In-vitro and In-vivo Relationship of Gabapentin from Floating and Immediate Release Tablets

Main Article Content

E. E. Zien El-Deen
H. A. Yassin


Gabapentin is effective against post-traumatic spinal injury-induced neuropathic pain. It requires high dosage and frequency in the management of neuropathic pain. The present research work was an attempt to formulate and evaluate gabapentin gastro-retentive tablets to prolong gastric residence and increase drug absorption and further increase bioavailability. The floating tablets of gabapentin were prepared in two doses (300 and 600 mg) by using two polymers (hydroxyl propyl methyl cellulose and hydroxyl propyl cellulose). Immediate release tablets of gabapentin containing the same doses were prepared and used as reference formulations. The physicochemical characteristics of the prepared tablets were determined (drug content, weight variation, friability, hardness, thickness and diameter).  Drug release from the prepared tablets was followed and found that by increasing drug concentration in the tablets release rate increases. Floating tablets showed prolonged drug release (over 96%) to more than 15 hrs. Immediate release tablets showed over 97% drug release within 48 min. In-vivo results showed that plasma exposure to gabapentin in animals receiving the drug does not dose proportional and therefore may not reach therapeutically useful levels. AUC0-24 and Cmax in case of 300 mg tablets are more than those in case of 600 mg tablets. The in-vivo release of gabapentin does not correlate with the in-vitro release of the drug.

Gabapentin, floating tablets, sustained release tablets, pharmacokinetics.

Article Details

How to Cite
El-Deen, E. E., & Yassin, H. A. (2019). In-vitro and In-vivo Relationship of Gabapentin from Floating and Immediate Release Tablets. Journal of Advances in Medicine and Medical Research, 30(6), 1-12.
Original Research Article


Brahmankar DM, Jaiswal SB. A Textbook of biopharmaceutics and pharmaco-kinetics. A treatise edn. 1, New Delhi. In Medical Application of Controlled Release. 1984;2:1-34.

Vikramaditya Reddy M, Vijayavani Ch. S, Uma Maheshwara Rao V. Formulation and evaluation of gabapentin muco-adhesive gastron retentive tablets. Int. J. of Ph. and Analyt. Res. 2013;2(4):151-163.

Kaushik A, Dwivedi A, Praveen K, Abhinav G. Floating drug delivery system a significant tool for stomach specific release of cardiovascular drugs. Int. J. Drug Dev. and Res. 2012;4(4):116-129.

Bryans JS, Wustrow DJ. 3-Substituted GABA analogs with central nervous system activity. Med. Res. Rev. 1999;19: 149-177.

Backonja MA, Beydoun KR, Edwards SL, Shwartz V, Gabapentin symptomatic treatment of painful neuropathy in patients with diabetes mellitus. A randomized controlled trials. J. Am Med. Assoc. 1998;280:1831-1836.

Celik EC, Erthan B, Lakse E. The clinical characteristics of neuropathic pain in patients with spinal cord injury. Spinal Cord. 2012;50:585-589.

Siddall PJ, Taylor DA, Cousins MJ. Classification of pain following spinal cord injury. Spinal Cord. 1997;35:69-75.

Thuret S, Moon LD, Gage FM. Therapeutic interventions of the spinal cord injury. Nat. Rev. Neurosci. 2006;7:628.

Demirel GH, Yllmaz B, Kesiktas N. Pain following spinal cord injury. Spinal Cord. 1998;36:25-28.

To TP, Lim TC, Hill ST, Frauman AG, Cooper N, Kirsa SW, Brown DJ. Gabapentin for neuropathic pain following spinal cord injury. Spinal Cord. 2002;40: 282-285.

Rowbotham M, Harden N, Stacey B. Gabapentin for the treatment of postherpetic neuralgia: A randomized controlled trial. J. Am Med. Assoc. 1998;280(21):1837–182.

Meimandi MS, Mobasher M, Reza G, Nargles A. Gabapentin increases the analgesic effect of chronic use of morphine while decreases withdrawal signs. Int. J. Pharmacol. 2005;1:161-166.

Hagen EM, Rekand T. Management of neuropathic pain associated with spinal cord injury. Pain Therapy. 2015;4:51-65.

Mellegers MA, Furlan AD, Mailis A. Gabapentin for neuropathic pain: Systemic review of controlled and uncontrolled literature. Clin. J. Pain. 2001;17:284-295.

Fennerup NB, Johannsen L, Sindrup SH, Bach FW, Jensen TS. Pain and dysesthesia in patients with spinal cord injury: A postal survey. Spinal Cord. 2001;39:256-262.

