scholarly journals Optimization of Hydroxy Propyl Methyl Cellulose and Carbomer In Diltiazem Hydrochloride Mucoadhesive Buccal Film

2021 ◽  
Author(s):  
Lina Winarti ◽  
Bagus Tri Laksono ◽  
Lusia Oktora Ruma Kumala Sari
Keyword(s):  
Residence Time ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Release Mechanism ◽  
Diltiazem Hydrochloride ◽  
Statistical Parameters ◽  
Dissolution Model ◽  
Diltiazem Hcl ◽  
Film Characteristics ◽  
Pass Metabolism

Diltiazem hydrochloride (HCl) is a category of calcium channel blocker used as an antihypertensive agent. Diltiazem HCl is a low bioavailable drug due to high first-pass metabolism and a short half-life (3-5 hours); hence mucoadhesive buccal film was made to overcome this weakness. Bioavailability of Diltiazem HCl increase if the buccal preparations can contact the mucosa for a sufficient time. Therefore, in this study, two polymers are combined to obtain good film characteristics, especially residence time and mucoadhesive strength. This study was aimed to optimize Hydroxy Propyl Methyl Cellulose (HPMC) and Carbomer's amount in Diltiazem HCl mucoadhesive buccal film. The formulas were prepared by the solvent casting method and optimized with design expert software. The release kinetics and mechanism were evaluated using DDSolver program. The optimum amount of polymer obtained from optimization was 40 mg of HPMC and 10 mg of Carbomer. The optimum formula's swelling index was 4.18. The mucoadhesive strength was 53.07 gF, and the mucoadhesive residence time was 529.33 min. The FTIR spectra showed there was no interaction between Diltiazem HCl and other excipients. Thus it did not disturb the therapeutic effect. Based on the DDSolver statistical parameters and curve-fitting, the dissolution model of Diltiazem HCl from buccal mucoadhesive film follows Korsmeyer-Peppas. The release exponent (n) is 0.55, which shows a non-fickian/anomalous diffusion release mechanism. These mechanisms represent drug release controlled by a combination of diffusion and erosion.

scholarly journals Optimasi Hidroksipropil Metilselulosa dan Polivinil Pirolidon dalam Sediaan Mucoadhesive Buccal Film Diltiazem Hidroklorida

2021 ◽  
Vol 9 (1) ◽  
pp. 9
Author(s):  
Lusia Oktora Ruma Kumala Sari ◽  
Septi Sudianingsih ◽  
Yudi Wicaksono
Keyword(s):  
Residence Time ◽  
Channel Blockers ◽  
Active Function ◽  
First Pass Metabolism ◽  
First Pass ◽  
Zero Order Release ◽  
Optimum Formula ◽  
Diltiazem Hcl ◽  
Release Model ◽  
Pass Metabolism

Diltiazem HCl is a class of benzodiazepine calcium channel blockers used to treat angina pectoris, arrhythmias, and hypertension. Diltiazem HCl improves first-pass metabolism, a short half time of 3-5 hours, and bioavailability of diltiazem for oral administration of about 40%. Mucoadhesive buccal film diltiazem HCl releases the drug to the buccal mucosa, so the first pass metabolism can be avoided because of its absorption through the venous system that flows from the cheek. This study aimed to study HPMC polymers and polyvinyl pyrrolidone (PVP) polymers on swelling index, residence time, mucoadhesive strength of mucoadhesive buccal film diltiazem HCl, FTIR, and drug release. The prepared film was evaluated for swelling index, mucoadhesive strength, and mucoadhesive residence time. The optimal amount for HPMC was 35 mg, and PVP was 15 mg. The combination of polymers with this amount can produce a swelling index was 3,00, mucoadhesive strength was 41,87 gF, and mucoadhesive residence time was 330,66. FTIR test indicated that there was no interaction between active function clusters of Diltiazem HCl and other excipients. The release of the optimum formula in the 360th minute was about 97.847%, following in the zero-order release model and Higuchi.

scholarly journals Release Kinetics Study of Azithromycin from Bi-layered Tablets

