scholarly journals Formulation and Evaluation of Transdermal Patch of Apixaban

2021 ◽  
Vol 69 (2) ◽  
Author(s):  
Dhaval J. Patel ◽  
Ajay M. Vyas ◽  
Sanjesh G. Rathi ◽  
Shrenik K. Shah
Keyword(s):  
Drug Release ◽  
Stability Study ◽  
Transdermal Patch ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Target Drug ◽  
Acceptable Range ◽  
Weight Variation ◽  
S 100 ◽  
Release Data

The aim of the present investigation was to develop and evaluate transdermal patch of Apixaban. Formulation development of Apixaban Transdermal patch was initiated using Eudragit S 100 and HPMC E50 LV as matrix controlling polymer for matrix type Transdermal Patch. PEG 400 was selected as plasticizer. Glycerin was selected as permeability enhancer. Preformulation study was performed to check the drug excipient compatibility. The IR spectra of Drug and final formulation found satisfactory. There are no any interaction between drug and excipients. Further the linearity curve was developed in UV for method of analysis. Trials A1-A14 was initiated using different concentration of polymers in the formulation. The prepared patches were transparent and smooth in surface. The weight variation was found well within acceptable range. The thickness of patches was found uniform in nature and the variation is found satisfactory. Further, the surface pH of the patches was found between 6.8 to 7.1 and it is acceptable. The drug content, folding endurance and %elongation results of A1-A14 batches were found well within acceptable range. Initially the trial batches were taken with a single polymer like HPMC and EudragitS100. The drug release was not achieved as per the target drug release profile for 8hours. Hence the combination of these two polymers are taken and found better results than the single polymers. Based on the drug release data, it was observed that the A8 batch was the most satisfactory batch with respect to drug release and other parameters. Hence, the A8 batch selected as optimized batch and Stability study of the same batch initiated.

scholarly journals Formulation development and evaluation of voriconazole sustained release tablets

2013 ◽  
Vol 2 (10) ◽  
pp. 165-169 ◽  
Author(s):  
Manivannan Rangasamy ◽  
Venkata Krishna Reddy Palnati ◽  
Lakshmi Narayana Rao Bandaru
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Angle Of Repose ◽  
Type I ◽  
Dissolution Test ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Weight Variation ◽  
Sustained Release Tablets

The present study involves in the formulation and evaluation of sustained release tablets of Voriconazole (250mg). The objective of the present study was to formulate Voriconazole sustained release tablets by wet granulation method by using natural (Xanthan gum, Karaya gum) and semi synthetic polymers (HPMC K100M). Lactose was used as diluting agent, Magnesium stearate was used as a lubricant and Talc was used as a glident. These sustained release tablets can release the drug up to 12 hours in predetermined rate. The formulated powder blend was evaluated for bulk density, tapped density, compressibility index and angle of repose. The formulated tablets were evaluated for physical characteristics of sustained release tablets such as thickness, hardness, friability, weight variation and drug content. The results of the formulations found to be within the limits specified in official books. The tablets were evaluated for In-vitro drug release studies by using USP type I dissolution test apparatus. The dissolution test was performed in 0.1 N HCL for 2 hr and phosphate buffer pH 6.8 for 10hrs. The in-vitro cumulative drug release profile of all formulations F1-F10 at 12 hours showed 84.25% to 99.82% drug release, respectively. From the data it was clear that by increasing the amount of polymer in the formulation the amount of drug release was decreased. Hence, Formulation F9 was the most promising formulation as it gives satisfactory release (99.82%) for 12 hours and F9 found to be the best formulation.DOI: http://dx.doi.org/10.3329/icpj.v2i10.16410 International Current Pharmaceutical Journal, September 2013, 2(10): 165-169

scholarly journals “FORMULATION DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING FILMS OF LAFUTIDINE”

2019 ◽  
Vol 7 (2) ◽  
Author(s):  
Hir. R. Mehta ◽  
Vijay K. Patel
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Stability Study ◽  
Formulation Development ◽  
Casting Technique ◽  
Drug Content ◽  
Peg 400 ◽  
Weight Variation ◽  
Folding Endurance

The present invention was aimed to formulate and evaluate Lafutidine gastro retentive films. The films were prepared by solvent casting technique using different film forming polymers like HPMC and Ethyl cellulose. PEG 400 used as a plastsizer. The prepared films were evaluated for number of parameters like Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, unfolding behavior, floating properties, drug content and In vitro drug release studies. From the trial batches the best release for gastroretentive film was shown by formulation T5 (Ethyl cellulose and PEG 400). Formulation T5 exhibited good appearance, better mechanical strength with acceptable flexibility. Also, formulation T5 was given more than 90 % drug released after 12 hr and 97.56 % Drug content.  For optimization of formulation, 32 factorial design was applied by taking Ethyl cellulose and PEG 400 as an independent variables. Drug release at 8 hour and folding endurance selected as dependent variables. Based on drug release study, L8 batch found most satisfactory in all formulation and the effect of Ethyl cellulose and PEG 400 found significant. L8 batch found stable during stability study. Key words: Lafutidine, Floating Films, Ethyl Cellulose.

