Asian Journal of Pharmacy and Technology

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Formulation and Optimization of Porous Osmotic Pump Based Controlled Release System of Ritonavir for the Treatment of HIV Infection


Affiliations
1 Department of Pharmaceutics, Faculty of Pharmacy, University College of Technology, Osmania University, Hyderabad, Telangana - 500007, India
2 Mekelle Institute of Technology, Mekelle University, Mekelle, Ethiopia
3 Department of pharmaceutics, Malla Reddy College of Pharmacy (Affiliated to Osmania University), Maisammaguda, Secunderabad, Telangana - 500014, India
4 Department of pharmaceutical Technology, Netaji Institute of Pharmaceutical Sciences, Toopranpet, Yadadri Bhongir, Telangana - 508252, India
5 Department of Pharmacognosy, Princeton College of Pharmacy, Korremula, Ghatkesar, R.R. District, Telangana - 500088, India
     

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The current research involves the development of controlled porosity osmotic pump (CPOP) tablets of ritonavir for the treatment of HIV infection. Core tablets were prepared by wet granulation method using hydroxyl propyl methyl cellulose (HPMCE5LV) polymer, mannitol as osmogen, MCC as diluents and other additives. The CPOP tablets were coated with cellulose acetate as wall forming material, poly ethylene glycol as flux regulating agent, and sorbitol acts as pore forming material in SPM. The prepared tablets were evaluated for FTIR, DSC, precompression parameters, post compression parameters, in vitro drug release study and scanning electron microscopy study. The optimized formulation RM5 showed 94.83% at the end of 14 hrs with zero order drug release. The difference factor (f1) and similarity factor (f2) for RM5 were observed 14.61 and 75.12 respectively. Optimized formulation did not show any significant change on the pH and agitation intensity, but it depends on osmotic pressure of dissolution media indicated that mechanism of drug release was due to osmotic pressure. SEM micrographs confirmed that no pores were found before dissolution and after dissolution had shown the porous nature of the membrane. Short term stability study at 40 ± 2 °C/75 ± 5% RH for three months on the RM5 formulation indicated that there was no significant change weight variation, %friability, drug content and in vitro drug release.

Keywords

Ritonavir, Wet Granulation, CPOP, Difference Factor, In Vitro Drug Release, Stability Study.
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  • Sahoo CK, Sahoo NK, Rao SRM, Sudhakar M. (2017) A Review on Prevention and Treatment of Aids. Pharm Pharmacol Int J 5(1): 00108.

  • Aungst BJ, P-glycoprotein, secretory transport, and other barriers to the oral delivery of anti-HIV drugs, Adv Drug Del Rev 39, 105-116, 1999.

  • Shafran SD et al. The effect of low-dose ritonavir monotherapy on fasting serum lipid concentrations. HIV Med 6: 421-425, 2005 4. Biswas M, Gupta RN, Parhi R, Sethi KK, Sahoo SK. Formulation and in vitro evaluation of gastroretentive floating drug delivery system of ritonavir, Turk. J. Pharm. Sci. 10(1), 69-86:2013.

  • Sahoo CK, Rao SRM, Sudhakar M and Sahoo NK. Advances in osmotic drug delivery system. J of Chemical and Pharmaceutical Research. 2015; 7:252-273.

  • Verma RK, Krishna DM, Garg S. Formulation aspects in the development of osmotically controlled oral drug delivery systems. J control release; 2000; 79:7-27.

  • Robinson JR, Eriksen SP.Theoratical formulation of sustained dosage forms. J Pharm.Sci. 1966; 55:1254-63.

  • Sahoo CK, Sahoo TK, Moharana AK, Panda KC. Formulation and optimization of porous osmotic pump based controlled release system of Residronate sodium for the treatment of postmenopausal osteoporosis, International Journal of Pharmaceutical Sciences Review and Research, 2012; 12(1):118-122.

  • Jadav MM, Teraiya SR, Patel KN, Patel BA, Patel PA.Formulation and Evaluation of Oral Controlled Porosity Osmotic Pump Tablet of Zaltoprofen International Journal for Pharmaceutical Research Scholars V-1, I-2, 2012, 254-267.

