Refine your search
Collections
Co-Authors
A B C D E F G H I J K L M N O P Q R S T U V W X Y Z All
Udupa, Nayanabhirama
- Formulation and Evaluation of Multiparticulate Drug Delivery System of Valsartan
Abstract Views :2044 |
PDF Views:0
Authors
Affiliations
1 Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka-576104, IN
1 Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka-576104, IN
Source
Research Journal of Pharmacy and Technology, Vol 6, No 1 (2013), Pagination: 96-104Abstract
The objective of the present study was to prepare valsartan pellets and to coat with pH-responsive polymers for chronomodulated delivery. The pellets containing valsartan, Avicel and lactose were prepared by extruder spheronizer using different binders HPMC E-5 and PVP K-30. The optimized pellets were coated with different weight ratios of pH-responsive polymers Eudragit® S100 or RS. The pellets were evaluated for physical properties namely, surface appearance, size analysis, content uniformity, micromeritic properties, friability, infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, Feret diameter, aspect ratio, stability study and in vitro release studies. Based on in vitro release studies and SEM analysis, pellets containing 2.5% PVP K-30 were found to be optimized for coating. The drug was compatible when mixed with excipients, which was confirmed by IR spectroscopy and differential scanning calorimetry. Pellets showed good micromeritic properties. Further, in vitro release study of coated pellets revealed optimum lag-time (6±0.25 h) before drug release and Eudragit® S100 with 25% weight gain was optimized. There was no significant change in the drug content and release profile of the pellets stored under accelerated conditions. Thus the multiparticulate delivery system of valsartan found to be suitable as potential chronomodulated drug delivery system to treat early morning surge in hypertensive patients.Keywords
Valsartan, Multiparticulate Drug Delivery System, Pellets, Chronomodulated Drug Delivery, Eudragit®
References
- Mohamad A and Dashevsky A. Development of pulsatile multiparticulate drug delivery system coated with aqueous dispersion Aquacoat ECD. International Journal of Pharmaceutics. 318; 2006: 124-131.
- Madat DV et al. Development of venlafaxine hydrochloride controlled release pellets prepared employing he blend of ethyl cellulose and polyethylene oxide. Research Journal of Pharmacy and Technology. 5; 2012: 1289-1292.
- Rakesh N et al. Drug Multiparticulate Production and Coating Technology – A Review. Research Journal of Pharmacy and Technology. 4; 2011: 1-18.
- Sapkal SR et al. Pellets as Controlled Release Drug Delivery System: A Review, Research Journal of Pharmaceutical Dosage Form and Technology. 1; 2009: 179-183.
- Roy P and Shahiwala A. Multiparticulate formulation approach to pulsatile drug delivery: current perspectives. Journal of Controlled Release.134; 2009: 74-80.
- Garekani HA et al. Preparation and characterization and release properties of Eudragit® RS based ibuprofen pellets prepared by extrusion spheronization: effect of binder type and concentration. Drug Development and Industrial Pharmacy. Early Online; 2012: 1–9.
- Chourasia MK and Jain SK. Polysaccharides based colon-specific drug delivery. In: Progress in Controlled and Novel Drug Delivery System, Edited by Jain NK. CBS Publishers & Distributors, New Delhi, 2005; pp. 405-432.
- Vasanth Kumar K et al. Phase -1 clinical trials on formulation and evaluation of colon specific methylprednisolone matrix enteric coated tablets. Research Journal of Pharmacy and Technology. 5; 2012: 905-911.
- Patil PB et al. Development and Evaluation of Mesalamine Tablet Formulation for Colon Delivery. Research Journal of Pharmacy and Technology. 4; 2011: 1751-1756.
- Jessy Shaji and Amol Shinde. Formulation and Evaluation of Floating Pulsatile Microspheres of Aceclofenac for Rheumatoid Arthritis. Research Journal of Pharmacy and Technology. 4; 2011: 1877-1881.
