• P-ISSN 0973-7200 E-ISSN 2454-8405
  • Follow us

Journal of Pharmaceutical Research

Article

Sublingual Tablets and the Benefits of the Sublingual Route of Administration
  • VIEWS 2527
  • PDF 1130

Journal of Pharmaceutical Research

DOI: 10.18579/jpcrkc/2017/16/3/118766

Year: 2017, Volume: 16, Issue: 3, Pages: 257-267

Original Article

Sublingual Tablets and the Benefits of the Sublingual Route of Administration

Arshad Bashir Khan *, Tarun Kingsley , Preeta Caroline
  • Krupanidhi College of Pharmacy, #12/1, Chikkabellandur, Carmelaram Post, Varthur Hobli , Bangalore - 560035, KA, India
Creative Commons License

This work is licensed under a Creative Commons Attribution 4.0 International License.

Abstract

Purpose: Sublingual drug delivery can be an alternative and better route when compared to oral drug delivery as sublingually administered dosage forms bypass hepatic metabolism. A rapid onset of pharmacological effect is often desired for some drugs, especially those used in the treatment of acute disorders. Sublingual tablets disintegrate rapidly and the small amount of saliva present is usually sufficient for achieving disintegration of the dosage form coupled with better dissolution and increased bioavailability.Approach: Published articles from PubMed and other standard sources were utilized to review and compile an overview of sublingual tablets and the benefits of the sublingual route of administration.Findings: Sublingual tablets were found to have better characteristics when compared to conventional dosage forms. Sublingually administered tablets achieved better bioavailability, rapid onset of action and better dissolution properties due to fast disintegration. The addition of super-disintegrants facilitated rapid disintegration and this approach can be used to treat acute disorders or emergency conditions.Conclusion: Sublingual tablets or any sublingual dosage form can be used to achieve a rapid onset of action, better patient compliance and increased bioavailability. The sublingual route of administration can be used for drugs which undergo extensive first pass metabolism or degradation in the GIT. Drugs administered sublingually tend to have better bioavailability which correlates to dose reduction when compared to conventional oral tablets.

References

  • Zhang H, Zhang J, Streisand JB. Oral mucosal drug delivery. Clin Pharmacokinet. 2002 Aug 1;41 (9):661-80.

  • Ashraf VA. Considerations in Developing Sublingual Tablets�An Overview. Pharm Tech. 2014 Nov 2;38(11) 34-72.

  • Squier CA, Wertz PW. Structure and function of the oral mucosa and implications for drug delivery. Drugs Phar Sci. 1996;74:1-26.

  • Edgar WM. Saliva: its secretion, composition and functions. Br Dent J. 1992 Apr;172(8):305-12.

  • Shojaei AH. Buccal mucosa as a route for systemic drug delivery: a review. J Pharm Pharm Sci. 1998 Jan 1;1(1):15-30.

  • Thompson IO, Van der Bijl P, Van Wyk CW, Van Eyk AD. A comparative lightmicroscopic, electron-microscopic and chemical study of human vaginal and buccal epithelium. Arc Oral Bio. 2001 Dec 31;46(12):1091-8.

  • Galey WR, Lonsdale HK, Nacht S. The in vitro permeability of skin and buccal mucosa to selected drugs and tritiated water. Jour Invest Derm. 1976 Dec 1;67(6):713-7.

  • Harris D, Robinson JR. Drug delivery via the mucous membranes of the oral cavity. Jour Phar Sci. 1992 Jan 1;81(1):1-0.

  • Home FD. Orange Book: approved drug products with therapeutic equivalence evaluations.

  • Wu SG, Lin SL, Shiao WY, Huang HW, Lin CF, Yang YH. Comparison of sublingual captopril, nifedipine and prazosin in hypertensive emergencies during hemodialysis. Nephron. 1993 Jul 1;65(2):284-7.

