Formulation and Evaluation of the Sustained Release Tablet of Ketorolac Tromethamine Using Natural Polymer as an Extended Releasing Agent

Author(s):  
Gadhave M. V. ◽  
Deokar Rutuja V. ◽  
Jadhav S. L. ◽  
Gaikwad D. D.

Sustained release tablets of Ketorolac Tromethamine were formulated using Aloe vera Gel Powder as extended drug releasing agent. The tablets were evaluated for preformulation studies like angle of repose, bulk density, compressibility index and physical characteristics like hardness, weight variation, friability and drug content. In-vitro release of drug was carried out in phosphate buffer solution pH 6.8 for twelve hours. All the physical characters of the formulated tablet were found within the acceptable limit. The tablet with Aloe Vera gel powder in Batch-F3 exhibited greater drug release than other batches. It is proved from the dissolution profile of Ketorolac Tromethamine, that Aloe Vera gel powder possess the drug release retarding ability.

Author(s):  
HARSHAD PADEKAR ◽  
OMKAR LOHOTE

Objective: The objective of the present investigation is to design formulate and characterized the bilayer tablet containing Diclofenac sodium and Aloe Vera gel powder. In which diclofenac sodium is sustained release and Aloe Vera gel powder is immediate release. In order to produce a single dosage form containing two different classes, drug are widely prescribed by the physician to have better patient compliance. Methods: Bilayer tablet was prepared by direct compression, The immediate release layer of Aloe Vera gel powder was prepared by using different excipients such as starch, sodium starch glycolate, lactose, talc etc. sustained release layer of diclofenac sodium was prepared by using HPMC K4M, lactose, Talc Magnesium stearate, talc etc. for preparation of bilayer tablet sodium starch glycolate are use as super disintegrants in immediate release tablet and HPMC K4M are use as controlled release polymer. Various Preformulation parameter i.e. Identification, melting point, compatibility study, solubility are checked. Micromeritics properties of powder blend such as bulk density, tapped density, hausner’s ratio, Carr’s index, angle of repose are performed. Post-compression parameter was done such as hardness, friability, weight variation, drug content uniformity, thickness, in vitro drug release. Results: Result was found within the limit of the standard of optimized formulation. The drug release of the tablet was in the range of 82 to 92%in 8 h. Conclusion: Bilayer tablet was prepared by optimized batches of both layers. The prepared tablets showed satisfactory results for various evaluation parameters. The optimized formulation based on all the parameter A1 (Sodium starch glycolate) is selected for the immediate release layer and D3 (HPMC K4M) was selected for the controlled release layer. The drug release mechanism was found to be zero order release depends upon diffusion.


Author(s):  
C Suja ◽  
Sismy C

The goal of this study was to formulate and evaluate norfloxacin sustained release tablets. Norfloxacin sustained release tablets were prepared by wet granulation method using two polymers such as HPMC K 100 M (hydrophilic polymer) and guar gum (natural polymer) and with three polymer ratios (0.5, 1.0 and 1.5). The prepared granules were evaluated to preformulation studies such as angle of repose, bulk density, tapped density, bulkiness, compressibility index and Hauser’s ratio. All the parameters shows that the granules having good flow properties. Then the formulated tablets were taken to evaluation studies such as hardness, weight variation, friability, drug content and thickness. All the parameters were within the acceptable limits. IR spectral analysis showed that there was no interaction between the drug and polymers. The in vitro release study was performed in phosphate buffer pH 7.4 at 293 nm. The in vitro release study showed that if the polymer ratio is increased, then the release of the drug is prolonged. HPMC K 100M shows a prolonged release when compared to guar gum.


Author(s):  
Mayuri B. Patil ◽  
Avish D. Maru ◽  
Jayshree S. Bhadane

The aim of the present study was to design and evaluate bilayer tablets of metformin hydrochloride as sustained release form for the treatment of Type-II diabetes mellitus. The basic aim of any Bi-layer tablet formulation is to separate physically or chemically incompatible ingredients and to produce repeat action or prolonged action of tablet. They are many drugs for treating type-II diabetes. Sulphonyl urea and biguanides are used commonly by a wide section of patients. Melt granulation process was used for the formulation of sustained comprising metformin layer and wet granulation of immediate comprising layer of glimepiride. The precompression studies like bulk density, tapped density, angle of repose, compressible index and post formulation studies includes weight variation, hardness, thickness, friability and dissolution study. The in-vitro release profile of Glimepiride was dissolved within 45 min, and Metformin Hydrochloride was able to release more than 12 hrs. They all the formulation was optimized formula due to its higher rate of dissolution and collate all other parameters with the official specifications.