- Kendall RA and Basit AW. The role of polymers in solid oral dosage forms. In: Polymers in Drug Delivery, Edited by Uchegbu IF, Schatzlein AG. CRC Press, Taylor and Francis group, 2006; pp. 35-48.
- Sureshkumar R et al. Formulation and evaluation of pectinhydroxypropyl methylcellulose coated curcumin pellets for colon delivery. Asian Journal of Pharmaceutics. 3; 2009: 138-142.
- Akhgari A, Sadeghi F and Garekani HA. Combination of timedependent and pH-dependent polymethacrylates as a single coating formulation for colonic delivery of indomethacin pellets International Journal of Pharmaceutics. 320; 2006: 137-142.
- Shivakumar HN, Sarasija S and Desai BG. Design and evaluation of pH sensitive multiparticulate systems for chronotherapeutic delivery of diltiazem hydrochloride. Indian Journal of Pharmaceutical Sciences. 68; 2006: 781-787.
- Nayak UY et al. Chronotherapeutic drug delivery for early morning surge in blood pressure: a programmable delivery system. Journal of Controlled Release. 136; 2009: 125-131.
- Liebermann HA, Lachman L and Schwartz JB. Pharmaceutical Dosage Forms: Tablets. Vol. 2, Marcel Dekker, New York, 1990; pp. 201-243.
- Wells JI and Aulton ME. Pharmaceutical preformulation. In: Aultons Pharmaceutics—the Design and Manufacture of Medicines, Edited by Aulton ME. Elsevier, Churchill Livingstone, 2007; 3rd ed: pp. 337–360.
- Shavi GV et al. Multiparticulate drug delivery system of aceclofenac: Development and in vitro studies. Drug Development and Industrial Pharmacy. 35; 2009: 252–258.
- O’Connor RE and Schwartz JB. Powders. In: Gennaro, A.R. (Ed.) Remington, The Science and Practice of Pharmacy, Vol. 1, Lippincott Williams and Wilkins, USA, 2000; pp. 681-699.
- Rodriguez EC et al. Micromeritic and packing properties of diclofenac pellets and effects of some formulation variables. Drug Development and Industrial Pharmacy. 27; 2001: 847- 855.
- Heng PW, Liew CV and Gu L. Influence of teardrop studs on rotating frictional base plate on spheroid quality in rotary spheronization. International Journal of Pharmaceutics. 241; 2002: 173-184.
- Bornhoft M, Thommes M and Kleinebudde P. Preliminary assessment of carrageenan as excipient for extrusion/spheronisation. European Journal of Pharmaceutics and Biopharmaceutics. 59; 2005: 127–131.
- McConnell EL, Fadda HM and Basit AW. Gut instincts: explorations in intestinal physiology and drug delivery. International Journal of Pharmaceutics. 364; 2008: 213-226.
- McConnell EL, Short MD and Basit AW. An in vivo comparison of intestinal pH and bacteria as physiological trigger mechanisms for colonic targeting in man. Journal of Controlled Release. 130; 2008: 154-160.
