scholarly journals Design and Evaluation of Press Coated Formulation of Aceclofenac and Comparison with Marketed Preparations.

2021 ◽  
Vol 23 (07) ◽  
pp. 387-393
Author(s):  
Mr. Jadhav S.B. ◽  
◽  
Dr. Wadher S.J. ◽  
Dr. Kawtikwar P.S. ◽  
◽  
...  
Keyword(s):  
Drug Release ◽  
Lag Time ◽  
Primary Objective ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Evening Dose ◽  
In Vitro Drug Release ◽  
Drug Plasma ◽  
Compression Coating

The primary objective of the studies is to investigate whether compression coating could be used to produce tablets providing maximum drug plasma concentration 6 to 8 hours after an evening dose taken at approximately 22:00. Fast Dispersible core tablets containing Aceclofenac were prepared using super disintegrants like Ac-Di-Sol, Crospovidone, and Sodium starch glycolate through wet granulation method and evaluated for various parameters. Prepared press-coated tablets were characterized for physical parameters, drug content, lag time, in vitro drug release characteristics. Aceclofenac formulation tablets of batch F4 containing combination Methocel K4M and Methocel K100M showed desired lag time along with drug release as compared to other formulations. The Comparative dissolution study of an optimized formulation containing Aceclofenac was carried with marketed preparations also showed good results.

scholarly journals Formulation and Evaluation of Floating Tablets of Sitagliptin with Extract of Triphala

2019 ◽  
Vol 9 (4-A) ◽  
pp. 38-47
Author(s):  
Revathi Sundaramoorthy ◽  
V Gopal ◽  
G Jeyabalan
Keyword(s):  
Drug Release ◽  
Chemical Interaction ◽  
Lag Time ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Drug Content ◽  
Soxhlet Apparatus

The aim of the present work is to formulate, optimize and evaluate hydrodynamically balanced antidiabetic system incorporated with sitagliptin and phytochemical constituents of Triphala extract for the treatment of constipation associated with diabetes.  The Triphala churna of two different ratios, 1:1:1 (TC1) and 1:2:4 (TC2) were subjected to hot percolation using Soxhlet apparatus using methanol as solvent. The floating matrix tablets of Sitagliptin with methanolic Triphala extract was prepared by wet granulation technique using HPMC K4M as polymer, starch/honey as binder and sodium bicarbonate & citric acid as effervescent agents by 24 factorial design.  The compatibility studies showed that there is no chemical interaction between the drug, polymer and the excipients used in the tablets.  The independent variables are drug & Triphala extract ratio (X1), Triphala proportion (X2), binder used for granulation (X3), and amount of effervescent excipients used (X4).  The dependent variables are hardness (Y1), buoyancy lag time (Y2), total floating time (Y3), in-vitro drug release (Y4), and T50% (Y5).  The prepared floating tablets were subjected to all post compression parameters such as hardness, friability, swelling capacity, buoyancy, total floating time, drug content & in-vitro drug release and were found to be within normal limits.  Based on drug content, buoyancy lag time and in-vitro drug release the formulations F14 and F16 were selected for in-vivo study of the formulation.  Keywords:  Triphala, Sitagliptin, honey, floating tablet. 

FORMULATION AND CHARACTERIZATION OF MEDICATED CHEWING GUMS OF DEXTROMETHORPHAN HYDROBROMIDE

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (12) ◽  
pp. 29-35
Author(s):  
N.G.N Swamy ◽  
◽  
P Shilpa ◽  
Z. Abbas
Keyword(s):  
Drug Release ◽  
Systemic Absorption ◽  
Chewing Gum ◽  
Release Mechanism ◽  
Physical Parameters ◽  
In Vitro Drug Release ◽  
Chewing Gums ◽  
Dextromethorphan Hydrobromide ◽  
Spray Dried

