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.

scholarly journals Novel Floating Pulsatile Approach for Chronotherapeutic Release of Indomethacin

1970 ◽  
Vol 6 (1) ◽  
pp. 37-41
Author(s):  
Shaji Jessy ◽  
Patole Vishal
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Small Intestine ◽  
Drug Release ◽  
Basic Medium ◽  
Lag Phase ◽  
Burst Release ◽  
Distal Small Intestine ◽  
Pulsatile Drug Delivery ◽  
Time Specific

The main objective of the present study was to develop a multiple-unit, floating-pulsatile drug delivery system for obtaining no drug release during floating and in the proximal small intestine followed by pulsed, rapid drug release in distal small intestine to achieve chronotherapeutic release of indomethacin. The system developed consists of drug containing core pellets prepared by extrusion-spheronization process, which were coated with an inner pH-dependent layer of Eudragit S100 and outer effervescent layer of sodium bicarbonate and HPMC K100M. Pellets showed instantaneous floating with no drug release in acidic medium followed by pulsed drug release in basic medium. Concentration of HPMC K100M and layering level of effervescent agent significantly affected performance of pellets. The system showed excellent lag phase followed by burst release in the distal small intestine which gives site and time specific delivery of indomethacin acting as per chronotherapy of rheumatoid arthritis. Key words: Floating-pulsatile drug delivery, Chronotherapeutic release, Indomethacin, Pellets, Rheumatoid arthritis. Dhaka Univ. J. Pharm. Sci. 6(1): 37-41, 2007 (June) The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

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.

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 Characterization of Mucoadhesive Microcapsules of Gliclazide with Natural Gums

1970 ◽  
Vol 4 (1) ◽  
pp. 38-48 ◽  
Author(s):  
Santhosh Kumar Mankala ◽  
Nishanth Kumar Nagamalli ◽  
Ramakrishna Raprla ◽  
Rajyalaxmi Kommula
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Guar Gum ◽  
Release Kinetics ◽  
Insulin Dependent Diabetes Mellitus ◽  
Dependent Diabetes Mellitus ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
Release Formulation

Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mellitus. Among people who are suffering from long term disorders, the major were categorized under diabetes so, a dosage form is needed to provide continuous therapy with high margin of safety & such dosage form can be achieved by microencapsulation. Gliclazide microspheres with sodium alginate (coat material, gum kondagogu, gum guar and xanthan gum (mucoadhesive agents) were prepared by orifice-ionic gelation and emulsification ionic gelation techniques varying concentrations (1:0.25, 1:0.5, 1:0.75 and 1:1). Formulations were then evaluated for surface morphology, particle shape, Carr’s index, microencapsulation efficiency, drug release, mucoadhesion studies. Compatibility studies were performed by FTIR, DSC, and XRD techniques and no interactions were found between drug and excepients used. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400-600μm. % drug content and encapsulation efficiency found in the range of 55%-68% and, 86.23%-94.46% respectively. All microspheres showed good mucoadhesive property in in-vitro wash of test. In vitro drug release studies showed that the guar gum has more potentiality to retard the drug release compared to other gums and concentrations. Drug release from the microspheres was found slow following zero order release kinetics with non-fickian release mechanism stating release depended on the coat: core ratio and the method employed. The concentration of 1:1 of SA: GG (EMG 4) found suitable for preparing the controlled release formulation of gliclazide stating emulsification gelation technique is the best among followed.   Key words: Gliclazide; Natural gums; orifice ionic gelation technique; emulsification ionic gelation technique DOI: http://dx.doi.org/10.3329/sjps.v4i1.8865 SJPS 2011; 4(1): 38-48

Combine Drug Delivery of Thymoquinone-Doxorubicin by Cockle Shellderived pH-sensitive Aragonite CaCO3 Nanoparticles

2020 ◽  
Vol 10 (4) ◽  
pp. 518-533 ◽  
Author(s):  
Kehinde M. Ibiyeye ◽  
Abu B.Z. Zuki ◽  
Norshariza Nurdin ◽  
Mokrish Ajat
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Calcium Carbonate ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Ph Sensitive ◽  
Multiple Drug ◽  
Burst Release ◽  
Cockle Shell

Background: Cockleshell-derived aragonite calcium carbonate nanoparticles were prepared by the top-down approach for combine delivery of two types of drugs. Objective: The aim of this study was to synthesize and characterize thymoquinone-doxorubicin loaded cockle shell-derived aragonite calcium carbonate nanoparticle. Aragonite calcium carbonate nanoparticles encapsulating thymoquinone and doxorubicin alone were also prepared. Methods: The blank and drug-loaded nanoparticles were characterized by field emission scanning electron microscopy, transmission electron microscopy, Zeta potential, Fourier transformed infrared and X-ray diffraction. Drug delivery properties, in vitro drug release study at pH 7.4, 6 and 4.8, and effect of blank nanoparticles on MCF10A, 3T3, MDA MB231 cells were also analyzed. Results: The blank and drug-loaded nanoparticles were pleomorphic and their sizes varying from 53.65 ± 10.29 nm to 60.49 ± 11.36 nm with an overall negative charge. The entrapment efficiency of thymoquinone and doxorubicin were 41.6 and 95.8, respectively. The FTIR showed little alteration after loading thymoquinone and doxorubicin while XRD patterns revealed no changes in the crystallizations of nanoparticles after drug loading. The drug release kinetics of doxorubicin and thymoquinone from the nanoparticles showed a continuous and gradual release after an initial burst release was observed. At pH 4.8, about 100% of drug release was noticed, 70% at pH 6 while only 50% at pH 7.4. The cell viability was 80% at a concentration of 1000 ug/ml of blank nanoparticle. Conclusion: The cockle shell-derived pH sensitive aragonite calcium carbonate nanoparticle provides an effective and simple means of multiple drug delivery and function as a platform for pH controlled release of loaded therapeutic agents.

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 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 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.

Optimization Study to Develop Once-a-day Controlled Release Formulation of Metoclopramide with Predictable Design Space

1970 ◽  
Vol 1 (1) ◽  
pp. 71-76
Author(s):  
Rajesh Dubey ◽  
Udaya K. Chowdary ◽  
Venkateswarlu V.
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Design Space ◽  
Release Kinetics ◽  
Release Profile ◽  
Release Formulation ◽  
Linear Effect ◽  
Controlled Release Formulation ◽  
The Difference ◽  
Face Centered

A controlled release formulation of metoclopramide was developed using a combination of hypromellose (HPMC) and hydrogenated castor oil (HCO). Developed formulations released the drug over 20 hr with release kinetics following Higuchi model. Compared to HCO, HPMC showed significantly higher influence in controlling the drug release at initial as well as later phase. The difference in the influence can be explained by the different swelling and erosion behaviour of the polymers. Effect of the polymers on release was optimized using a face-centered central composite design to generate a predictable design space. Statistical analysis of the drug release at various levels indicated a linear effect of the polymers’ levels on the drug release. The release profile of formulations containing the polymer levels at extremes of their ranges in design space was found to be similar to the predicted release profile

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

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