scholarly journals Development and Evaluation of Salbutamol Sulphate Loaded Ethyl Cellulose Microcapsules using Emulsion Solvent Evaporation Technique

2015 ◽  
Vol 18 (2) ◽  
pp. 132-136 ◽  
Author(s):  
Md Shamsul Alam ◽  
Jakir Ahmed Chowdhury ◽  
Sams Mohammad Anowar Sadat ◽  
Md Selim Reza
Keyword(s):  
Ethyl Cellulose ◽  
In Vitro Release ◽  
Solvent Evaporation ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Salbutamol Sulphate ◽  
Evaporation Technique ◽  
Vitro Release

Ethyl cellulose (EC) microcapsules containing Salbutamol sulphate (SS) were prepared through emulsion-solvent evaporation technique. Microcapsules were compressed and in-vitro release profiles were studied from both microcapsules and their compressed matrix tablets. Different amounts of drug were added in order to obtain various drugs to polymer ratios and it was found that the size of microcapsules reduced with the increase in core loading. In the preparation of formulations, Tween 80 was used as an emulsifying or dispersing agent and light liquid paraffin (LLP) was used as oil phase. The in-vitro release of EC microcapsules was studied in distilled water at 37º ± 0.5°C. A biphasic release behavior of SS from microcapsules was observed. In case of microcapsules, an immediate release was observed but for their compressed tablet form, initially a burst effect and then slow release were observed which was extended for 8 hours. In order to further investigate the type of drug release mechanism, the dissolution data were plotted according to the different kinetic models. In-vitro dissolution studies showed that zero-order and square-root of time (Higuchi model) release characteristics were exhibited.Bangladesh Pharmaceutical Journal 18(2): 132-136, 2015

scholarly journals Formulation and In vitro Release Behavior of Hydroxypropyl Methylcellulose (HPMC) Matrix Tablet Containing Poorly Soluble Fenofibrate

2020 ◽  
Vol 23 (1) ◽  
pp. 10-16
Author(s):  
Ramesh Kandel ◽  
Tushar Saha ◽  
Zia Uddin Masum ◽  
Jakir Ahmed Chowdhury
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Pharmaceutical Journal ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Dissolution Profile ◽  
The Matrix

Fenofibrate, a water insoluble drug was used to prepare matrix tablet with four different viscosity grades of Hydroxypropyl Methylcellulose (HPMC) which were Methocel K4M CR, Methocel K15M CR, Methocel K100M CR and Methocel K100LV CR. The concentration of those excipients was 5, 10, 20, and 40% (w/w), respectively. The content of drug in a fixed quantity of powder in every formulation was ranged between 96.47 to 104.78 %. The dissolution study was done by using USP dissolution apparatus II. The kinetics of release was analyzed by using zero-order, first order, Korsmeyer-Peppas, Higuchi and Hixon-crowell equations to explain the drug release mechanism from the matrix tablets. In-vitro dissolution profile of matrix tablets were dependent upon the HPMC concentration and dissolution was rapid for tablets containing lower polymer proportion i.e. 5,10, and 20% Percentage (w/w) HPMC than those containing 40% (w/w) HPMC. Bangladesh Pharmaceutical Journal 23(1): 10-16, 2020

scholarly journals β-Cyclodextrin Inclusion Complexes of Budesonide with Enhanced Bioavailability for COPD Treatment

2021 ◽  
Vol 11 (24) ◽  
pp. 12085
Author(s):  
Georgia Michailidou ◽  
George Z. Papageorgiou ◽  
Dimitrios N. Bikiaris
Keyword(s):  
Inclusion Complexes ◽  
In Vitro Release ◽  
Solvent Evaporation ◽  
Degree Of Crystallinity ◽  
Solvent Ratio ◽  
Release Behavior ◽  
Evaporation Technique ◽  
The Degree Of Crystallinity ◽  
Vitro Release

Chronic obstructive pulmonary disease (COPD) is a life-threatening disease of the respiratory system, affecting many patients worldwide. Budesonide (BUD), a synthetic glucocorticosteroid applied for the treatment of COPD patients, is a hydrophobic compound with low bioavailability. The formation of inclusion complexes of hydrophobic compounds with β-cyclodextrin (CD) through the solvent evaporation technique is an appealing method for the amelioration of the compounds’ in vitro release behavior. In the present study, CD–BUD complexes were prepared through the solvent evaporation technique. The effect of the applied solvent was evaluated through FTIR, scanning electron microscopy (SEM), X-ray diffraction (XRD) analysis, and in vitro release behavior measurements. It was found that the optimum complexes with the minimum degree of crystallinity and the optimum in vitro release behavior are prepared in the solvent ratio H2O/EtOH 80/20 v/v. In a further step, the formation of CD–BUD complexes containing different amounts of BUD was prepared. Through XRD measurements, the degree of crystallinity of the samples was calculated confirming the diminished crystallinity of BUD in CD complexes. The in vitro release of the samples showed the improved release behavior of BUD from the complexes in comparison to neat BUD while a direct correlation between the degree of crystallinity and in vitro release behavior was demonstrated.

scholarly journals Formulation and evaluation of bi-layer floating tablets of ziprasidone HCl and trihexyphenidyl HCl

2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Chemical Properties ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Floating Tablets ◽  
Ir Studies ◽  
Weight Variation ◽  
The Matrix

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.

scholarly journals In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
High Viscosity ◽  
Matrix Tablets ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

scholarly journals FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

2021 ◽  
pp. 206-215
Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Release Studies ◽  
Swelling Studies ◽  
Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

scholarly journals A study on the influence of the formulation factors on in vitro release of ketoprofen from sustained release tablets