scholarly journals Formulation, Development and Evaluation of Bisoprolol Sustained Release Tablets

2021 ◽  
Vol 13 (1) ◽  
pp. 209-219
Author(s):  
M. Masum ◽  
M. A. R. Ripon ◽  
D. R. Bhowmik ◽  
M. T. Amin ◽  
S. Arefin ◽  
...  
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Flow Property ◽  
Water Soluble ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Disintegration Time ◽  
Weight Variation ◽  
Compressibility Index ◽  
Poly Ethylene

Bisoprolol is a type of antihypertensive drug (β-blocker). It is a poorly water-soluble and highly permeable drug that belongs to class II biopharmaceutical classification. This investigation represents the formulation development of bisoprolol to sustain the drug release. Different types of polymers like hypromellose, xanthan gum, avicel, poly ethylene glycol (PEG) were used in this study. Three different formulations were developed by using different excipients at various ratios. The granules were evaluated for bulk density, tapped density, flow property whereas tablets were evaluated for thickness, hardness, weight variation, compressibility index, uniformity of content, disintegration time, and drug release profile. The concentration of the diffused drug was measured using a UV-visible spectrophotometer at λmax= 225 nm. Granules showed good flow ability and all the formulations passed the quality. Among all the formulations, F-2 and F-3 showed better efficiency. PEG along with hypermellose, and guar gum showed a good combination for sustaining the drug release

Formulation and Evaluation of Transdermal patch of Methimazole

2021 ◽  
pp. 4667-4672
Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Transdermal Patch ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Percent Moisture ◽  
Release Study

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

scholarly journals OPTIMIZATION AND PREPARATION OF SOLID LIPID NANOPARTICLE INCORPORATED TRANSDERMAL PATCH OF TIMOLOL MALEATE USING FACTORIAL DESIGN

2019 ◽  
pp. 100-107
Author(s):  
PARVEEN KUMAR ◽  
BIRENDRA SHRIVASTAVA ◽  
MADAN MOHAN GUPTA ◽  
ANIL KUMAR SHARMA
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Hydroxypropyl Methylcellulose ◽  
Lipid Nanoparticles ◽  
Content Uniformity ◽  
Transdermal Patch ◽  
Timolol Maleate ◽  
Solid Lipid ◽  
Weight Variation

Objective: Transdermal patch of timolol maleate was prepared in order to increase the permeability of the drug topically. Methods: The timolol maleate (TM) loaded solid lipid nanoparticles (SLN) were prepared by the solvent evaporation method. For the optimization process full factorial (three-factor and three-level), hydroxypropyl methylcellulose (HPMC) range from 100 to 300 mg, ethylcellulose 100 to 200 gm and almond oil 3 to 4 ml. The response noted in form of tensile strength and percent drug release. These transdermal patches were evaluated for physical characterization like weight variation, thickness, percentage moisture absorption, percentage moisture loss, water vapor transmission rate, folding endurance, tensile strength, and content uniformity. Results: Solid lipid nanoparticles of TM were optimized and prepared, the data presented that drug release percent ranged from 66.12 to 91.75. 2FI model was observed to fit for response % drug permeation with a p and F value of 0.0271 and 4.50. The tensile strength varies from 0.358 to 0.508. The linear model was observed to fit for the tensile strength response with a p-value and F-value of<0.0001 and 52.41. Conclusion: The controlled release formulation of Timolol Maleate was successfully optimized and prepared, a study conducted to investigate the effect of different polymers and type of permeation time profiles from Timolol Maleate patches.

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 DESIGN, DEVELOPMENT AND EVALUATION OF MOUTH DISSOLVING TABLETS OF TOFACITINIB CITRATE

2022 ◽  
pp. 238-245
Author(s):  
MEGHANA RAYKAR ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Release ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Design Development ◽  
Disintegration Time ◽  
Drug Content ◽  
Weight Variation ◽  
Wetting Time ◽  
Bulk Drug

Objective: This study aims to Formulate Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate with the increase in bioavailability and patient compliance. Methods: Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate were developed by full factorial design at 32levelsand prepared by direct compression method using super integrants like sodium starch glycolate, Ludiflash. The tablets were compressed into compacts on a 10 station tablet machine. The bulk drug was characterised by determining, MP, Solubility, pH and FTIR spectra. Results: The weight variation, hardness and diameter, thickness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies, and stability study, tablet thickness, weight variation and drug content post compression parameters remained consistent and reproducible. All the formulations showed, almost 100 percent of drug release within 75 min. Formulations F1, F2 and F3 were prepared with 5 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F1<F2<F3. Formulations F4, F5 and F6 were prepared with 10 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F4<F5<F6. Formulations F7, F8 and F9 were prepared with 15 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F7<F8<F9. Conclusion: It is concluded that the amount of superdisintegrants decreases disintegration time of tablets, decreases wetting time, increases the cumulative % drug release causes better absorption.

scholarly journals Formulation development and evaluation of Luliconazole Topical Emulgel

