scholarly journals In-vitro and In-vivo Relationship of Gabapentin from Floating and Immediate Release Tablets

2019 ◽  
pp. 1-12
Author(s):  
E. E. Zien El-Deen ◽  
H. A. Yassin
Keyword(s):  
Neuropathic Pain ◽  
Drug Release ◽  
Research Work ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Immediate Release ◽  
Floating Tablets ◽  
Weight Variation

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.

COMPARATIVE EVALUATION OF POLYMER COMBINATION IN THE DESIGN OF BRIMONIDINE TARTRATE OCULAR INSERTS

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (07) ◽  
pp. 30-35
Author(s):  
P Goudanavar ◽  
◽  
N Ambhore ◽  
D. Hiremath ◽  
R Udupi
Keyword(s):  
Polymer Concentration ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Carboxymethyl Chitosan ◽  
Moisture Loss ◽  
In Vivo Release ◽  
Weight Variation ◽  
Brimonidine Tartrate

Brimonidine is an anti-glaucoma agent useful in treatment of intraocular pressure. In the present study an attempt was made to formulate ophthalmic inserts of brimonidine tartrate (BT) in combination with polymers like methylcellulose, carboxymethyl chitosan and HPMC. Prepared ocular films were evaluated for uniformity in thickness, weight variation, % moisture absorption, % moisture loss, in vitro and in vivo release studies. The physical characteristics of the films were found to be within acceptable limits. The study confirmed that brimonidine tartrate can be delivered through films made of methyl cellulose, carboxymethyl chitosan and HPMC combination matrix cast with ethyl cellulose (EC). In vitro release study revealed that increasing the proportion of polymer concentration decreased the rate of release of brimonidine tartrate. In vivo release profile of ocular inserts revealed controlled release of drug over a period of 24 h. Optimized formulation CH3 was evaluated for in vivo release characteristics using rabbits as animal model. The optimized formulation CH3 was found to be stable at accelerated storage condition of 40/75 % RH.

scholarly journals FORMULATION AND EVALUATION OF TOPICAL GEL OF ACYCLOVIR FOR TREATMENT OF VIRAL DISEASE

2019 ◽  
Vol 8 (6) ◽  
Author(s):  
Vivek Jatwa ◽  
M.K. Gupta ◽  
Neetesh K Jain ◽  
Urvashi Sharma ◽  
Rahul Sisodiya
Keyword(s):  
Drug Release ◽  
Research Work ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Viral Disease ◽  
Pharmacokinetic Data ◽  
Permeation Enhancer ◽  
Topical Gel ◽  
Carbopol 940

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

Formulation and Development of Divalproex Sodium Bi-Layered Tablets using Superdisintegrants and Release Retardant Polymers

2017 ◽  
Vol 10 (2) ◽  
pp. 3669-3675
Author(s):  
Ankit Acharya ◽  
Mohammed Gulzar Ahmed ◽  
Ravi Chaudhari ◽  
Renukaradhya Chitti
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Immediate Release ◽  
Physical Parameters ◽  
Content Uniformity ◽  
Divalproex Sodium ◽  
In Vitro Drug Release ◽  
Weight Variation

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.  

scholarly journals Development and Evaluation of Floating Tablets of Pantoprazole

2019 ◽  
pp. 452-467
Author(s):  
Sandhyarani Awatade ◽  
Ritesh Bathe ◽  
Swapna Mane
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Research Work ◽  
Methyl Cellulose ◽  
Sustained Drug Release ◽  
Gastric Residence Time ◽  
Weight Variation ◽  
Floating Tablet ◽  
High Level

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.

scholarly journals Formulation and Evaluation of Floating Tablets of Tofacitinib Citrate

2021 ◽  
Vol 69 (1) ◽  
Author(s):  
Sanjesh G. Rathi ◽  
JayKumar G. Chaudhari
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Research Work ◽  
Methyl Cellulose ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Work Done ◽  
Preparation And Evaluation

The present research work done with an objective of preparation and evaluation of floating tablets of Tofacitinib Citrate drug with Hydroxy propylene methyl cellulose (HPMC), Polyox N-60K, Carbopol 934 P and Guar gum polymers. Floating tablets were based on effervescent approach using sodium bicarbonate a gas releasing agent. Direct compression method was used in present study for preparation of tablets. Effect of polymers was evaluated by studying drug release and floating time. In-vitro drug release profile indicates that sustained nature increased by increasing the concentration of polymer. The formulation containing Polyox N-60K and Carbopol 934 P in combination was optimized as it showed drug release up to 12hrs. Optimized formulation F18 was found stable during stability condition up to 1 month.

