scholarly journals Development and Evaluation of Floating Tablets of Pantoprazole

Author(s):  
Sandhyarani Awatade ◽  
Ritesh Bathe ◽  
Swapna Mane

The present study was undertaken with an aim to design, develop and evaluate floating tablet of Pantoprazole, which release the drug in a sustained manner over a period of 12 hours. In this research work used hydroxy propyl methyl cellulose (HPMC K4M), gas generating agent sodium bicarbonate and citric acid. The high level of HPMC K4M and citric acid favors preparation of floating tablet Pantoprazole. The tablets were prepared by direct compression techniques and evaluated thickness, hardness, weight variation, friability, floating lag time and In-vitro drug release studies indicated that the floating dosage form showed slower release as concentration of HPMC K4M increases. Formulation F1 was considered as optimized formulation which shows satisfactory sustained drug release and remained buoyant on the surface of medium for more than 12 hrours. It can also conclude that floating drug delivery system of Pantoprazole can be successfully formulated as an approach to increase gastric residence time and thereby improving its bioavailability.

Author(s):  
Sunil T. Galatage ◽  
Suresh G. Killedar ◽  
Rushikesh B. Katakar ◽  
Ravindra B. Kumbhar ◽  
Maya Sharma ◽  
...  

The objective of the present research work is to develop an ideal floating drug delivery system of nizatidine to increase the gastric residence time in stomach. To overcome the short half life and lower bioavailability of drug in tablet form we developed the drug in the form of effervescent floating tablet containing HPMC K100 and sodium bicarbonate by direct compression methodology. The prepared effervescent floating tablets were characterized by thickness, weight variation, hardness, friability, drug content uniformity, in vitro buoyancy time, swelling test, in vitro study and stability study and found that all formulations showed satisfactory results with enhanced half life and bioavailability that is among all formulations F1 formulation exhibited good drug release of 95.03% & has shown floating lag time 55 sec. Finally, it was concluded that formulations of nizatidine floating tablet were successfully prepared and found prolonged drug release for 12 hours thereby getting enhanced bioavailability, patient compliance by reducing dose frequency and gastric residence time.


Author(s):  
E. E. Zien El-Deen ◽  
H. A. Yassin

Gabapentin is effective against post-traumatic spinal injury-induced neuropathic pain. It requires high dosage and frequency in the management of neuropathic pain. The present research work was an attempt to formulate and evaluate gabapentin gastro-retentive tablets to prolong gastric residence and increase drug absorption and further increase bioavailability. The floating tablets of gabapentin were prepared in two doses (300 and 600 mg) by using two polymers (hydroxyl propyl methyl cellulose and hydroxyl propyl cellulose). Immediate release tablets of gabapentin containing the same doses were prepared and used as reference formulations. The physicochemical characteristics of the prepared tablets were determined (drug content, weight variation, friability, hardness, thickness and diameter).  Drug release from the prepared tablets was followed and found that by increasing drug concentration in the tablets release rate increases. Floating tablets showed prolonged drug release (over 96%) to more than 15 hrs. Immediate release tablets showed over 97% drug release within 48 min. In-vivo results showed that plasma exposure to gabapentin in animals receiving the drug does not dose proportional and therefore may not reach therapeutically useful levels. AUC0-24 and Cmax in case of 300 mg tablets are more than those in case of 600 mg tablets. The in-vivo release of gabapentin does not correlate with the in-vitro release of the drug.


Author(s):  
Parasuram Rajam Radhika ◽  
Nishala N ◽  
Kiruthika M ◽  
Sree Iswarya S

Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate theintragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulationswere formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration ofdrug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent.Methods: The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitrobuoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion.Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimizedformulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMCK100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studiesand was found to be stable as no significant change was observed in various evaluated parameters of the formulation.Conclusion: It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach toincrease gastric residence time, thereby improving its bioavailability.Keywords: Venlafaxine hydrochloride, Intragastric buoyant, Floating drug delivery systems, Hydroxypropyl methyl cellulose K100M, Carbopol 934 P,Xanthan gum.


2018 ◽  
Vol 6 (11) ◽  
pp. 61-80 ◽  
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma

