Novel co-processed excipients of mannitol and microcrystalline cellulose for preparing fast dissolving tablets of glipizide

S. Jacob, A. Shirwaikar, A. Joseph, K. Srinivasan

Research output: Contribution to journalArticle

50 Citations (Scopus)

Abstract

Co-processed particles of microcrystalline cellulose and mannitol were fabricated by spray drying technique to be used as a direct compression excipient in fast dissolving tablet formulation. Microcrystalline cellulose passed through sieve no.80, having a volumetric mean diameter (d50) of 28.35 μm, was used to form composite particles with powdered mannitol which was previously passed through sieve no. 80, in various mixing ratios. The composite particles were evaluated for their powder and compression properties. An increase in the microcrystalline cellulose proportion imparted greater compressibility to the composite particles, but the flowability of these mixtures was decreased. Although microcrystalline cellulose and mannitol have been extensively used in the formulation of fast dissolving tablets, the non-wetting property of the hard compact central core may delay the disintegration time. Optimized co-processed formulation containing mannitol and microcrystalline cellulose in the ratio of 1.25:1 was found to have optimized powder and compressibility characteristics with fast disintegrating property (< 15 s). Photomicrographs have shown that the mannitol crystals are fine and uniformly distributed in the microcrystalline matrix in spray dried form compared to physical mixture of the same combination. The fast disintegration may be due to the partial amorphization and formation of submicron particles of mannitol. These results indicated that improved fast dissolving tablets could be prepared by the co-processed mixture of microcrystalline cellulose and mannitol. Finally fast dissolving tablets of glipizide were prepared by blending with other excipients and compressed into tablets. Sensory study on disintegration time and mouth feel attributes ranked the present formulation based on grittiness, chalkiness and overall preference as the best.
Original languageEnglish
Pages (from-to)633-639
Number of pages7
JournalIndian Journal of Pharmaceutical Sciences
Volume69
Issue number5
Publication statusPublished - 2007

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Glipizide
Excipients
Mannitol
Tablets
Powders
microcrystalline cellulose
Mouth