Chewing gums are mobile drug delivery systems, with a potential for administering drugs either for local action or for systemic absorption via buccal route. Dextromethorphan hydrobromide chewing gum formulations were made employing Pharmagum M as the base with an aim to overcome the firstpass effect, reducing the risk of overdosing, ease of administration and for achieving faster systemic absorption. Dextromethorphan hydrobromide was further transformed into spray dried form and incorporated into Pharmagum M base with the object of solubility enhancement and masking the bitter taste of the drug. The prepared medicated chewing gums were evaluated for various precompression and postcompression parameters. The in vitro drug release profiles were carried out employing Erweka DRT chewing apparatus. It was observed that increasing the chewing gum base concentration resulted in a decreased drug release profile. The drug in the spray dried form revealed improved performance in comparison to the directly contained drug. The drug release data were fitted into various kinetic models. It was observed that the drug release was matrix diffusion controlled and revealed a non-Fickian drug release mechanism. Accelerated stability studies were carried out on select formulations as per ICH guidelines. The formulations were found to be stable in respect to physical parameters and no significant deviations were seen in respect to in vitro drug release characteristics.

scholarly journals Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

2021 ◽  
Vol 4 (2) ◽  
pp. 99-109
Author(s):  
Priyanka Singh ◽  
Amit Kumar Shrivastava ◽  
Sachin Kumar ◽  
Manish Dhar Dwivedi
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Hydrophilic Polymers ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Study Results

This study aimed to improve the dissolution rate of aceclofenac and release the drug in a controlled manner over a period of 24 hours. Matrix tablets were prepared by direct compression method, using hydrophilic polymers (HPMC/guar gum). Matrix tablets were prepared by wet granulation method using different hydrophilic polymers (HPMC/guar gum). Tablets were evaluated for in vitro drug release profile in phosphate buffer with pH 6.8 (without enzymes). The thickness and hardness of prepared tablets were 3.23 ± 0.035 to 3.28 ± 0.008 mm and 3.26 ± 0.115 to 3.60 ± 0.200 kg/cm2, respectively. The friability was within the acceptable limits of pharmacopoeial specifications (0.31 to 0.71%), which indicates the good mechanical strength of the tablets. Drug release was retarded with an increase in polymer concentration due to the gelling property of polymers. The in vitro drug release from the proposed system was best explained by Higuchi’s model, indicating that drug release from tablets displayed a diffusion-controlled mechanism. The results clearly indicate that guar gum could be a potential hydrophilic carrier in developing oral controlled drug delivery systems. Based on the study results, formulations F8 was selected as the best formulation.

scholarly journals FORMULATION AND EVALUATION OF GASTRORETENTIVE TABLETS OF ANTIULCER DRUG

2016 ◽  
Vol 9 (6) ◽  
pp. 48
Author(s):  
Pranali Shivaji Salunkhe
Keyword(s):  
Drug Release ◽  
Extended Period ◽  
Lag Time ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Gastric Residence Time ◽  
Target Drug ◽  
Weight Variation

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.

scholarly journals Formulation and evaluation of Prednisolone retention enema as dispersible tablet and vehicle for the treatment of ulcerative colitis

2019 ◽  
Vol 8 (2) ◽  
pp. 545-552
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Evaluation Studies ◽  
Wet Granulation ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Retention Enema ◽  
Dispersible Tablet ◽  
Dispersible Tablets

Ulcerative colitis is a chronic idiopathic inflammatory bowel disease that causes chronic inflammation and damage in the gastrointestinal (GI) tract that typically presents in the second or third decade of life with bloody diarrhoea and abdominal cramps. The objective of the present work was to formulate and evaluate of Prednisolone retention enema as a dispersible tablet and it is suspended in suitable vehicle for the treatment of ulcerative colitis. In the present work, an attempt has been made to formulate and evaluate Prednisolone retention enema as a dispersible tablet by using three different methods (direct compression (F1 to F3, wet granulation (F4 and F5) and slugging method (F6)). Prepared dispersible tablets were administered with the help of vehicle for the effective treatment of ulcerative colitis. Dispersible tablets were evaluated for various parameters. In vitro drug release and microbiological evaluation studies were performed to the best formulation in rectal suspension. Then the best formulation was subjected to carry out for stability studies at three different temperatures. Among the six formulations, F6 formulation showed better results. FT-IR study showed that there was no interaction between a drug and excipients. In vitro drug release and microbiological evaluation studies were performed for F6 formulation in rectal suspension. About 99.06 % of the drug was released at 60 min. and also it was found to be microbiologically stable. Results from the stability studies showed that F6 formulation alone and with rectal suspension was stable for a period of 90 days. It was concluded that F6 formulation in rectal suspension possesses a promising future for the treatment of ulcerative colitis.

