Open Access Open Access  Restricted Access Subscription Access
Open Access Open Access Open Access  Restricted Access Restricted Access Subscription Access

A Review on Emerging Oral Dosage Forms which Helps to bypass the Hepatic First Pass Metabolism


Affiliations
1 Department of Pharmaceutics, P. R. Pote Patil College of Pharmacy, Amravati – 444604, India
     

   Subscribe/Renew Journal


The initial pass metabolism or pre-circulatory system is a metabolic process in which the concentration of the drug is significantly reduced or shortened in the liver before it reaches the circulatory system. A fraction of the drug lost in the entire absorption process is often associated with the liver and skin wall. Oral delivery, the simplest form of drug management has its limitations, most of which are the low availability of drugs due to the first internal organ passing through metabolism. Drugs with low bioavailability need to be administered at a better dose as a small fraction of the controlled dose is injected into the bloodstream and reaches the target. Therefore, the worst dose of the drug is destroyed and the unauthorized drug ends up having unwanted side effects within the canal. Various forms of oral contraceptives are used. The current review focuses on the importance of passing the first hepatic pass, the biological findings, the reasons for the negative findings and the various methods used to skip the initial hepatic pass metabolism.

Keywords

Hepatic First Pass Metabolism, Bioavailability, Novel Drug Delivery System, Low Bioavailability, Gut Wall, Site Targeted
Subscription Login to verify subscription
User
Notifications
Font Size


  • Malviya V, Ladhake V, Gajbiye K, Satao J, Tawar M. Design and Characterization of Phase Transition System of Zolmitriptan Hydrochloride for Nasal Drug Delivery System. International Journal of Pharmaceutical Sciences and Nanotechnology. 2020 May 31; 13(3):4942-51.
  • Yoshida M, Hazekawa M, Haraguchi T, Uchida T. Influence of Swallowing Aids on The Adsorption and Palatability of Kremezin. Chem Pharm Bull (Tokyo), 2011; 59: 434-7.
  • Tsuji E, Uchida T, Fukui A, Fujii R, Sunada H. Evaluation of Bitterness Suppression of Macrolide Dry Syrups by Jellies. Chem Pharm Bull (Tokyo), 2006; 54: 310-4.
  • Carter SJ. Cooper and Gunn’s Dispensing for Pharmaceutical Students. 12thed. New Delhi: CBS Publishers and Distributors, 2008; 214-8.
  • Shargel L, Yuab. Applied Biopharmaceutics and Pharmacokinetics. 4th Ed. Stamford: Appleton and Lange, 2010.
  • Dubey M, Sheth Z, Design and Development of Oral Medicated Jelly of Palonosetron HCl. Paripex-Indian Journal of Research, 2015; 4(6): 253-255.
  • Jadhav SB, Bharkad VB, Shinde MK, Kadam VS and Katkam P. Development and Evaluation 0f Oral Medicated Jelly of Ondansetron Hydrochloride, World Journal of Pharmacy and Pharmaceutical Sciences, 2017; 6(9): 1537-1549.
  • Olmez SS, Vural I. Advantages and quality control of disintegrating tablets. FABAD Journal of Pharmaceutical Sciences 2009; 34 (1):167-172.
  • Kawano Y, Ito A, Sasatsu M, Machida Y. Preparation of orally disintegrating tablets with taste-masking function: masking effect in granules prepared with correctives using the dry granulation method and evaluation of tablets prepared using the taste-masked granules. Yakugaku Zasshi 2010; 130(1):81- 86.
  • Panigrahi R, Behera SP, Panda CS. A review on fast dissolving tablets. Webmed Central Pharmaceutical Sciences 2010; 1(11):1-16.
  • Douroumis DD, Gryczke A, Schminke S. Development and evaluation of cetirizine hcl tastemasked oral disintegrating tablets. American Association of Pharmaceutical Scientists PharmSciTech 2011; 12(1):141-151.
  • Shyamala B, Narmada GY, Rapid dissolving tablets: A novel dosage form. The Indian pharmacist 2002; 13(8):9-12.
  • Neeta, Dureja H, Bhagwan H, Dahiya S. Fast dissolving tablet: An overview. Novel Science International Journal of Pharmaceutical Science 2012; 1(5):228-232.
  • Konapure SA, Chaudhari PS, Oswal RJ, Kshirsagar SS, Antre RV, Chorage TV. Mouth dissolving tablets an innovative technology. International Journal of Applied Biology and Pharmaceutical Technology 2011; 2(1):496- 503.
  • Bangale SG, Shinde GV, Rathinaraj BS. New generation of orodispersible tablets: recent advances and future prospects. International Journal of Advances in Pharmaceutical Sciences 2011; 2(3):17-28.
  • Jesmeen T, Uddin R. Orodispersible tablets: A short review. Stamford Journal of Pharmaceutical Sciences 2011; 4(1):96-99.
  • Pilgaonkar P, Rustomjee M, Gandhi A, Badge PM. Orally disintegrating tablets. United States Patent. 2009.
  • Shukla D, Chakarborty S. Mouth dissolving tablets: An overview of formulation technology. Scientia Pharmaceutica 2009; 77 (2):309-326.
  • Kumare MM, Marathe RP, Kawade RM, Ghante MH, Shendarkar GR. Design of fast dissolving tablet of atenolol using novel coprocessed superdisintegrant. Asian Journal of Pharmaceutical and Clinical Research 2013; 6 (3):81-85.
  • Malviya V, Thakur Y, Gudadhe SS, Tawar M. Formulation and evaluation of natural gum based fast dissolving tablet of Meclizine hydrochloride by using 3 factorial design 2. Asian Journal of Pharmacy and Pharmacology. 2020; 6(2):94-100.
  • Malviya VR, Pande SD, Bobade NN. Preparation and Evaluation of Sustained Release Beads of Zolmitriptan Hydrochloride. Research Journal of Pharmacy and Technology. 2019; 12(12):5972-6.
  • Behnke K, Sogaard J, Martin S, Bauml J, Ravindran AV, Agren H, et al. Mirtazapine orally disintegrating tablet versus sertraline: a prospective onset of action study. Journal of Clinical Psychopharmacology 2003; 23(4): 358-364.
  • Malviya VR, Tawar MG. Preparation and Evaluation of Oral Dispersible Strips of Teneligliptin Hydrobromide for Treatment of Diabetes Mellitus. International Journal of Pharmaceutical Sciences and Nanotechnology. 2020 Jan 31; 13(1):4745-52.
  • Oral, quickly disintegrating film, which cannot spit out, for an antiemetic or ant migraine agent. Petra O, Thomas K, Kai-Thomas K, Karin K. US2008/0213343 A1 2008.
  • Exploration of film-forming properties of film formers used in the formulation of rapid dissolving films. Choudhary DR, Patel V, Patel H, Kundawala JA. Int J Chemtech Res 2011; 3(2):531–3.
  • Approaches for taste masking of bitter drugs: a Review. Priya YD, Chowdary YA, Murthy TEGK, Seshagiri B. J Adv Drug Res 2011; 1(2):58–67.
  • Orally fast dissolving innovation in formulation and technology. Bhyan B, Jangra S, Kaur M, Singh H. Int J Pharm Sci Rev Res 2011; 9(2):50–7.
  • Formulation flexibility broadens the scope for oral thin film technology. Sloboda M, Bharnatt S. Adhesive Res 2011; 22–4.
  • Dissolvable film. Reema P, Richard GZ. US 2007/0042023 A12007:1–8.
  • M.E. Aulton, Pharmaceutics the Science Of Dosage Form Design. 2nd edition p.no. 416
  • The Pharmaceutics & Compounding Laboratories at the UNC Eshelman School of Pharmacy. [Cited 2015 December 29]; [about 1p.].
  • Mohan H. Text book of Pathology – The oral cavity and salivary glands. 4th ed. NewDelhi: Jaypee Brothers Medical Publishers (P) Ltd; 2000: 494-496.
  • J F Firriolo. Oral cavity- A Review. OralSurg Med Oral Pathol. 1994; 78(2): 189-193.
  • SV Sastry, JR Nyshdham, JA. Reviw of formulation used in oral cavity. Pharm SciandTechnolToday. 2000; (3): 138-145.
  • Batheja P, Thakur R, Michniak B. Basic biopharmaceutics of buccal and sublingual absorption, enhancement in drug delivery. London, New York: Touitou E, Barry BW editors. CRC Press, Taylor and Francis Group.2006; 1: 189.
  • Greey P, Macdonald IB. Penicillin Agar Pastilles. Canadian Medical Association Journal. 1945; 52(4): 327-330.
  • Shukla D, Chakraborty S, Mishra B. Evaluation of in vivo behavior of controlled and pulsatile release pastilles using pharmacokinetic and γ-scintigraphic techniques. Expert Opin Drug Deliv. 2012; 9(11): 1333-1345
  • V.R. Malviya, S.D. Pande. Preparation and evaluation of zolmitriptan hydrochloride lozenges. Journal of Pharma Research 2019; 8:624–9.