2017 ◽  
Vol 20 (1) ◽  
pp. 54-63
Author(s):  
FM Shah Noman Ul Bari ◽  
Muhammad Rashedul Islam ◽  
Md Mizanur Rahman Moghal ◽  
Israt Jahan Ira
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Pharmaceutical Journal ◽  
High Viscosity ◽  
Release Mechanism ◽  
Low Viscosity ◽  
Release Studies ◽  
Vitro Release

The objective of this study was to analysis in vitro release kinetics of Azithromycin from bi-layer tablets prepared by direct compression using high viscosity to low viscosity grades of hydroxypropyl methyl cellulose (HPMC K15M, HPMC K4M, HPMC 50 cps), Carbopol 934p and Carbopol 974p. In addition, it also includes evaluating the effect of formulation variables like polymer proportion and polymer viscosity on the release of Azithromycin. In vitro release studies were performed using USP Type-II (Rotating paddle method) at 100 rpm. The dissolution medium consisted of 0.1N HCl (900 ml) for the first 2 hr and the phosphate buffer (pH 6.0) from 3rd to 10th hour. From twenty five different formulations (F-1 to F-25) based on polymer variation, model-dependent and independent methods were used for data analysis and the best results were observed for HPMC 50cps in Korsmeyer- Peppas (R2=0.995 on F-23) kinetic model. The release mechanism of all formulations was Fickian.Bangladesh Pharmaceutical Journal 20(1): 54-63, 2017

scholarly journals Development and Evaluation of Mouth Dissolving Films of Amlodipine Besylate for Enhanced Therapeutic Efficacy

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
K. M. Maheswari ◽  
Pavan Kumar Devineni ◽  
Sravanthi Deekonda ◽  
Salma Shaik ◽  
Naga Pravallika Uppala ◽  
...  
Keyword(s):  
Therapeutic Efficacy ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Vinyl Pyrrolidone ◽  
Release Mechanism ◽  
Amlodipine Besylate ◽  
Disintegration Time ◽  
Dissolution Properties ◽  
Pvp K30

The present investigation was undertaken with an objective of formulating mouth dissolving films (MDFs) of Amlodipine Besylate (AMLO) to enhance convenience and compliance of the elderly and pediatric patients for better therapeutic efficacy. Film formers like hydroxy propyl methyl cellulose (HPMC) and methyl cellulose (MC) along with film modifiers like poly vinyl pyrrolidone K30 (PVP K30), and sodium lauryl sulphate (SLS) as solubilizing agents were evaluated. The prepared MDFs were evaluated for in vitro dissolution characteristics, in vitro disintegration time, and their physicomechanical properties. All the prepared MDFs showed good mechanical properties like tensile strength, folding endurance, and % elongation. MDFs were evaluated by means of FTIR, SEM, and X-RD studies. MDFs with 7.5% (w/w) of HPMC E3 gave better dissolution properties when compared to HPMC E5, HPMC E15, and MC. MDFs with PVP K30 and SLS gave superior dissolution properties when compared to MDFs without PVP K30 and SLS. The dissolution properties of MDFs with PVP K30 were superior when compared to MDFs with SLS. In the case of F3 containing 7.5% of HPMC E3 and 0.04% of PVP K30, complete and faster release was observed within 60 sec when compared to other formulations. Release kinetics data reveals diffusion is the release mechanism.

scholarly journals Formulation and Evaluation of Chlorpheniramine Maleate Mouth Dissolving Films

2019 ◽  
Vol 9 (1-s) ◽  
pp. 244-251 ◽  
Author(s):  
D Teja ◽  
E Jasvanth ◽  
B Mounika ◽  
Buchi N Nalluri
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
The Elderly ◽  
Physicomechanical Properties ◽  
Vinyl Pyrrolidone ◽  
Release Mechanism ◽  
Chlorpheniramine Maleate ◽  
Poly Ethylene ◽  
Poly Vinyl Pyrrolidone

