You are hereFormulation and in Vitro Evaluation of Sustained Release Matrix Tablets of Lornoxicam

Formulation and in Vitro Evaluation of Sustained Release Matrix Tablets of Lornoxicam


About Author: G. Anand Rao*, V. Venu, R. Senthil Selvi, P. Perumal,
Department of Pharmaceutics,
J. K. K. Nattraja College of Pharmacy,
Komarapalayam - 638 183, Namakkal (D.T),
Tamil Nadu, India

Abstract
The main objective of the present work was to develop sustained release matrix tablets of Lornoxicam using Hydrophilic polymers viz. Hydroxy propyl methyl cellulose (HPMC K4M, HPMC K10M, HPMC K15M) was developed using wet granulation technique at varying ratios of drug and polymer like 1:1, 1:2 and 1:3 were selected for the study. Micro crystalline cellulose and Lactose was added in this formulation as a function of binder and diluent. Prior to compression, the prepared granules were evaluated for flow and compression characteristics. After evaluation of physical properties of tablet, the in vitro release study was performed in 0.1 N Hcl, pH 1.2 for 2 hrs and in phosphate buffer pH 6.8 up to 12 hrs. The effect of polymer concentration and polymer blend concentration were studied. Dissolution data was analyzed by Korsmeyer- Peppas law expression. It was observed that matrix tablets contained polymer HPMC K10M was successfully sustained the release of drug up to 12 hrs. Among all the formulations, formulation F9 which contains 1:3 ratios of drug and polymer release the drug which follows Zero order kinetics via, swelling, diffusion and erosion. Stability studies (40±2oc/75±5%RH) for three months indicated that Lornoxicam was stable in the matrix tablets. The FTIR study revealed that there was no chemical interaction between drug and excipients.

Reference ID: PHARMATUTOR-ART-1123

Introduction
Lornoxicam is a non-steroidal anti-inflammatory drug (NSAID) with potent analgesic and anti-inflammatory activity and belongs to the class of oxicams. In common with other NSAIDs, the analgesic and anti-inflammatory activity of Lornoxicam is related to its inhibitory action on prostaglandin synthesis, via inhibition of cyclo-oxygenase (COX) activity. Lornoxicam inhibits both isoforms in the same concentration range, that is, the ratio of COX-1inhibition to COX-2inhibition. It readily penetrates into the synovial fluid.Unlike some NSAIDs, however, Lornoxicam does not inhibit 5-lipoxygenase activity and thus does not inhibit leukotriene synthesis or shunt arachidonic acid to the 5-lipoxygenase pathway. Activation of the opioid neuropeptides system may be a component of the analgesic effect of Lornoxicam.

Lornoxicam is a non-steroidal anti-inflammatory drug of the oxicam class, with analgesic, anti-inflammatory and antipyretic properties. It is used for inflammatory disease of the joints, osteoarthritis, pain surgery as well as pain in the lower back and hip which travels down the back of the thigh into the leg. The mean elimination half life is 4 hrs and requires dosing every 4 hours in order to maintain optimal relief of chronic pain. Consequently, once daily sustained release tablets have been formulated. Long term treatment with sustained release lornoxicam once daily is generally safe in patients with osteoarthritis or rheumatoid arthritis and is well tolerated. Non steroidal anti-inflammatory drugs (NSAIDs) are widely used for patients suffering from LBP. A quick release formulation of lornoxicam (LNX), a potent NSAID from the chemical class of oxicams, provides a faster onset of pain relief (PAR) compared to the standard tablet formulation. The aim of the study was to assess analgesic efficacy and safety of lornoxicam quick release formulation versus diclofenac potassium (DP) in acute LBP. LNX administered as quick release formulation was proven to be as effective as the equivalent DP formulation in terms of onset of PAR and more effective on most of the major standard efficacy outcomes.

Lornoxicam is a potent balanced COX-1/ COX-2 inhibitors whose short half life of 3- 4 hours may beneficially influence safety and tolerability. Lornoxicam was associated with a significantly lower risk of adverse events compared with comparator analgesics and carried no increase risk of adverse events verses placebo. Pain control after dental surgery lornoxicam 8, 16 and 20 mg was superior to placebo and at least as effective as morphine 20 mg in controlling moderate to severe pain. Painrelief: Adult: 8-16 mg daily. Max: 24 mg daily. Osteoarthritisand rheumatoid arthritis: Adult: 12 mg daily in 2-3 divided doses. Lornoxicam is absorbed rapidly and almost completely from the GIT following oral administration, no first pass was observed. Oral bioavailability is 90%, Plasma binding 99% and Peak plasma concentration 270µg/L.

These biopharmaceutical and physicochemical properties reveal that Lornoxicam is an ideal candidate to develop into a sustained release matrix tablet. To maintain oral bioavailability for longer period of time with the relative lack of peak plasma concentration Lornoxicam is formulated as sustained release matrix tablet.

The most common controlled delivery system have been the matrix type such as the tablets and granules where the drug is uniformly dissolved or dispersed thoroughly out the polymer, because of its effectiveness, low cost, ease of manufacturing and prolongation delivery time period. Hydrophilic polymers are becoming more popular in formulating oral controlled release tablets, it is well documented that the dissolution curve of drug release from a hydrophilic matrix shows a typical time dependent profile. The release of a dissolved drug inherently follows near first order diffusion either an initially high release rate, due to the dissolution of the drug present at the surface of the matrix followed by a rapid declining drug release rate.

The enhanced release rate observed at the beginning for the short time of release process is known as ‘burst effect’ and is many a time undesirable since it may, have negative therapeutic consequences. After this burst, hydration and consequent swelling and /or erosion of related polymer occur. These phenomenon control the release process but with time, the diffusion path length increase and saturation effect is attained, resulting in a progressively slow release rate during the end of dissolution span.

The main objective of the present work was to develop sustained release matrix tablet of lornoxicam using different polymers viz. Hydroxy propyl methyl cellulose (HPMC K4M, HPMC K10M, HPMC K15M) was developed using wet granulation techniqueat varying ratios of drug and polymer like 1:1, 1:2 and 1:3 were selected for the study. Micro crystalline cellulose and Lactose was added in this formulation as a function of binder and diluent. Before go for formulation find evaluation characterization of granules then go for compression. The matrix tablets were prepared and evaluated for different physiochemical parameters such as appearance, weight variation, thickness, hardness, friability, drug content and in vitro release.

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