  • Fern�ndez ML, S�nchez MH, Mu�oz PP, Fern�ndez NG. Management of addictions in the elderly from primary health care. Quality of life, caregivers and intervention for health improvement in aging Volume III. 2015: 573.

  • John DN, Fort S, Lewis MJ, Luscombe DK. Pharmacokinetics and pharmacodynamics of verapamil following sublingual and oral administration to healthy volunteers. Br J Clin Pharmacol. 1992 Jun 1;33(6):623-7.

  • Fort S, Lewis MJ, Luscombe DK, John DN. Preliminary investigation of the efficacy of sublingual verapamil in the management of acute atrial fibrillation and flutter. Br J Clin Pharmacol. 1994 May 1;37(5):460-3.

  • Haegeli L, Rocca BL, Peter H, Wenk M, Pfisterer M, Drewe J, Kr�henb�hl S. Sublingual administration of furosemide: new application of an old drug. Br J Clin Pharmacol. 2007 Dec 1;64(6):804-9.

  • McIntyre J, Robertson S, Norris E, Appleton R, Whitehouse WP, Phillips B, Martland T, Berry K, Collier J, Smith S, Choonara I. Safety and efficacy of buccal midazolam versus rectal diazepam for emergency treatment of seizures in children: a randomised controlled trial. The Lancet. 2005 Jul 22;366(9481):205-10.

  • Fudala PJ, Bridge TP, Herbert S, Williford WO, Chiang CN, Jones K, Collins J, Raisch D, Casadonte P, Goldsmith RJ, Ling W. Office-based treatment of opiate addiction with a sublingual-tablet formulation of buprenorphine and naloxone. New Eng Jour Med. 2003 Sep 4;349(10):949-58.

  • Bayrak Z, Tas C, Tasdemir U, Erol H, Ozkan CK, Savaser A, Ozkan Y. Formulation of zolmitriptan sublingual tablets prepared by direct compression with different polymers: In vitro and in vivo evaluation. Euro Jour Pharm, Biopharm. 2011 Aug 31;78(3):499-505.

  • Supervia A, Pedro-Botet J, Nogues X, Echarte JL, Minguez S, Iglesias ML, Gelabert A. Piroxicam fast-dissolving dosage form vs diclofenac sodium in the treatment of acute renal colic: a double-blind controlled trial. Br J Clin Pharmacol. 1998 Jan 1;81:27-30.

  • Rawas-Qalaji MM, Simons FE, Simons KJ. Sublingual epinephrine tablets versus intramuscular injection of epinephrine: dose equivalence for potential treatment of anaphylaxis. JAllergy Clin Immunol Pract. 2006 Feb 28;117(2):398-403.

  • Gu X, Simon KJ, Simons F. Is epinephrine administration by sublingual tablet feasible for the firts-aid treatmentof anaphylaxis? A proof-of-concept study Biopharm Drug Disp. 2002 Jul 1;23(5):213-6.

  • Volterrani M, Rosano G, Coats A, Beale C, Collins P. Estrogen acutely increases peripheral blood flow in postmenopausal women. Am J Med Sci. 1995 Aug 1;99(2):119-22.

  • Price TM, Blauer KL, Hansen M, Stanczyk F, Lobo R, Bates GW. Single-dose pharmacokinetics of sublingual versus oral administration of micronized 17?estradiol. Int J Gynaecol Obstet. 1997 Mar 1;89(3):340-5.

  • Pedersen GK, Ebensen T, Gjeraker IH, Svindland S, Bredholt G, Guzman CA, Cox RJ. Evaluation of the sublingual route for administration of influenza H5N1 virosomes in combination with the bacterial second messenger c-di-GMP. PloS one. 2011 Nov 1;6(11):e26973.

  • Song JH, Nguyen HH, Cuburu N, Horimoto T, Ko SY, Park SH, Czerkinsky C, Kweon MN. Sublingual vaccination with influenza virus protects mice against lethal viral infection. Proc Natl Acad Sci U S A. 2008 Feb 5;105(5):1644-9.

