scholarly journals Formulation and Evaluation of Bio-adhesive Pulsatile Drug Delivery System of Telmisartan

2020 ◽  
Vol 11 (2) ◽  
pp. 1282-1287
Author(s):  
Patil S. V. ◽  
Salokhe P. A. ◽  
Patil S. S. ◽  
Ustad J. Y. ◽  
Shedbale S. S.
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Early Morning ◽  
Pulsatile Drug Delivery ◽  
Hypertensive Drug ◽  
Time Specific ◽  
Core Tablet

The main objective of this study was to formulate and evaluate of Bio-adhesive pulsatile drug delivery system of Telmisartan, an anti-hypertensive drug in order to achieve better therapeutic efficacy and patient compliance. The approach of combination of bio-adhesive pulsatile formulation is suitable for gastro retention and time specific drug delivery. The study was carried by preparation of fast disintegrating core tablet followed by incorporation of core tablet to design bio-adhesive pulsatile tablet by press coating. The press coated tablet was prepared with the polymersethyl cellulose and carbopol. The formulation was evaluated for precompression and post compression parameters, lag time, drug release and bio-adhesive study. All evaluation parameters were found within limits. The lag time expected for this disease was 8 hours as need of drug release for this disease was more likely to act in early morning. The 8 hour lag time was obtained in optimized formulation which has shown muco-adhesion for the same period. Thus bio-adhesive pulsatile drug delivery system could be the best precautionary alternative for the drugs having maximum absorption in stomach and used for diseases which follows circadian rhythm.

scholarly journals FORMULATION AND EVALUATION OF PULSATILE DRUG DELIVERY SYSTEM OF SALBUTAMOL SULFATE FOR THE CHRONOTHERAPY OF ASTHMA

2018 ◽  
Vol 11 (9) ◽  
pp. 305
Author(s):  
Chiranjibi Adhikari ◽  
Gururaj S Kulkarni ◽  
Shivakumar Swamy
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Release Profile ◽  
Salbutamol Sulfate ◽  
Pulsatile Drug Delivery ◽  
Core Tablet

Objective: The main objective of the present study was to design and evaluate a time-controlled single unit oral pulsatile drug delivery system containing salbutamol sulfate for the prevention of nocturnal asthma attacks.Methods: Drug containing core tablets (C1-C10) with different composition of superdisintegrants such as sodium starch glycolate, croscarmellose sodium, and crospovidone were prepared by direct compression technique. The fast disintegrating core tablet formulation was selected, and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic and hydrophilic polymers: Ethylcellulose-20 (EC-20), hydroxypropyl methylcellulose K4M, and low substituted hydroxypropyl cellulose (L-HPC LH11). The coating polymers were selected and quantified based on in vitro lag time and drug release profile in simulated gastric and intestinal fluids.Results: Formulation C10 with 7.5% crospovidone showed least disintegrating time, i.e., 0.31 min and was selected as the best immediate release core tablet. The press-coated tablet formulation P11 having 360 mg barrier layer of EC-20 and L-HPC LH11 in ratio 14:1 over the core tablet C10 showed rapid and complete drug release nearly after 6 h lag time. Accelerated stability studies of the optimized formulation P11 indicated no significant difference in release profile after a period of 6 months.Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.

Formulation and Evaluation of Floating Pulsatile Drug Delivery System of Ibuprofen and Ranitidine Combination

2015 ◽  
Vol 8 (4) ◽  
pp. 3009-3017
Author(s):  
Behin Sundara Raj ◽  
I S R Punitha ◽  
M J Gifty
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Early Morning ◽  
In Vivo Study ◽  
Pulsatile Release ◽  
Pulsatile Drug Delivery ◽  
Core Tablet

Since rheumatoid arthritis patients experience severe pain, inflammation, and joint stiffness in the early morning hours a pulsatile drug delivery system of a suitable anti-inflammatory drug that is administered at bedtime but release the drug in the early morning would be a promising system. The objective of this work was to develop a pulsatile release tablet containing a combination of ibuprofen and ranitidine HCl from which ibuprofen gets released after a lag time of 6-7 hours. The methodology involves; analytical method development for simultaneous estimation of combination drugs, development of pulsatile release tablet and an in vivo study in rats. Lag time was controlled by coating the rapid release core tablet with different grades and concentrations of HPMC polymer. A floating gastroretentive layer was applied on top to prevent metabolism of ranitidine at the last part of the intestine. Six different formulations were prepared with three different concentrations of HPMCK4M and HPMCK100M. In vitro studies showed that the lag time increased with an increase in both concentration and viscosity of polymers. The formulation where the core tablet was coated with 100 mg of HPMCK100M had an optimum lag time of 6.3 hrs. In vivo study evaluated the ulcer protection of the formulation in four animal groups; first group remained as control, the second group received ibuprofen at a dose of 180 mg/kg, third and fourth groups received a combination of both the drugs but ranitidine in different doses. Based on this research, it can be concluded that pulsatile release of ibuprofen tablets can be successfully formulated by using HPMC polymers. The usage of ranitidine along with ibuprofen reduces the ulcerogenecity of the later.

Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Oral Dosage ◽  
Lag Phase ◽  
Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

Preparation And Evaluation Of ‘3 Cap’pulsatile Drug Delivery System Of Ramipril

2020 ◽  
Vol 18 ◽  
Author(s):  
Priyanka Kriplani ◽  
Kamla Pathak ◽  
Anil Philip
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Flow Rate ◽  
Circadian Variation ◽  
Surface Design ◽  
Pulsatile Drug Delivery ◽  
Hypertensive Drug ◽  
Time Density

Background: Chronotherapeutics, the drug delivery based on circadian rhythm, is recently gaining much attention worldwide. Various diseases like asthma, hypertension, and arthritis show circadian variation that demands time scheduled drug release for effective drug action. So, Pulsatile drug delivery system have been designed to confer preprogrammed drug delivery. Objective: In the present study, a ‘3 Cap’ pulsatile drug delivery system has been developed, optimized and characterized in order to achieve floating and pulsatile release of Ramipril. Methods: An optimal response surface design was employed to investigate the effect of isopropanol: formaldehyde vapours for varying time on drug release from the capsules. ‘3 Cap’ pulsatile drug delivery system was evaluated in terms of floating time, density, effect of gastric flow rate and type of dissolution apparatus on drug release. Results: Independent variables exhibited significant effect on the drug release of the prepared formulations. Results showed that time between the release of fractions of dose increased with increase in formaldehyde: isopropanol ratio and duration of exposure to formaldehyde vapours with no effect of gastric flow rate. Conclusion: The design results revealed that an optimum exposure of 1:2 of isopropanol: formaldehyde vapours for sixty minutes resulted in desired release of second pulse of dose after a predetermined lag time of 5 hours as desired. ‘3Cap’ system was successful in achieving floating and pulsed release of hypertensive drug opening a ‘new lease of life’ to the existing drug molecule.

Formulation and Evaluation of Modified Pulsincap as Pulsatile Drug Delivery System for Treatment of Rheumatoid Arthritis

2016 ◽  
Vol 9 (5) ◽  
pp. 3476-3487
Author(s):  
Chavda D Hiral ◽  
Sonpal N Rakshit ◽  
Paresh Prajapati A ◽  
Madhabhai M Patel
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Phosphate Buffer ◽  
Lag Time ◽  
Contour Plot ◽  
Independent Variables ◽  
Pulsatile Drug Delivery

The aim of the present study was to design and evaluate a modified pulsincap pulsatile drug delivery system of etodolac for treatment of rheumatoid arthritis. Capsule body was made water insoluble by cross linking with formaldehyde vapour. It was filled with drug, osmogen NaCl and super disintegrant sodium starch glycolate to expel the drug after predetermined lag time. A hydro gel plug made of HPMC K4M was placed in the capsule body to achieve desired drug release after lag time for chronotherapy of rheumatoid arthritis. Untreated cap was then fitted to the treated body was sealed. Entire unit was coated with 5% Eudragit S-100 to prevent variable gastric emptying. A 32 full factorial design was used for optimization in which concentration ratio of NaCl and SSG (X1), and the weight of hydrogel plug (X2) were selected as independent variables while lag time and t90% were taken as dependent variables. FTIR and DSC studies confirmed drug excipient compatibility. Developed formulation was evaluated for in-vitro drug release in pH 1.2, phosphate buffer pH 6.8 and phosphate buffer pH 7.4. Statistical analysis confirmed the significance of selected independent variables. Response surface plot and contour plot indicate augmentation of the line toward the weight of hydrogel plug factor indicating greater significance. Formulation with highest desirability containing 34.4 mg of SSG, 137.6 mg of NaCl and 48 mg of HPMC K4M plug was selected as an optimized formulation as it provided the desired lag time of 6 hours and t90% of about 477 mins. Accelerated stability study performed on optimized formulation suggested stable and viable formulation. A stable, efficient formulation modified pulsincap of Etodolac as a pulsatile drug delivery system was developed with proposed increased patient compliance and improved dosage form efficiency.

scholarly journals Formulation and In Vitro Evaluation of Compressed Coated Tablets of Simvastatin for Pulsatile Drug Delivery

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Kumari P.V. Kamala ◽  
Mounica V. ◽  
Rao Y. Srinivasa
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Guar Gum ◽  
Lag Time ◽  
Blood Cholesterol ◽  
In Vitro Dissolution ◽  
Pulsatile Drug Delivery