- Analysis of Midazolam in Small Volumes of Plasma Using High Performance Liquid Chromatography and UV-Detection Method:Pharmacokinetics of Midazolam in Rats
Abstract Views :182 |
PDF Views:1
Authors
Swapnil J. Dengle
1,
Shriram M. Pathak
1,
Chandra Mohan
2,
Arumugam Karthik
1,
Prashant Musmade
1,
Krishnamurthy Bhat
1,
Nayanabhirama Udupa
1
Affiliations
1 Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal-576104, Karnataka, IN
2 Manipal Acunova Clinical Research Centre, 4th Floor, Shirdi Sai Baba Cancer Hospital, Manipal- 576104, IN
1 Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal-576104, Karnataka, IN
2 Manipal Acunova Clinical Research Centre, 4th Floor, Shirdi Sai Baba Cancer Hospital, Manipal- 576104, IN
Source
Asian Journal of Research in Chemistry, Vol 4, No 3 (2011), Pagination: 406-414Abstract
This research work aims to exploit the high selectivity and sensitivity of UV detector to develop and validate a high performance liquid chromatography (HPLC) method having very small sampling volume, much better mass-sensitive detection limit and lower operating cost for the determination of midazolam, known to have low oral bioavailability, in rat plasma. The chromatographic separation was achieved using a Vydac C18 monomeric (250 × 4. 6 mm inner diameter × 5-μm particle size) column with mobile phase comprising of acetonitrile and potassium dihydrogen phosphate buffer (50:50 v/v), delivered isocratically at a flow rate of 1. 0 ml min-1. Diazepam was used as an internal standard (I. S.). The chromatographic peak-area ratio, based on UV absorbency at 245 nm, was used for quantitative analysis. The statistical evaluation of the method was examined and the method was found to be precise and accurate with a linearity range of 5–3000 ng ml-1 (r > 0. 9980). The intra-day and inter-day precision studies showed good reproducibility with coefficients of variation (C. V.) less than 4. 70%. The developed method is simpler and more sensitive than previously reported methods. The analytical sensitivity and accuracy of this assay were adequate for characterization of midazolam in rat plasma and the assay has been applied successfully to the in vivo pharmacokinetic study of midazolam in rats. After midazolam (5 mg kg-1) was given orally, the maximum concentration (Cmax) and the area under curve (AUC) were 120 ± 35. 38 ng ml-1 and 446. 52 ± 49. 04 ng h ml-1, respectively. The oral bioavailability, F (%), was approximately 24. 75 ± 2. 72%. The developed method holds upper hand over other methods reported in literature so far in terms of both, a small sample volume (200 μl), short analysis time (12. 5 min). Our laboratory is actually involved in a study to investigate the drug-drug interaction studies using oral midazolam as one of the cytochrome P450 (CYP3A) marker compounds in the rat model. The established method provides a reliable bioanalytical methodology to carry out midazolam pharmacokinetics in rat plasma. The small sample volume required makes it possible to study the full pharmacokinetic profile in individual small animals, like the rat.
Keywords
Midazolam, Rat Plasma, HPLC, Validation, Pharmacokinetics.- Mechanisms and Therapeutics of N-acetylcysteine:A Recent Update
Abstract Views :171 |
PDF Views:0
Authors
Affiliations
1 STEER Life India Pvt Ltd, Bengaluru, 560058, Karnataka State, IN
2 Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576104, Karnataka State, IN
1 STEER Life India Pvt Ltd, Bengaluru, 560058, Karnataka State, IN
2 Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576104, Karnataka State, IN
Source
Research Journal of Pharmacy and Technology, Vol 12, No 5 (2019), Pagination: 2584-2588Abstract
N-acetylcysteine (NAC), a precursor and a source of glutathione, which has been used for past four decades, with well-established safety, widely used for the treatment of acetaminophen poisoning and as a mucolytic. NAC also would be administered in combination with certain drugs, imparting beneficial effects and having a medical rationale. NAC is a molecule having a wider therapeutic index with a broad spectrum of prophylactic and therapeutic applications and has become an important social need. Research is ongoing to understand the various pharmacological and biochemical pathways by which NAC exhibits various therapeutic effects. Clinical uses of NAC is attributed, to the presence of thiol group, which acts as a direct antioxidant and also replenishes glutathione levels, which is decreased in various disease conditions. This review aims to understand the role of NAC in various clinical conditions. The article concludes that NAC may be beneficial in some conditions, especially in patients with depleted glutathione, or with oxidative stress, for which patients can be screened before prescribing NAC.Keywords
N-Acetylcysteine, Oxidative Stress, Antioxidant, Glutathione, Free Radicals.References
- Green J.L., Heard K.J., Reynolds K.M., Albert D. Oral and intravenous acetylcysteine for treatment of acetaminophen toxicity: a systematic review and meta-analysis West. J. Emerg. Med. 2013; 14 (3), 218–226
- Hurst, G. A., Shaw, P. B., and Le Maistre, C. A. Laboratory and clinical evaluation of the mucolytic properties of acetylcysteine. Am Rev Respir Dis. 1967;96, 962–970.