  • Raghavan S, �stberg AK, Flach CF, Ekman A, Blomquist M, Czerkinsky C, Holmgren J. Sublingual immunization protects against Helicobacter pylori infection and induces T and B cell responses in the stomach. Am J Infect Control. 2010 Oct 1;78(10):4251-60.

  • Tayel SA, Soliman II, Louis D. Formulation of ketotifen fumarate fast-melt granulation sublingual tablet. AAPS PharmSciTech. 2010 Jun 1;11(2):679-85.

  • Beckett AH, Boyes RN, Triggs EJ. Kinetics of buccal absorption of amphetamines. J Pharm Sci Pharmacol. 1968 Feb 1;20(2):92-7.

  • Ho NF, Higuchi WI. Quantitative interpretation of in vivo buccal absorption of nalkanoic acids by the physical model approach. Int J Pharm Sci Invent. 1971 Apr 1;60(4):537-41.

  • Vora KR, Higuchi WI, Ho NF. Analysis of human buccal absorption of drugs by physical model approach. Int J Pharm Sci Invent. 1972 Nov 1;61(11):1785-91.

  • Schanker LS. Physiological transport of drugs. Adv Drug Res. 1964;1:71.

  • Sadoogh-Abasian F, Evered DF. Absorption of vitamin C from the human buccal cavity. Br J Nutr. 1979 Jul 1;42(01):15-20.

  • Rathbone MJ, Hadgraft J. Absorption of drugs from the human oral cavity. Int J Pharm Sci Res. 1991 Aug 2;74(1):9-24.

  • Evered DF, Sadoogh-Abasian F, Patel PD. Absorption of nicotinic acid and nicotinamide across human buccal mucosa invivo. Life sciences. 1980 Nov 3;27(18):1649-51.

  • Evered DF, Mallett C. Thiamine absorption across human buccal mucosa invivo. Life sciences. 1983 Mar 21;32(12):1355-8.

  • Roy SD, Flynn GL. Solubility behavior of narcotic analgesics in aqueous media: solubilities and dissociation constants of morphine, fentanyl, and sufentanil. Phar Res. 1989 Feb 1;6(2):147-51.

  • Bredenberg S, Duberg M, Lennern�s B, Lennern�s H, Pettersson A, Westerberg M, Nystr�m C. In vitro and in vivo evaluation of a new sublingual tablet system for rapid oromucosal absorption using fentanyl citrate as the active substance. Eur J Pharm Sci. 2003 Nov 30;20(3):327-34.

  • Riahi S, Beheshti A, Mohammadi A, Ganjali MR, Norouzi P. Partition coefficient prediction of a large set of various drugs and poisons by a genetic algorithm and artificial neural network. Jour Chi Chem Soc. 2008 Apr 1;55(2):345-55.

  • Li NY, Li Y, Gorrod JW. Determination of partition coefficients and ionisation constants of(S)(-)-nicotine and certain metabolites. Med Sci Res. 1992;20(23).

  • Lipinski CA, Lombardo F, Dominy BW, Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev. 1997 Jan 15;23(1-3):3-25.

  • Al-Ghananeem AM, Malkawi AH, Crooks PA. Effect of pH on sublingual absorption of oxycodone hydrochloride. AAPS PharmSciTech. 2006 Mar 1;7(1):E163-7.

  • Wehling F, Schuehle S, Madamala N, inventors; Cima Labs, Inc., assignee. Effervescent dosage form with microparticles. U S patent US 5,178,878. 1993 Jan 12.

  • Nibha KP, Pancholi SS. An overview on: Sublingual route for systemic drug delivery. Adv Drug Deliv Rev. 2012 Apr;2:913-23.

  • Reo JP, Fredrickson JK. Taste Masking Science and Technology Applied to Compacted Oral Solid Dosage Forms-Part 1. Amer Pharm Rev. 2002;5:8-15.

