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The aim of the present study was to develop Sublingual tablets containing Tamsulosin hydrochloride, using various hydrophilic and hydrophobic polymers such as HPMC, Pectin, Polyvinylpyrrolidone (pvp), Î²-Cyclodextrin, Ethyl cellulose (EC), to know whether which release pattern it follows whether it may give onset of action or prolonged action. In this work Tamsulosin Hydrochloride was selected as an ideal drug candidature to treat Benign Prostatic Hyperplasia & Urinary tract infection manly by blockage of Î±- 1Asub type adrenoceptor causes relaxation of smooth muscles in the bladder neck and prostate, and thus decreases urinary outflow resistance in men.
FORMULATION OF SUBLINGUAL TABLETS:
In the present study, an attempt was made to prepare different formulations of oromucosal drug delivery system, using various hydrophilic and hydrophobic polymers. There are two methods has been adapted for preparation of sublingual tablets. In the first method, the core tablet was prepared by direct compression of Tamsulosin hydrochloride with ethylcellulose (F1 EC, F2 EC, F3 EC, F4 EC, and F5 EC) and similarly with HPMC, Pectin, Polyvinylpyrrolidone (pvp), Î²-Cyclodextrin( F1HP, F2 HP, F3 HP, F4 HP, F5 HP, F1 P, F2 P, F3 P, F4 P, F5 P & F1 PVP, F2 PVP, F3 PVP, F4 PVP, F5 PVP & F1 CD, F2 CD, F3 CD, F4 CD, F5 CD) and without using polymers directly with mannitol C1, C2. In second method, bilayered tablets were prepared using tamsulosin hydrochloride, mannitol as core tablet and EC compressed over it as a backing layer (B1, B2). The prepared various tablets were subjected to physicochemical evaluation, incompatability studies, in vitro drug release and finally t-test was performed to the obtained results.
The compatability studies of the drug and the polymer and various formulations were estimated by using FT-IR (Jasco- T-IR 8201 PC). The IR spectrum of the pure drug (Tamsulosin Hydrochloride) showed a intense peaks at 3305.39cm-1, 1159.01cm-1, 2983.34cm-1, 748.245cm-1, 1251.58cm-1 and these were compared with the standard IR spectrum (IP). Similarly the same peaks were observed in all formulations. From the spectra, shown in the fig. , finally there was no significant incompatibility between the pure drug, polymer and in all 34 formulations, indicating the stability of the drug in these formulations.
EVALUATION OF PHYSICOCHEMICAL PARAMETERS:
The thickness of all the tablets falls in the range of 2.300±0.108 to 2.369±0.107 for EC containing formulations, 2.359±0.041 to 2.4347±0.037 for pectin containing formulations, 2.3421±0.00 to 2.3814±0.00145 for Î²- cyclodextrin containing formulation, 2.210±0.003 to 2.2475±0.0029 for pvp containing formulations, 2.3522±0.003 to 2.4161±0.0039 for hpmc containing formulations. For the formulations B1 and B2 thickness was found to be 2.364±0.019, 2.4162±0.001, and for C1 and C2 it was found to be 2.365±0.015, 2.349±0.021.
B. Weight Variation Test
In weight variation test, the Pharmacopoeial limit (United States Pharmacopoeia, 2000) for percentage deviation less than or equal to 150 mg is ±7.5%. The average percentage deviation of all tablet formulations was found to be within the limits, and hence all formulations passed the uniformity of weight as per official requirements of the United States Pharmacopoeia, 2000.
C. Hardness Test
Formulated Tamsulosin Hydrochloride Sublingual tablets were tested for hardness using Pfizer hardness tester. The hardness increased as the concentration of the binder increased. All Formulations showed a maximum hardness of 1 kg/cm2, whose hardness was nearly similar to that of the reference marketed isosorbide Dinitrate sublingual tablet (isordil-5) (1.5 kg/cm2).
D. Friability Test (Banker and Ander, 1987)
Tablet hardness is not a complete indication of strength. An additional measure of a tablet's strength is friability. Conventional compressed tablets that lose less than 1% of their weight are generally considered acceptable. In the present study, the percentage friability for all the formulations were below 1%, indicating that the friability was within the prescribed limits. The results were 0.9472 to 1.47 for EC, 0.476 to 0.924 for Pectin, 0.7304 to 0.874 for Î²- cyclodextrin, 0.74 to 0.9 for PVP, 0.469 to 0.997 for HPMC containing formulations and for B1 & B2 obtained were 0.261 , 0.177, C1 &C2 0.784, 0.867.
E. Disintegration Test
Disintegration test was carried out for formulated tablets using disintegration test apparatus as prescribed in USP, 2000. All formulations disintegration test were shown to be between 92-177 seconds.
F. DRUG CONTENT UNIFORMITY
Tamsulosin Hydrochloride Sublingual tablets are tested for drug content as prescribed in IP, 2007. Good uniformity in content was found among different formulations and the percentage of drug content was more than 100% and all the batches were in the limit according to the limits mention in the I.P. The Percentages of drug content uniformity present in all the formulations were found to be in between 91.87-108%
G. DRUG CONTENT ASSAY
Tamsulosin Hydrochloride Sublingual tablets are tested for drug content assay as prescribed in IP, 2007. Drug content assay was found among different formulations and all the batches were in the limit according to the limits mention in the I.P. The Percentages of drug content present in all the formulations were found to be 95.43-104%.
H. IN-VITRO DISSOLUTION STUDIES
Figuresshows the dissolution profile of the prepared Tamsulosin Hydrochloride sublingual tablet formulations. In-vitro release profile of the drug from the tablets was major governing criteria using binder and diluents as mannitol. The release profile for the drug was taken to be best for a period of 10min without polymer and whereas 15min was observed with polymer HPMC, Pectin, PVP, Î²-cyclodextrin at ratio of (1:0.25) and which can best be depicted by graph between percentage drug release and time.