- Prescott, L. F., Park, J., Ballantyne, A., Adriaenssens, P., and Proudfoot, A. T. Treatment of paracetamol (acetaminophen) poisoning with N-acetylcysteine. Br Med J 1977; 432–434.
- Samuni Y, Goldstein S, Dean OM, Berk M. The chemistry and biological activities of N- acetylcysteine. Biochim Biophys Acta. 2013 Aug;1830(8):4117–29.
- WO2010090611A2.pdf [Internet]. Available from: https://patentimages.storage.googleapis.com/69/cb/89/9d6adfa6c53396/WO2010090611A2.pdf Last accessed Nov 21, 2018
- Cattermole G. Should N-Acetylcysteine be Administered Orally or Intravenously for the Treatment of Paracetamol Overdose? Hong Kong Journal of Emergency Medicine. 2009 Apr;16(2):106–16.
- Cotgreave IA. N-acetylcysteine: pharmacological considerations and experimental and clinical applications. Adv Pharmacol. 1997; 38: 205–27.
- Borgström L, Kågedal B, Paulsen O. Pharmacokinetics of N-acetylcysteine in man. Eur J Clin Pharmacol. 1986;31(2):217–22.
- RxList website. https://www.rxlist.com/cetylev-drug.htm. Last accessed Nov 21, 2018
- Witschi A, Reddy S, Stofer B, Lauterburg BH. The systemic availability of oral glutathione. Eur J Clin Pharmacol. 1992;43(6):667–9.
- Sjödin K, Nilsson E, Hallberg A, Tunek A. Metabolism of N-acetyl-L-cysteine. Some structural requirements for the deacetylation and consequences for the oral bioavailability. Biochem Pharmacol. 1989 Nov 15;38(22):3981–5.
- Mallard WG, Ross AB, Helman WP. NIST Standard Reference Database 1998;40, Version 3.0, NIST, Gaithersburg, MD
- Trujillo M, Radi R. Peroxynitrite reaction with the reduced and the oxidized forms of lipoic acid: new insights into the reaction of peroxynitrite with thiols. Arch Biochem Biophys 2002; 397: 91–98.
- Omara FO, Blakley BR, Bermier J, Fournier M. Immunomodulatory and protective effects of N-acetylcysteine in mitogen-activated murine splenocytes in vitro. Toxicology 1997; 116: 219–226.
- Emet S, Memis D, Pamukçu Z. The influence of N-acetyl-L-cystein infusion on cytokine levels and gastric intramucosal pH during severe sepsis. Critical Care 2004; 8: 172–179.
- Pajonk F, Riess K, Sommer A, McBride WH. N-acetyl-L-cysteine inhibits 26S proteosome function: implications for effects on NF-kappaB activation. Free Radical Biol Med 2002; 32 (6): 536–543.
- Astiz M, de Alaniz MJT, Marra CA. The oxidative damage and inflammation caused by pesticides are reverted by lipoic acid in rat brain. Neurochemistry International 2012; 61: 1231–1241
- Ullian, M. E., Gelasco, A. K., Fitzgibbon, W. R., Beck, C. N., and Morinelli, T. A. (2005). N-acetylcysteine decreases angiotensin II receptor binding in vascular smooth muscle cells. J Am Soc Nephrol. 2005;16, 2346–2353.
- Hayakawa M, Miyashita H, Sakamoto I, Kitagawa M, Tanaka H, Yasuda H, Karin M, Kikugawa K. Evidence that reactive oxygen species do not mediate NF‐κB activation. The EMBO journal. 2003;22(13):3356-66.
- Greene SC, Noonan PK, Sanabria C, Peacock WF. Effervescent N-Acetylcysteine Tablets versus Oral Solution N-Acetylcysteine in Fasting Healthy Adults: An Open-Label, Randomized, Single-Dose, Crossover, Relative Bioavailability Study. Curr Ther Res Clin Exp. 2016 Jun 27; 83:1–7.
