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

scholarly journals Formulation and evaluation of nanoparticulate ofloxacin ophthalmic gel using ionic gelation method

2019 ◽  
Vol 1 (2) ◽  
pp. 73-78
Author(s):  
B Syed Salman ◽  
Mohd Abdul Hannan Baig
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Entrapment Efficiency ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
In Vitro Drug Release ◽  
Entire Study ◽  
Drug Content ◽  
Higuchi Model

Oflaxacin is an ophthalmic and topical anti-bacterial agent used in the management of Allergic conjunctivitis, Trachoma, Blepharitis. The basic idea behind the development of such a system is to maintain a sustained drug release from the dosage form. Oflaxacin is suitable candidate for formulation into sustained dosage form in order to prolong the release of drug. The drug-excipient compatibility studies were carried out by using FTIR technique. Based on the results, excipients were found to be compatible with ofloxacin. In preformulation study, estimation of Ofloxacin was carried out by systronics UV spectrophotometer at λmax 284nm using distilled water, which had a good reproducibility and this method was used in entire study. Formulation was prepared by using ionic gelation method .The response drug content, entrapment efficiency, diffusion, spreadability, In vitro drug release was evaluated Drug content ranging from to 82.6 % to 91.24% entrapment efficiency values are ranged from 91.25% to 94.02% and in -vitro drug release studies are also studied. The In-vitro drug release study of Ofloxacin was carried out by using In-vitro diffusion apparatus.100ml of using tear fluid was taken in a beaker. The solution was stirred with 100rpm by maintaining the temperature of 37˚c ± 5˚c. The drug release data were explored for this type of release mechanism followed. The best fit with the highest determination R2 coefficients was shown by both the models (zero and peppas) followed by Higuchi model which indicate the drug release via diffusion mechanism. However as indicated by the values of R both of the models (zero and peppas) followed by Higuchi model were found to be efficient in describing the release of Ofloxacin.

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

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 FORMULATION AND EVALUATION OF RAMIPRIL MOUTH DISSOLVING FILMS

2019 ◽  
pp. 124-129
Author(s):  
Jasvanth E ◽  
Teja D ◽  
Mounika B ◽  
Buchi N Nalluri
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Release Mechanism ◽  
Onset Of Action ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism ◽  
Preparation And Evaluation ◽  
Pvp K30

Objective: The present investigation was aimed at preparation and evaluation of mouth dissolving films (MDFs) of Ramipril to enhance patient convenience, compliance and to improve bioavailability. Methods: MDFs with 0.5% w/w Ramipril were prepared by a solvent casting method using a wet film applicator. The effects of film formers, wetting/solubilizing, saliva stimulating agents and film modifiers on the physicomechanical and in vitro Ramipril release from MDFs were evaluated. Results: The MDFs prepared were transparent, smooth and showed no re-crystallization upon storage. MDFs casted with hydroxypropyl methylcellulose (HPMC) E3 as film former and polyethylene glycol (PEG-400) as plasticizer showed superior Ramipril release rates and good physicomechanical properties when compared to MDFs with E5 and E15 as film formers. HPMC E3 MDFs with polyvinyl pyrrolidone K30 (PVP K30) and sodium lauryl sulphate (SLS) gave superior drug release properties than MDFs without PVP K30 and SLS. The HPMC E3 MDFs with citric acid (CA) as saliva stimulating and xylitol as soothing agent gave significantly superior in vitro drug release than the MDFs without CA and xylitol. Release kinetics data reveals diffusion as a drug release mechanism. Conclusion: From the obtained results, it can be concluded that the administration of Ramipril as MDF may provide a quick onset of action with enhanced oral bioavailability and therapeutic efficacy.

