Pre-Formulation Studies: Physicochemical Characteristics and In Vitro Release Kinetics of Insulin from Selected Hydrogels

Insulin loaded to the polymer network of hydrogels may affect the speed and the quality of wound healing in diabetic patients. The aim of our research was to develop a formulation of insulin that could be applied to the skin. We chose hydrogels commonly used for pharmaceutical compounding, which can provide a form of therapy available to every patient. We prepared different gel formulations using Carbopol® UltrezTM 10, Carbopol® UltrezTM 30, methyl cellulose, and glycerin ointment. The hormone concentration was 1 mg/g of the hydrogel. We assessed the influence of model hydrogels on the pharmaceutical availability of insulin in vitro, and we examined the rheological and the texture parameters of the prepared formulations. Based on spectroscopic methods, we evaluated the influence of model hydrogels on secondary and tertiary structures of insulin. The analysis of rheograms showed that hydrogels are typical of shear-thinning non-Newtonian thixotropic fluids. Insulin release from the formulations occurs in a prolonged manner, providing a longer duration of action of the hormone. The stability of insulin in hydrogels was confirmed. The presence of model hydrogel carriers affects the secondary and the tertiary structures of insulin. The obtained results indicate that hydrogels are promising carriers in the treatment of diabetic foot ulcers. The most effective treatment can be achieved with a methyl cellulose-based insulin preparation.

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Release Kinetics Study of Azithromycin from Bi-layered Tablets

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v20i1.32094 ◽

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

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Formulation Development and Evaluation of Floating Microsphere of Famotidine for the Treatment of Peptic Ulcer

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i4-s.3350 ◽

2019 ◽

Vol 9 (4-s) ◽

pp. 426-431

Author(s):

Dharmendra Rai ◽

Durga Pandey ◽

Nishi Prakash Jain ◽

Surendra Kumar Jain

Keyword(s):

Ethyl Cellulose ◽

Release Kinetics ◽

In Vitro Release ◽

Methyl Cellulose ◽

Extended Period ◽

Prolonged Release ◽

Formulation Development ◽

Evaporation Method ◽

Solvent Diffusion

The purpose of this research was to prepare a floating drug delivery system of famotidine. The floating microspheres can be prepared for the improvement of absorption and bioavailability of famotidine by retaining the system in the stomach for prolonged period of time. Floating microspheres of famotidine were prepared using different polymers like ethyl cellulose, hydroxy propyl methyl cellulose by solvent diffusion-evaporation method. The microspheres had smooth surfaces with free-flowing and good-packing properties. The yield of the microspheres was up to 73.32±0.14% and ethyl cellulose microspheres entrapped the maximum amount of the drug. Scanning electron microscopy confirmed their hollow structures with sizes in 331.6 nm. The prepared microspheres exhibited prolonged drug release and Percentage buoyancy was found to 73.25±0.23. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies. The formulations were subjected to stability studies and In-vitro release and release kinetics data was subjected to different dissolution models. It was concluded that developed floating microspheres of famotidine offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved. Keywords: Famotidine, Solvent diffusion evaporation method, Ethyl cellulose, Hydroxyl propyl methyl cellulose

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DESIGN AND EVALUATION OF BUCCAL PATCHES CONTAINING COMBINATION OF HYDROCHLOROTHIAZIDE AND ATENOLOL

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i2.24460 ◽

2018 ◽

Vol 10 (2) ◽

pp. 105

Author(s):

Ashutosh Roda ◽

Prabhakara Prabhu ◽

Akhilesh Dubey

Keyword(s):

Tensile Strength ◽

Sustained Release ◽

Ex Vivo ◽

In Vitro Release ◽

Methyl Cellulose ◽

Physicochemical Characteristics ◽

Content Uniformity ◽

Casting Technique ◽

Weight Variation

Objective: Buccal patch is a non-dissolving thin matrix modified release dosage form which was developed to administer into the unconscious and less co-operative patients.Methods: The mucoadhesive buccal patches of hydrochlorothiazide (HCZ) and atenolol (ATN) were prepared by solvent casting technique using various concentrations of sodium alginate, hydroxyl propyl methyl cellulose, carbopol 934P and sodium carboxy methyl cellulose polymer and polyvinyl alcohol as a backing layer. The formulated patches were evaluated for their physicochemical parameters like thickness, weight variation, surface pH, content uniformity, folding endurance, swelling percentage studies and tensile strength, in vitro and ex vivo drug permeation. Results: The infra-red (IR) spectra showed no interaction between drug and polymer. Physicochemical characteristics of all the samples were found to be satisfactory and well within the range. Swelling of the films were increased with the increasing content of the polymers and it was found that swelling front erosion was comparably slower in the formulations with the carbopol 934 and HPMC. This is probably due to their marked viscous properties and therefore formulation provided sustained release of the drug. The percentage drug content of all the formulations were found to be in the range of 97-99 %. Among the patches, FC (Carbopol 934 and HPMC) patches were considered satisfactory for maintaining the in vitro residence in the oral cavity for almost 8h. Formulations FD (with CP and NaCMC) and FC showed high tensile strength and % E/B which is an indication of the strength and elasticity of the patch. The films were exhibited sustained release for more than 6 h which was confirmed by the in vitro release data and kinetic data reveals the combination of diffusion and erosion mechanism. The best mucoadhesive performance and matrix controlled release was exhibited by the formulation FC.Conclusion: The formulation of HCZ and ATN mucoadhesive buccal patch was found to be satisfactory and reasonable.