- Blackford MG, Felter T, Gothard MD, Reed MD. Assessment of the clinical use of intravenous and oral N-acetylcysteine in the treatment of acute acetami- nophen poisoning in children: a retrospective review. Clin Ther. 2011;33: 1322–30.
- WO2011128230A1.pdf [Internet]. [cited 2018 Nov 7]. Available from: https://patentimages.storage.googleapis.com/20/df/2c/060b487cff1426/WO2011128230A1.pdf
- Mahmut B. Stable, taste and odor masked pharmaceutical compositions comprising acetylcystein and vitamin c [Internet]. WO2010090612A1, 2010 [cited 2018 Nov 7]. Available from https://patents.google.com/patent/WO2010090612A1/en?oq=WO2010%2f090612;+Bilgic+Mahmut%2c+2010).+
- Smilkstein MJ, Knapp GL, Kulig KW, Rumack BH. Efficacy of oral N-acetylcysteine in the treatment of acetaminophen overdose. Analysis of the national multicenter study (1976 to 1985). N Engl J Med 1988; 319:1557.
- Smilkstein MJ, Bronstein AC, Linden C, et al. Acetaminophen overdose: a 48-hour intravenous N-acetylcysteine treatment protocol. Ann Emerg Med 1991; 20:1058.
- Prescott LF, Park J, Ballantyne A, et al. Treatment of paracetamol (acetaminophen) poisoning with N-acetylcysteine. Lancet 1977; 2:432.
- Prescott LF. Treatment of severe acetaminophen poisoning with intravenous acetylcysteine. Arch Intern Med 1981; 141:386.
- Nambiar NJ. Management of Paracetamol Poisoning: The Old and the New. Journal of Clinical and Diagnostic Research. 2012;6(6).
- Chyka PA, Butler AY, Holliman BJ, Herman MI. Utility of acetylcysteine in treating poisonings and adverse drug reactions. Drug safety. 2000;22(2):123-48.
- Rowe SM, Clancy JP. Advances in cystic fibrosis therapies. Current opinion in pediatrics. 2006;18(6):604-13.
- Sheffner AL, Medler EM, Jacobs LW, Sarett HP. The in vitro reduction in viscosity of human tracheobronchial secretions by acetylcysteine. American Review of Respiratory Disease. 1964;90(5):721-9.
- Rahman I, MacNee W. Regulation of redox glutathione levels and gene transcription in lung inflammation: therapeutic approaches. Free Radical Biology and Medicine. 2000;28(9):1405-20.
- Ratjen F, Grasemann H. New therapies in cystic fibrosis. Current pharmaceutical design. 2012;18(5):614-27. I have removed this reference
- Grassi C. Long-term oral acetylcysteine in chronic bronchitis. A double- blind controlled study. Eur. J. Respir. Dis. 1980; 61:93-108.
- Dworski R. Oxidant stress in asthma. Thorax. 2000;55(suppl 2): S51-3.
- Carbonell N, Sanjuán R, Blasco M, Jordá Á, Miguel A. N-acetylcysteine: short-term clinical benefits after coronary angiography in high-risk renal patients. Revista Española de Cardiología (English Edition). 2010;63(1):12-9.
- Koc F, Ozdemir K, Kaya MG, Dogdu O, Vatankulu MA, Ayhan S, Erkorkmaz U, Sonmez O, Aygul MU, Kalay N, Kayrak M. Intravenous N-acetylcysteine plus high-dose hydration versus high-dose hydration and standard hydration for the prevention of contrast-induced nephropathy: CASIS—a multicenter prospective controlled trial. International journal of cardiology. 2012;155(3):418-23.
- Goldenberg I, Shechter M, Matetzky S, Jonas M, Adam M, Pres H, Elian D, Agranat O, Schwammenthal E, Guetta V. Oral acetylcysteine as an adjunct to saline hydration for the prevention of contrast-induced nephropathy following coronary angiography: a randomized controlled trial and review of the current literature. European heart journal. 2004;25(3):212-8.