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title = "Novel co-processed excipients of mannitol and microcrystalline cellulose for preparing fast dissolving tablets of glipizide",
abstract = "Co-processed particles of microcrystalline cellulose and mannitol were fabricated by spray drying technique to be used as a direct compression excipient in fast dissolving tablet formulation. Microcrystalline cellulose passed through sieve no.80, having a volumetric mean diameter (d50) of 28.35 μm, was used to form composite particles with powdered mannitol which was previously passed through sieve no. 80, in various mixing ratios. The composite particles were evaluated for their powder and compression properties. An increase in the microcrystalline cellulose proportion imparted greater compressibility to the composite particles, but the flowability of these mixtures was decreased. Although microcrystalline cellulose and mannitol have been extensively used in the formulation of fast dissolving tablets, the non-wetting property of the hard compact central core may delay the disintegration time. Optimized co-processed formulation containing mannitol and microcrystalline cellulose in the ratio of 1.25:1 was found to have optimized powder and compressibility characteristics with fast disintegrating property (< 15 s). Photomicrographs have shown that the mannitol crystals are fine and uniformly distributed in the microcrystalline matrix in spray dried form compared to physical mixture of the same combination. The fast disintegration may be due to the partial amorphization and formation of submicron particles of mannitol. These results indicated that improved fast dissolving tablets could be prepared by the co-processed mixture of microcrystalline cellulose and mannitol. Finally fast dissolving tablets of glipizide were prepared by blending with other excipients and compressed into tablets. Sensory study on disintegration time and mouth feel attributes ranked the present formulation based on grittiness, chalkiness and overall preference as the best.",
author = "S. Jacob and A. Shirwaikar and A. Joseph and K. Srinivasan",
note = "Cited By :43 Export Date: 10 November 2017 CODEN: IJSID Correspondence Address: Shirwaikar, A.; Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, MAHE, Manipal - 576 104, India; email: arunshirwaikar@yahoo.co.in Chemicals/CAS: glipizide, 29094-61-9; mannitol, 69-65-8, 87-78-5; microcrystalline cellulose, 39394-43-9, 51395-75-6 References: Hanawa, T., New oral dosage form for elderly patients: Preparation and characterization of silk fibroin gel (1995) Chem Pharm Bull, 47, pp. 284-288; York, P., Crystal engineering and particle design for the powder compaction process (1992) Drug Develop Ind Pharm, 18, pp. 677-722; Armstrong, N.A., Palfrey, L.P., The effect of machine speed on the consolidation of four directly compressible tablet diluents (1989) J Pharm Pharmacol, 41, pp. 149-151; Moreton, R.C., Tablet Excipients to the year 2001: A look into the crystal ball (1996) Drug Develop Ind Pharm, 22, pp. 11-23; Reimerdes, D., The near future of tablet Excipients (1993) Manuf Chem, 64, pp. 14-15; Dev, K.M., Coprocessed microcrystalline cellulose and calcium carbonate and its preparation (1988), US Patent No, 4744987; Bolnius, G.K., Chowhan, R.T., Materials for direct compaction in pharmaceutical powder compaction technology (1996) Powder compaction technology, pp. 419-429. , Alderborn G, Nystrom C, editors, Marcel Dekker Inc: New York;; Casohoursat, L., Lemogen, G., Larrowture, D., (1988) Drug Develop Ind Pharm, 14, pp. 2179-2182; Train, D., Some aspects of the property of angle of repose of powders (1958) J Pharm Pharmacol, 10, pp. 127-135; Carr, R.L., Evaluating flow properties of solids (1965) Chem Eng, 72, pp. 163-168; Hausner, H.H., Friction conditions in a mass of metal powder (1967) Int J Metall, 3, pp. 7-13; Terzaghi, T., Peck, S., (1948) Theoretical soil mechanics in engineering practice, pp. 112-115. , Wiley J: New York;; Koizumi, K., New method of preparing high porosity saliva soluble compressed tablets using mannitol with camphor (1997) Int J Pharm, 152, pp. 127-131; Marshall, K., (1987) The theory and practice of industrial pharmacy, pp. 234-236. , Lachman L, Liberman HA, Kanig JI, editors, 3rd ed. Verghese Publishing House: Mumbai;; Bi, Y.X., Sunada, H., Yonezawa, Y., Danjo, K., Evaluation of rapidly disintegrating tablets prepared by a direct compression method (1996) Chem Pharm Bull, 44, pp. 2121-2125; Tracqui, A., Kintz, P., Mangin, P., Systematic toxicological analysis using HPLC/DAD (1995) J Forensic Sci, 40, pp. 254-262; The United States Pharmacopoeia-24/National Formulary-19, 2000, Asian Edition; US Pharmacopeial Convention. Inc: Rockville, MD; 1945-1946; Ishikawa, T., Watanabe, Y., Utoguchi, N., Matsumoto, N., Preparation and evaluation of tablets rapidly disintegrating in saliva containing bitter taste masked granules by the compression method (1999) Chem Pharm Bull, 47, pp. 1451-1456; Maarschalk, K.S., Bolhius, G.K., Improving properties of material for direct compression (1999) Pharm Technol, 23, pp. 34-41; Kim, A.I., Akers, M.J., Nail, S.L., The physical state of mannitol after freeze-drying: Effects of mannitol concentration, freezing rate and a non crystallizing cosolute (1998) J Pharm Sci, 87, pp. 931-935; Yu, L., Milton, N., Groleau, E.G., Mishra, D.S., Vanisickle, R.E., Existence of mannitol hydrate during freeze-drying and practical implications (1999) J Pharm Sci, 88, pp. 196-199",
year = "2007",
language = "English",
volume = "69",
pages = "633--639",
journal = "Indian Journal of Pharmaceutical Sciences",
issn = "0250-474X",
publisher = "Medknow Publications and Media Pvt. Ltd",
number = "5",

}

Novel co-processed excipients of mannitol and microcrystalline cellulose for preparing fast dissolving tablets of glipizide. / Jacob, S.; Shirwaikar, A.; Joseph, A.; Srinivasan, K.

