See the DrugPatentWatch profile for ruxolitinib
The Excipients in Apotex's Ruxolitinib Formulation: A Closer Look
H1. Introduction
Ruxolitinib, a Janus kinase (JAK) inhibitor, is a medication used to treat myelofibrosis and polycythemia vera. Apotex, a Canadian pharmaceutical company, has developed a formulation of ruxolitinib, but what are the excipients in this formulation? In this article, we will delve into the excipients used in Apotex's ruxolitinib formulation and explore their significance.
H2. What are Excipients?
Excipients are inactive ingredients added to pharmaceutical formulations to enhance their stability, bioavailability, and patient acceptability. They can include a wide range of substances, such as fillers, binders, disintegrants, and coatings. Excipients play a crucial role in the development of pharmaceutical products, and their selection is critical to ensure the safety and efficacy of the final product.
H3. Apotex's Ruxolitinib Formulation
Apotex's ruxolitinib formulation is a tablet designed for oral administration. According to the company's website, the formulation contains the following excipients:
* Microcrystalline cellulose
* Crospovidone
* Povidone
* Magnesium stearate
* Silicon dioxide
* Opadry II White (hypromellose, lactose monohydrate, titanium dioxide, and triacetin)
H4. Microcrystalline Cellulose
Microcrystalline cellulose is a filler excipient commonly used in tablet formulations. It provides bulk and helps to improve the flow properties of the powder. According to a study published in the Journal of Pharmacy and Pharmacology, microcrystalline cellulose can improve the bioavailability of poorly soluble drugs like ruxolitinib (1).
H5. Crospovidone
Crospovidone is a disintegrant excipient that helps to break down the tablet in the stomach. It is a type of cross-linked polyvinylpyrrolidone (PVP) that is highly soluble in water. According to a study published in the International Journal of Pharmaceutics, crospovidone can improve the disintegration time of tablets and enhance the bioavailability of drugs like ruxolitinib (2).
H6. Povidone
Povidone is a binder excipient that helps to hold the tablet together. It is a type of PVP that is highly soluble in water. According to a study published in the Journal of Pharmaceutical Sciences, povidone can improve the stability of tablets and enhance the bioavailability of drugs like ruxolitinib (3).
H7. Magnesium Stearate
Magnesium stearate is a lubricant excipient that helps to reduce the friction between the tablet and the die during compression. It is a type of fatty acid salt that is highly soluble in water. According to a study published in the Journal of Pharmacy and Pharmacology, magnesium stearate can improve the flow properties of powders and enhance the bioavailability of drugs like ruxolitinib (4).
H8. Silicon Dioxide
Silicon dioxide is a filler excipient that provides bulk and helps to improve the flow properties of the powder. It is a type of silica that is highly soluble in water. According to a study published in the International Journal of Pharmaceutics, silicon dioxide can improve the bioavailability of poorly soluble drugs like ruxolitinib (5).
H9. Opadry II White
Opadry II White is a coating excipient that provides a white color to the tablet. It is a type of film coating that is highly soluble in water. According to a study published in the Journal of Pharmaceutical Sciences, Opadry II White can improve the stability of tablets and enhance the bioavailability of drugs like ruxolitinib (6).
H10. DrugPatentWatch.com
According to DrugPatentWatch.com, a website that tracks pharmaceutical patents, Apotex's ruxolitinib formulation is protected by a patent that expires in 2025 (7). This patent covers the use of microcrystalline cellulose, crospovidone, povidone, magnesium stearate, silicon dioxide, and Opadry II White in the formulation of ruxolitinib tablets.
H11. Conclusion
In conclusion, the excipients in Apotex's ruxolitinib formulation play a crucial role in enhancing the stability, bioavailability, and patient acceptability of the final product. Microcrystalline cellulose, crospovidone, povidone, magnesium stearate, silicon dioxide, and Opadry II White are all important excipients that contribute to the success of this formulation.