- Gurm HS, Smith DE, Berwanger O, Share D, Schreiber T, Moscucci M, Nallamothu BK, BMC2 (Blue Cross Blue Shield of Michigan Cardiovascular Consortium. Contemporary use and effectiveness of N-acetylcysteine in preventing contrast-induced nephropathy among patients undergoing percutaneous coronary intervention. JACC: Cardiovascular Interventions. 2012;5(1):98-104.
- Sun Z, Fu Q, Cao L, Jin W, Cheng L, Li Z. Intravenous N-acetylcysteine for prevention of contrast-induced nephropathy: a meta-analysis of randomized, controlled trials. PloS one. 2013;8(1):55124.
- Lapenna D, de Gioia S, Ciofani G, Mezzetti A, Ucchino S, Calafiore AM, Napolitano AM, Di Ilio C, Cuccurullo F. Glutathione-related antioxidant defenses in human atherosclerotic plaques. Circulation. 1998 May;97(19):1930-4.
- Mazzanti L, Mutus B. Diabetes-induced alterations in platelet metabolism. Clinical biochemistry. 1997;30(7):509-15.
- Martina V, Masha A, Gigliardi VR, Brocato L, Manzato E, Berchio A, et al. Long-term N-acetylcysteine and L-arginine administration reduces endothelial activation and systolic blood pressure in hypertensive patients with type 2 diabetes. Diabetes Care. 2008;31, 940–944.
- Treweeke AT, Winterburn TJ, Mackenzie I, Barrett F, Barr C, Rushworth GF, Dransfield I, Mac Rury SM, Megson IL. N-Acetylcysteine inhibits platelet–monocyte conjugation in patients with type 2 diabetes with depleted intraplatelet glutathione: a randomised controlled trial. Diabetologia. 2012;55(11):2920-8.
- De Flora S, Izzotti A, D'agostini F, Balansky RM. Mechanisms of N-acetylcysteine in the prevention of DNA damage and cancer, with special reference to smoking-related end-points. Carcinogenesis. 2001;22(7):999-1013.
- Van Zandwijk N, Dalesio O, Pastorino U, De Vries N, Van Tinteren H. EUROSCAN, a randomized trial of vitamin A and N-acetylcysteine in patients with head and neck cancer or lung cancer. Journal of the National Cancer Institute. 2000;92(12):977-86.
- Wanamarta AH, van Rijn J, Blank LE, Haveman J, van Zandwijk N, Joenje H. Effect of N-acetyl cysteine on the antiproliferative action of X-rays or bleomycin in cultured human lung tumor cells. J Cancer Res Clin Oncol. 1989; 115(4): 340-344.
- Dean O, Giorlando F, Berk M. N-acetylcysteine in psychiatry: current therapeutic evidence and potential mechanisms of action. Journal of psychiatry and neuroscience: JPN. 2011;36(2):78.
- Martinez-Banclocha MA. N-acetyl cysteine in the treatment of Parkinson’s disease. What are we waiting for? Med Hypotheses. 2012; 79(1): 8-12.
- Hardan AY, Fung LK, Libove RA, Obukhanych TV, Nair S, Herzenberg LA, Frazier TW, Tirouvanziam R. A randomized controlled pilot trial of oral N-acetylcysteine in children with autism. Biological psychiatry. 2012;71(11):956-61.
- Nasr A. Effect of N-acetyl cysteine after ovarian drilling in clomiphene citrate-resistant PCOS women: a pilot study. Reprod Biomed Online. 2010; 20(3): 403-409.
- Fulghesu AM, Ciampelli M, Muzj G, Belosi C, Selvaggi L, Ayala GF, et al. N-acetyl-cysteine treatment improves insulin sensitivity in women with polycystic ovary syndrome. Fertil Steril 2002;77:1128–35.