Abstract Views: 147

PDF Views: 0




  • A Review on Emerging Oral Dosage Forms which Helps to bypass the Hepatic First Pass Metabolism

Abstract Views: 147  |  PDF Views: 0

Authors

Vishal Mahanur
Department of Pharmaceutics, P. R. Pote Patil College of Pharmacy, Amravati – 444604, India
Rahul Rajge
Department of Pharmaceutics, P. R. Pote Patil College of Pharmacy, Amravati – 444604, India
Mukund Tawar
Department of Pharmaceutics, P. R. Pote Patil College of Pharmacy, Amravati – 444604, India

Abstract


The initial pass metabolism or pre-circulatory system is a metabolic process in which the concentration of the drug is significantly reduced or shortened in the liver before it reaches the circulatory system. A fraction of the drug lost in the entire absorption process is often associated with the liver and skin wall. Oral delivery, the simplest form of drug management has its limitations, most of which are the low availability of drugs due to the first internal organ passing through metabolism. Drugs with low bioavailability need to be administered at a better dose as a small fraction of the controlled dose is injected into the bloodstream and reaches the target. Therefore, the worst dose of the drug is destroyed and the unauthorized drug ends up having unwanted side effects within the canal. Various forms of oral contraceptives are used. The current review focuses on the importance of passing the first hepatic pass, the biological findings, the reasons for the negative findings and the various methods used to skip the initial hepatic pass metabolism.

Keywords


Hepatic First Pass Metabolism, Bioavailability, Novel Drug Delivery System, Low Bioavailability, Gut Wall, Site Targeted

References