Preparation and In vivo Evaluation of Mucoadhesive Microspheres for Gastroretentive Delivery of Misoprostol

2017 ◽  
Vol 10 (2) ◽  
pp. 3676-3683
Author(s):  
Bhikshapathi D.V. R. N. ◽  
Ranjith Kumar K
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Gi Tract ◽  
In Vivo Evaluation ◽  
Upper Gi ◽  
Upper Gi Tract

The aim of the present investigation was to prepare and evaluate the Misoprostol mucoadhesive microspheres for gastroretentive drug delivery. Sodium alginate and sodium carboxy methyl cellulose were used as mucoadhesive polymers. Microsphere formulations were prepared using Ionotropic gelation technique. All the microspheres were characterized for particle size, scanning electron microscopy, FT-IR study, percentage yield, drug entrapment, stability studies and for in vitro release kinetics. Based on the results, the formulation M12 was selected as optimized formulation. In vitro drug release study of optimized formulation M12 showed 98.23% after 12 h in a controlled manner, which is essential for anti ulcer therapy. The marketed product shows the drug release of 95.23 within 1 h. The results of mucoadhesion study showed better retention of prepared microspheres (8) h in chic duodenal and jejunum regions of intestine. The results showed significant higher retention of mucoadhesive microspheres in upper GI tract. Pharmacokinetic study revealed that the bioavailability was found to be increased significantly when compared with marketed tablets. The drug release of Misoprostol optimized formulation M12 followed zero order, Higuchi and Korsmeyer-Peppas kinetics indicating diffusion controlled with non-Fickian (anomalous) transport thus it projected that delivered its active ingredient by coupled diffusion and erosion. Overall, the result indicated prolonged delivery with improved bioavailability of Misoprostol from mucoadhesive microspheres due to higher retention in the upper GI tract.

Cashew Nut Starch as Natural Excipient for Improved Bioavailability of Drugs

2019 ◽  
Vol 12 (4) ◽  
pp. 4616-4622
Author(s):  
Anjali Kushwaha
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Disintegration Time ◽  
Cashew Nut ◽  
Weight Variation ◽  
Release Studies ◽  
The Given

The bioavailability of drug is affected by various excipients present in the formulation. In case of tablets, the role of binders is very important for release of drug and bioavailability. In the present study, starch was extracted from the cashew nuts and used as binding agentat a concentration of 2% w/v, 4% w/v, 6% w/v and 8% w/v. The tablets were formulated by using famotidine drug and they were further evaluated for various parameters like weight variation, hardness, friability, disintegration time, in vitro and in vivo drug release. The results show that all parameters were found within the given Indian Pharmacopeial limits. The in vitro release studies were performed in 0.1 N HCl using dialysis methods. This shows that tablets containing 2 % of cashew starch showed maximum drug release (89%) then other formulations. Then optimized formulation was further used for in vivo study and results shows better bioavailability as compared to marketed products.

scholarly journals Developement and Characterization of Floating Tablets of Nizatidine for Peptic Ulcer

2020 ◽  
pp. 1-12
Author(s):  
Sunil T. Galatage ◽  
Suresh G. Killedar ◽  
Rushikesh B. Katakar ◽  
Ravindra B. Kumbhar ◽  
Maya Sharma ◽  
...  
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Half Life ◽  
Research Work ◽  
Content Uniformity ◽  
Floating Tablets ◽  
Gastric Residence Time ◽  
Weight Variation ◽  
Floating Tablet

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.

Preparation and Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets in Healthy Human Volunteers

2017 ◽  
Vol 10 (1) ◽  
pp. 3623-3630
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Haarika B ◽  
Jyothi Sri S ◽  
K Abbulu
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Drug Bioavailability ◽  
Floating Tablets

The purpose of present investigation was to develop floating matrix tablets of gemifloxacin mesylate, which after oral administration could prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. Tablets containing drug, various viscosity grades of hydroxypropyl methylcellulose such as HPMC K4M and HPMC K15M as matrix forming agent, Sodium bicarbonate as gas-forming agent and different additives were tested for their usefulness in formulating gastric floating tablets by direct compression method. The physical parameters, in vitro buoyancy, release characteristics and in vivo radiographic study were investigated in this study. The gemifloxacin mesylate floating tablets were prepared using HPMC K4M polymer giving more sustained drug release than the tablet containing HPMC K15M. All these formulations showed floating lag time of 30 to 47 sec and total floating time more than 12 h. The drug release was decreased when polymer concentration increases and gas generating agent decreases. Formulation that contains maximum concen-tration of both HPMC K15M and sodium bicarbonate (F9) showing sufficiently sustained with 99.2% of drug release at 12 h. The drug release from optimized formulation follows Higuchi model that indicates the diffusion controlled release. The best formulation (F9) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent and the tablet remained in the stomach for about 6 h.   

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

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