Author(s):  
OMAR SAEB SALIH ◽  
ZAHRAA M. HAMODDI ◽  
SALAM S. TAHER

Objective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs like candesartan cilexetil. Candesartan cilexetil is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β-cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β-cyclodextrin. Fourier transform infrared spectroscopy and differential scanning calorimetry were used to study compatibility. Results:The angle of repose determination showed good flow for most of the formulas besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement showed accepted values. Friability and hardness of tablets were within the allowed values. Higher tablet swelling was obtained for the formulas containing hydroxy propyl methyl cellulose (HPMC) K100M (F3x and F15z) in which the ratio of the polymer was (1:1) and (1:3) respectively. In vitro release showed that F1x to F13z were studied depends on the type and amount of polymer i.e. (1:1), (1:2) and (1:3) respectively. F1x release after 8h was 95% which contain (1:1) polymer ratio in compare to F3x, which showed 85% after 8h, Which include 1:3 (drug: HPMC K100). Kinetic studies showed a zero-order model. Conclusion: The use of β-cyclodextrin modify the release profile of the drug, and control the sustained release formulas. The lower the time of the release but in a range that a sustained release of the drug was observed in compare with the formulas prepared without β-cyclodextrin.


The aim of the present study is to design and develop sustained release pellets formulations for Amlodipine besylate. Amlodipine is an oral antihypertensive agent, commonly used as calcium channel blocker for treating high blood pressure. It is frequently used to treat heart diseases like angina pectoris. The dose of Amlodipine in case of hypertension or angina initially 5 mg daily later adjusted to 10 mg daily by oral route. Amlodipine has a maximum solubility in acidic pH. Amlodipine has a high bioavailability ranging from 60 to 80 % and slow rate of elimination. Amlodipine besylate at different drug to polymer ratios were prepared by extrusion and spheronization technique. The influence of the proportion of the polymer on the release rate of the drug from the pellets was studied. The in-vitro release studies of pellets were carried out in 0.1N HCl for 12 hours. The studies indicated that the drug release can be modulated by varying the concentration of the polymer. Pellets were prepared and evaluated for loose bulk density, tapped bulk density, compressibility index and angle of repose, shows satisfactory results. Formulation was optimized on the basis of acceptable pellet properties and in-vitro drug release. The resulting formulation produced robust pellets with acceptable drug content and low friability. The release data was fitted to various mathematical models such as, Higuchi, Korsmeyer- Peppas, First-order and Zero-order to evaluate the kinetics and mechanism of the drug release. Keywords: Sustained release, Ethyl cellulose, HPMC, Pellets, Amlodipine besylate


2013 ◽  
Vol 2 (10) ◽  
pp. 165-169 ◽  
Author(s):  
Manivannan Rangasamy ◽  
Venkata Krishna Reddy Palnati ◽  
Lakshmi Narayana Rao Bandaru

The present study involves in the formulation and evaluation of sustained release tablets of Voriconazole (250mg). The objective of the present study was to formulate Voriconazole sustained release tablets by wet granulation method by using natural (Xanthan gum, Karaya gum) and semi synthetic polymers (HPMC K100M). Lactose was used as diluting agent, Magnesium stearate was used as a lubricant and Talc was used as a glident. These sustained release tablets can release the drug up to 12 hours in predetermined rate. The formulated powder blend was evaluated for bulk density, tapped density, compressibility index and angle of repose. The formulated tablets were evaluated for physical characteristics of sustained release tablets such as thickness, hardness, friability, weight variation and drug content. The results of the formulations found to be within the limits specified in official books. The tablets were evaluated for In-vitro drug release studies by using USP type I dissolution test apparatus. The dissolution test was performed in 0.1 N HCL for 2 hr and phosphate buffer pH 6.8 for 10hrs. The in-vitro cumulative drug release profile of all formulations F1-F10 at 12 hours showed 84.25% to 99.82% drug release, respectively. From the data it was clear that by increasing the amount of polymer in the formulation the amount of drug release was decreased. Hence, Formulation F9 was the most promising formulation as it gives satisfactory release (99.82%) for 12 hours and F9 found to be the best formulation.DOI: http://dx.doi.org/10.3329/icpj.v2i10.16410 International Current Pharmaceutical Journal, September 2013, 2(10): 165-169


2014 ◽  
Vol 50 (4) ◽  
pp. 799-818 ◽  
Author(s):  
Tariq Ali ◽  
Muhammad Harris Shoaib ◽  
Rabia Ismail Yousuf ◽  
Sabahat Jabeen ◽  
Iyad Naeem Muhammad ◽  
...  

