PREPARATION, EVALUATION AND OPTIMIZATION OF MUCOADHESIVE MINI TABLETS OF TELMISARTAN BY USING SINGLE UNIT ENCAPSULATION SYSTEM

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (05) ◽  
pp. 64-67
Author(s):  
I. S. Patil ◽  
◽  
O. A. Patil ◽  
R. R Chavan ◽  
D. S. Randive ◽  
...  
Keyword(s):  
Drug Release ◽  
Single Unit ◽  
Chemical Interaction ◽  
Extended Period ◽  
Controlled Drug Release ◽  
Wet Granulation ◽  
Dissolution Study ◽  
Capsule Shell ◽  
Physical And Chemical

The objective of the present study was to develop and optimize capsule filled oral mucoadhesive minitablets of telmisartan. Wet granulation method was employed for the development of minitablets. All the formulations (F1- F13) exhibited more than 21% drug release at 4h and at the end of 12h it showed drug release more than 90%. During the dissolution study it was observed that the capsule shell in which the minitablets were filled got completely dissolved in the first 5 min. FTIR and UV study showed absence of any significant physical and chemical interaction between drug and polymers. Formulation F 10 was found to possess higher drug release at 4h and 12 h. Combination of HPMC and Carbopol was found to be suitable for formulation of mucoadhesive minitablets, showed promising mucoadhesive strength and exhibited controlled drug release over an extended period of time.

PREPARATION, EVALUATION AND OPTIMIZATION OF MUCOADHESIVE MINI TABLETS OF TELMISARTAN BY USING SINGLE UNIT ENCAPSULATION SYSTEM

INDIAN DRUGS ◽  
2019 ◽  
pp. 64-67
Author(s):  
Indrajeet S. Patil ◽  
Omkar A. Patil ◽  
Rohankumar R. Chavan ◽  
Dheeraj S. Randive ◽  
Mangesh A. Bhutkar ◽  
...  
Keyword(s):  
Drug Release ◽  
Single Unit ◽  
Chemical Interaction ◽  
Extended Period ◽  
Controlled Drug Release ◽  
Wet Granulation ◽  
Dissolution Study ◽  
Capsule Shell ◽  
Physical And Chemical

The objective of the present study was to develop and optimize capsule filled oral mucoadhesive minitablets of telmisartan. Wet granulation method was employed for the development of minitablets. All the formulations (F1- F13) exhibited more than 21% drug release at 4h and at the end of 12h it showed drug release more than 90%. During the dissolution study it was observed that the capsule shell in which the minitablets were filled got completely dissolved in the first 5 min. FTIR and UV study showed absence of any significant physical and chemical interaction between drug and polymers. Formulation F 10 was found to possess higher drug release at 4h and 12 h. Combination of HPMC and Carbopol was found to be suitable for formulation of mucoadhesive minitablets, showed promising mucoadhesive strength and exhibited controlled drug release over an extended period of time.

scholarly journals FORMULATION AND IN-VITRO EVALUATION OF THEOPHYLLINE HYDROCHLORIDE EFFERVESCENT FLOATING TABLETS: EFFECT OF POLYMER CONCENTRATION ON TABLET BUOYANCY

2019 ◽  
pp. 59-65
Author(s):  
AKPABIO E. I. ◽  
EFFIONG D. E. ◽  
UWAH T. O. ◽  
SUNDAY N. I.
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Wet Granulation ◽  
Floating Tablets ◽  
Swelling Characteristics