Kukkar A, Bail A, Singh, Jaggi AS. Implications and Mechanism of action of gabapentin in neuropathic pain. Arch. Pharmacol. Res. 2013;36:237-251.

Stevenson CM, Kim J, Fleisher D. Colonic absorption of antiepileptic agents. Epilepsia. 1997;38:63-67.

Kriel RL, Birnbaum AK, Cloyd JC, Ricker BJ, Jones, Saete C, Caruso KJ. Failure of absorption of gabapentin after rectal administration. Epilepsia. 1997;38:1242-1244.

Leon Lachmann, Lieberman HA, Kanig JL. The theory and practice of industrial pharmacy. CBS Publishers and Distributer. 2009:297-301.

Shaikh A, Pawar YD, Kumbhar ST. Effect of chitosan and sodium alginate on mucoadhesion on drug release of itraconazole tablets. Int. J. of Res. in Pharm. Biomed. Sci. 2012;3(1):293-297.

Goswami Dhrnba Sanker. Formulation and evaluation of mucoadhesive tablets of famotidine. J. of Pharm. And Biomed. Sci. 2011;12(06).

Government of India Ministry of Health and Family Welfare. The pharmacopeia of India Delhi, India. Controller of Publication. 1997;1020-1022.

Inderbir GA, Karann M, Inderbir S, Sandeep A, Vikas R. Formulation and evaluation of controlled release matrix mucoadhesive tablets of domperidone using saliva plebeian gum. J. of Adv. Pharm. Tech. and Res. 2012;2(3):163- 169.

Stepensky D, Friedman M, Srour W, Raz I, Hoffman A. Preclinical evaluation of pharmacokinetic-pharmacodynamic rationale for oral CR metformin formulation. J. Control. Release. 2001;71: 107-115.

Klausner EA, Lavy E, Stepensky D, Friedman M, Hoffman A. Novel gastroretentive dosage form evaluation of gastroretentivity and its effect on riboflavin absorption in dogs. Pharmacol Res. 2002;19:1516-23.

Cao Qing-Ri, Choi Yun-Woong, Cui Jing-Hao, Lee Beom Jin. Formulation, release characteristics and bioavailability of novel monolithic hydroxy propyl methyl cellulose matrix tablets containing acetaminophen. J. Control. Rel. 2005;108(2-3):351-361.

Tiwari Sandip B, Rajabi-Siahboomi A. Modulation of drug release from hydrophilic matrices. Pharm. Tech. Europe. 2008;1:1-8.

Tiwari Sandip B, Rajabi-Siahboomi A. Extended release oral drug delivery technology, monolithic matrix system. Drug Deliv. Syst. 2008;437:217-243.

Yun-Seok Rhee, Seok Park, Tae-Won Lee, Chun-Woong Park, Tae-Young Nam Tack-Oon Oh. In Vitro/in Vivo relationship of gabapentin from a sustained-release tablet formulation: A pharmacokinetic study in the beagle dog. Arch. Pharm. Res. 2008;31(7):911-917.

Peng-Ju Ma, Guo-Jun Gao, Hai-Gang Chang, Fa-Zheng Shen Lei, Bao-Zhe Jin. Prolonged and floating drug delivery system of gabapentin for effective management of pain in spinal cord injury.Int. J. Pharm. 2016;10:435-439.

Fujioka K, Pans M, Joyal, S, Glycemic control in patients with type 2 diabetes mellitus switched from twice-daily immediate-release metformin to a once-daily extended release formulation. Clin. Ther. 2003;25:515-529.

Klausner EA, Eyal S, Lavy E, Friedman M, Hoffman. A novel levodopa gastroretentive dosage form: In-Vivo vvaluation in dogs. J. Contr. Rel. 2003a;88:117-26.

Klausner EA, Lavy E, Barta M, Cserepes E, Friedman M, Hoffman A. Novel gasrtroretentive dosage forms: Evaluation of gastroretentivity and its effect on Ievodopa absorption in humans. Pharmacol Res. 2003b;20:1466-73.

Noel M. Kinetic study of normal and sustained dosage forms of metformin in normal subjects. Res. Clin. Forums. 1979;1:35-50.

Karttunen P, Uusitupa M, Lamminsivu U. The pharmacokinetics of metformin: A comparison of the properties of a rapid-release and a sustained-release Preparation. Int. J. Clin. Pharmacol. Ther Toxicol. 1983;21:31-36.

Abdelkader H, Abdalla O, Salem H. Formulation of controlled-release baclofen matrix tablets: Influence of some hydrophilic polymers on the release rate and in vitro evaluation. AAPS. Pharm. Sci. Tech. 2007;8:156-166.