Effect of viscosity of hydrophilic coating polymer on lag time of atenolol pulsatile press coated tablets

2014 ◽  
Vol 1 (1) ◽  
pp. 15 ◽  
Author(s):  
Rajesh A Keraliya ◽  
Madhabhai M Patel
Keyword(s):  
Drug Delivery ◽  
Lag Time ◽  
Burst Release ◽  
Pulsatile Release ◽  
Hydrophilic Coating ◽  
Coated Tablet ◽  
Viscosity Grade ◽  
Pulsatile Drug Delivery ◽  
Pulsatile Delivery ◽  
Core Tablet

A method for the development of press coated tablet of atenolol for pulsatile delivery was investigated for chronotherapy of hypertension. Effect of viscosity of Hydroxypropylcellulose (HPC) on pulsatile release of atenlol was studied by press coating atenolol core tablet using different viscosity grade HPC and varying coat weight. L-HPC, M-HPC and H-HPC viscosity garde with 75, 100 and 150 mg coat weight were press coated over atenolol core tablets to delay release of atenolol. The batches, HP1-HP9, exhibited an increase in lag time in response to increase in viscosity and coat weight. Two of the batches HP5 and HP7 have shown a burst release of atenolol after 6.5 and 6.0 h lag time respectively, which is suitable for pulsatile drug delivery of atenolol for chronotherapy of hypertension.

scholarly journals Preparation and characterization of timed drug delivery system of sumatriptan using natural polymers

2018 ◽  
Vol 27 (1) ◽  
pp. 89-99
Author(s):  
Mina Shihab Al-anbagi ◽  
Nawal A. Rajab ◽  
Yehia I.Khalil
Keyword(s):  
Drug Delivery ◽  
Circadian Rhythm ◽  
Active Pharmaceutical Ingredient ◽  
Lag Time ◽  
Natural Polymers ◽  
The Press ◽  
Coated Tablet ◽  
Pulsatile Drug Delivery ◽  
Core Tablet

Pulsatile drug delivery systems are time-controlled dosage forms which are designed to release the active pharmaceutical ingredient after a predetermined lag time to synchronize the disease circadian rhythm. A migraine shows circadian rhythm with a marked increase in attacks between 6 a.m. and 8 a.m. Sumatriptan is a selective agonist at serotonin (5-Hydroxy tryptamine1  (5-HT1))receptors, is an effective treatment for acute migraine attacks. The aim of this work is to prepare time-controlled press-coated tablet with a lag time of 5.45 hrs. Six formulas of fast dissolving core tablets and three formulas of press-coated tablets were prepared by using direct compression method using different variables to prepare core tablets which include: different types and concentrations of superdisintegrants While different concentrations of natural and synthetic polymers were utilized in the preparation of press-coated tablets. The obtained results showed that formula  F4 of core tablet, which contained 25 mg of sumatriptan, 5% w/w sodium starch glycolate and avicel PH 102 as the diluent, was the selected formula that gave the fastest and complete release of sumatriptan. Also, formula C3 of the press-coated tablet, which contained pectin: EC100 mpa.s: HPMCK15M in concentration30mg: 10mg:160mg respectively, was selected as the best coating layer since it gave 5.45  hours lag time.

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.

scholarly journals Development and evaluation of a chronotherapeutic drug delivery system of torsemide

2011 ◽  
Vol 47 (3) ◽  
pp. 593-600 ◽  
Author(s):  
Songa Ambedkar Sunil ◽  
Nali Sreenivasa Rao ◽  
Meka Venkata Srikanth ◽  
Michael Uwumagbe Uhumwangho ◽  
Kommana Srinivas Phani Kumar ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Lag Time ◽  
Delivery Systems ◽  
Burst Release ◽  
Treatment Of Hypertension ◽  
Drug Polymer Interaction ◽  
Compression Coating ◽  
Core Tablet ◽  
Polymer Interaction

The objective of this study was to prepare and evaluate chronotherapeutic drug delivery systems (ChrDDs) of torsemide. Compression coated tablets (CCT) containing torsemide in the core tablet were prepared by the compression coating technique with different grades of polyethylene oxide (PEO WSR 301 & 1105). The optimized formulations were characterised for tabletting parameters and drug polymer interaction by Fourier-Transform Infrared Spectroscopy (FTIR).The hardness of all the CCT using PEO WSR 301 & PEO WSR 1105 were in the range 6-8 kg/cm² & 5.5 to 7 kg/cm² respectively. Their friability values were <0.3%. All the CCT showed a clear lag time but finalized as per the predetermined lag time. As the amount of PEO was increased in the outer layer the drug released was delayed. The drug content of all the CCT was >99%. The FTIR studies showed no interaction throughout the process of development. Formulations of F7 and of P7 were considered optimized formulations since they yielded a predetermined lag time of 6h before burst release. Hence, these formulations can be exploited to achieve chronotherapeutic drug delivery systems of Torsemide for the treatment of hypertension at the time the patient needs it.

scholarly journals Optimization Studies on Compression Coated Floating-Pulsatile Drug Delivery of Bisoprolol