scholarly journals Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index

The objective of this study was to develop a sustained release matrix tablet of aceclofenac usinghydroxypropyl methylcellulose (HPMC K15M and HPMC K100M CR) in various proportions as release controllingfactor by direct compression method. The powders for tableting were evaluated for angle of repose, loose bulkdensity, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected tothickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolutionstudy was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus inphosphate buffer (pH 7.4). The granules showed satisfactory flow properties, compressibility index and drug contentetc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that theformulations F-2 and F-3 could extend the drug release up to 24 hours. By comparing the dissolution profiles with themarketed product, it revealed that the formulations exhibited similar drug release profile. From this study, a decreasein release kinetics of the drug was observed when the polymer concentration was increased. Kinetic modeling of invitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport toanomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. Thedrug release followed both diffusion and erosion mechanism in all cases. The drug release from these formulationswas satisfactory after 3 months storage in 40°C and 75% RH. Besides, this study explored the optimum concentrationand effect of polymer(s) on acelofenac release pattern from the tablet matrix for 24 hour period.Key words: Aceclofenac; sustained release; hydrophillic matrix; HPMC; direct compression.DOI: 10.3329/dujps.v8i1.5332Dhaka Univ. J. Pharm. Sci. 8(1): 23-30, 2009 (June)

scholarly journals Porous nanoparticles of metoprolol tartrate produced by spray-drying: development, characterization and in vitro evaluation

2012 ◽  
Vol 62 (3) ◽  
pp. 383-394 ◽  
Author(s):  
Mohammed S. Khan ◽  
Gowda D. Vishakante ◽  
H. G. Shivakumar
Keyword(s):  
Drug Release ◽  
Spray Drying ◽  
Release Kinetics ◽  
Drug Loading ◽  
Release Mechanism ◽  
Metoprolol Tartrate ◽  
Pore Former ◽  
Porous Nanoparticles ◽  
Zero Order Release

The present investigation was undertaken to fabricate porous nanoparticles of metoprolol tartrate by spray-drying using ammonium carbonate as pore former. Prepared nanoparticles were coated with Eudragit S100 polymer in order to prevent the release of metoprolol tartrate in the upper GI tract. It was shown that nanoparticles with low size ranges can be obtained with a low feed inlet rate. Micromeritic studies confirmed that nanoparticle batches are discrete and free flowing. Effects of the pore former on drug loading, porosity and in vitro release were studied. It was found that there was an increase in drug loading and porosity with increasing the amount of pore former. In vitro drug release studies showed that an increase in pore former made drug release faster. Release kinetics proved that nanoparticles follow a zero-order release mechanism.

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.

Development of colon targeted matrix tablets of Metformin HCl using various concentration of selected polymers

2017 ◽  
Vol 1 (1) ◽  
pp. 01-02
Author(s):  
Swathi Goli
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Physical Changes ◽  
Metformin Hcl

The aim of the present study was to develop colon targeted matrix tablets of Metformin HCl using various conc. of selected polymers such as HPMC, Ethyl Cellulose Guar gum and combination of the same. Tablets were prepared by direct compression method and both pre-compression and post- compression parameters for all batches shows in the acceptable ranges. Short term accelerated stability studies was performed according to ICH guidelines temperature of 400±20 and relative humidity of 75%±5% RH to study any physical changes and chemical decomposition of drug, no formulation shown any physical or chemical changes. The compatibility of drugs, polymers and excipients were determined by FT-IR Spectroscopy results showed that the drug was compatible with polymers and all excipients. Dissolution studies were performed for 12 hours study in 1.2 pH for first 2 hrs then in 7.4 pH for next 3hrs followed by 6.8pH phosphate buffer at the temperature of 37±0.50C at 100rpm. The dissolution data so obtained was fitted to various mathematical kinetic models and the drug release followed mixed order and Higuchi’s model. To study release mechanism of drug from matrices the data were fitted to Koresmeyer-Peppas model and the release. In –vitro release profile of Metformin HCl from various polymers showed that drug increasing the conc. of polymers resulted in reduction in the release rate of drug (MTF1 to MTF12). Formulation containing combination of E.C-G.G, HPMC-G.G and E.C-HPMC showed drug release profile for MTF-12 about 38.72% after 12 hrs, MTF-11 about 40.66% after 12 hrs, for MTF-10 about 45.45% after 12 hrs. This is an indicative of retardation of drug release when polymer combination was changed. Results showed that the tablets with higher binding concentration showed minimum drug release. Combination of polymers shows greater retarding of drug release.