In: Indian Journal of Pharmaceutical Sciences, Vol. 69, No. 5, 2007, p. 633-639.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Novel co-processed excipients of mannitol and microcrystalline cellulose for preparing fast dissolving tablets of glipizide

AU - Jacob, S.

AU - Shirwaikar, A.

AU - Joseph, A.

AU - Srinivasan, K.

N1 - Cited By :43 Export Date: 10 November 2017 CODEN: IJSID Correspondence Address: Shirwaikar, A.; Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, MAHE, Manipal - 576 104, India; email: arunshirwaikar@yahoo.co.in Chemicals/CAS: glipizide, 29094-61-9; mannitol, 69-65-8, 87-78-5; microcrystalline cellulose, 39394-43-9, 51395-75-6 References: Hanawa, T., New oral dosage form for elderly patients: Preparation and characterization of silk fibroin gel (1995) Chem Pharm Bull, 47, pp. 284-288; York, P., Crystal engineering and particle design for the powder compaction process (1992) Drug Develop Ind Pharm, 18, pp. 677-722; Armstrong, N.A., Palfrey, L.P., The effect of machine speed on the consolidation of four directly compressible tablet diluents (1989) J Pharm Pharmacol, 41, pp. 149-151; Moreton, R.C., Tablet Excipients to the year 2001: A look into the crystal ball (1996) Drug Develop Ind Pharm, 22, pp. 11-23; Reimerdes, D., The near future of tablet Excipients (1993) Manuf Chem, 64, pp. 14-15; Dev, K.M., Coprocessed microcrystalline cellulose and calcium carbonate and its preparation (1988), US Patent No, 4744987; Bolnius, G.K., Chowhan, R.T., Materials for direct compaction in pharmaceutical powder compaction technology (1996) Powder compaction technology, pp. 419-429. , Alderborn G, Nystrom C, editors, Marcel Dekker Inc: New York;; Casohoursat, L., Lemogen, G., Larrowture, D., (1988) Drug Develop Ind Pharm, 14, pp. 2179-2182; Train, D., Some aspects of the property of angle of repose of powders (1958) J Pharm Pharmacol, 10, pp. 127-135; Carr, R.L., Evaluating flow properties of solids (1965) Chem Eng, 72, pp. 163-168; Hausner, H.H., Friction conditions in a mass of metal powder (1967) Int J Metall, 3, pp. 7-13; Terzaghi, T., Peck, S., (1948) Theoretical soil mechanics in engineering practice, pp. 112-115. , Wiley J: New York;; Koizumi, K., New method of preparing high porosity saliva soluble compressed tablets using mannitol with camphor (1997) Int J Pharm, 152, pp. 127-131; Marshall, K., (1987) The theory and practice of industrial pharmacy, pp. 234-236. , Lachman L, Liberman HA, Kanig JI, editors, 3rd ed. Verghese Publishing House: Mumbai;; Bi, Y.X., Sunada, H., Yonezawa, Y., Danjo, K., Evaluation of rapidly disintegrating tablets prepared by a direct compression method (1996) Chem Pharm Bull, 44, pp. 2121-2125; Tracqui, A., Kintz, P., Mangin, P., Systematic toxicological analysis using HPLC/DAD (1995) J Forensic Sci, 40, pp. 254-262; The United States Pharmacopoeia-24/National Formulary-19, 2000, Asian Edition; US Pharmacopeial Convention. Inc: Rockville, MD; 1945-1946; Ishikawa, T., Watanabe, Y., Utoguchi, N., Matsumoto, N., Preparation and evaluation of tablets rapidly disintegrating in saliva containing bitter taste masked granules by the compression method (1999) Chem Pharm Bull, 47, pp. 1451-1456; Maarschalk, K.S., Bolhius, G.K., Improving properties of material for direct compression (1999) Pharm Technol, 23, pp. 34-41; Kim, A.I., Akers, M.J., Nail, S.L., The physical state of mannitol after freeze-drying: Effects of mannitol concentration, freezing rate and a non crystallizing cosolute (1998) J Pharm Sci, 87, pp. 931-935; Yu, L., Milton, N., Groleau, E.G., Mishra, D.S., Vanisickle, R.E., Existence of mannitol hydrate during freeze-drying and practical implications (1999) J Pharm Sci, 88, pp. 196-199

