Physicochemical Properties of Ritonavir

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Physicochemical Properties

of Ritonavir
• Ritonavir – A HIV protease inhibitors.

Molecular • 720.9 g/mol


Weight • Large, peptide-like molecule

Melting • 120- 122 ⁰C (Tiwari & Bonde, 2011)


Point

Purity • 99.4%, high purity (Chinnaiah et al., 2015)

LogP • 3.546 (DrugBank; Tiwari & Bonde, 2011)


• Ritonavir = weak-base drug with pH-dependent solubility
Pka • Pka values = 1.8 and 2.6 (Law et al., 2001; Xu et al., 2017)

• Soluble in inorganic solvent like ethanol (5 mg/ml), DMSO


Solubility (15 mg/ml)
• Poorly soluble in water .

• Store between 5° and 30°.


• Thermal degradation study (Gambhir et al., 2015)
• drug started degrading at 80 °C
Stability • major structural changes after exposure to thermal
radiation at 100 °C
• completely decomposed after 200 °C.
References
1. Chinnaiah P, Lanka AR, Pamidi S, Govada PP, LNSR Jillella V. NEW VALIDATED RP-HPLC METHOD FOR IDENTIFICATION AND
QUANTITATION OF PROCESS AND DEGRADATION RELATED IMPURITIES IN THE COMBINED DOSAGE TABLETS OF ATAZANAVIR AND
RITONAVIR [Internet]. Vol. 2, Palavan Chinnaiah /J Compr Phar. 2015 [cited 2020 Nov 11]. Available from: www.jcponline.in
2. Ritonavir | 155213-67-5 [Internet]. [cited 2020 Nov 11]. Available from:
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB0119429.htm
3. Tiwari RN, Bonde CG. LC, LC-MS/TOF and MSn studies for the separation, identification and characterization of degradation products
of ritonavir. Anal Methods [Internet]. 2011 Jul [cited 2020 Nov 11];3(7):1674. Available from: http://xlink.rsc.org/?DOI=c1ay05140g
4. Xu H, Vela S, Shi Y, Marroum P, Gao P. In Vitro Characterization of Ritonavir Drug Products and Correlation to Human in Vivo
Performance. Mol Pharm [Internet]. 2017 Nov 6 [cited 2020 Nov 11];14(11):3801–14. Available from:
https://pubs.acs.org/doi/10.1021/acs.molpharmaceut.7b00552
5. Law D, Krill SL, Schmitt EA, Fort JJ, Qiu Y, Wang W, et al. Physicochemical considerations in the preparation of amorphous ritonavir-
poly(ethylene glycol) 8000 solid dispersions. J Pharm Sci [Internet]. 2001 Aug [cited 2020 Nov 11];90(8):1015–25. Available from:
https://linkinghub.elsevier.com/retrieve/pii/S0022354916307869
6. Gambhir K, Singh P, Jangir DK, Mehrotra R. Thermal stability and hydration behavior of ritonavir sulfate: A vibrational spectroscopic
approach. J Pharm Anal [Internet]. 2015 Dec 1 [cited 2020 Nov 11];5(6):348–55. Available from:
https://linkinghub.elsevier.com/retrieve/pii/S2095177915000519
7. (No Title) [Internet]. [cited 2020 Nov 11]. Available from: https://www.caymanchem.com/pdfs/13872.pdf

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