The present investigation was aimed at preparation and evaluation of mouth dissolving films (MDFs) of an anti-histamine drug, Chlorpheniramine Maleate (CPM) to enhance convenience and compliance to the elderly and paediatric patients. The MDFs were prepared using wet film applicator and evaluated for physicochemical and physicomechanical properties. MDFs were prepared with 0.6% and 0.8% w/w CPM. The MDFs with 0.8% w/w drug load showed re-crystallisation within 10 days, while the MDFs with 0.6% w/w CPM load were transparent with no re-crystallization. The effect of film formers, film thickness, film modifiers, saliva stimulating and soothing agents on the physicomechanical properties and CPM release from MDFs were evaluated. MDFs casted at 30mil thickness containing poly ethylene glycol (PEG-400) as plasticizer showed superior CPM release rates along with good physicomechanical properties. MDFs with hydroxy propyl methyl cellulose (HPMC) E3 as film former gave superior CPM release rate when compared to E5 and E15 formulations. MDFs with poly vinyl pyrrolidone K30 (PVPK30) gave superior drug release properties when compared to MDFs without PVP K30. The MDFs with citric acid (CA) and xylitol gave superior CPM release than the other MDFs. Release kinetics data reveals diffusion as drug release mechanism.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF CONTROLLED RELEASE FAMOTIDINE MATRIX TABLETS CONTAINING COMPLEXES

2017 ◽  
Vol 9 (4) ◽  
pp. 38
Author(s):  
Shabnam Ain ◽  
Babita Kumar ◽  
Kamla Pathak
Keyword(s):  
Controlled Release ◽  
Polymer Blend ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Zero Order ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Cyclodextrin Complex ◽  
Controlled Release Tablets

Objective: The aim of the present study was to formulate the controlled release (CR) tablets of famotidine-cyclodextrin complexes to make the feasibility of complex in CR tablets and to access the kinetic of drug release mechanismMethods: In this work the solubility study of famotidine was performed in various solvents like 0.1 N HCl, phosphate buffer pH 7.4 and distilled water. Enhancement of the solubility and dissolution rate of famotidine was done by complexation with cyclodextrin before formulation into controlled release tablets. Tablets were prepared in different batches by using different concentration of HPMC K15M (hydroxy propyl methyl cellulose) and EC (ethyl cellulose) polymers and polymer blend. All batches were evaluated for pre-compression and post-compression parameters. Release kinetics was analyzed using zero order, first order, higuchi, peppas and hixon-crowell model.Results: All the formulation showed compliance with Pharmacopoeial standards. Release studies indicated that polymer blend (62%HPMCK15M and 38%EC) based matrix tablets with complexed drug was able to control the release of famotidine up to 12 h. Optimized formulation F13 containing complexed drug with same polymer blend showed zero order release and the release mechanism was predominant matrix swelling with erosion.Conclusion: Results of the present study demonstrated that the drug: β-cyclodextrin complex would be a suitable candidate for preparing controlled release tablets of famotidine to improve drug solubility, flow properties and compressibility. Thus the complex used in matrix tablet is a promising approach to achieve appropriate controlled release dosage.

scholarly journals Formulation and Evaluation of Release Kinetics of Diltiazem Hydrochloride from Kollicoat SR 30 D Coated Pellets Prepared by Air Suspension Technique

1970 ◽  
Vol 43 (3) ◽  
pp. 321-332
Author(s):  
Afsana Akhter ◽  
Monzurul Amin Roni ◽  
Mohammad Shahriarul Absar ◽  
Golam Kibria ◽  
Reza-ul Jalil
Keyword(s):  
Polyvinyl Acetate ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Physical Parameters ◽  
Diltiazem Hydrochloride ◽  
Significant Difference ◽  
Kinetics Of

The purpose of the present study is to investigate the effect of polyvinyl acetate on the release kinetics of diltiazem hydrochloride from coated pellets prepared by solution and suspension layering technique. Kollicoat SR 30 D, an aqueous dispersion of polyvinyl acetate with different weight ratios was chosen to sustain the release of the drug. Drug was loaded with hydroxypropyl methyl cellulose on nonpareil seeds then coated with the Kollicoat SR 30 D. In vitro dissolution studies were carried out using USP dissolution apparatus Type-2. No significant difference was found in drug release from uncoated pellets and the pellets coated with 5% polymer load. With 10% polymer load, the initial release was minimized but from 2nd hour the release was quick-tempered. Better sustaining effect was found from 15- 20% polymer loaded pellets. The mean dissolution time was 2.5h and 4h while the polymer load was 15% and 20% respectively. Also these two cases 80% drug was released at 6h and 9h respectively. The physical parameters of the prepared pellets were also compared in this study. The release of drug from the coated pellets appeared to follow Higuchi's release kinetics.Key words: Diltiazem, Pellets, Kollicoat SR 30 D, Aqueous coating, Physical parameters, Release kinetics.DOI = 10.3329/bjsir.v43i3.1147Bangladesh J. Sci. Ind. Res. 43(3), 321-332, 2008

