Research Journal of Pharmacy and Technology

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Adsorption of Nifedipine on Porous Calcium silicate for Enhancement of Solubility and Dissolution Rate


Affiliations
1 Annasaheb Dange College of B Pharmacy, Ashta, Sangli - 416301 Maharashtra, India
2 Krishna Institute of Medical Sciences, Krishna Institute of Pharmacy, Karad, Satara 415110 Maharashtra, India
3 Rajarambapu College of Pharmacy, Kasegaon, Sangli -415404 Maharashtra, India
     

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The enhancement in solubility and dissolution rate of poorly soluble drug Nifedipine was achieved by its adsorption on porous calcium silicate by using common volatile organic solvent chloroform. The yield of the adsorption process was found in a range of 90 -95% which indicates negligible loss during chloroform treatment. Saturation solubility studies showed 273% increase as compared to pure drug indicating adsorption of poorly soluble drug on porous calcium silicate was prominent in solubility enhancement. Physicochemical properties of pure Nifedipine compared to adsorbed product studied by FT-IR, DSC and PXRD. The FTIR and DSC studies does not show any unexpected interaction between Nifedipine and calcium silicate, while slight broadening in peak as well reduction in intensity and early onset as compared to the pure drug indicates adsorption of Nifedipine on porous calcium silicate. PXRD diffractograms showed a Significant reduction in peak intensities in drug adsorbed product compare to Nifedipine was attributed to the dilution effect of porous calcium silicate and confirms conversion of crystalline nature of drug in amorphous. Adsorption of the drug over FLR particles seen in SEM images of the adsorbed product while a significant change in surface morphology of Nifedipine was observed due to complete solubilization of Nifedipine and FLR in common solvent. The dissolution rate of the drug from adsorbed products was significantly rapid compared with pure drug, and the dissolution rate increases with increase in the proportion of FLR from 1:1.5 to 1:3, but further increase in the proportion of FLR not showed a significant increase in its dissolution indicating saturation. The drug adsorbed product was found stable as there was no any significant change in appearance and drug dissolution after three months stability studies.

Keywords

Nifedipine, Calcium Silicate, Adsorption, Solubility Enhancement.
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  • AV Bhosale, SR Hardikar, Naresh Patil, Rajesh Jagtap, Nilesh Jamdade Bhavin Patel, IVIVC and BCS: A Regulatory Perspective, Research J. Pharm. and Tech, 2009;2(1):72-79

  • Hiroyuki o. atsuo, M takurou, K Yuji, M Yasunori, I Takashi, S Shigeru, Freeze-dried nifedipine-lipid nanoparticles with long-term nano-dispersion stability after reconstitution. Int. J. Pharm, 2009; 377: 180-184.

  • Paun J.S., Tank H.M. Nanosuspension: An Emerging Trend for Bioavailability Enhancement of Poorly Soluble Drugs. Asian J. Pharm. Tech. 2012; 2(4): 157-168.

  • Manoj K. Baladaniya, Ankit P. Karkar, Jatin R Kambodi. Enhancement of Dissolution Properties of Glibenclamide by using Liquisolid Compact Technique. Res. J. Pharm. Dosage Form. and Tech. 2015; 7(3):199-211.

  • Shrinivas K. Mohite, Shantanu B. Kuchekar, Application of 32 Factorial Design in the Formulation of Fast Release Olmesartan Medoxomil Liquisolid Tablets, Research J. Pharm. and Tech,2015; 8(7)

  • Kevin C Garala, Anil J Shinde, Harinath N More. Solubility Enhancement of Aceclofenac Using Dendrimer. Research J. Pharma. Dosage Forms and Tech. 2009; 1(2): 94-96 .

  • Mitchell, S.A., Reynolds, T.D., Dasbach, T.P., A compaction process to enhance dissolution of poorly water-soluble drugs using hydroxypropyl methylcellulose. Int. J. Pharm.; 25: 3–11.

