | 20 | 21 |
Product I—product of the interaction of FBZ and SA in co-crystallization reaction in dioxane | absent | 22 |
Product II—product of the interaction of FBZ and SA in the co-crystallization reaction in acetonitrile | absent | 95 |
Product III—product of the interaction of FBZ and SA in the co-crystallization reaction in propanol-2 | absent | 75 |
Sample | The Content of FBZ, % | Dose by Weight of Powder, mg/kg | Dose According to FBZ, mg/kg | Discovered Trichinella spiralis, ind./mouse | Reduction in the Average Number of Nematodes in Relation to Control, % |
---|---|---|---|---|---|
1.Composition No 1 | 10 | 10 | 1 | 2.5 ± 0.4 | 90.64 |
2. Composition No 2 | 10 | 10 | 1 | 0 | 100 |
3. Composition No 3 | 20 | 10 | 2 | 79.2 ± 7.1 | 54.17 |
4. Composition No 4 | 20 | 10 | 2 | 103.0 ± 8.7 | 40.40 |
6. Product II | 75 | - | - | 120.0 ± 9.8 | 30.56 |
7. Product III | 95 | - | - | 108.0 ± 8.5 | 37.50 |
FBZ, substance | 98 | 2 | 2 | 132.0 ± 9.7 | 23.62 |
Control group | - | - | - | 172.8 ± 12.2 | - |
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Khalikov, S.S.; Khakina, E.A.; Khalikov, M.S.; Varlamova, A.I. Solid Dispersions of Fenbendazole with Polymers and Succinic Acid Obtained via Methods of Mechanochemistry: Their Chemical Stability and Anthelmintic Efficiency. Powders 2023, 2, 727-736. https://doi.org/10.3390/powders2040045
Khalikov SS, Khakina EA, Khalikov MS, Varlamova AI. Solid Dispersions of Fenbendazole with Polymers and Succinic Acid Obtained via Methods of Mechanochemistry: Their Chemical Stability and Anthelmintic Efficiency. Powders. 2023; 2(4):727-736. https://doi.org/10.3390/powders2040045
Chicago/Turabian StyleKhalikov, Salavat S., Ekaterina A. Khakina, Marat S. Khalikov, and Anastasiya I. Varlamova. 2023. "Solid Dispersions of Fenbendazole with Polymers and Succinic Acid Obtained via Methods of Mechanochemistry: Their Chemical Stability and Anthelmintic Efficiency" Powders 2, no. 4: 727-736. https://doi.org/10.3390/powders2040045
APA StyleKhalikov, S. S., Khakina, E. A., Khalikov, M. S., & Varlamova, A. I. (2023). Solid Dispersions of Fenbendazole with Polymers and Succinic Acid Obtained via Methods of Mechanochemistry: Their Chemical Stability and Anthelmintic Efficiency. Powders, 2(4), 727-736. https://doi.org/10.3390/powders2040045