BILAYER TABLET OF TRAMADOL AND GABAPENTIN FOR COMBINATION PHARMACOTHERAPY OF NEUROPATHIC PAIN: DEVELOPMENT AND CHARACTERIZATION
DOI:
https://doi.org/10.22159/ijap.2018v10i3.25250Keywords:
Bilayer tablet, Tramadol, Neuropathic pain, Gabapentin, GBDDSAbstract
Objective: Experiments were performed to design, develop and characterize bilayer buoyant tablets having tramadol (TH), immediate release (IR) layer and gabapentin (GBP), sustained release (SR) layer.
Methods: Natural hydrophilic polysaccharide disintegrants were modified by sequential processes to obtain treated xanthan gum (TXG) and treated gellan gum (TGG), utilized for IR layer whereas carbopol and sodium carboxymethylcellulose, as sustaining polymers for SR layer and gas producing substance sodium bicarbonate which librates carbon dioxide for adequate buoyancy, was used in formulated bilayer tablet. A full two-level factorial experimental design was used for sustaining GBP release from buoyant SR layer.
Results: Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) studies conducted, explain overall drug and excipients compatibility. More than 90% of tramadol was released from IR layer within 30 min. Diffusion exponents (0.36-0.59) and T50% (2.4-4.4h) were determined for all SR tablet formulations. Optimised (S7) formulation exhibited 95.77% GBP released over 12h.
Conclusion: Developed tablet can provide excellent therapeutic result by the sequential immediate release of TH and sustained release of GBP for effective combination pharmacotherapy of neuropathic pain with once a day administration.
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References
Dworkin RH, Argoff CR, Haythornthwaite JA, Saltarelli M, Turk DC. Neurological review: Advances in neuropathic pain. Arch Neurol 2003;60:1524-34.
Kamble SR, Poul BN, Udapurkar PP. Peripheral neuropathy: diagnosis, management and pharmacotherapy. J Pharma Res 2016;5:25-9.
Lee CR, McTavish D, Sorkin EM. Tramadol: a preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in acute and chronic pain states. Drugs 1993;46:313-40.
Taylor CP. Mechanisms of action of gabapentin. Rev Neurol 1997;153:S39-45.
Rose MA, Kam PCA. Gabapentin: pharmacology and its use in pain management. Anaesthesia 2002;57:451-62.
Chaparro LE, Wiffen PJ, Moore RA, Gilron. Combination pharmacotherapy for the treatment of neuropathic pain in adults. Cochrane Database Systematic Rev 2012;7:1-57.
Hwang SJ, Park H, Park K. Gastric retentive drug delivery systems-critical reviews. Ther Drug Carrier Syst 1998;15:243-84.
Arora S, Ali J, Ahuja A, Khar RK, Baboota S. Floating drug delivery system a review. AAPS PharmSciTech 2005;6:372-90.
Narendra C, Srinath MS, Ganesh B. Optimization of bilayer floating tablet containing metoprolol tartrate as a model drug for gastric retention. AAPS PharmSciTech 2006;7:E1-7.
Puneeth KP, Kavitha K, Tamizh MT. Development and evaluation of rosiglitazone maleate floating tablets. Int J Appl Pharm 2010;2:6-10.
Sharma V, Pathak K. Modified xanthan gum as a hydrophilic disintegrating excipient for rapidly disintegrating tablets of roxithromycin. Ind J Pharm Edu Res 2013;47:79-87.
Heng PW, Chah LW. Drug substance and excipients characterization. In: Parikh DM. editor. Handbook of pharmaceutical granulation technology, New York: Decker; 1997. p. 52-5.
Indian Pharmacopoeia. Ministry of health and family welfare, Indian Pharmacopoeia Commission. Indian Pharmacopoeia, New Delhi: Controller of Publications; 2007;1:175-88.
Nayak S, Singh V, Bhaskar V. Development and validation of UV spectrophotometric method for tramadol hydrochloride. World J Pharm Pharm Sci 2015;4:773-81.
United States Pharmacopeia (USP)/National Formulary (NF): Physical tests: disintegration, 22/17 ed. Rockville MD. United States Pharmacopeial Convention Inc; 1990.
Reddy KR, Mutalik S, Reddy S. Once-daily sustained release matrix tablets of nicorandil: formulation and in vitro evaluation. AAPS PharmSciTech 2003;44:E61-6.
Gujral RS, Haque SM, Shanker P. A sensitive uv spectrophotometric method for the determination of gabapentin. Chem Sci Trans 2009;6:S163-70.
Merchant HA, Shoaib HM, Tazeen J, Yousuf R. Once-daily tablet formulation and in vitro release evaluation of cefpodoxime using hydroxypropyl methylcellulose: a technical note. AAPS PharmSciTech 2006;7:E1-6.
Kumar L, Reddy MS, Shirodkar RK, Pai GK, Krishna VT, Verma R. Preparation and characterization of fluconazole vaginal films for the treatment of vaginal candidiasis. Indian J Pharm Sci 2013;5:585-90.
Kamble SR, Poul BN, Udapurkar PP. Fabrication and evaluation of bilayer floating tablet containing conventional ibuprofen and modified release pregabalin for combination pharmacotherapy of neuropathic pain. Asian J Pharm 2016;10:S290-9.
Kumar GH, Jaganathan K, Kumar RS, Perumal P. Formulation and in vitro evaluation of bilayer floating tablets of metformin hydrochloride and sitagliptin phosphate. Int J Adv Pharm 2012;2:64-81.
Gahiwade HP, Patil MV, Tekade W, Thakare VM, Patil VR. Formulation and in vitro evaluation of trifluoperazine hydrochloride bilayer floating tablet. Int J Pharma Bio Sci 2012;2:166-72.
Sarfaraz Md, Reddy PKC, Udupi RH, Doddayya H. Formulation and in vitro evaluation of bilayer floating tablets of tramadol hydrochloride. Int J Drug Dev Res 2012;4:335-47.
Mukherjee K, Chakraborty S, Biswanath Sa. Quick/slow biphasic release of a poorly water-soluble antidiabetic drug from bi-layer tablets. Int J Pharm Pharm Sci 2015;11:250-8.
Saripilli R, Kudamala S, Murthy KVR. Development, formulation and evaluation of a bilayer gastric retentive floating tablets of ranitidine HCl and clarithromycin using natural polymers. Int J Pharm Pharm Sci 2017;9:164-77.
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