The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2) results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.


2020 ◽  
Vol 8 (02) ◽  
pp. 40-45
Author(s):  
Chhitij Thapa ◽  
Roma Chaudhary

INTRODUCTION Domperidone is a unique compound with gastro kinetic and antiemetic effects. It is used in the management of disorder by impaired motility like gastroesophageal reflux (in some instances), gastroparesis, dyspepsia, heartburn, epigastric pain, nausea, vomiting, and colonic inertia. The sustained release system is a widely accepted approach for slow drug release over an extended period to address the challenges of conventional oral delivery, including dosing frequency, drug safety, and efficacy. The study aims to formulate a domperidone sustained release tablet and compare the dissolution rate with the marketed formulations. MATERIAL AND METHODS Sustained release matrix tablets of domperidone were prepared by wet granulation method using different polymers such as HPMC K4M, ethyl cellulose, Gum acacia. Pre-compression studies like angle of repose, bulk density, tapped density, Carr's index, and Hausner’s ratio, and post-compression studies like weight variation, thickness, hardness, friability, drug content, and in-vitro drug release were evaluated.   RESULTS The release profile of domperidone sustained-release tablets was studied spectrophotometrically. The in-vitro dissolution study suggests the minimum %-cumulative drug release with 98.33% in F5. The %-cumulative drug release was maximum in F3 with 99.69%. The in-vitro drug release of all the formulations was non-significant compared to the marketed formulation (p<0.05), exhibiting the sustained-release property by all the formulations. CONCLUSION The pre-compression study concludes the better flow property of the granules of different formulations. The sustained release domperidone tablets were prepared successfully by the wet granulation method. The post-compression parameters of different formulations were within the acceptable range.


Author(s):  
Ankit Acharya ◽  
Mohammed Gulzar Ahmed ◽  
Ravi Chaudhari ◽  
Renukaradhya Chitti

Divalproex sodium is considered as the most important antiepileptic drug and widely used for treatment of epilepsy and bi-polar disorders and prophylaxis of migraine. The present work has been done to formulate bi-layered tablet of Divalproex sodium containing immediate release layer and sustained release layer. The FTIR study revealed that there was no interaction between drug and polymer and combination. Both layers were prepared by wet granulation technique as poor flow property exhibited by pure drug. The immediate release layer was formulated by using superdisintegrants and evaluated for physical parameters, disintegration time and in vitro drug release. The optimized immediate release layer (IF6) with highest in vitro release of 98.11 was selected for bi-layered tablet formulation. HPMC K4M and HPMC K100M polymer were used to retard the drug release from sustained release layer in different proportion and combination and evaluated for physical parameter along with in vitro drug release studies. The optimized sustained release layer (SF8) which extends the Divalproex sodium release more than 18 hrs was selected. Finally, bi-layered tablets were prepared by double compression of selected sustained release layer and immediate release layer of Divalproex sodium. The tablets were evaluated for hardness, thickness, weight variation, friability, drug content uniformity and in vitro drug release. All the physical parameters were in acceptable limit of pharmacopeial specification. The stability studies, shown the bi-layer tablet was stable at 40oC / 75% RH for a period of 3 months.  


1970 ◽  
Vol 9 (1) ◽  
pp. 47-52 ◽  
Author(s):  
Muhammad Rashedul Islam ◽  
Ishtiaq Ahmed ◽  
Mohiuddin Abdul Quadir ◽  
Md Habibur Rahman

The objective of the present study was to develop once-daily sustained-release matrix tablets of naproxen, one of the most potent non-steroidal anti-inflammatory agents used in the treatment of arthritic pain. The tablets were prepared by direct compression method using hydrophilic matrix materials like Methocel® K4M CR and Methocel® K15M CR. The tablets were subjected to measurement of thickness, diameter, weight variation, drug content, hardness and friability, the results of which were within compendial specification range. In vitro release studies were carried out by the USP basket method and were carried out at pH 7.4 buffer for ten hours. The results of dissolution studies indicated that higher polymer content in the matrix (40%) decreased the release rate of the drug as shown in formulation NMK4MF6 and NMK15MF6 (where lactose content is zero). The most successful formulations of the study, exhibited satisfactory drug release which was very close to the theoretical release profile. All the formulations exhibited diffusion-dominated drug release. Key words: Naproxen; Methocel® K4M CR; Methocel® K15M CR; Sustained release; Matrix tablets DOI: 10.3329/dujps.v9i1.7429 Dhaka Univ. J. Pharm. Sci. 9(1): 47-52 2010 (June)


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