scholarly journals Formulation Development and In Vitro Characterization of Zolmitriptan Controlled Release Drug Delivery Systems

Author(s):  
Shambhavi Pandala ◽  
Vasudha Bakshi ◽  
Rajendra Kumar Jadi

Background: Zolmitriptan is an artificial tryptamine, employed for the acute cure of migraine attack with or exclusive of aura and cluster headaches. Objective: It is an attempt to develop the extended release (ER) of Zolmitriptan matrix (ZMT) tablets to treat migraine safely and effectively. Methods: All formulations were prepared with natural polymers or gums like guar gum, xanthan gum, karaya gum through direct compression method using 6mm punch. Results: Powder blend of all formulations (F1 - F12) using different ratios of the above mentioned gums (5%, 10%, 15% and 20%) were characterized with pre-compression parameters (angle of repose, bulk density, tapped density, compressibility index, hausner ratio, compatibility studies) and post-compression parameters (weight variation, thickness, friability, hardness, assay, in vitro dissolution studies). F1 - F4 formulations were prepared with gum karaya and compared with remaining gums; gum karaya shows more retardance capacity. F9 - F12 (with guar gum) formulations were unable to produce the desired release, whereas F5 - F8 formulations containing with xanthan gum exhibited more retarding effect with increasing concentration of polymer. Conclusion: All prepared formulations (F1 - F12) were characterized and F3 formulation was optimized (97.3% drug released in 8 hours). All prepared formulations (F1 - F12) showed good flow properties and release patterns. Hence, formulations of ZMT matrix tablets have a promising delivery system which will enhance bio-availability and achieve greater therapeutic efficacy.

Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Vuppula Sruthi ◽  
Damineni Saritha

The aim of the present work was to prepare floating tablets of galantamine HBr using sodium alginate and xanthan gum as matrix forming carriers. Galantamine HBr is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments, in particular those of vascular origin. The matrix tablet formulations were prepared by varying the concentrations of sodium alginate and xanthan gum. The tablets were prepared by direct compression technique using PVP K-30 as a binder and sodium bicarbonate for development of CO2. The prepared matrix tablets were evaluated for properties such as hardness, thickness, friability, weight variation, floating lag time, compatibility using DSC and FTIR. In vitro dissolution was carried out for 12 hrs in 0.1N HCl at 37±0.5 ºC using USP paddle type dissolution apparatus. It was noted that, all the prepared formulations had desired floating lag time and constantly floated on dissolution medium by maintaining the matrix integrity. The drug release from prepared tablets was found to vary with varying concentration of the polymers, sodium alginate and xanthan gum. From the study it was concluded that floating drug delivery system for galantamine HBr can be prepared by using sodium alginate and xanthan gum as a carrier.


Author(s):  
RASHMITHA V ◽  
MADHUSUDAN RAO Y ◽  
PAVANI S

Objective: The purpose of this research was to develop a fenoverine gastroretentive drug delivery system which, following oral administration should have the ability to enhance and prolong the period of gastric residence time (GRD) with the desired in vitro release profile. Methods: In the present study, fenoverine floating tablets were prepared using an effervescent method using sodium bicarbonate and citric acid as a gas-generating agent. The tablets were formulated using direct compression technology using xanthan gum and sodium alginate as polymers. Pre-compression powders were evaluated for angle of repose, bulk density, tapped density, Carr’s index, and Hausner’s ratio, and the prepared tablets were evaluated for weight variation, thickness, diameter, hardness, friability, drug content, floating lag time, total floating time, and in vitro dissolution studies. The formulations were optimized for the different concentrations of xanthan gum, sodium alginate, and their combinations. Results: All the prepared formulations showed well in vitro buoyancy. The tablets remained buoyant for 6–12 h. The in vitro drug-release pattern of fenoverine floating tablets was adapted to different kinetic models with the highest regression to zero-order and Korsmeyer-Peppas, and the mechanism was found to be a Fickian mechanism. Conclusion: Out of all the formulations prepared, in vitro dissolution studies of the F4 formulation were found to be maximum than other batches, which exhibited desired sustained release time followed by acceptable floating properties.