Objective: This study was undertaken to formulate a floating drug delivery system of theophylline hydrochloride using different concentrations of a chosen polymer and then investigate how polymer concentration affects buoyancy and drug release properties of the tablets. Methods: Hydroxypropyl methylcellulose (HPMC) at different concentration levels of 15% (F1), 20% (F2) and 30% (F3) was used to form the three formulation batches of floating tablets. Wet granulation method was used for the granule preparation while Sodium bicarbonate and citric acid were used as the gas generating agent. The physical properties of the granules and the floating tablets were evaluated. Also determined were the physicomechanical properties, buoyancy and swelling characteristics of the tablets. The in vitro drug release study was carried out according to the USP I (basket method) for 8h in 900 ml 0.1N HCl at 50 rpm. Samples withdrawn at the regular predetermined time were analyzed spectrophotometrically at a wavelength of 271 nm and data obtained statistically analyzed by one-way analysis of variance (ANOVA). The differences between means were considered significant at P<0.05. Results: The result showed that polymer (HPMC) concentration significantly (p>0.05) increased swelling index and improved floating lag time, it had no significant effect on the total floating time. Percentage drug release at the end of 8 h was 100%, 98.2% and 96.13% for formulation F1, F2 and F3, respectively. All three formulations followed the Higuchi drug release kinetics model and the mechanism of drug release was the non Fickian diffusion with exponents of 0.46, 0.51 and 0.56 for the respective batch. Conclusion: Batch F3 gave a better-controlled drug release and floating properties in comparison to batch F1 and F2 thus Polymer concentration influenced the onset of floating and controlled the release of Theophylline.

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. 

Electrospun Fibre Composite for Controlled Drug Release

MRS Advances ◽  
2020 ◽  
Vol 5 (46-47) ◽  
pp. 2409-2417
Author(s):  
Ryan Go ◽  
Shadi Houshyar ◽  
Kate Fox ◽  
Yen Bach Truong
Keyword(s):  
Drug Release ◽  
Fibre Composite ◽  
Extended Period ◽  
Controlled Drug Release ◽  
Burst Release ◽  
The Core ◽  
Potential System ◽  
Shell Composition ◽  
Severe Health Problem

AbstractA drug delivery system with sustainable controlled drug release can improve the quality of life of a patient by reducing the side-effects and better absorption of the drug locally. However, the main disadvantageous of this delivery model is the burst release of the drug, which can result in severe health problem, such as toxicity. Here in this study, a new coaxial microfiber has been developed with encapsulated anti-inflammatory drug, ibuprofen, inside the core structure of the coaxial fibre. The core consisting of polyethylene oxide (PEO) carrying the drug was covered with the polylactic acid (PLA)/PEO and shell to prevent the burst release of the drug and provide sustainable release over a prolonged time. The release profiles showed that the burst release was reduced from 20% in control scaffold, core only, to 5% in core-shell structure after 6 hrs. The higher percentage of PLA in the shell composition provides a slower release of ibuprofen, due to the slower degradation of PLA in comparison with PEO. The result indicates the developed structure can be a potential system for the localized release of the various drug system, which leads to a more sustainable and controlled release of the drug over the more extended period and deliver a better outcome along with side-effect prevention.

Formulation and Evaluation of Microbially- triggered tablets of Valdecoxib

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Surender Verma ◽  
S. Singh ◽  
D. Mishra ◽  
Atul Gupta ◽  
Rakesh Sharma
Keyword(s):  
Phosphate Buffer ◽  
Guar Gum ◽  
Oral Route ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Dissolution Study ◽  
Caecal Content ◽  
Model Drug

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.

Influence of Formulation Variables and Processing Techniques on Drug Release from Carbopol-971 based Matrix Tablets of Cinnarizine and Nimodipine.

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Singh K. ◽  
Pandit K. ◽  
Mishra N.
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Weight Variation ◽  
Diffusion Controlled ◽  
The Matrix ◽  
Processing Techniques ◽  
Formulation Variables

The matrix tablets of cinnarizine and nimodipine were prepared with varying ratio of Carbopol- 971P and co-excipients of varying hydrophilicity (i.e. dicalcium phosphate and spray dried lactose) by direct compression and wet granulation using alcoholic mucilage. The prepared tablets were evaluated for weight variation, hardness and friability. The influence of concentration of the matrix forming material and co-excipients on the release rate of the drug was studied. The release rate of Cinnarizine (more soluble drug) from tablets followed diffusion controlled mechanism whereas for nimodipine (less soluble drug), the drug release followed case-II or super case- II transport mechanism based on Korsmeyer- Peppas equation. The results indicated that the drug release from matrix tablets was increases with increase in hydrophilicity of drug and co-excipients. The release of drug also increased with thermal treatment and decreasing polymer concentration.

