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Formulation and Evaluation of Indinavir Sulfate Capsules by Novel Technology Using Qbd Approach
Corresponding Author(s) : Mohammed Muzaffar Ahmed
International Journal of Allied Medical Sciences and Clinical Research,
Vol. 12 No. 4 (2024): 2024 Volume -12 - Issue 4
Abstract
The formulation the drug release up to 45 minutes. The formulation prepared with lactose monohydrates Crospovidone and magnesium stearates.G granulation procedure was the chosen technology for the preparation of Indinavir Sulfate capsule. Based on the preliminary studies, different formulation trials (F1-F7) were carried out with different concentrations of Disintegrants, diluents. From the various formulations it was decided that the formulation batch of F7 was finalized as the optimized formula.. Formulation F7 showed satisfactory results with various physicochemical evaluation parameters like Disintegration time, Dissolution profile, Assay when matched with that of the marketed product. The stability studies at all conditions, indicates that the formulated capsules were found to be stable. Hence, it is finally concluded that, Indinavir Sulfate capsules are pharmaceutically comparable, low cost, quality improved and stable formulation. This study has potential commercial and industrial applications after establishing the real-time stability, safety and efficacy.
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- Dailly, E.; Thomas, L.; Kergueris, T.M.F.; Jolliet, P.; Bourin, M. High-performance liquid chromatographic assay to determine the plasma levels of HIV-protease inhibitors (amprenavir, indinavir, nelfinavir, ritonavir and saquinavir) and the non-nucleoside reverse transcriptase inhibitor (nevirapine) after liquid–liquid extraction. J. Chromatogr., B, v.758, n.2, p.129–135, 2001.
- FOISY, M.L.; SOMMADOSSI, J.P. Rapid quantification of indinavir in human plasma by high-performance liquid chromatography with ultraviolet detection. J. Chromatogr., B, v.721, n.2, p.239–247, 1999.
- Haas, D.W.; Stone, J.; Clough, L.A.; Johnson, B.; Spearman, P.; Harris, V.L.; Nicotera,J.; Johnson, R.H.; Raffanti, S.; Zhong, L.; Bergqwist, P.; Chaberlin, S.; Hoagland, V.D.; Ju, W. Steady-state pharmacokinetics of Indinavir in cerebrospinal fluid and plasma among adults with human immunodeficiency virus type 1 infection. J. Clin. Pharm. Ther., v.68, n. p.367-374, 2000.
- Hugen, P.W.H.; Verweij-Van, C.P.W.G.M.; Burger, D.M.; Wuis, E.W.; Koopmans, P.P.; Hekster, Y.A. Simultaneous determination of the HIV-protease inhibitors indinavir, nelfinavir, saquinavir and ritonavir in human plasma by reversed-phase high-performance liquid chromatography. J. Chromatogr., B, v.727, n.1/2, p.139– 149, 1999.
- Hurwitz, S.J.; Schinazi, R.F. Development of a pharmacodynamic model for HIV treatment with nucleoside reverse transcriptase and protease inhibitors. Antiviral Res., v.56, n.2, p.115-127, 2002.
- JAYEWARDENE, A.L.; ZHU, F.; AWEEKA, F.T.; GAMBERTOGLIO, J.G. Simple high-performance liquid chromatographic determination of the protease inhibitor Indinavir in human plasma. J. Chromatogr., B, v.707, n.1/ 2, p.203–211, 1998.
- JAYEWARDENE, A.L.; KEARNEY, B.; STONE, J.A.; GAMBERTOGLIO, J.G.; AWEEKA, F.T. An LC-MSMS method for the determination of indinavir, an HIV-1 protease inhibitor, in human plasma. J. Pharm. Biomed. Anal., v.25, n.2, p.309–317, 2001. A
- Pereira EA, Micke GA, Tavares MFM. Development and Validation of a Capillary Electrophoresis Method for the Determination of Sulfate in Indinavir Sulfate Raw Material. J. Braz. Chem. Soc. 2007; 17: 251-256.
- Gulick RM, Meibohm A, Havlir D. Six-year follow-up of HIV-1 infected adults in a clinical trial of antiretroviral therapy with indinavir, zidovudine and lamivudine. AIDS. 2003; 17: 2345–2349.
- Kopp JB, Miller KD, Mican JA. Crystalluria and urinary tract abnormalities associated with indinavir. Ann Intern Med. 1997; 127: 119–125. 4. Boubaker K, Sudre P, Bally F. Changes in renal function associated with indinavir. AIDS. 1998; 12: F249–F254.
- Berns JS, Cohen RM, Silverman M. Acute renal failure due to indinavir crystalluria and nephrolithiasis: report of two cases. Am J Kidney Dis. 1997; 30: 558–560.
- .Vigano A, Rombola G, Barbiano DI, Belgioioso G. Subtle occurrence of indinavir-induced acute renal insufficiency. AIDS. 1998; 12: 954–955.
- Jain S, Sapre R, Tiwary AK, Jain NK. Proultraflexible lipid vesicles for effective transdermal delivery of levonorgestrel: development, characterization, and performance evaluation. AAPS PharmSciTech. 2005;
- Mezei M, Gulasekharn V. Liposomes a selective drug delivery system for topical route of administration 1. Lotion dosages form. Life Sci. 1980; 26: 1473–1477.
- Touitou E, Junginger HE, Weiner ND, Nagai T, Mezei M. Liposomes as a carrier for topical and transdermal delivery. J. Pharm. Sci. 1994; 83: 1189–1203.