scholarly journals Formulation and Evaluation of Floating Matrix Tablets of Sacubitril and Valsartan

2019 ◽  
Vol 9 (4-s) ◽  
pp. 298-309
Author(s):  
Sudhakar Pathak ◽  
Harish Pandey ◽  
Sunil Kumar Shah
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Potential Candidate ◽  
In Vitro Drug Release ◽  
Gastric Emptying Rate ◽  
Floating Tablets

Floating Drug Delivery Systems (FDDS) have a bulk density lower than gastric fluids and thus remain buoyant in the stomach for a prolonged period of time, without affecting the gastric emptying rate. While the system is floating on the gastric contents, the drug is released slowly at a desired rate from the system. These floating tablets mainly prepared for reduction of lag time and release the drug up to 12 hours and may also increase the bioavailability of the drugs by utilizing the drug to full extent avoiding unnecessary frequency of dosing. The purpose of this research was to develop and evaluated floating matrix tablets of sacubitril and valsartan. The floating matrix tablets of sacubitril and valsartan were prepared by direct compression method using altered concentrations of HPMC K4M, HPMC K100M, sodium alginate as polymers and sodium bicarbonate, citric acid as gas generating agent. FTIR, DSC studies conformed that there was no incompatibility between the polymers and the drug. Tablet preformulation parameters were within the pharmacopoeias limit. Tablets were evaluated by different parameters such as weight uniformity, content uniformity, thickness, hardness, in vitro release studies, buoyancy determination and kinetic analysis of dissolution data. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. Tablet showed ≤ 1min lag time, continuance of buoyancy for >12 h. The in-vitro drug release pattern of sacubitril and valsartan optimized floating tablets (F16) was fitted to different kinetic models which showed highest regression (r2 = 0.9838) for Higuchi model. The Optimized formulation (F16) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months.  Prepared floating tablets of sacubitril and valsartan may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.  

scholarly journals DESIGN AND DEVELOPMENT OF TOPICAL HYDROGEL FORMULATION OF IRBISARTAN

2019 ◽  
pp. 79-83
Author(s):  
ZEESHAN SHAIKH
Keyword(s):  
Angiotensin Ii ◽  
Drug Release ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Burst Release ◽  
Angiotensin Ii Receptor ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir

Objective: Irbesartan is an antihypertensive with limited bioavailability. The objective of the study was to develop controlled release matrix tablets of irbisartan drug. Methods: Tablets were prepared by wet granulation process. Result: In vitro drug release study revealed that HPMC causes initial burst release of drug hence combining HPMC sustained the action for 8 h (95.92±0.57% release). Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism for drug release. Compared to conventional tablets, the release of model drug from these HPMC matrix tablets was prolonged, leading to achieve an effective therapy with a low dosage of the drug, to reduce the frequency of medication. The pharmacological and clinical properties of irbesartan, a noncompetitive angiotensin II receptor type 1 antagonist, successfully used for more than a decade in the treatment of essential hypertension. Results: Compatibility Studies In order to investigate the possible interactions between irbesartan and distinct polymers and/or diluents, FT-IR and DSC studies were carried out. FT-IR results proved that the drug was found to be compatible with excipients as wave numbers are almost similar for pure drug and also drug excipients mixture. In picture 1 and 2. DSC studies indicate that chosen excipients for the formulation were found to be compatible with the active ingredient as the melting endothermic peaks are in the range of 250-320 °C which is same as the melting point of irbisartan. Conclusion: Irbesartan exerts its antihypertensive effect through an inhibitory effect on the pressure response to angiotensin II. Irbesartan 150–300 mg once daily confers a lasting effect over 24 h, and its antihypertensive efficacy is further enhanced by the coadministration of hydrochlorothiazide.