A Comparative Study of Matrix Tablets Designed by Different Methods

2017 ◽  
Vol 10 (2) ◽  
pp. 3645-3652
Author(s):  
Tulsi Bisht ◽  
Rishishwar Poonam
Keyword(s):  
Drug Release ◽  
Comparative Study ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Once Daily ◽  
Gum Acacia ◽  
Weight Variation ◽  
Evaluation Parameters

The aim of present work was to develop once daily sustained release matrix tablet of aceclofenac by wet granulation technique using natural gums i.e.: gum acacia, guar gum and Xanthan gum. In this present study matrix tablets were prepared using three different methods and a comparative study was done. Aceclofenac sodium being the newer derivative of diclofenac having short biological half life (4hrs.), so it requires more than one dose per day to maintain therapeutic dose. The prepared tablets were evaluated for various parameters like weight variation, hardness, swelling index, friability, percent drug release and various release profile like zero order, first order, Higuchi's, and Koshemeyrs-peppa. All the evaluation parameters met pharmacopoeial specifications and through dissolution studies it was matrix tablets prepared with method 2 shows heighest percent drug release and matrix tablet prepared by method 3 showed lowest percent drug release at the end of 8 hrs. (Shown in fig. 8, comparative release study of all three formulations). Matrix tablet of aceclofenac were successfully prepared and evaluated and it can be concluded that matrix tablet prepared with natural gums showed release rate for a prolonged time and can be of great importance for “once daily” tablet to reduce side effects and toxicity related with NSAIDs.  

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.

Preparation and Evaluation of a Gas Formation-based Multiple-Unit Gastro-Retentive Floating Delivery System of Dipyridamole

2012 ◽  
Vol 5 (1) ◽  
pp. 1607-1616
Author(s):  
Y. Madhusudan Rao ◽  
Katakam V V ◽  
S Reddy ◽  
J M Somagoni ◽  
P K Panakanti ◽  
...  
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Polymeric Membrane ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Gastric Residence Time ◽  
Gas Formation ◽  
Multiple Unit ◽  
Model Drug

The aim of this study was to prepare mini tablets to be filled into a capsule that is designed to float on the gastric contents based on gas formation technique. The drug-containing core mini-tablets were prepared by wet granulation method followed by a coating of the core units with seal coating, an effervescent layer and a gas-entrapping polymeric membrane (Eudragit RS30D, RL30D). Dipyridamole, which is predominantly absorbed in the upper part of GI tract and unabsorbed/insoluble at the lower intestine, was used as a model drug. The effect of the preparative parameters like amount of the effervescent agent layered onto the seal coated units, type and coating level of the gas-entrapping polymeric membrane, floating ability and drug release properties of the multiple-unit FDDS were evaluated. The formulations were evaluated for pharmacopoeial quality control tests. Physical parameters were found to be within the acceptable limits. The system using Eudragit® RL30D as a gas-entrapping polymeric membrane exhibited floating properties. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapping polymeric membrane decreased. The optimum system exhibited complete floating within 3 minutes and maintained that buoyancy over a period of 8 hours. The drug release was sustained and linear with the square root of time. Increasing the coating level of the gas-entrapping polymeric membrane decreased drug release. Both the rapid-floating and sustained-release properties were achieved in the multiple-unit floating delivery system developed in this study. The in vivo gastric residence time was examined by radiograms and it was found that the units remained in the stomach for about 6 hours. The analysis of the dissolution data after storage at 40°C and 75% RH for 6 months showed no significant change indicating good stability.

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