  • Sahoo CK, Sahoo NK, Rao SRM, Sudhakar M, Satyanarayana K. A review on controlled porosity osmotic pump tablets and its evaluation Bulletin of Faculty of Pharmacy, Cairo University 2015; 53 (2):195-205.

  • Sahoo CK, Rao SRM, Sudhakar M.Evaluation of controlled porosity osmotic pump tablets: a review Research J. Pharm. and Tech. 2015; 8(12):119-125.

  • Ranjit Prasad Swain, Nagamani Ragolu, Satyajit Panda. Formulation, In vitro Characterization and Stability Studies of fast Dispersing Tablets of Diclofenac Sodium. J App Pharm Sci, 2015; 5 (07): 094-102.

  • Al-Achi A, Patel B. Formulation and optimization of potassium iodide tablets,Saudi Pharmaceutical Journal, 2015; 23:95-101.

  • El-Bagory I, Barakat N, Ibrahim MA, El-Enazi F. Formulation and in vitro evaluation of theophylline matrix tablets prepared by direct compression: effect of polymer blends,Saudi Pharmaceutical Journal, 2012; 20: 229-238.

  • Shanmugam S, Banthala RS, Ayyappan T, Sundaramoorthy K,Vetrichelvan T.Formulation and evaluation of sustained release matrix tablet of zidovudine using different polymers, Research J. of Pharmaceutical, Biological and Chemical Sciences 2011; 2(1): 576-589.

  • Padmapriya S, Ravichandran V, Suba V. Development and evaluation of swellable elementary osmotic pump tablets of metoprolol succinate and ramipril. Glob J Pharmacol 2013; 7(2):179-86.

  • Moore JW,Flanner HH., Mathematical comparison of curves with an emphasis on in vitro dissolution profiles. Pharm.Tech., 1996, 20, 64-74.

  • Sahoo CK, Rao SRM, Sudhakar M and Kokkula S.The kinetic modeling of drug dissolution for drug delivery systems: an overview.Der Pharmacia Lettre 2015; 7(9):186-194.

  • Costa P,Lobo JMS. Modelling and comparision of dissolution profiles, European J of Pharmaceutical Sciences, 2001; 13:123-133.

  • Banerjee A,Verma PRP,Gore S.Controlled porosity solubility modulated osmotic pump tablets of Gliclazide. AAPS Pharm Sci Tech 2015; 16(3):554-568.

  • Sahoo CK, Rao SRM, Sudhakar M, Bhanja S and Panda N. Development of controlled porosity osmotic pump of ritonavir design, optimization and characterization International Journal of Pharmaceutical Sciences Review and Research 2017; 47(1): 36-44.

  • Khan ZA, Tripathi R, Mishra B. Design and evaluation of enteric coated microporous osmotic pump tablet (ECMOPT) of quetiapine fumarate for the treatment of psychosis.Acta Poloniae –Drug Research 2012; 69(6):1125-1136.

  • Sahoo CK, Rao SRM, and Sudhakar M. Development and evaluation of controlled release formulation of lamivudine based on microporous osmotic tablet technology using fructose as osmogen Indonesian Journal of Pharmacy 2017; 28(3):168- 178.

  • Kumaravelrajan R, Narayanan N, Suba V.Development and evaluation of controlled porosity osmotic pump for Nifedipine and Metoprolol combination. Lipids in Health and Disease. 2011; 10:51.

  • Sahoo CK, Rao SRM, and Sudhakar M. Formulation and optimization of porous osmotic pump tablets based controlled release system of stavudine for the treatment of HIV infection. Current Trends of Pharmaceutical Biotech and Pharmacy 2017; 11(4): 358-370.

  • Dasankoppa FS, Ningangowdar M, Sholapur H. Formulation and evaluation of controlled porosity osmotic pump for oral delivery of ketorolac. Journal of Basic and Clinical Pharmacy. 2013; 4(1):2-9.

  • Sahoo CK, Rao SRM, and Sudhakar M. Formulation and Optimization of Controlled Porosity Osmotic Pump Tablets of Zidovudine using Mannitol as Osmogen for the Treatment of AIDS. International Journal of ChemTech Research 2017; 10(5): 216-235.

  • Kanagale P, Lohray BB, Misra A, Davadra P, Kini R. Formulation and Optimization of Porous Osmotic Pump based Controlled Release System of Oxybutynin. AAPS Pharm Sci Tech. 2007; 8(3): E1-E7.