  • Sugimoto, M., Okagaki, T., Narisawa, S., Koida, Y., Nakajima, K., Improvement of dissolution characteristics and bioavailability of poorly water-soluble drugs by novel co grinding method using water-soluble polymer. Int. J. Pharm. 1998; 160: 11–19.

  • Hajare AA, Shetty YT, Mali MN, Sarvagod SM. Characterization of Melt (Fusion) Solid Dispersions of Nifedipine. Research J. Pharm. and Tech. 2008; 1(3): 230-234.

  • Shaikh Mohammed Vasim. Effervescent Mixture Based Solid Dispersion a Novel Approach for Solubility Enhancement. Research J. Pharm. and Tech. 2011; 4(11):1682-1686.

  • Hirayama, F., Wang, Z., Uekema, K., Effect of 2- hydroxypropyl-beta-cyclodextrin on crystallization and polymorphic transition of nifedipine in solid state. Pharm. Res.1994;11: 1766–1770.

  • Jagtap Rajesh, Doijad Rajendra, Mohite Shrinivas, Enhancement Of Solubility and Dissolution Rate Of Nifedipine By Using Novel Solubilizer Sepitrap 80 and Sepitrap 4000, Journal of drug delivery and Therapeutics, 2018; 8(5-s): 293-300

  • Streubel A, Siepmann J, Bodmeier R. Floating matrix tablet based on low-density foam powder: effects of formulation and processing parameters on drug release. Eur J Pharm Sci. 2003;18: 37-45.

  • Yuasa H, Takashima Y, Kanaya Y. Studies on the development of intragastric floating and sustained release preparation. I. Application of calcium silicate as a floating carrier. Chem Pharm Bull (Tokyo). 1996;44: 1361-1366.

  • Streubel A, Siepmann J, Bodmeier R. Floating microparticles based on low-density foam powder. Int J Pharm. 2002; 241: 279-292.

  • Yuasa H, Asahi D, Takashima Y, Kanaya Y, Shinozawa K. Application of calcium silicate for medicinal preparation. I. Solid preparation adsorbing an oily medicine to calcium silicate. Chem Pharm Bull (Tokyo). 1994; 42: 2327-2331

  • Kinoshita M, Baba K, Nagayasu A, et al. Highly stabilized amorphous 3-bis (4-methoxyphenyl) methylene-2-indolinone (TAS-301) in melt-adsorbed products with silicate compounds. Drug Dev Ind Pharm. 2003; 29:523-529.

  • Manoj Goyal, Narendra Prajapati, Preparation and characterization of solid dispersion of Itraconazole, Journal of pharmaceutical and scientific Innovation, 2013; 2(5): 23-28

  • Namdeo R. Jadhav, Anant R. Paradkar, Gourav N. Shah. Adsorption Studies of Bromhexine Hydrochloride on Talc. Research J. Pharm. and Tech. 2013; 6(11): 1247-1250

  • Sameer Sharma, Praveen Sher, Shraddha Badve, and Atmaram P. Pawar, Adsorption of Meloxicam on Porous Calcium Silicate: Characterization and Tablet Formulation, AAPS PharmSciTech, 2005; 6 (4): 618-625

  • Naveen A, Katare O, Singh B, Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers. Eur. J. Pharm. Biopharm, 2007; 65: 26-38.

  • Ayshath Nureesha P, Ravikumar, Mufeeda Kathija, V.B Narayanaswamy. Formulation and Evaluation of Gastroretentive Matrix Tablet of Nifedipine. Research J. Pharm. and Tech. 2015; 8(5): 549-553.

  • Ramana M.V, Himaja M, Dua K, A new approach: enhancement of solubility of rofecoxib. Asian J. Pharm., 2008; 2: 96-101

  • Sarfaraz Md., Prasad Y., Reddy S.R, Doddayya H., Udupi R.H. Development and Evaluation of Press Coated Time-Release Tablet of Nifedipine. Asian J. Pharm. Res. 2011; 1(3): 58-63.

