BILAYER TABLET OF TRAMADOL AND GABAPENTIN FOR COMBINATION PHARMACOTHERAPY OF NEUROPATHIC PAIN: DEVELOPMENT AND CHARACTERIZATION


Santosh Kamble, Bhagwat Poul, Prachi Udapurkar

Abstract


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 where as carbopol and sodium carboxymethyl cellulose, 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 sequential immediate release of TH and sustained release of GBP for effective combination pharmacotherapy of neuropathic pain with once a day administration.

 


Keywords


Bilayer tablet, Tramadol, Neuropathic pain, Gabapentin, GBDDS

References


Dworkin RH, Argoff CR, Haythornthwaite JA, Saltarelli M, Turk DC. Neurological Review: Advances in Neuropathic Pain. Arch Neurol 2003; 60:1524-1534.

Kamble SR, Poul BN, Udapurkar PP. Peripheral Neuropathy: Diagnosis, Management and Pharmacotherapy. J Pharma Res 2016;5:25-29.

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; 46:313-340.

Taylor CP, Mechanisms of action of gabapentin. Rev Neurol 1997; 153:S39-S45.

Rose MA, Kam PCA, Gabapentin: pharmacology and its use in pain management. Anaesthesia 2002; 57:451-462.

Chaparro LE, Wiffen PJ, Moore RA, Gilron. Combination pharmacotherapy for the treatment of neuropathic pain in adults. Cochrane Database of Systematic Reviews 2012; 7(Art: CD008943):01-57.

Hwang SJ, Park H, Park K. Gastric Retentive Drug Delivery Systems - Critical Reviews. Therapeutic Drug Carrier Systems 1998;15:243-284.

Arora S, Ali J, Ahuja A, Khar RK, Baboota S. Floating Drug Delivery System a Review. AAPSPharmSciTech 2005; 6:372-390.

Narendra C, Srinath MS, Ganesh B. Optimization of bilayer floating tablet containing metoprolol tartrate as a model drug for gastric retention. AAPSPharmSciTech 2006; 7:E1-E7.

Puneeth KP, Kavitha K, Tamizh MT. Development and evaluation of rosiglitazone maleate floating tablets. Int J Appl Pharm 2010; 2:06-10.

Sharma V, Pathak K. Modified Xanthan Gum as 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 1997:52-55.

Indian Pharmacopoeia. Ministry of Health and Family Welfare, Indian Pharmacopoeia Commission. Indian Pharmacopoeia, New Delhi: Controller of Publications 2007; 1:175-188.

Nayak S, Singh V, Bhaskar V. Development and validation of UV spectrophotometric method for tramadol hydrochloride. World J Pharm & Pharm Sci 2015; 4:773-781.

United States Pharmacopeia (USP)/ National Formulary (NF): Physical Tests: Disintegration (701), 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. AAPSPharmSciTech 2003; 44:E61-E66.

Gujral RS, Haque SM, Shanker P. A sensitive uv spectrophotometric method for the determination of gabapentin. Chem Sci Trans 2009; 6:S163-S170.

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. AAPSPharmSciTech 2006; 7:E1–E6.

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 Pharmaceutics 2016; 10:S290-S299.

Kamble S, Poul B. Development and characterization of bilayer tablet containing tramadol and pregabalin as a gastric buoyant drug delivery system for combination pharmacotherapy of neuropathic pain. Int J Pharm Sci & Res 2018; 9:1000-1011

Sravanthi, Abbulu K, Saxena A. Formulation and evaluation of bilayer floating tablets of amlodipine besylate and metoprolol succinate. Innovations in Pharmaceuticals and Pharmacotherapy 2014; 2:328-339.

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 Sciences 2012; 2:166-172.

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; 4:335-347.




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