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FORMULATION, CHARACTERIZATION AND IN VITRO EVALUATION OF FLOATING MICROSPHERES OF MEBENDAZOLE AS A GASTRO RETENTIVE DOSAGE FORM

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i5-s.1980 ◽

2018 ◽

Vol 8 (5-s) ◽

pp. 311-314

Author(s):

Lokesh Parmar ◽

Mansi Gupta ◽

Geeta Parkhe

Keyword(s):

Ethyl Cellulose ◽

Release Kinetics ◽

In Vitro Release ◽

Methyl Cellulose ◽

Entrapment Efficiency ◽

Drug Bioavailability ◽

Evaporation Method ◽

Solvent Diffusion ◽

Model Drug

The present study involves preparation and evaluation of floating microspheres using Mebendazole (MBZ) as a model drug for improving the drug bioavailability by prolongation of gastric retention time. Ethyl cellulose, hydroxyl propyl methyl cellulose microspheres loaded with mebendazole were prepared by solvent diffusion evaporation method. The microspheres had smooth surfaces, with free-flowing and good-packing properties. The yield of the microspheres was up to 85.65±0.14% and ethyl cellulose microspheres entrapped the maximum amount of the drug. Scanning electron microscopy confirmed their hollow structures with sizes in the range 215.1 to 251.80 nm. The prepared microspheres exhibited prolonged drug release and Percentage buoyancy was found to70.25±0.15. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies. The formulations were subjected to Stability studies and In-vitro release and Release kinetics data was subjected to different dissolution models. Keywords: solvent diffusion evaporation method, Mebendazole, Ethyl cellulose, Hydroxyl propyl methyl cellulose

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Preparation and In vivo Evaluation of Mucoadhesive Microspheres for Gastroretentive Delivery of Misoprostol

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.2.6 ◽

2017 ◽

Vol 10 (2) ◽

pp. 3676-3683

Author(s):

Bhikshapathi D.V. R. N. ◽

Ranjith Kumar K

Keyword(s):

Drug Release ◽

Release Kinetics ◽

In Vitro Release ◽

Methyl Cellulose ◽

Gi Tract ◽

In Vivo Evaluation ◽

Upper Gi ◽

Upper Gi Tract

The aim of the present investigation was to prepare and evaluate the Misoprostol mucoadhesive microspheres for gastroretentive drug delivery. Sodium alginate and sodium carboxy methyl cellulose were used as mucoadhesive polymers. Microsphere formulations were prepared using Ionotropic gelation technique. All the microspheres were characterized for particle size, scanning electron microscopy, FT-IR study, percentage yield, drug entrapment, stability studies and for in vitro release kinetics. Based on the results, the formulation M12 was selected as optimized formulation. In vitro drug release study of optimized formulation M12 showed 98.23% after 12 h in a controlled manner, which is essential for anti ulcer therapy. The marketed product shows the drug release of 95.23 within 1 h. The results of mucoadhesion study showed better retention of prepared microspheres (8) h in chic duodenal and jejunum regions of intestine. The results showed significant higher retention of mucoadhesive microspheres in upper GI tract. Pharmacokinetic study revealed that the bioavailability was found to be increased significantly when compared with marketed tablets. The drug release of Misoprostol optimized formulation M12 followed zero order, Higuchi and Korsmeyer-Peppas kinetics indicating diffusion controlled with non-Fickian (anomalous) transport thus it projected that delivered its active ingredient by coupled diffusion and erosion. Overall, the result indicated prolonged delivery with improved bioavailability of Misoprostol from mucoadhesive microspheres due to higher retention in the upper GI tract.

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Formulation and Release Characteristic of a Bilayer Matrix Tablet Containing Glimepride Immediate Release Component and Metformin Hydrochloride as Sustained Release Component

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2010.3.1.8 ◽

2010 ◽

Vol 3 (1) ◽

pp. 851-859

Author(s):

Y Madhusudan Rao ◽

Sunil Reddy ◽

Panakanti Pavan Kumar ◽

Rajanarayana Kandagatla

Keyword(s):