Author(s):  
S Shanmugam

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism.  Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies 


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):  
Sudarshan Singh ◽  
Sunil B Bothara

Diospyros melonoxylon Roxb is a small tree with rather slender stem and smooth grey bark belonging to family Ebenaceae found widely in Chhattisgarh. The present investigation reports the isolation of mucilage from Diospyros melonoxylon seeds as per AOAC guideline and evaluating it as mucoadhesive agent. Physiochemical characteristics of mucilage, such as appearance, solubility, swelling index, microbial count, loss on drying, viscosity, hydration capacity, flow property, hausner ratio and pH were studied. The mucilage was evaluated for its mucoadhesive properties in compressed tablet, using Losartan Potassium as model drug. Granules were prepared by wet granulation process using polyvinylpirroli-done as binding agent. Mucilage was used in four different concentrations i.e. 20, 40 and 60 % w/w. The prepared granules were evaluated for micrometrics property. The tablet were prepared and evaluated for weight variation, thickness diameter, hardness, percent friability, in vitro dissolution and degree of swelling. The property of bioadhesive strength of isolated mucilage was compared with Guar Gum and HPMC E5LV, which was used as standard mucoadhesive agent concentration. Bioadhesive strength of the tablet was measured on the modified physical balance. The tablets had good physiochemical properties, and drug release was retarded as concentration of mucilage was increased. The force of adhesion was obtained 0.2063N, 0.3837N, 0.5175N, 0.8679N and 0.3983N respectively for F1, F2, F3, F4 and F5. Formulations were subjected for study of effect of intensity of agitation at different rpm (50 and 150) and electrolyte (NaCl and CaCl2), and formulation showed relative effect on release of drug from formulation. All the formulations were subjected to stability studies for three months all formulation showed stability with respect to release pattern.


Author(s):  
Mona Semalty ◽  
T Bisht ◽  
A Semalty

The aim of the present study was to develop sustained release, multilayered-matrix tablet of aceclofenac using natural polymers-guar gum (GG) and xanthan gum (XG) as carrier for core matrix and hydroxyl propylmethyl cellulose (HPMC K-15M), sodium carboxymethylcellulose (NaCMC) and ethyl cellulose (EC) and polyvinylpyrrolidone (PVP-K30) for preparing bottom and top layers. The formulated tablets were evaluated for uniformity of weight, drug content, friability, hardness, thickness, swelling index and in vitro drug release. The physicochemical properties of tablets were found within the limits. The physiochemical investigation showed that aceclofenac matrix tablet prepared with xanthan gum showed better dissolution profile as compared to that of guar gum. Matrix tablets of xanthan gum with 6% W/V xanthan gum (MTX1) showed the highest percent drug release (88.98%), while matrix tablets of guar gum with 6% W/V guar gum (MTG1) showed the highest percent drug release (73.89%) at the end of 8 hours in pH 6.8 phosphate buffer. Among the matrix tablet of xanthan gum MTX4 (with 24% W/V of xanthan) showed the lowest percent drug release (49.6%) and while among the guar gum tablets MTG4  (with 24% W/V of guar gum) showed the lowest percent drug release (48.65%) at the end of 8 hours. It was concluded that increasing the concentration of gum from 6% W/V to 24% W/V in the formulation decreased the amount of drug release from the tablet. The xanthan gum based matrix tablets of aceclofenac were found to be superior to that of guar gum matrix tablets for potential therapeutic uses. 


Author(s):  
Dr. Dilip Agrawal ◽  
Dr. Rakesh Goyal ◽  
Dr. Mukesh Bansal ◽  
Ashok Kumar Sharma ◽  
Mohit Khandelwal

The demands for fast dissolving tablets have received ever increasing day by day during the last decade. In the present projected study, the effect of natural Super disintegrants was compared with synthetic Super disintegrants and conventional Super disintegrants in the of fast dissolving tablet formulation of Meclofenamate Sodium. Meclofenamate sodium NSAID is used for the treatment of mild to moderate pain in various conditions like (e.g., dental pain, osteoarthritis) and to decrease pain and blood loss during menstrual periods. It is also used for other treatments like reducing pain, swelling, and joint stiffness caused with rheumatoid arthritis. In the present work 9 formulations of FDT (Fast dissolving tablet) of Meclofenamate Sodium were prepared by using Super disintegrants was evaluated and compiles with the official parameters and specifications. Various formulations were prepared using four different super disintegrants namely natural super disintegrant Banana Powder, sodium starch glycolate, crosscarmelose sodium with three concentrations (2%, 4%, 6%) by direct compression method. The blend was evaluated for pre-compression parameters like Angle of repose, bulk density, tapped density, and then tablet evaluated with various post-compression parameters like thickness, drug content, hardness, weight variation, wetting time, friability, disintegration time, dissolution time, drug release study. Formulation F2 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation F2 showed 98.55% drug release at the end of 3 minutes. The best formulations among these were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline.


Author(s):  
Surender Verma ◽  
S. Singh ◽  
D. Mishra ◽  
Atul Gupta ◽  
Rakesh Sharma

The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher amount of drug which was also significantly higher than the dissolution media of same pH without caecal content (microflora) and it was concluded that guar gum can be used as a potential carrier for targeting drugs to colon.


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.


2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.


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