  • Streubel A, Siepmann J, Bodmeier R. Floating matrix tablet based on low-density foam powder: effects of formulation and processing parameters on drug release. Eur J Pharm Sci. 2003; 18: 37-45.

  • Naidu NB, Chowdary KP, Murthy KV, Satyanarayana V, Hayman AR, Becket G. Physicochemical characterization and dissolution properties of meloxicam-cyclodextrin binary systems. J Pharm Biomed Anal. 2004; 35:75-86.

  • Tran HT, Park JB, Hong KH, Choi HG, Han HK, et al. Preparation and characterization of pH-independent sustained release tablet containing solid dispersion granules of a poorly water-soluble drug. Int J Pharm, 2011;415: 83-88.

  • International conference on Harmonization (ICH) harmonized tripartite guideline for stability testing of new drugs substances and products Q1A (R2) Aug-2003. Q1 (R2) Mar2004.

  • C.T. Rhodes, T. Cartesan. Drug stability principle and procedure, 3rd ed, New York, 2001

  • Harpal Sinh Rathod. Preparation and Evaluation of Gelucire Based Matrix Pellets Loaded with Antihypertensive Drug for Controlled Release. Research J. Science and Tech, 2014; 6(3): 156-172.

  • Bhavin Patel, Piyush Patel, Ashok Bhosale, Evaluation of Tamarind Seed Polysaccharide (TSP) as a Mucoadhesive and sustained release component of nifedipine buccoadhesive tablet and Comparison with HPMC and Na CMC, International Journal of Pharm Tech Research,2009;1(3): 404-410


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  • Adsorption of Nifedipine on Porous Calcium silicate for Enhancement of Solubility and Dissolution Rate

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Authors

Rajesh S. Jagtap
Annasaheb Dange College of B Pharmacy, Ashta, Sangli - 416301 Maharashtra, India
Rajendra C. Doijad
Krishna Institute of Medical Sciences, Krishna Institute of Pharmacy, Karad, Satara 415110 Maharashtra, India
Shrinivas K. Mohite
Rajarambapu College of Pharmacy, Kasegaon, Sangli -415404 Maharashtra, India

Abstract


The enhancement in solubility and dissolution rate of poorly soluble drug Nifedipine was achieved by its adsorption on porous calcium silicate by using common volatile organic solvent chloroform. The yield of the adsorption process was found in a range of 90 -95% which indicates negligible loss during chloroform treatment. Saturation solubility studies showed 273% increase as compared to pure drug indicating adsorption of poorly soluble drug on porous calcium silicate was prominent in solubility enhancement. Physicochemical properties of pure Nifedipine compared to adsorbed product studied by FT-IR, DSC and PXRD. The FTIR and DSC studies does not show any unexpected interaction between Nifedipine and calcium silicate, while slight broadening in peak as well reduction in intensity and early onset as compared to the pure drug indicates adsorption of Nifedipine on porous calcium silicate. PXRD diffractograms showed a Significant reduction in peak intensities in drug adsorbed product compare to Nifedipine was attributed to the dilution effect of porous calcium silicate and confirms conversion of crystalline nature of drug in amorphous. Adsorption of the drug over FLR particles seen in SEM images of the adsorbed product while a significant change in surface morphology of Nifedipine was observed due to complete solubilization of Nifedipine and FLR in common solvent. The dissolution rate of the drug from adsorbed products was significantly rapid compared with pure drug, and the dissolution rate increases with increase in the proportion of FLR from 1:1.5 to 1:3, but further increase in the proportion of FLR not showed a significant increase in its dissolution indicating saturation. The drug adsorbed product was found stable as there was no any significant change in appearance and drug dissolution after three months stability studies.

Keywords


Nifedipine, Calcium Silicate, Adsorption, Solubility Enhancement.

References