2021 ◽  
Vol 14 (1) ◽  
pp. 41-48
Author(s):  
Larisa Cimpoaie ◽  
◽  
Luca Liviu Rus ◽  
Rareș Iuliu Iovanov ◽  
◽  
...  
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Inert Matrix ◽  
Sustained Release Tablets ◽  
Formulation Factors ◽  
Release Data ◽  
Vitro Release ◽  
Inert Matrix Tablets

Objectives. The aim of this study was to investigate the influence of formulation factors on in vitro release of ketoprofen from sustained release inert matrix tablets. Materials and methods. Laboratory scale, Ketoprofen sustained release inert matrix tablets were manufactured using Kollidon® SR as matrix formator, by direct tableting of powder blends. The influence of the formulation factors (X1 – matrix formator excipient and X2 – diluent type) on in vitro release of ketoprofen from sustained release tablets was studied by using a full factorial 23 experimental plan. Outcomes. Pharmacotechnical characterization of manufactured laboratory scale batches was performed and all 12 batches fulfilled European Pharmacopeia requests. In vitro release showed a sustained release profile in all cases. Variance analysis (ANOVA) showed a good correlation between experimental conditions and answers. In vitro release testing was performed in phosphate buffer pH = 7.4. Percentage release was determined spectrophotometrically at 258 nm. A decrease in the rate of in vitro release was registered, up to 4 h and 6 h when lactose DC and mannitol DC were used as diluents, respectively. Isomalt DC has increased the rate of in vitro release up to 6 h. Conclusions. In vitro release data, corresponding to formulation N1 shoed a good fitting with Weitbull, Korshmeyer-Peppas and Higuchi models while in vitro release data corresponding to formulation N8 presented a good fitting with Weitbull and Korsmeyer-Peppas. In case of formulations N1 and N8 a non-Fickian diff usion mechanism seems to be involved in drug release from the matrix tablets.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF SALBUTAMOL SULPHATE AND THEOPHYLLINE EXTENDED-RELEASE TABLETS USING MODIFIED POLYMERS

2018 ◽  
Vol 10 (8) ◽  
pp. 67
Author(s):  
Naveen Goyal ◽  
Anil Kumar
Keyword(s):  
Ethyl Cellulose ◽  
Extended Release ◽  
Research Work ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Compression Method ◽  
Salbutamol Sulphate ◽  
Modified Polymers

Objective: The main objective of this research work was to design, prepare and evaluate extended release (ER) tablets of anti-asthmatic drugs (salbutamol sulphate and theophylline) by direct compression method using diverse ratios of hydroxypropyl methylcellulose (HPMC K100M) and ethyl cellulose (EC) along with some other excipients.Methods: Extended-release matrix tablets of salbutamol sulphate and theophylline were successfully fabricated by direct compression method and coded the formulations as F1 to F7 depending on the ratios of modified polymers. The core tablets composed of hydrophilic polymers of various ratios that allow the discharge of drugs at a controlled rate after coming in contact with the aqueous medium. The designed tablets were subjected to various assessment parameters i.e. friability test, hardness test, drug content consistency and In vitro dissolution tests.Results: Prepared formulations were subjected to various assessment parameters and the findings obtained were within the prescribed limit. To perform the in vitro drug dissolution tests of fabricated tablets, the calibration plots of pure drugs using various solvents i.e. 0.1N HCl, phosphate buffer (pH 6.8) and distilled water were plotted. Dosage forms F1-F7 containing ethyl cellulose and HPMC K100M in various concentration demonstrates the prolonged medications discharge for up to 8 h, among these formulations, F6 shows 95.32±0.24 % for salbutamol sulphate and 94.19±0.39 % for theophylline release at the end of 8 h. This finding reveals that a particular window of concentrations of ethylcellulose and HPMC K100M was capable of providing prolonged drugs discharge.Conclusion: The results obtained in this research work clearly showed a promising potential of extended-release tablets containing a specific ratio of HPMC K100M and ethylcellulose as a release rate controlling polymers for effective treatment of asthma and chronic obstructive pulmonary diseases (COPD).

scholarly journals DESIGN AND CHARACTERISATION OF TRANSDERMAL PATCHES OF PHENFORMIN HYDROCHLORIDE

2017 ◽  
Vol 9 (6) ◽  
pp. 90
Author(s):  
Pratik Swarup Das ◽  
Puja Saha
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Chemical Properties ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Transdermal Patches ◽  
The Matrix

Objective: In present work was designed to develop suitable transdermal matrix patches of Phenformin hydrochloride using various hydrophilic (HPMC) and hydrophobic (EUDRAGID) polymers as matrix formers.Methods: Transdermal patches containing Phenformin hydrochloride were prepared by the solvent casting evaporation technique.Results: Revealed that prepared patches showed good physical characteristics, no drug-polymer interaction and no skin irritation was observed. The in vitro release study revealed that F3 formulation showed maximum release in 24 h. Formulation F3 was subjected for accelerated stability studies. The F3 formulation was found to be stable as there was no drastic change in the Physico-chemical properties of the patches, which was also confirmed by FTIR.Conclusion: Thus conclusion can be made that stable transdermal patches of Phenformin hydrochloride has been developed. F1, F2, F3, F4 formulations showed highest cumulative percentage drug release of 98.13%, 95.50%, 98.65%, 97.21% were obtained during in vitro drug release studies after 24 h. The release of Phenformin hydrochloride appears to be dependent on lipophilicity of the matrix. Moderately lipophillic matrices showed best release. The predominant release mechanism of drug through the fabricated matrices was believed to be by diffusion mechanism. Based upon the in vitro dissolution data the F3 formulation was concluded as optimized formulation.

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