  • Kannuri R, Challa T, Chamarthi H. Taste masking and evaluation methods for orodispersible tablets. Int Jour PharmInd Res. 2011;1(3):201-10.

  • Morella AM, Pitman IH, Heinicke GW, inventors; FH Faulding & Co., Limited, assignee. Taste masked liquid suspensions. US patent US 6,197,348. 2001 Mar 6.

  • Jacobson IM, Gordon SC, Kowdley KV, Yoshida EM, Rodriguez-Torres M, Sulkowski MS, Shiffman ML, Lawitz E, Everson G, Bennett M, Schiff E. Sofosbuvir for hepatitis C genotype 2 or 3 in patients without treatment options. N Engl J Med. 2013 May 16;368(20):1867-77.

  • Bredenberg S, Duberg M, Lennern�s B, Lennern�s H, Pettersson A, Westerberg M, Nystr�m C. In vitro and in vivo evaluation of a new sublingual tablet system for rapid oromucosal absorption using fentanyl citrate as the active substance. Eur J Pharm Sci. 2003 Nov 30;20(3):327-34.

  • Bredenberg S, Nystr�m C. In-vitro evaluation of bioadhesion in particulate systems and possible improvement using interactive mixtures. J Pharm Sci Pharmacol. 2003 Feb 1;55(2):169-77.

  • Van Scoik KG, inventor; Abbott Laboratories, assignee. Solid pharmaceutical dosage in tablet triturate form and method of producing same. US patent US 5,082,667. 1992 Jan 21.

  • Dobetti L, inventor; Eurand International SPA, assignee. Fast disintegrating tablets. US patent US 6,596,311. 2003 Jul 22.

  • Okada M, Ikeda Y, Ono K, Kurazumi T, Kasai S, Imamori K, inventors; SSP Co., Ltd., assignee. Quickly soluble solid preparations. US patent US 6,455,053. 2002 Sep 24.

  • Dobetti L. Fast-melting tablets: Developments and technologies. Phar Tech. 2001 Sep;25(9; SUPP):44-50.

  • Doelker E. Pharmaceutical dosage forms: Tablets: HA Lieberman, L. Lachman and JB Schwartz (Eds.), in three volumes, 2nd edn., revised and expanded, Marcel Dekker, New York, NY, 1989�1990, 1990, 592�616�560 pp.,

  • Chaudry IA, King RE. Migration of potent drugs in wet granulations. J Pharm Sci. 1972 Jul 1;61(7):1121-5.

  • Goodhart FW, Gucluyildiz H, Daly RE, Chafetz L, Ninger FC. Stabilized compressed nitroglycerin tablets. J Pharm Sci. 1976 Oct 1;65(10):1466-71.

  • Makino T, Yamada M, Kikuta J. Fast dissolving tablet and its production, 1993. Euro Patent.;553777:A2.

  • Mahajan U, Parashar B, Sharma N, Jadhav Y, Musasvad S, Patil V. Fast dissolving tablet-An overview of formulation technology. Ind GloJour Phar Sci. 2012;2(2):157-66.

  • Fu Y, Yang S, Jeong SH, Kimura S, Park K. Orally fast disintegrating tablets: developments, technologies, taste-masking and clinical studies. Crit Rev Therap Drug Car Sys. 2004;21(6).

  • Bayrak Z, Tas C, Tasdemir U, Erol H, Ozkan CK, Savaser A, Ozkan Y. Formulation of zolmitriptan sublingual tablets prepared by direct compression with different polymers: In vitro and in vivo evaluation. Euro Jour PharBiophar. 2011 Aug 31;78(3):499-505.

  • Chang RK, Xiaodi G, Burnside BA, Couch RA. Fast-dissolving tablets. Pharm Tech. 2000;24(6):52-8.

  • Di Costanzo MF. T-Mask Technologies. In:,proceedings of the 7th International Glatt Symposium, USA 1997 (pp. 1-9).