scholarly journals OPTIMIZATION OF DILTIAZEM HYDROCHLORIDE NANOPARTICLES FORMULA AND ITS RELEASE KINETICS EVALUATION

2021 ◽  
pp. 194-199
Author(s):  
LINA WINARTI ◽  
LUSIA OKTORA RUMA KUMALA SARI ◽  
EKA DEDDY IRAWAN DWI NURAHMANTO ◽  
VIDDY AGUSTIAN ROSYIDI ◽  
LIDYA AMELIANA ◽  
...  
Keyword(s):  
Particle Size ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
Cross Linking ◽  
Release Mechanism ◽  
Prolonged Release ◽  
Ionic Gelation ◽  
Optimum Formula ◽  
Diltiazem Hcl

Objective: The purpose of this study was to determine the optimum formula of diltiazem HCl-loaded chitosan nanoparticles due to variations in the speed and duration of stirring and evaluating the release kinetics in vitro using DDSolver. Methods: The method used to prepare nanoparticles is ionic gelation. The ionic gelation method involves an ionic cross-linking between cations on the backbone of chitosan and anion, such as sodium tripolyphosphate (Na TPP).  Results: Stirring speed of 1200 rpm and stirring time of 2 h produce an optimum response. The optimum formula has an entrapment efficiency of 71.10%, a particle size of 110.2 nm, and a polydispersity index of 0.268. The dry powder of diltiazem HCl nanoparticles produced a drug loading of 66.14±1.71% and a yield of 34.07±0.73%. The FT-IR showed ionic interaction (cross-linking) between ammonium ions from chitosan and phosphate ions from Na TPP. Scanning electron microscopy (SEM) analysis showed a particle size of 150 µm, a spherical shape, and rough surface morphology. In vitro release profiles indicated prolonged release, which follows the Korsmeyer Peppas model.  Conclusion: It can be concluded that increasing the speed and duration of stirring will improve drug entrapment and reduce the particles size variation. The dry nanoparticles release mechanism is by diffusion and matrix erosion.

scholarly journals Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

2011 ◽  
Vol 61 (2) ◽  
pp. 217-226 ◽  
Author(s):  
Komuravelly Someshwar ◽  
Kalyani Chithaluru ◽  
Tadikonda Ramarao ◽  
K. Kumar
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Floating Tablets ◽  
Gastric Residence Time

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h.

Formulation and evaluation of proniosome loaded sertaconazole nitrate for topical application

2021 ◽  
Vol 1 (2) ◽  
pp. 023-037
Author(s):  
Shailaja D ◽  
Latha K ◽  
Manasa D ◽  
Shirisha A ◽  
Padmavathi R ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Release Kinetics ◽  
Skin Irritation ◽  
Water Soluble ◽  
Ionic Surfactants ◽  
Release Mechanism ◽  
Stability Studies ◽  
Zero Order Release ◽  
Poorly Soluble

Proniosomal technology is a novel solution for poorly soluble drugs. Proniosomes are water-soluble carrier particles which are coated with non-ionic surfactants. Proniosomal gels were prepared by coacervation phase separation method using non-ionic surfactants, lipid carriers and cholesterol as a membrane stabilizer. FTIR compatibility studies revealed that the drug and excipients were compatible. All formulations were evaluated for pH, drug content, extrudability, spreadability, viscosity, in-vitro, ex-vivo, skin irritation and stability studies. Among formulations prepared, F80H1 has shown higher % EE (83.02) and least diffusion through dialysis membrane i.e., 17.68%. With ex-vivo studies, F80H1 formulation has shown highest skin deposition and lower flux of sertaconazole nitrate through the rat skin. F80H1 was selected as final optimized formulation. F80H1 exhibited good stability and SEM studies revealed that the vesicles were spherical in shape. The optimized formulation was found to follow zero order release kinetics and korsmeyer-peppas release mechanism. F80H1 found to be non-irritant and stable from skin irritation and stability studies.

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