PY - 2007

Y1 - 2007

N2 - Co-processed particles of microcrystalline cellulose and mannitol were fabricated by spray drying technique to be used as a direct compression excipient in fast dissolving tablet formulation. Microcrystalline cellulose passed through sieve no.80, having a volumetric mean diameter (d50) of 28.35 μm, was used to form composite particles with powdered mannitol which was previously passed through sieve no. 80, in various mixing ratios. The composite particles were evaluated for their powder and compression properties. An increase in the microcrystalline cellulose proportion imparted greater compressibility to the composite particles, but the flowability of these mixtures was decreased. Although microcrystalline cellulose and mannitol have been extensively used in the formulation of fast dissolving tablets, the non-wetting property of the hard compact central core may delay the disintegration time. Optimized co-processed formulation containing mannitol and microcrystalline cellulose in the ratio of 1.25:1 was found to have optimized powder and compressibility characteristics with fast disintegrating property (< 15 s). Photomicrographs have shown that the mannitol crystals are fine and uniformly distributed in the microcrystalline matrix in spray dried form compared to physical mixture of the same combination. The fast disintegration may be due to the partial amorphization and formation of submicron particles of mannitol. These results indicated that improved fast dissolving tablets could be prepared by the co-processed mixture of microcrystalline cellulose and mannitol. Finally fast dissolving tablets of glipizide were prepared by blending with other excipients and compressed into tablets. Sensory study on disintegration time and mouth feel attributes ranked the present formulation based on grittiness, chalkiness and overall preference as the best.

AB - Co-processed particles of microcrystalline cellulose and mannitol were fabricated by spray drying technique to be used as a direct compression excipient in fast dissolving tablet formulation. Microcrystalline cellulose passed through sieve no.80, having a volumetric mean diameter (d50) of 28.35 μm, was used to form composite particles with powdered mannitol which was previously passed through sieve no. 80, in various mixing ratios. The composite particles were evaluated for their powder and compression properties. An increase in the microcrystalline cellulose proportion imparted greater compressibility to the composite particles, but the flowability of these mixtures was decreased. Although microcrystalline cellulose and mannitol have been extensively used in the formulation of fast dissolving tablets, the non-wetting property of the hard compact central core may delay the disintegration time. Optimized co-processed formulation containing mannitol and microcrystalline cellulose in the ratio of 1.25:1 was found to have optimized powder and compressibility characteristics with fast disintegrating property (< 15 s). Photomicrographs have shown that the mannitol crystals are fine and uniformly distributed in the microcrystalline matrix in spray dried form compared to physical mixture of the same combination. The fast disintegration may be due to the partial amorphization and formation of submicron particles of mannitol. These results indicated that improved fast dissolving tablets could be prepared by the co-processed mixture of microcrystalline cellulose and mannitol. Finally fast dissolving tablets of glipizide were prepared by blending with other excipients and compressed into tablets. Sensory study on disintegration time and mouth feel attributes ranked the present formulation based on grittiness, chalkiness and overall preference as the best.

M3 - Article

VL - 69

SP - 633

EP - 639

JO - Indian Journal of Pharmaceutical Sciences

JF - Indian Journal of Pharmaceutical Sciences

SN - 0250-474X

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