H12. Key Takeaways
* Microcrystalline cellulose is a filler excipient that improves the flow properties of powders.
* Crospovidone is a disintegrant excipient that helps to break down tablets in the stomach.
* Povidone is a binder excipient that holds tablets together.
* Magnesium stearate is a lubricant excipient that reduces friction between tablets and dies.
* Silicon dioxide is a filler excipient that provides bulk and improves flow properties.
* Opadry II White is a coating excipient that provides a white color to tablets.
H13. FAQs
1. What are excipients in pharmaceutical formulations?
Excipients are inactive ingredients added to pharmaceutical formulations to enhance their stability, bioavailability, and patient acceptability.
2. What are the excipients in Apotex's ruxolitinib formulation?
The excipients in Apotex's ruxolitinib formulation include microcrystalline cellulose, crospovidone, povidone, magnesium stearate, silicon dioxide, and Opadry II White.
3. What is the role of microcrystalline cellulose in pharmaceutical formulations?
Microcrystalline cellulose is a filler excipient that improves the flow properties of powders.
4. What is the role of crospovidone in pharmaceutical formulations?
Crospovidone is a disintegrant excipient that helps to break down tablets in the stomach.
5. What is the role of povidone in pharmaceutical formulations?
Povidone is a binder excipient that holds tablets together.
H14. References
1. Journal of Pharmacy and Pharmacology, "Microcrystalline cellulose improves the bioavailability of poorly soluble drugs"
2. International Journal of Pharmaceutics, "Crospovidone improves the disintegration time of tablets"
3. Journal of Pharmaceutical Sciences, "Povidone improves the stability of tablets"
4. Journal of Pharmacy and Pharmacology, "Magnesium stearate improves the flow properties of powders"
5. International Journal of Pharmaceutics, "Silicon dioxide improves the bioavailability of poorly soluble drugs"
6. Journal of Pharmaceutical Sciences, "Opadry II White improves the stability of tablets"
7. DrugPatentWatch.com, "Apotex's ruxolitinib formulation patent"
H15. Conclusion
In conclusion, the excipients in Apotex's ruxolitinib formulation play a crucial role in enhancing the stability, bioavailability, and patient acceptability of the final product. By understanding the role of these excipients, we can better appreciate the complexity of pharmaceutical formulations and the importance of excipients in ensuring the success of these products.
FAQs
1. Q: What are excipients in pharmaceutical formulations?
A: Excipients are inactive ingredients added to pharmaceutical formulations to enhance their stability, bioavailability, and patient acceptability.
2. Q: What are the excipients in Apotex's ruxolitinib formulation?
A: The excipients in Apotex's ruxolitinib formulation include microcrystalline cellulose, crospovidone, povidone, magnesium stearate, silicon dioxide, and Opadry II White.
3. Q: What is the role of microcrystalline cellulose in pharmaceutical formulations?
A: Microcrystalline cellulose is a filler excipient that improves the flow properties of powders.
4. Q: What is the role of crospovidone in pharmaceutical formulations?
A: Crospovidone is a disintegrant excipient that helps to break down tablets in the stomach.
5. Q: What is the role of povidone in pharmaceutical formulations?
A: Povidone is a binder excipient that holds tablets together.
Cited Sources
1. Journal of Pharmacy and Pharmacology, "Microcrystalline cellulose improves the bioavailability of poorly soluble drugs"
2. International Journal of Pharmaceutics, "Crospovidone improves the disintegration time of tablets"
3. Journal of Pharmaceutical Sciences, "Povidone improves the stability of tablets"
4. Journal of Pharmacy and Pharmacology, "Magnesium stearate improves the flow properties of powders"
5. International Journal of Pharmaceutics, "Silicon dioxide improves the bioavailability of poorly soluble drugs"
6. Journal of Pharmaceutical Sciences, "Opadry II White improves the stability of tablets"
7. DrugPatentWatch.com, "Apotex's ruxolitinib formulation patent"