scholarly journals Cellulose Acetate 398-10 Asymmetric Membrane Capsules for Osmotically Regulated Delivery of Acyclovir

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Alka Sonkar ◽  
Anil Kumar ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Cellulose Acetate ◽  
Asymmetric Membrane ◽  
Pore Former ◽  
Independent Variables ◽  
Wet Process ◽  
Zero Order Kinetics ◽  
Phase Inversion Technique ◽  
Sem Micrograph

The study was aimed at developing cellulose acetate asymmetric membrane capsules (AMCs) of acyclovir for its controlled delivery at the absorption site. The AMCs were prepared by phase inversion technique using wet process. A 23 full factorial design assessed the effect of independent variables (level(s) of polymer, pore former, and osmogen) on the cumulative drug release from AMCs. The buoyant optimized formulation F7 (low level of cellulose acetate; high levels of both glycerol and sodium lauryl sulphate) displayed maximum drug release of 97.88±0.77% in 8 h that was independent of variation in agitational intensity and intentional defect on the cellulose acetate AMC. The in vitro data best fitted zero-order kinetics (r2=0.9898). SEM micrograph of the transverse section confirmed the asymmetric nature of the cellulose acetate capsular membrane. Statistical analysis by Design Expert software indicated no interaction between the independent variables confirming the efficiency of the design in estimating the effects of variables on drug release. The optimized formulation F7 (desirability = 0.871) displayed sustenance of drug release over the drug packed in AMC in pure state proving the superiority of osmotically active formulation. Conclusively the AMCs have potential for controlled release of acyclovir at its absorption site.

3 (2) Factorial Design Assisted Crushed Puffed Rice-HPMC-Chitosan based Hydrodynamically Balanced System of Metoprolol Succinate

2020 ◽  
Vol 10 (3) ◽  
pp. 237-249
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Batch Size ◽  
Metoprolol Succinate ◽  
Zero Order Kinetics ◽  
Two Factors ◽  
Puffed Rice ◽  
Model Drug

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.

Mesoporous Silica Nanoparticles of Hydroxyurea: Potential

2020 ◽  
Vol 10 ◽  
Author(s):  
Kumar Nishchaya ◽  
Swatantra K.S. Kushwaha ◽  
Awani Kumar Rai
Keyword(s):  
Drug Release ◽  
Silica Nanoparticles ◽  
Mesoporous Silica Nanoparticles ◽  
Release Kinetics ◽  
Average Particle Size ◽  
Silica Nanoparticle ◽  
Average Particle ◽  
Independent Variables ◽  
Lower Temperature

Background: Present malignant cancer medicines has the advancement of magnetic nanoparticles as delivery carriers to magnetically accumulate anticancer medication in malignant growth tissue. Aim: In the present investigation, a silica nanoparticles (MSNs) stacked with hydroxyurea were combined and was optimized for dependent and independent variables. Method: In this study, microporous silica nanoparticle stacked with neoplastic medication had been prepared through emulsification followed with solvent evaporation method. Prepared MSNs were optimized for dependent and independent variables. Different formulations were prepared with varying ratio of polymer, lipid and surfactant which affects drug release and kinetics of drug release pattern. The obtained MSNs were identified by FTIR, SEM, drug entrapment, in-vitro drug release, drug release kinetics study, stability testing in order to investigate the nanoparticle characteristics. Results: The percentage drug entrapment of the drug for the formulations F1, F2, F3, was found to be 27.78%, 65.52% and 48.26%. The average particle size for F2 formulation was found to be 520 nm through SEM. The cumulative drug release for the formulations F1, F2, F3 was found to be 64.17%, 71.82% and 32.68%. The formulations were found to be stable which gives controlled drug delivery for 6 hours. Conclusion: From the stability studies data it can be culminated that formulations are most stable when stored at lower temperature or in refrigerator i.e. 5˚C ± 3˚C. It can be concluded that MSN’s loaded with hydroxyurea is a promising approach towards the management of cancer due to its sustained release and less side effects.