  • Sahoo CK, Rao SRM, Sudhakar M., and Shashikala P. Formulation and Optimization of Controlled Porosity Osmotic Pump Tablets of Ritonavir, Journal of Chemical and Pharmaceutical Sciences 2017; 10(3): 1345-1352.

  • Rani M, Mishra B. Comparative in vitro and in vivo evaluation of matrix,osmotic matrix and osmotic pump tablets for controlled delivery of diclofenac sodium.AAPS Pharm. Sci Tech. 2004; 5(4):17.

  • Sahoo CK, Rao SRM, Sudhakar M. and Satyanarayana K. Development and Evaluation of Controlled Release Formulation of Zidovudine Based on Microporous Osmotic Tablet Technology Using Fructose as Osmogen. Research J. Pharm. and Tech. 2017; 10(5): 1459-1470.

  • Syed MS, Lahoti S, Syed AA.Controlled porosity osmotic tablet of atenolol: in vitro and in vivo evaluation,Marmara Pharmaceutical Journal, 2016; 20:325-332.

  • Sahoo CK, Rao SRM, and Sudhakar M. Formulation and evaluation of controlled porosity osmotic pump tablets for Zidovudine and Lamivudine combination using fructose as osmogen, Journal of Drug Delivery and Therapeutics. 2017; 7(4):41-50.

  • Sanjay Bajaj, Dinesh Singla and Neha Sakhuja, Stability Testing of Pharmaceutical Products, Journal of Applied Pharmaceutical Science 02 (03); 2012: 129-138.

  • Sahoo CK, Rao SRM, and Sudhakar M. Controlled Porosity Osmotic Pump Tablets of Zidovudine and Lamivudine Combination: Optimization and Characterization. Research Journal of Pharmaceutical Dosage Forms and Technology 2017; 9(3):114-122.


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  • Formulation and Optimization of Porous Osmotic Pump Based Controlled Release System of Ritonavir for the Treatment of HIV Infection

Abstract Views: 451  |  PDF Views: 2

Authors

Chinmaya Keshari Sahoo
Department of Pharmaceutics, Faculty of Pharmacy, University College of Technology, Osmania University, Hyderabad, Telangana - 500007, India
Surepalli Ram Mohan Rao
Mekelle Institute of Technology, Mekelle University, Mekelle, Ethiopia
Muvvala Sudhakar
Department of pharmaceutics, Malla Reddy College of Pharmacy (Affiliated to Osmania University), Maisammaguda, Secunderabad, Telangana - 500014, India
D. Venkata Ramana
Department of pharmaceutical Technology, Netaji Institute of Pharmaceutical Sciences, Toopranpet, Yadadri Bhongir, Telangana - 508252, India
K. Satyanarayana
Department of Pharmacognosy, Princeton College of Pharmacy, Korremula, Ghatkesar, R.R. District, Telangana - 500088, India

Abstract


The current research involves the development of controlled porosity osmotic pump (CPOP) tablets of ritonavir for the treatment of HIV infection. Core tablets were prepared by wet granulation method using hydroxyl propyl methyl cellulose (HPMCE5LV) polymer, mannitol as osmogen, MCC as diluents and other additives. The CPOP tablets were coated with cellulose acetate as wall forming material, poly ethylene glycol as flux regulating agent, and sorbitol acts as pore forming material in SPM. The prepared tablets were evaluated for FTIR, DSC, precompression parameters, post compression parameters, in vitro drug release study and scanning electron microscopy study. The optimized formulation RM5 showed 94.83% at the end of 14 hrs with zero order drug release. The difference factor (f1) and similarity factor (f2) for RM5 were observed 14.61 and 75.12 respectively. Optimized formulation did not show any significant change on the pH and agitation intensity, but it depends on osmotic pressure of dissolution media indicated that mechanism of drug release was due to osmotic pressure. SEM micrographs confirmed that no pores were found before dissolution and after dissolution had shown the porous nature of the membrane. Short term stability study at 40 ± 2 °C/75 ± 5% RH for three months on the RM5 formulation indicated that there was no significant change weight variation, %friability, drug content and in vitro drug release.

Keywords


Ritonavir, Wet Granulation, CPOP, Difference Factor, In Vitro Drug Release, Stability Study.

References