Formulation and Ex-vivo Evaluation of Glipizide Buccal Tablets

2014 ◽  
Vol 7 (2) ◽  
pp. 2487-2493
Author(s):  
Sudarshan Singh ◽  
Sandip G Maru ◽  
Sunil Bothara B
Keyword(s):  
Guar Gum ◽  
Chemical Interaction ◽  
Ex Vivo ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Aloe Vera ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Buccal Tablets

Bioadhesive materials are agents which adhere to the mucous membrane due to specific properties and release the drug at the site of action in controlled manner. Since the biodegradability of the synthetic polymer is at some instance hesitant. In this exploration, a bioadhesive polymer has been developed which was isolated from leaves of Aloe vera (L.) Burm. f. The mucilage isolated from A. vera were used as a bioadhesive polymer in tablet formulation and evaluated for the parameters such as swelling, pH, and bioadhesive property like bioadhesive strength, record of adherence and ex-vivo residence time. The buccal bioadhesive tablet was prepared using glipizide as model drug. The prepared tablet was evaluated against existing bioadhesive polymer such as guar gum and hydroxyl propyl cellulose. Swelling index and surface pH was found to be 13.12-18.06% and 6.5-6.9 respectively. The drug permeation through goat buccal mucosa was found to be 60.21 ± 0.06 % in the end of 7 h with a Jss of 0.24 mg h-1 cm-2. The stability studies were performed on optimized formulation as per ICH guideline, result showed that there was no significant change in physical characteristic, adhesive strength and in vitro release. It was observed that as the concentration of mucilage increases swelling index also increases. Results of pH showed that mucilage is slightly near to neutral in nature. Formulations were evaluated for preformulation parameters, in vitro drug release profile and release kinetics. The formulations were found to have good preformulation characteristics. FTIR spectroscopy showed no significant chemical interaction within drug and excipients. The release mechanism of glipizide from buccal tablets indicated anomalous (non-fickian) transport mechanism and followed zero order kinetics. It was concluded that the mucilage of A. vera can be used as a pharmaceutical excipient in buccal bioadhesive drug delivery systems.

scholarly journals Formulation and In vitro Evaluation of Eudragit RL 100 Loaded Fexofenadine HCl Microspheres

2016 ◽  
Vol 19 (1) ◽  
pp. 58-67
Author(s):  
Paroma Arefin ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Release Kinetics ◽  
Drug Loading ◽  
Release Mechanism ◽  
Order Release ◽  
Eudragit Rl ◽  
Fexofenadine Hcl

The present study deals with the formulation and evaluation of Fexofenadine hydrochloride (HCl) loaded sustained release microspheres by emulsion solvent evaporation method with Eudragit RL 100. The effects of percent drug loading on drug encapsulation efficiency, drug content and drug release rate were assessed. In vitro dissolution study was performed spectrophotometrically according to USP paddle method using phosphate buffer (pH 6.8) for 10 hours. The release rate of Fexofenadine HCl from the microspheres was significantly increased with the increase of drug loading. The drug release patterns were simulated in different kinetic orders such as zero order release kinetics, first order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism and Higuchi release kinetics was found to be the predominant release mechanism. Morphological changes due to different drug loading were assessed by scanning electron microscopic (SEM) technique. Differential scanning calorimetry and fourier transform infra-red (FT-IR) spectroscopy was performed to evaluate compatibility of drug with the polymer. A statistically significant variation indrug encapsulation efficiency and release rate was observed for variation in drug loading.Bangladesh Pharmaceutical Journal 19(1): 58-67, 2016

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