DEVELOPMENT AND EVALUATION OF MODIFIED RELEASE MATRIX TABLETS OF MILNACIPRAN HCL USING MELT GRANULATION TECHNIQUE

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (02) ◽  
pp. 68-71
Author(s):  
N. C Ratnakara ◽  
◽  
M. C. Gohel
Keyword(s):  
Drug Release ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Modified Release ◽  
Independent Variables ◽  
Dependent Variables ◽  
Formulation Parameters ◽  
Predicted Values ◽  
Melt Granulation

The objective of the present study was to identify critical formulation parameters affecting the drug release from modified release wax matrix tablet of milnacipran hydrochloride employing the concept of design of experiments.The optimized amount of Compritol 888 ATO(intragranular) (X1), lactose (X2) and Compritol 888ATO (extragranular)(X3) were determined employing simplex latticedesign. The tablets were prepared using melt granulation technique. The in vitro drug release study was carried out in an acidic medium (pH 1.2) for 2 h and thereafter the dissolution study was conducted in phosphate buffer (pH 6.8).The selected dependent variables were the cumulative percentage of milnacipran hydrochloride dissolved at 1 (Y1), 8 (Y8), 16 (Y16) and 24 h (Y24). Mathematical models, correlating the independent variables with dependent variables were evolved. Optimization was performed for the three independent variables using the stated target ranges; Y1≤20%; Y8=45±5%; Y16=72±5%; Y24=100%. The optimized amounts of Compritol ATO888 (intragranular)(X1), lactose (X2) and Compritol 888ATO (extragranular)(X3), were found to be 60, 55 and 30 mg, respectively.The optimized formulation showed a release profile that was close to the predicted values. The drug was released by anomalous diffusion from the optimized formulation. Compritol 888ATO (intragranular) (X1), lactose (X2) and Compritol 888ATO(extragranular) (X3) were identified as critical variables.

scholarly journals Ranitidine Loaded Biopolymer Floats: Designing, Characterization, and Evaluation

2017 ◽  
Vol 2017 ◽  
pp. 1-12
Author(s):  
Abdul Karim ◽  
Muhammad Ashraf Shaheen ◽  
Tahir Mehmood ◽  
Abdul Rauf Raza ◽  
Musadiq Aziz ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Lag Time ◽  
Zero Order ◽  
Release Profile ◽  
Drug Release Profile ◽  
Independent Variables ◽  
Zero Order Kinetics ◽  
Model Drug ◽  
Predicted Values

The float formulation is a strategy to improve the bioavailability of drugs by gastroretentive drug delivery system (GRDDS). A drug delivery model based on swellable and reswellable low density biopolymers has been designed to evaluate its drug release profile using ranitidine (RNT) as a model drug and formulations have been prepared utilizing 32factorial designs. The drug release (DR) data has been subjected to various kinetic models to investigate the DR mechanism. A reduction in rate has been observed by expanding the amounts of PSG and LSG parts, while an expansion has been noted by increasing the concentration of tragacanth (TG) and citric acid (CA) with an increment in floating time. The stearic acid (SA) has been used to decrease the lag time because a decrease in density of system was observed. The kinetic analysis showed that the optimized formulation (S4F3) followed zero-order kinetics and power law was found to be best fitted due to its minimum lag time and maximum floating ability. The resemblance of observed and predicted values indicated the validity of derived equations for evaluating the effect of independent variables while kinetic study demonstrated that the applied models are feasible for evaluating and developing float for RNT.

scholarly journals FORMULATION AND IN VITRO CHARACTERISATION OF SOYBEAN OIL-HPMCK4M BASED BIGEL MATRIX FOR TOPICAL DRUG DELIVERY

2019 ◽  
pp. 33-38
Author(s):  
SHUBHAM MUKHERJEE ◽  
SUTAPA BISWAS MAJEE ◽  
GOPA ROY BISWAS
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Soybean Oil ◽  
Skin Permeation ◽  
Topical Drug Delivery ◽  
Zero Order Kinetics ◽  
Wide Range ◽  
Span 60 ◽  
Hydrophilic Gel