In the present experimental investigation an attempt has been made to assess the utility of Crushed Puffed Rice (CPR)-High Molecular Weight Chitosan (HMWCH)-Hydroxypropyl Methylcellulose K15M (HPMC K15M) as a polymeric carrier for the sustained stomach delivery of Piroxicam (PRX). A total of nine formulations were prepared by using 3 (2) Taguchi factorial design, physically blending drug and polymer(s) followed by encapsulation into hard gelatin capsules size 1. The prepared capsules were evaluated for various performance such as weight variation, drug contents, in vitro buoyancy and drug release in 0.1 M HCl. The effect of drug loading on in vitro performance of the formulations was also determined. Crushed puffed rice (CPR) remained buoyant for up to average time span of 06 hr as an unwetted irregular mass in 0.1 M HCl. However, when combined with HMWCH or HPMC K15M or HPMC K15M + HMWCH a low -density cylindrical raft type hydrogel was formed which remained buoyant for up to 12 hr and released up to 99% drug in a sustained manner from 8 to 12 hr following zero order release kinetics. It was also observed that drug release from drug + CPR matrices followed Fickian mechanism. Combination of CPR + HMWCH or HMWCH + HPMC K15M also follows Fickian mechanism. Obtained data from the research work suggests that CPR in combination with HMWCH or HPMC K15M or HPMC has sufficient potential to be used as a carrier for stomach specific delivery of gastric irritant drug like PRX.Soni et al., International Current Pharmaceutical Journal, April 2018, 6(11): 61-80http://www.icpjonline.com/documents/Vol6Issue11/01.pdf


2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain

The objective of the present work was to develop Gastro retentive dosage forms which would remain in the stomach and upper part or GIT for a prolonged period of time thereby maximizing the drug release at desired site within the time before GRDFs left the stomach and upper part of the GIT, has provoked a great deal of increased interest in the formulation of such drug as floating drug delivery systems. Levofloxacin, (BCS class I) is a fluoroquinolone anti-bacterial agent. The rationale for the formulation of floating matrix tablet are acidic solubility of levofloxacin, residence of Halicobactor pylori mainly in sub region of stomach and the overdosing associated adverse effect due to continuous intake of drug in acute infection. A simple visible spectrophotometric method was employed for the estimation of levofloxacin at 294 nm and Beer’s law is obeyed in the concentration range of 2-10 μg /ml. Floating matrix tablet of levofloxacin was prepared by direct compression method using different polymers like hydroxyl propyl methyl cellulose (HPMC K4) and carbopol 934 as matrix formation polymers, sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the levofloxacin and other excipients alone and in combination show the compatibility of the drug and excipients. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on levofloxacin release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F4were fitted in different models. The optimized formulation F4 showed 99.25% drug content and swelling index of 79.85 %. Drug release mechanism was found to be first order kinetics. Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.  


Author(s):  
Hemant A. Deokule ◽  
Smita S. Pimple ◽  
Praveen D. Chaudhari ◽  
Ajit S. Kulkarni

Fast dissolving strips are used as novel approaches, as it dissolves rapidly in mouth and directly reaches the systemic circulation. In present research work, an attempt has been made to prepare mouth dissolving strips of Metoclopramide hydrochloride by using a novel film former Pullulan by solvent casting method. A33 full factorial design was utilized for the optimization of the effect of independent variables such as the amount of Pullulan, amount of PEF 400, amount of SSG on mechanical properties, and % drug release of strips. The drug compatibility studies using FTIR and DSC studies formulated strips were characterized for their physicochemical parameter like weight variation, visual appearance, folding endurance, thickness, disintegration time, drug content, and in vitro dissolution studies. FTIR and DSC studies revealed that the polymer is compatible with the drug. It was found that the optimum levels of the responses for a fast release strip could be obtained at low levels of Pullulan, PEG400, and SSG. The prepared strip was clear transparent and had a smooth surface. The surface pH was found 4.8 to 5.2 be in the range of to which is close to salivary pH, which indicates that strips may have less potential to irritate the oral mucosa, thereby they are comfortable. The drug release was found to be between 90.94 to 100.5% in 2 min. The in-vitro disintegration time of strips prepared with Pullulan was in the range of 19 to 57 sec. As the concentration of SSG increases the decrease in the disintegration time of strips a decrease. The dissolution rate increased with an increase in the concentration of SSG. Hence, it can be inferred that the fast dissolving oral strips of Metoclopramide hydrochloride may produce rapid action thereby improving bioavailability and enhance the absorption by avoiding the first-pass effect.


2017 ◽  
Vol 15 (2) ◽  
pp. 177-186
Author(s):  
Abhijeet Ojha ◽  
NV Satheesh Madhav

The aim of our research work was to isolate a biomaterial from Colocasia. esculenta and prepare phenytoin loaded mucoadhesive biofilms using this biomaterial. The biomaterial was isolated from C. esculenta tubers by an economical process. The isolated biomaterial was subjected to various physical evaluation, chemical tests as well as spectral analysis. The drug-biomaterial interaction study was performed to see if there was any interaction of biomaterial with phenytoin. Phenytoin loaded biofilms were prepared using biomaterial, flexicizer and other co- processing agents. The prepared biofilms were evaluated for physical appearance, weight, thickness, folding endurance, swelling index, surface pH, tensile strength, percent elongation, percent moisture uptake, percent moisture loss, vapor transmission rate and content uniformity. The mucoadhesivity of biofilms was investigated using rotating basket method. The in-vitro drug release study of biofilms was performed on static MS diffusion apparatus. The stability studies of biofilms were carried out at different conditions of temperature and relative humidity. The results were compared with the standard hydroxy propyl methyl cellulose (HPMC) and sodium carboxymethyl cellulose (Sodium CMC) films. The experimental results revealed that the phenytoin loaded biofilms of C. esculenta possessed excellent mucoadhesivity, sufficient stability as well as appreciable release characteristics. The best biofilm formulation was PK6 with a cumulative drug release of 95.35 % over 36 hours. Hence, C. esculenta biomaterial can serve as a potential film forming agent for transmucosal drug delivery systems.Dhaka Univ. J. Pharm. Sci. 15(2): 177-186, 2016 (December)