- ANGMANN, P.; KLINDER, H.; SCHIRMER, D.; ZILLY, M.; RICHTER, E. High-performance liquid chromatographic method for the simultaneous determination of HIV-1 protease inhibitors indinavir, saquinavir and ritonavir in plasma of patients during highly active antiretroviral therapy. J. Chromatogr., B, v.735, n.1, p.41–50, 1999.
- LIN, J.H. Role of pharmacokinetics in the discovery and development of Indinavir. Adv. Drug Delivery Rev., v.39, n.1/3, p.33-49, 1999. LIN, J.H. Human immunodeficiency virus protease inhibitors from drug design to clinical studies. Adv. Drug Delivery Rev., v.27, n.2/3, p.215-233, 1997.
References
Dailly, E.; Thomas, L.; Kergueris, T.M.F.; Jolliet, P.; Bourin, M. High-performance liquid chromatographic assay to determine the plasma levels of HIV-protease inhibitors (amprenavir, indinavir, nelfinavir, ritonavir and saquinavir) and the non-nucleoside reverse transcriptase inhibitor (nevirapine) after liquid–liquid extraction. J. Chromatogr., B, v.758, n.2, p.129–135, 2001.
FOISY, M.L.; SOMMADOSSI, J.P. Rapid quantification of indinavir in human plasma by high-performance liquid chromatography with ultraviolet detection. J. Chromatogr., B, v.721, n.2, p.239–247, 1999.
Haas, D.W.; Stone, J.; Clough, L.A.; Johnson, B.; Spearman, P.; Harris, V.L.; Nicotera,J.; Johnson, R.H.; Raffanti, S.; Zhong, L.; Bergqwist, P.; Chaberlin, S.; Hoagland, V.D.; Ju, W. Steady-state pharmacokinetics of Indinavir in cerebrospinal fluid and plasma among adults with human immunodeficiency virus type 1 infection. J. Clin. Pharm. Ther., v.68, n. p.367-374, 2000.
Hugen, P.W.H.; Verweij-Van, C.P.W.G.M.; Burger, D.M.; Wuis, E.W.; Koopmans, P.P.; Hekster, Y.A. Simultaneous determination of the HIV-protease inhibitors indinavir, nelfinavir, saquinavir and ritonavir in human plasma by reversed-phase high-performance liquid chromatography. J. Chromatogr., B, v.727, n.1/2, p.139– 149, 1999.
Hurwitz, S.J.; Schinazi, R.F. Development of a pharmacodynamic model for HIV treatment with nucleoside reverse transcriptase and protease inhibitors. Antiviral Res., v.56, n.2, p.115-127, 2002.
JAYEWARDENE, A.L.; ZHU, F.; AWEEKA, F.T.; GAMBERTOGLIO, J.G. Simple high-performance liquid chromatographic determination of the protease inhibitor Indinavir in human plasma. J. Chromatogr., B, v.707, n.1/ 2, p.203–211, 1998.
JAYEWARDENE, A.L.; KEARNEY, B.; STONE, J.A.; GAMBERTOGLIO, J.G.; AWEEKA, F.T. An LC-MSMS method for the determination of indinavir, an HIV-1 protease inhibitor, in human plasma. J. Pharm. Biomed. Anal., v.25, n.2, p.309–317, 2001. A
Pereira EA, Micke GA, Tavares MFM. Development and Validation of a Capillary Electrophoresis Method for the Determination of Sulfate in Indinavir Sulfate Raw Material. J. Braz. Chem. Soc. 2007; 17: 251-256.
Gulick RM, Meibohm A, Havlir D. Six-year follow-up of HIV-1 infected adults in a clinical trial of antiretroviral therapy with indinavir, zidovudine and lamivudine. AIDS. 2003; 17: 2345–2349.
Kopp JB, Miller KD, Mican JA. Crystalluria and urinary tract abnormalities associated with indinavir. Ann Intern Med. 1997; 127: 119–125. 4. Boubaker K, Sudre P, Bally F. Changes in renal function associated with indinavir. AIDS. 1998; 12: F249–F254.
Berns JS, Cohen RM, Silverman M. Acute renal failure due to indinavir crystalluria and nephrolithiasis: report of two cases. Am J Kidney Dis. 1997; 30: 558–560.
.Vigano A, Rombola G, Barbiano DI, Belgioioso G. Subtle occurrence of indinavir-induced acute renal insufficiency. AIDS. 1998; 12: 954–955.
Jain S, Sapre R, Tiwary AK, Jain NK. Proultraflexible lipid vesicles for effective transdermal delivery of levonorgestrel: development, characterization, and performance evaluation. AAPS PharmSciTech. 2005;
Mezei M, Gulasekharn V. Liposomes a selective drug delivery system for topical route of administration 1. Lotion dosages form. Life Sci. 1980; 26: 1473–1477.
Touitou E, Junginger HE, Weiner ND, Nagai T, Mezei M. Liposomes as a carrier for topical and transdermal delivery. J. Pharm. Sci. 1994; 83: 1189–1203.
ANGMANN, P.; KLINDER, H.; SCHIRMER, D.; ZILLY, M.; RICHTER, E. High-performance liquid chromatographic method for the simultaneous determination of HIV-1 protease inhibitors indinavir, saquinavir and ritonavir in plasma of patients during highly active antiretroviral therapy. J. Chromatogr., B, v.735, n.1, p.41–50, 1999.
LIN, J.H. Role of pharmacokinetics in the discovery and development of Indinavir. Adv. Drug Delivery Rev., v.39, n.1/3, p.33-49, 1999. LIN, J.H. Human immunodeficiency virus protease inhibitors from drug design to clinical studies. Adv. Drug Delivery Rev., v.27, n.2/3, p.215-233, 1997.