Objective: Hydrogels with scope for utilization in numerous fields possess limited applications due to problems in incorporating wide range of drugs and crossing the lipophilic barrier of the skin. Attempts to overcome these problems by developing organogel hold drawbacks. Challenges posed by drug lipophilicity or skin permeation can be solved by developing bigel formed via combination of lipophilic and hydrophilic gel phases in a definite proportion. The objective of the present study is to formulate and characterize matrix type bigel of soybean oil and HPMCK4M for topical drug delivery. Methods: Four batches of bigels were developed with two organogel formulations of soybean oil containing 20 and 22% w/v Span 60. Both organogels and bigels were examined for compatibility by FTIR spectroscopy, hemocompatibility and characterized for physical appearance, pH, rheological behavior and in vitro drug release pattern. Results: FTIR study confirmed compatibility between paracetamol and components of organogel or bigel. The oily feel of organogels disappeared with bigels which possessed a creamy and smooth texture. Pseudoplastic behaviour was confirmed by Ostwald-de wale power-law model in both organogels and bigels. Improved drug release was observed in bigel (BG1) formulation containing 3%w/v HPMCK4M and soybean oil based organogel with 20% w/v Span 60 as compared to the corresponding organogel (OG1). Organogels were foundto follow either zero-order kinetics (OG1) or Korsmeyer-Peppasmodel (OG2) while the formation of matrix was exhibited in bigels with drug diffusion predominantly of non-Fickian type. Conclusion: Therefore, bigels of soybean oil based organogel with HPMCK4M hydrogel formed gel matrix demonstrating improved drug release for topical application compared to organogel.

scholarly journals Development and Optimization of Osmotically Controlled Asymmetric Membrane Capsules for Delivery of Solid Dispersion of Lycopene

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Nitin Jain ◽  
Rashmi Sareen ◽  
Neeraj Mahindroo ◽  
K. L. Dhar
Keyword(s):  
Drug Release ◽  
Osmotic Pressure ◽  
Correlation Coefficient ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Dip Coating ◽  
Asymmetric Membrane ◽  
Independent Variables ◽  
Coating Method ◽  
Dip Coating Method

The aim of the present investigation is to develop and statistically optimize the osmotically controlled asymmetric membrane capsules of solid dispersion of lycopene. Solid dispersions of lycopene withβ-cyclodextrin in different ratios were prepared using solvent evaporation method. Solubility studies showed that the solid dispersion with 1 : 5 (lycopene : β-cyclodextrin) exhibited optimum solubility (56.25 mg/mL) for osmotic controlled delivery. Asymmetric membrane capsules (AMCs) were prepared on glass mold pins via dip coating method. Membrane characterization by scanning electron microscopy showed inner porous region and outer dense region. Central composite design response surface methodology was applied for the optimization of AMCs. The independent variables were ethyl cellulose (X1), glycerol (X2), and NaCl (X3) which were varied at different levels to analyze the effect on dependent variables (percentage of cumulative drug release (Y1) and correlation coefficient of drug release (Y2)). The effect of independent variables on the response was significantly influential. The F18was selected as optimized formulation based on percentage of CDR (cumulative drug release) of 85.63% and correlation coefficient of 0.9994. The optimized formulation was subjected to analyze the effect of osmotic pressure and agitational intensity on percentage of CDR. The drug release was independent of agitational intensity but was dependent on osmotic pressure of dissolution medium.

scholarly journals Design and Development of Controlled Porosity Osmotic Pump Tablets of Zidovudine Using Sodium Chloride as Osmogen for the Treatment of Aids

2019 ◽  
Vol 4 (1) ◽  
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Concentration Effect ◽  
Membrane Thickness ◽  
Pore Former ◽  
Permeable Membrane ◽  
Agitation Intensity ◽  
Controlled Porosity

The present study investigates the feasibility of the design and develops controlled porosity osmotic pump (CPOP) tablets to prolong the drug release of an antiretroviral drug zidovudine of 600mg once daily. Five formulations (ZS1to ZD5) were prepared by wet granulation method using various excipients. The CPOP consisted of an osmotic core coated with a micro porous membrane made up of cellulose acetate, poly ethylene glycol and sorbitol as in situ micro pore former. The prepared tablets were evaluated for pre compression parameters, post compression parameters, in vitro drug release study, Fourier Transform Infrared Spectroscopy (FTIR) study, Differential Scanning Calorimetry (DSC) study and scanning electron microscopy (SEM) study. The formulation variables such as effect of osmogen concentration, effect of pore former concentration, effect of membrane thickness of semi permeable membrane were evaluated for drug release characteristics. For the optimized formulation (ZS4) effect of osmotic pressure, effect of pH and effect of agitation intensity was evaluated. The in vitro release kinetics were analyzed for different batches by different pharmacokinetic models such as zero order, first order, Higuchi, Korsmeyer-Peppas and Hixson-Crowell model. The result of optimized formulation releases drug up to 16 hrs in a controlled manner and follows Higuchi kinetics and which is independent of the pH and agitation intensity. The optimized formulation was found to be stable up to 3 months when tested for stability study at 40±2ºC/ 75±5% RH