Design, Development and Optimization of Pulsatile Core in Cup Tablets of Naproxen

2017 ◽  
Vol 7 (03) ◽  
Author(s):  
Rutu H. Patel ◽  
ImadHadi Hameed ◽  
Kunal N. Patel ◽  
Madhabhai M. Patel
Keyword(s):  
Drug Release ◽  
Lag Time ◽  
Major Effect ◽  
Stability Study ◽  
Design Development ◽  
In Vitro Drug Release ◽  
Box Behnken Design ◽  
Accelerated Stability ◽  
Excipient Compatibility

The aim of the present study to prepare Pulsatile release tablet of naproxen for the treatment of rheumatoid arthritis. The drug delivery system was designed to deliver the drug at a time when it could be most needful for the patient. Drug excipient compatibility studies were carried out using DSC and found to be compatible with each other. Pulsatile tablet was prepared by direct compression method using different type and amount of superdisintegrants and coating polymers and evaluated for pre and post compression parameters. Box Behnken design was applied to optimize responses. Concentrations of Sodium starch glycolate (SSG) (X1), Ethyl cellulose (EC) (X2), and HPMC K100M (X3) were selected as independent variables while Lag time (Y1) and % drug release at 8 hrs (Y2) were selected as dependent variables. The prepared tablets were evaluated for post compression parameters and results indicated that concentration of SSG has major effect on in vitro drug release while concentration of EC and HPMC K100M has major effect on Lag time. Batch BE13 prepared with SSG 35mg, EC 175mg, and HPMC K100M 75 mg was found to be best batch as it achieves predetermined lag time of 5 hr 02 min and 99.32% of drug release. There was no significant variation in formulation at the end of six month accelerated stability study.

Development and In Vivo Evaluation of Mesalazine Colon Targeted Tablets

2019 ◽  
Vol 12 (3) ◽  
pp. 4552-4558
Author(s):  
Rawoof MD ◽  
Rajnarayana K ◽  
Ajitha M
Keyword(s):  
Drug Release ◽  
Wet Granulation ◽  
Time Intervals ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Ph Dependent ◽  
Rapid Hydrolysis

The main objective of the present study was to develop colon-targeted tablets of mesalazine by wet granulation method using 33 Response surface method with design of experiment software and HPMC K4M, Eudragit RL100, Ethyl cellulose and PVP K-30 used as pH dependent polymers. All the formulations (F1 to F27) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Mesalazine released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F26 released 98.16 % of mesalazine after 24 h, whereas marketed product drug release was 92.02 ± 2.15 after  24 h. From in vivo bioavailability studies, after oral administration of colon targeted tablet containing 400 mg mesalazine, the Cmax, Tmax, and AUC0–∞ of optimized formulation and marketed product was found to be 683.21 ± 0.03 ng/mL, 6.01 ± 0.04 h, 4150.12 ± 5.12 ng*h/mL and 445.34 ± 3.22 ng/mL, 4.00 ± 0.01 h, 3457.18 ± 5.32 ng*h/mL respectively. Cmax, Tmax and AUC values of optimized formulation were found to be significantly higher than of marketed product. The pH dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of mesalazine for the treatment of disease at colon region.

Design, in vitro and in vivo Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets

1970 ◽  
Vol 9 (1) ◽  
pp. 3143-3149
Author(s):  
Sushma Appala ◽  
Ramesh Bomma ◽  
Kishan Veerabrahma
Keyword(s):  
Helicobacter Pylori ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Gastro Retentive

Objective of the investigation was to develop gastro retentive dosage form of gemifloxacin mesylate for local action in the stomach as it has antibacterial activity against Helicobacter pylori. Gemifloxacin mesylate is a synthetic broad-spectrum antibacterial agent for oral administration, having 7 hrs half-life and 71% oral bioavailability. In present study, gemifloxacin mesylate floating matrix tablets were prepared by direct compression method using polymers (HPMC K4M, HPMC K15M and polyox WSR 1105) and evaluated for various parameters like drug content, floating behavior (floating lag time and total floating time), in vitro drug release, swelling index, weight variation, friability, hardness and thickness. Sodium bicarbonate was incorporated as gas generating agent in all formulations. Drug-excipients compatibility was studied by Differential Scanning Calorimetry. Results have shown that the amount of polymer in the formulation affected the drug release. Optimized formulation (F8 containing polyox WSR1105 as release retarding agent) was selected based on in vitro drug release, floating lag time, floating time and other parameters. This formulation followed zero order kinetics and non-Fickian mechanism of drug release. In vivo radiographic study was conducted in healthy human volunteers using tablets containing BaSO4 as radio opaque agent. The average residence time was found to be 4.5± 0.86 h (n=3). This design of gastro retentive drug delivery system helps in increasing the local delivery of drug in patients with Helicobacter pylori infection

Sign in / Sign up

Export Citation Format

Share Document