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Swati C. Jagdale ◽  
Nilesh A. Bari ◽  
Bhanudas S. Kuchekar ◽  
Aniruddha R. Chabukswar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Active Ingredient ◽  
Dosage Form ◽  
Release Kinetics ◽  
Lag Phase ◽  
Burst Release ◽  
Release Formulation ◽  
Pulsatile Drug Delivery ◽  
Core Tablet

The purpose of the present work was to design and optimize compression coated floating pulsatile drug delivery systems of bisoprolol. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. The prepared system consisted of two parts: a core tablet containing the active ingredient and an erodible outer shell with gas generating agent. The rapid release core tablet (RRCT) was prepared by using superdisintegrants with active ingredient. Press coating of optimized RRCT was done by polymer. A 32full factorial design was used for optimization. The amount of Polyox WSR205 and Polyox WSR N12K was selected as independent variables. Lag period, drug release, and swelling index were selected as dependent variables. Floating pulsatile release formulation (FPRT) F13 at level 0 (55 mg) for Polyox WSR205 and level +1 (65 mg) for Polyox WSR N12K showed lag time of 4 h with >90% drug release. The data were statistically analyzed using ANOVA, andP<0.05was statistically significant. Release kinetics of the optimized formulation best fitted the zero order model.In vivostudy confirms burst effect at 4 h in indicating the optimization of the dosage form.

Chronomodulated Delivery of Pantoprazole for Nocturnal Hyperacidity

2015 ◽  
Vol 8 (4) ◽  
pp. 3038-3044
Author(s):  
Mahalakshmi P ◽  
Suriyaprakash T N K ◽  
S. Lakshmana Prabu
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Lag Time ◽  
Delivery Systems ◽  
Burst Release ◽  
Dependent Manner ◽  
Compression Technique ◽  
Pulsatile Drug Delivery

The objective of this work was to design and evaluate an oral site-specific, pulsatile drug delivery system containing Pantoprazole sodium which can be targeted to colon in a pH and time dependent manner, to modulate the drug level in synchrony with the circadian rhythm of nocturnal hyperacidity. Five different composition of Core tablets were prepared by direct compression technique. Based on the release studies of core tablets, nine different compositions of press coated tablets were prepared and analyzed. The press coated tablet further coated by using five different proportions of Eudragit RS PO for providing consistent, reproducible chronomodulated release profile. Formulation FPC3 is more suitable among the formulations to design pulsatile release formulations of pantoprazole sodium for 6 hours lag time. After this lag time burst release was observed which exhibited sigmodial release pattern and that was considered to be an ideal for the pulsatile drug delivery system. The chronomodulated drug delivery systems for pantoprazole sodium for the treatment of hyperacidity was successfully developed and the release of the drug was sharp and complete after the lag time which is necessary for any pulsatile drug delivery systems.   

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.

scholarly journals DESIGN AND DEVELOPMENT OF FLOATING PULSATILE DRUG DELIVERY OF LOSARTAN POTASSIUM

2020 ◽  
pp. 218-227
Author(s):  
ANIL KUMAR J. SHINDE ◽  
NIDHI S. PATIL ◽  
TRUPTI S. JADHAV ◽  
HARINATH N. MORE
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Lag Time ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Lag Phase ◽  
Burst Release ◽  
Distal Small Intestine ◽  
Pulsatile Drug Delivery

Objective: The objective of the present investigation was to the development of floating pulsatile drug delivery system of Losartan potassium (LP) tablets for obtaining no drug release during floating followed by pulsed, rapid drug release to achieve chronotherapeutic release. In hypertension, the risk of getting heart attacks early in the morning is high and therefore, there was need to develop drug delivery, which will release drugs at morning hours and provide efficacious therapy. LP is a short biological half-life (1.5-2.5h) and readily absorbed from the stomach and upper gastrointestinal tract. Methods: Tablet formulation was prepared by press coating of rapid release core tablets and core tablets were further top coated with a buoyant layer of HPMC K4M and sodium bicarbonate. Various grades of HPMC polymer (E5/E15/E50) were used for the pulsatile coating layer. The developed formulations were characterized for physical characteristics, floating lag time, floating time, release lag time, drug content, swelling index, in vitro dissolution studies, DSC and XRD. Results: The FTIR and DSC studies predicted that there was no chemical interaction between drug and excipients. The core tablet coated with HPMC E50 showed a high swelling index and release the drug 97.60±1.2% at 6h. Buoyant layer with 80 mg HPMC K4M and 25 mg sodium bicarbonate gave satisfactory floating lag time. Conclusion: The system showed an excellent lag phase followed by burst release in the distal small intestine, which gives site and time-specific delivery of LP acting as per chronotherapy for treatment of hypertension.

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.

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.

scholarly journals Applicability of Gum Karaya in the Preparation and in Vitro Evaluation of Losartan Potassium as Chronotherapeutic Drug Delivery System

2015 ◽  
Vol 7 (1-2) ◽  
pp. 65-74
Author(s):  
K. Latha ◽  
V. V. Srikanth ◽  
S. A. Sunil ◽  
N. R. Srinivasa ◽  
M. U. Uhumwangho ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Tensile Strength ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
Gum Karaya

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively.  All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively.  The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension. 

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