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 Oleic Acid Based Emulgel for Topical Delivery of Ofloxacin

2019 ◽  
Vol 9 (4-A) ◽  
pp. 183-190
Author(s):  
A. Manaswitha ◽  
P. V. L. D. Sai Swetha ◽  
N.K.D. Devi ◽  
K. Naveen Babu ◽  
K. Ravi Shankar
Keyword(s):  
Oleic Acid ◽  
Drug Release ◽  
Ph Value ◽  
Liquid Paraffin ◽  
Tween 80 ◽  
Gelling Agent ◽  
Compatibility Study ◽  
Zero Order Kinetics ◽  
Carbopol 940

The objective of the present study is to formulate and evaluate ofloxacin emulgel. Emulgel formulations of ofloxacin were prepared using different concentrations of gelling agent’s Carbopol-940 and Xanthum gum. Tween-80 and span-80 were used as emulsifiers and propylene glycol as a humectant in the preparation of emulgel. The effect of the concentration of gelling agent on the drug release from the prepared emulgel was investigated. The compatibility study was conducted using Fourier-transform infrared (FTIR). The formulated emulgel was characterized by their physical appearance, pH determination, viscosity, spreadability, drug content, microbial test and in vitro diffusion study. FTIR indicated that the drug and excipients used in the study are compatible with each other. All the prepared formulations showed acceptable physical properties, homogeneity, consistency, spreadability, viscosity, and pH value. Drug release from all the formulations depended upon the concentration of the polymer used. As the concentration of Carbopol 940 increased the spreadability and drug release was found to be decreased. Emulgels formulated with oleic acid gave a much higher release rate of ofloxacin than emulgels formulated with liquid paraffin. The release of drug from all the emulgels prepared followed Zero-order kinetics. The linear Higuchi plots indicated that the drug release from all the emulgels prepared followed diffusion kinetics. Emulgel formulated with oleic acid exhibited greater flux when compared with those formulated with liquid paraffin. The formulations were found to be stable during stability testing. It can be concluded that Carbopol 940 and oleic acid are recommended for the formulation and preparation of Ofloxacin emulgels for topical drug delivery. Key words: Ofloxacin, Emulgel, Spreadibility, Zone of inhibition.

Formulation and Evaluation of Isabgol and Liquorice Based Nutraceuticals Floating Tablets for Management of Gastric Ulcer

2020 ◽  
Vol 01 ◽  
Author(s):  
Ritesh Kumar Tiwari ◽  
Lalit Singh ◽  
Shashi Verma ◽  
Vijay Sharma
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Magnesium Stearate ◽  
Gastric Ulcers ◽  
Physical Parameters ◽  
Floating Tablets ◽  
Zero Order Kinetics ◽  
Liquorice Extract ◽  
Tablet Formulations

Background: Floating tablets extend drug residence time, enhance bioavailability and promote the delivery of local drugs to the stomach. With this objective, floating tablets were prepared for the treatment of gastric ulcers containing aqueous extract of liquorice and Isabgol. Methods: Tablets containing HPMC K100M (hydrophilic polymer), liquorice extract, sodium bicarbonate (gas generating agent), talc, and magnesium stearate were prepared using direct compression method. Physical parameters of formulations such as diameter, thickness, hardness, friability, weight uniformity, drug content, buoyancy time, dissolution, and mechanism for drug release, were assessed. The formulations have been optimized based on buoyancy time and in- vitro drug release. Results: The diameter of all formulations was in the range 11.310-11.833 mm; thickness was in the range 4.02-4.071 mm. The hardness ranged from 3.1 to 3.4 kg/cm. All formulations passed the USP requirements for friability and uniformity of weight. All tablet formulations had a buoyancy period of less than 5 min and throughout the research, the tablet stayed in floating condition. All tablet formulations were accompanied in drug discharge by zero-order kinetics and model Korsemeyer-Peppas. Conclusion: It was discovered that the optimized formulation was F7, which released 98.5 percent of the drug in 8 hr. invitro, while the buoyancy time was 3.5 min. For gastroretentive drug delivery systems, formulations containing Isabgol, sodium bicarbonate and HPMC K100 M in combination may be promising.

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