- Solubility Enhancement of Lumefantrine by Hot Melt Extrusion Process
Abstract Views :157 |
PDF Views:0
Authors
Rakshith Shetty
1,
Vaishnavi Tallapaneni
2,
M. Sreenivasa Reddy
2,
Nayanabhirama Udupa
2,
Srinivas Mutalik
2,
Vijay Kulkarni
1,
Vinay Rao
1,
Aravind Kumar Gurram
1
Affiliations
1 STEER Life India Pvt Ltd, Bengaluru 560058, Karnataka State, IN
2 Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576104, Karnataka State, IN
1 STEER Life India Pvt Ltd, Bengaluru 560058, Karnataka State, IN
2 Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576104, Karnataka State, IN
Source
Research Journal of Pharmacy and Technology, Vol 12, No 6 (2019), Pagination: 2929-2935Abstract
Lumefantrine is a BCS class -II drug having a poor aqueous solubility. There is a need for improvement in solubility, in order to enhance the therapeutic efficacy and reduce the dose. Hence in the present work, the solubility of lumefantrine is enhanced by formulating solid dispersions of lumefantrine using a hot melt extrusion process in a twin-screw processor using three different polymers such as Kollidon VA64, Soluplus and HPMC AS at a weight ratio of 1:2, 1:3 and 1:4, processed at different barrel temperatures and screw speeds. The obtained solid dispersions were characterized by differential scanning calorimetry and solubility studies. Solid dispersions prepared with KollidonVA64 and Soluplus showed a clear extrudate indicating a complete amorphous conversion of the lumefantrine at all the three ratios evaluated. Increase in polymer concentration, increased the solubility of the lumefantrine. With Kollidon VA 64 and Soluplus, lumefantrine to polymer ratio of 1:4 showed the highest increase in solubility, compared to that of the pure lumefantrine.Keywords
Lumefantrine, Polymers, Twin Screw Extrusion, Solid Dispersion, Solubility.References
- Fule R, Meer TA, Sav A, Amin P. Solubility and dissolution rate enhancement of lumefantrine using hot melt extrusion technology with physicochemical characterisation. Journal of Pharmaceutical Investigation. 2013 Aug 1;43.
- Kolter K, Karl M, Gryczke A. Hot-Melt Extrusion with BASF Pharma Polymers. :201.
- Maniruzzaman M, Boateng JS, Snowden MJ, Douroumis D. A Review of Hot-Melt Extrusion: Process Technology to Pharmaceutical Products [Internet]. International Scholarly Research Notices. 2012 [cited 2018 Aug 29]. Available from: https://www.hindawi.com/journals/isrn/2012/436763/
- Patil H, Tiwari RV, Repka MA. Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation. AAPS Pharm SciTech. 2015 Jul 10; 17(1):20–42.
- Enose AA, Dasan PK, Sivarama krishnan H, Shah SM. Formulation and Characterization of Solid Dispersion Prepared by Hot Melt Mixing: A Fast Screening Approach for Polymer Selection [Internet]. Journal of Pharmaceutics. 2014 [cited 2018 Aug 29]. Available from: https://www.hindawi.com/journals/jphar/2014/105382/
- Malaria: Symptoms, treatment, and prevention [Internet]. Medical News Today. [cited 2018 Aug 29]. Available from: https://www.medicalnewstoday.com/articles/150670.php
- Jain JP, Leong FJ, Chen L, Kalluri S, Koradia V, Stein DS, et al. Bioavailability of Lumefantrine Is Significantly Enhanced with a Novel Formulation Approach, an Outcome from a Randomized, Open-Label Pharmacokinetic Study in Healthy Volunteers. Antimicrobial Agents and Chemotherapy. 2017 Sep 1;61(9):e00868-17.
- MA091part4v1.pdf [Internet]. [cited 2018 Aug 19]. Available from: https://extranet.who.int/prequal/sites/default/files/documents/MA091part4v1.pdf
- Coartem (Artemether Lumefantrine Tablets): Side Effects, Interactions, Warning, Dosage & Uses [Internet]. Rx List. [cited 2018 Nov 27]. Available from: https://www.rxlist.com/coartem-drug.htm
- Gryczke A. Solid Dispersions by Hot-Melt Extrusion [Internet]. [cited 2018 Aug 15]. Available from: http://www.pharmtech.com/solid-dispersions-hot-melt-extrusion