Pulsatile drug delivery system is one type of drug delivery system, where the delivery device is capable of releasing drugs after a predetermined time-delay (i.e. lag time). This system has a peculiar mechanism of delivering the drug rapidly and completely after a "lag time," i.e., a period of "no drug release." These systems are beneficial for drugs having high first-pass effect drugs administered for diseases that follow chrono pharmacological behavior such as drugs having specific absorption sites in GIT, targeting to colon; and cases where nighttime dosing is required. The objective of the present study was to formulate and evaluate a press coated pulsatile drug delivery system of simvastatin in order to attain a time controlled release to lower the blood cholesterol level by releasing the drug with a distinct predetermined lag time of five hrs. Simvastatin is a water insoluble drug and its absorption is dissolution rate limited. The core formulations were composed of simvastatin and disintegrants like lycoat, SSG, ludiflash in different ratios and was coated with xanthan gum, guar gum, HPMC K4M, HPMC K15M as a release modifier. Press coated tablets were evaluated for hardness, friability, drug content, and in vitro drug release. Result of in vitro dissolution study of the prepared tablet suggested that, the release of drug from press coated tablets match with chrono-biological requirement of disease.

scholarly journals Prepartion And Bio Pharmaceutical Evaluation Of Chronopharmaceutical Drug Delivery System Of Metoprolol

2021 ◽  
Vol 23 (09) ◽  
pp. 1052-1068
Author(s):  
Apollo James ◽  
◽  
Mohanraj Palanisamy ◽  
Jasmina Khanam ◽  
Mohanraj Palanisamy ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Immediate Release ◽  
Early Morning ◽  
Optimal Drug ◽  
Basic Purpose ◽  
Pulsatile Drug Delivery ◽  
Preformulation Studies

The basic purpose of constructing drug delivery systems is to design when and where the drug will be released. The episode of many biological events is really important for such knowledge. Metoprolol pulsatile drug delivery system was developed for this purpose, which can release the drug when blood pressure needs to be modulated in the early morning. The Cup and core techniques were used to build this system, which included immediate release (IR), sustained-release (SR), and a polycaprolactone plug layer. The formulation of the ingredients was facilitated by various preformulation studies. The IR and SR tablets were bilayered, with polycaprolactone entirely coating the IR layer. The IR and SR tablet release profiles were optimised for the F5 batch, which was then used to construct a pulsatile drug delivery system. Clinical trials were conducted with the prepared tablet, which included the use of BaSO4 tagged tablets for X-ray examinations. All of the findings indicated the optimal drug release of metoprolol, which can be used for individuals who are more prone to blood pressure abnormalities in the morning.

scholarly journals Recent Trends in Chronopharmaceutics, Pulsatile Drug Delivery System

2019 ◽  
pp. 41-49
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Correct Position ◽  
Unit System ◽  
Recent Trends ◽  
Osmotic System ◽  
Pulsatile Drug Delivery ◽  
Fast Release

Pulsatile Drug Delivery Systems (PDDS) are getting considerable interest in delivering a drug at the correct position, at the correct time, and in the correct quantity, thus offering temporal, spatial, and intelligent delivery with improving patient compliance. These systems are intended to meet body's biological rhythm. Here, the delivery of drugs is assisted by the rhythm of disease. The main reason for the using pulsatile drug release is when the continuous drug release is not required. A PDDS must be designed in such a way that after the lag time a complete and fast release of drugs is achieved. The article deals with various systems such as osmotic system, capsular system, single and multi-unit system based on the utilization of erodible or soluble polymer coating and using of rupturable membrane. These systems are favorable to drugs with chronopharmacological behaviors such as drugs used to treat rheumatoid arthritis, ankylosing spondylitis, and osteoarthritis. The current review paper focus on the causes for pulsatile drug delivery system design, types of illness requiring pulsatile release, classification, benefits, and restriction of this drug delivery system

scholarly journals PREPARATION AND CHARACTERIZATION OF SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ANTI-HYPERTENSIVE DRUG’’

2020 ◽  
Vol 9 (4) ◽  
Author(s):  
Anukumar E ◽  
Nagaraja T S ◽  
Yogananda R ◽  
Bharathi D R
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Release Kinetics ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Hypertensive Drug

The present work is to prepare and characterization of self nano emulsifying drug delivery system containing Anti-hypertensive drug. Losartan is a competitive antagonist and inverse agonist of angiotensin 2 receptor. The SNEDDS is prepared by Sonication method using a components of SPAN 60/Eudragit RS 100 as a surfactant, PVA as a Co-surfactant, Iso propyl alcohol as a solvent and DCM as a co-solvent. The prepared SNEDDS was evaluated for Fourier transform infrared spectroscopy, Surface morphology, particle size, zeta potential,  drug entrapment efficiency, visual assessment, self-emulsification time, Robustness to dilution, in-vitro drug release and short term stability studies. The in-vitro drug release data of all the formulations were found to be zero order over a period of 24 h and Formulation F7 shows good results for the drug release kinetics as controlled release. The stability studies data was found that there was no such difference in drug EE and in-vitro drug release.

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