Author(s):  
Pranali Shivaji Salunkhe

ABSTRACTGastroretentive floating drug delivery system is utilised to target drug release in the stomach or to the upper part of intestine. Lansoprazole is proton pump inhibitor intended for oral administration used as antiulcer agent. The present investigation involved formulation and evaluation of Gastroretentive floating tablets of Lansoprazole for prolongation of gastric residence time with a view to deliver the drug at sustained and controlled manner in gastrointestinal tract. The tablets of Lansoprazole were prepared by direct compression method using gas generating agent and different polymer combinations (HPMCK4M, HPMC K100M, Psyllium husk) . The prepared tablets of Lansoprazole were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, swelling index, in-vitro dissolution study. The varying concentration of gas generating agent and polymers were found to affect on in-vitro drug release, floating lag time and swelling index. In vitro drug release of floating Gastroretentive tablet of Lansoprazole shown that the formulation F2 was found to be the best formulation as it releases 97.9% Lansoprazole in a controlled manner for extended period of time (upto 12 hrs.)Keywords: Lansoprazole, Gastroretentive, floating tablet, total floating time.


Author(s):  
R. Shireesh Kiran ◽  
B. Chandra Shekar ◽  
B. Nagendra Babu

In the current study, gastro-retentive tablets of Ritonavir was developed to increase its oral bioavailability using hydrophilic polymers HPMC K 4M, K 15M, and K 100M as release retarding agents. Polyox WSR 303 was chosen as resin, sodium bicarbonate was used as effervescent agents. The tablets were prepared by direct compression method and FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K 100M, Crospovidone, Polyox WSR 303 and sodium bicarbonate, as gas generating agent was choosen as optimized formulation based on the evaluation parameters, floating lag time (33 sec) and total floating time (>24 h) and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product was shown 98.67% and 95.09 ± 5.01% of drug release respectively. From in vivo bioavailability studies, after oral administration of floating tablet containing 100 mg Ritonavir, the Cmax, Tmax, and AUC0–∞ of optimized gastroretentive formulation were found to be 30.11 ± 1.16μg/mL, 8.00±1.23 h and 173 ± 26.34μg*h/ml, respectively. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for improved bioavailability.


Author(s):  
Vivek Jatwa ◽  
M.K. Gupta ◽  
Neetesh K Jain ◽  
Urvashi Sharma ◽  
Rahul Sisodiya

Aim: Formulation & Evaluation of Topical Gel of Acyclovir for Treatment of Viral Disease. Material & Methods: Acyclovir gels were formulated using different polymers like Carbopol 934, Carbopol 940, hydroxy propyl methyl cellulose and Sodium Carboxy methyl cellulose. Different concentrations of polymer were used in the formulation of gels. All the formulations were evaluated for the various parameters. Results & Discussion: Different formulations with use of different polymers were prepared. The amount and percentage of drug present in gel formulation using different polymers were estimated as per the procedure. The prepared gel using 1% carbopol- 934(A2) showed maximum drug content (101.72%) compared to other formulations. The spreadability of gels was determined as per the procedure. From spreadability data is observed that the formulation with 1.0% carbopol-934 showed maximum (8cm), where as the formulations with 1% carbopol-940, 3%, HPMC and Sodium CMC 3% were showed significant spreadability. 1.0 % carbopol-934 shows maximum release (74.59%). The addition of DMSO as permeation enhancer improves the drug release from gel formulation. 1.0% carbopol-940 also showed a similar release pattern, but the release was lesser. In case of HPMC and Sodium CMC gels the release was much lesser than carbopol gels. The addition of DMSO as permeation enhancer drug release was improved. Stability study for the best formulation was done as per the procedure. The gel was both physically and chemically stable at 4-50C, Room temperature and 37±50C. Conclusion: From this investigation, it was concluded that formulation A2 with 1% Carbopol-934 may be the best formulation having good in vitro release profile, stability and bioavailability. Based on the results from the study further utility of the dosage form may depend on pharmacokinetic data. Forthcoming research work of antiviral activity may contribute in the challenging area. Keywords: Acyclovir, Topical gel, Viral Disease, Skin Disease, Formulation & Development


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