  • Cousin G, Bruna E, Gendrot E, inventors; Laboratoires Prographarm, assignee. Rapidly disintegratable multiparticular tablet. US patent US 5,464,632. 1995 Nov 7.

  • Murakami T. Rapidly disintegrating tablets with saccharides. InProc Int Symp Cont Bioact Mater 1999 (Vol. 26, pp. 855-856).

  • Habib W, Khankari R, Hontz J. Fast-dissolve drug delivery systems. Crit Rev Therap Drug Car Sys. 2000;17(1).

  • Sharma S, Gupta G. Formulation and characterization of fast-dissolving tablet of promethazine theoclate. Asi J pharm. 2008 Jan 1;2(1):70.

  • Battu SK, Repka MA, Majumdar S, Rao Y M. Formulation and evaluation of rapidly disintegrating fenoverine tablets: effect of superdisintegrants. Drug Dev Ind Pharm. 2007 Jan 1;33(11):1225-32.

  • El-Arini SK, Clas SD. Evaluation of disintegration testing of different fast dissolving tablets using the texture analyzer. Pharm Dev Tech. 2002 Jan 1;7(3):361-71.

  • Dor PJ, Fix JA. In vitro determination of disintegration time of quick-dissolve tablets using a new method. Pharm Dev Tech. 2000 Jan 1;5(4):575-7.

  • Bi YX, Sunada H, Yonezawa Y, Danjo K. Evaluation of rapidly disintegrating tablets prepared by a direct compression method. Drug Dev Ind Pharm. 1999 Jan 1;25(5):571-81.

  • Narang N, Sharma J. Sublingual mucosa as a route for systemic drug delivery. Int J Pharm Pharm Sci. 2011;3(Suppl 2):18-22.

  • Park JH, Holman KM, Bish GA, Krieger DG, Ramlose DS, Herman CJ, Wu SH. An alternative to the USP disintegration test for orally disintegrating tablets. Pharm Tech. 2008 Aug 2;32(8).

  • Rawas-Qalaji MM, Estelle F, Simons R, Simons KJ. Fast-disintegrating sublingual tablets: effect of epinephrine load on tablet characteristics. AAPS Pharm Sci Tech. 2006 Jun 1;7(2):E72-8.

  • Deepak S, Dinesh K, Mankaran S, Gurmeet S, Singh RM. Taste masking technologies: a novel approach for the improvement of organoleptic property of pharmaceutical active substance. Int Res J Pharm. 2012;3(4):108-6.

  • Tahara Y, Toko K. Electronic tongues�a review. IEEE Sens J. 2013 Aug;13(8):300111.

  • Hashimoto Y, Matsunaga C, Tokuyama E, Tsuji E, Uchida T, Okada H. The quantitative prediction of bitterness-suppressing effect of sweeteners on the bitterness of famotidine by sweetness-responsive sensor. Chem Pharm Bull. 2007;55(5):739-46.

  • Shishu K, Kapoor VR. Development of taste masked oral formulation of ornidazole. Ind J Phar Sci. 2010 Mar;72(2):211.

  • Singh GJ, Poochikian G. Development and approval of inhaled respiratory drugs: a US regulatory science perspective. InCont PulDrug Del 2011 (pp. 489-527). Springer New York.

  • Bennett CL, Chen B, Hermanson T, Wyatt MD, Schulz RM, Georgantopoulos P, Kessler S, Raisch DW, Qureshi ZP, Lu ZK, Love BL. Regulatory and clinical considerations for biosimilar oncology drugs. Lancet Oncol. 2014 Dec 31;15(13):e594-605.

  • Jacob S, Shirwaikar A. Preparation and evaluation of microencapsulated fast melt tablets of ambroxol hydrochloride. Ind J Pharm Sci. 2009;71(3):276.

  • 01 June 2017

Year: 2017, Volume: 16, Issue: 3


More articles

DON'T MISS OUT!

Subscribe now for latest articles and news.