2021 ◽  
pp. 79-87
Author(s):  
Naga sai divya K ◽  
T Malyadri ◽  
Ch.saibabu
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Formulation Development ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Zero Order Kinetics ◽  
Diffusion Controlled ◽  
Carbopol 940 ◽  
Vitro Release

The purpose of the present study was to develop and optimize the emulgel system for Luliconazole using different types of gelling agents: HPMCK15M, Carbopol 940, and Xanthan Gum. The prepared emulgels were evaluated in terms of appearance, pH, spreadability, viscosity, drug content, and in-vitro drug release. In-vitro release study demonstrated diffusion-controlled release of Luliconazole from formulation up to 12 hours. The drug release profile exhibited zero-order kinetics. All the prepared emulgels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and higher drug release. In the case of all evaluation parameters, carbopol based formulation showed better properties so, as a general conclusion, it was suggested that the Luliconazole emulgel formulation prepared with carbopol (F6) was the formula of choice.

scholarly journals DESIGN EXPERT SUPPORTED FORMULATION DEVELOPMENT, MATHEMATICAL OPTIMIZATION AND PREDICTABILITY STUDY OF FLOATING TABLETS OF BISOPROLOL FUMARATE

2021 ◽  
pp. 242-248
Author(s):  
SHAIKH SHAOOR AHMAD ◽  
SHAIKH SIRAJ N. ◽  
PATEL M. SIDDIK ◽  
KHALIFA MAHMADASIF YUNUS ◽  
MAKRANI SHAHARUKH I. ◽  
...  
Keyword(s):  
Drug Release ◽  
Scale Up ◽  
Mathematical Optimization ◽  
Lag Time ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Floating Tablets ◽  
Design Expert

Objective: Focus of the study was to formulate Design expert Software assisted floating tablet of Bisoprolol Fumarate. Bisoprolol Fumarate is a Beta adrenergic blocking agent, used to treat cardiac diseases favorable characters to be formulated as sustained release Gastro retentive floating tablets. Methods: Floating Tablets of Bisoprolol Fumarate were prepared by using polymers such as Polyox N 12 K and Carbapol 940 P. Formulations were prepared by using direct compression method and evaluated for various parameters like Hradness, thickness, weight variations, Floating lag time Total floating time,% drug release and Stability Study etc. Results: FTIR spectroscopic study indicates no drug-excipients interaction in the prepared formulations. Hardness or crushing strength of the tablets of all the formulation was found between 5.8 and 6.5 kg/cm2. Floating lag time of all batches is in range of 1.18±2.0 to 2.43±1.6 (minutes). All other parameters of all batches are within an acceptable range. The polymer Carbopol 940 P had the significant negative effect of on the floating lag times. The In vitro dissolution profiles of optimized A3 Floating formulation of Bisoprolol Fumarate were found to sustain drug release 99.25 % up to 12 h with floating lag time of 1.45 min; Designed formulation was stable after Stability study. Optimization study was carried out by using 32 factorial designs to fabricate formulations. Conclusion: It can be conclude that reproducible results of various parameters in this developed formulation can easily scale up. Furthermore designed formulation will be very effective for controlling blood pressure.

Formulation and In vitro Evaluation of Gastroretentive Floating Bioadhesive Tablets of Nizatidine using Factorial Design

2019 ◽  
Vol 9 (3) ◽  
pp. 234-239
Author(s):  
Vidya Sabale ◽  
Hardikkumar Chaudhari ◽  
Prafulla Sabale
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Methyl Cellulose ◽  
Lag Time ◽  
Content Uniformity ◽  
H2 Receptor Antagonist ◽  
Drug Release Profile ◽  
Drug Content ◽  
Weight Variation ◽  
Carbopol 934P

Background: The aim of the present study was to formulate and evaluate floating bioadhesive tablets of Nizatidine which is a competitive, reversible H2-receptor antagonist. Floatingbioadhesive drug delivery system exhibiting a unique combination of floatation and bioadhesion to prolong gastric residence time was prepared. Methods: Polymers used were Hydroxy Propyl Methyl Cellulose (HPMC) K15M as matrix forming water swellable release retarding polymer and carbopol 934P as bioadhesive polymer. The gas generating agents used were sodium bicarbonate and citric acid. The prepared floating bioadhesive tablets of Nizatidine were optimized by 32 factorial design to study independent variable X1 (concentration of CP 934P) and X2 (concentration of HPMC K15M) and dependent variables as floating lag time, cumulative percentage drug release at 12h and swelling index. Tablets were evaluated for various parameters such as hardness, friability, drug content, swelling behavior, floating lag time, bioadhesive strength, drug release profile and stability. Results: All the formulations passed the test for weight variation, hardness, content uniformity and showed acceptable results with respect to drug content (97.93 ± 0.57) and % friability. The tablet containing 25% HPMC K15M and 13.75 % Carbopol 934P was selected as optimized formulation which showed the floating lag time of 74.34±2.08 seconds, drug release of 97.03±0.55% at 12 h (R12h,%), S.I as 79.24±0.87 at 9 h and bioadhesive strength as 10.0023±21.47 g. Stability of the formulation was proved using stability study. Conclusion: The formulated tablets have a potential for controlled release of the drug through floatation and bioadhesion.

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