Sustained Release ◽

Release Kinetics ◽

In Vitro Release ◽

Methyl Cellulose ◽

Immediate Release ◽

Matrix Tablets ◽

Metformin Hydrochloride ◽

Matrix Tablet ◽

Metformin Hcl

The aim of present study was to design the concept of bilayered tablets containing Glimepride for immediate release using sodium starch glycolate as super disintegrant and Metformin hydrochloride (HCl) for sustained release by using Hydroxyl propyl methyl cellulose (HPMC K 4M) and Sodium Carboxy Methyl cellulose (SCMC) as the matrix forming polymer, and PVPK-30 as binder. The tablets were evaluated for physicochemical properties. All the values were found to be satisfactory. In vitro release studies were carried out as per USP in pH 1.2 with (0.1% sodium lauryl sulphate w/v) and phosphate buffer pH 6.8 using the apparatus I. The release kinetics of Metformin HCl was evaluated using the regression coefficient analysis. The formulated tablets (F5) shows zero order release and diffusion was the dominant mechanism of drug release. The polymer (HPMC K4M, SCMC) and binder PVPK-30 had significant effect on the release of Metformin HCl matrix tablets (F5). Thus formulated bilayer tablets provided immediate release of Glimepride and Metformin HCl as sustained release over a period of 8 hours. Stability studies and FT-IR studies clearly indicated that there is no drug –polymer interaction.

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RESVERATROL-HUMIC ACID LOADED COLLOIDAL POLYMERIC NANOPARTICLES: DESIGN OF EXPERIMENT AND IN VITRO EVALUATION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i4.41878 ◽

2021 ◽

pp. 177-184

Author(s):

RAHUL H. ◽

SUNDEEP C. ◽

SWATI G.

Keyword(s):

Humic Acid ◽

Polymeric Nanoparticles ◽

In Vitro Release ◽

Physicochemical Characteristics ◽

Polymeric Nanocarriers ◽

Eudragit E100 ◽

Formulation Factors ◽

The Stability ◽

Vitro Release

Objective: The study aims at fabrication and optimization of co-encapsulated resveratrol and humic acid in colloidal polymeric nanocarriers to improves the stability of insoluble antioxidant, resveratrol. Methods: The Eudragit E100 polymeric material was used to fabricate oral co-encapsulation of resveratrol and humic acid in colloidal polymeric nanocarriers, called Res-HA-co-CPNs by an emulsification-diffusion-evaporation method. Taguchi orthogonal array design was employed to check the effect of formulation factors on in vitro physicochemical characteristics. The optimized formulation was further evaluated for stability studies at different conditions. Results: Optimized Res-HA-co-CPNs demonstrated spherical and smooth surface including mean PS 120.56±18.8 nm, PDI 0.122, ZP+38.25mV, and EE 82.37±1.49%. Solid-state characterizations confirmed that optimized Res-HA-co-CPNs showed amorphous characteristics. In vitro release profile of Res-HA-co-CPNs showed an outstanding sustained release behavior up to 48h and remain stable at the refrigerated condition for 6 mo. Conclusion: Res-HA-co-CPNs would be a proficient and promising dosage form for increasing the stability of insoluble antioxidants, resveratrol.

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Release Profile of Losartan Potassium from Formulated Sustained Release Matrix Tablet

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v16i2.22301 ◽

2015 ◽

Vol 16 (2) ◽

pp. 177-183

Author(s):

Md Ziaur Rahman ◽

Sayed Koushik Ahamed ◽

Sujan Banik ◽

Mohammad Salim Hossain

Keyword(s):

Drug Release ◽

Sustained Release ◽

Release Kinetics ◽

In Vitro Release ◽

Methyl Cellulose ◽

Matrix Tablets ◽

Losartan Potassium ◽

Matrix Tablet ◽

Vitro Release

The present study was undertaken to develop sustained release (SR) matrix tablets of Losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method along with Kollidon SR and Methyl Cellulose as release retardant polymers. The evaluation involves two stages- the physical properties studies of tablets and in vitro release kinetics assessment. The USP paddle method was selected to perform the dissolution test and 900 ml phosphate buffer of pH 6.8 was used as dissolution medium at 50 rpm at 370C. The release kinetics were analyzed. All the formulations followed Higuchi release kinetics. When the release data was plotted into Korsmeyer-Peppas equation, then it was confirmed that F-1, F-2, F-3, F-4 and F-5 exhibited non-fickian type drug release whereas F-6 exhibited fickian type drug release from the tablet matrix. The in-vitro release studies revealed that the formulation F-2 can be taken as an ideal or optimized formulation of sustained release tablets for 24 hours release as it fulfills all the requirements for sustained release tablet. Furthermore, when the tablets were preheated at different temperature (300C, 450C, 600C) before dissolution they showed decrease in drug release compared with ambient temperature DOI: http://dx.doi.org/10.3329/bpj.v16i2.22301 Bangladesh Pharmaceutical Journal 16(2): 177-183, 2013

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Preparation and Evaluation of Sustained Release Matrix Tablets of Tolterodine Tartrate Using Guggul Resin

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v21i1.37902 ◽

2018 ◽

Vol 21 (1) ◽

pp. 24-34

Author(s):

K Latha ◽

T Chinni Kranthi ◽

Naseeb Basha Shaik

Keyword(s):

Drug Release ◽

Sustained Release ◽

In Vitro Release ◽

Physicochemical Characteristics ◽

Matrix Tablets ◽

Natural Polymers ◽

Duration Of Action ◽

Tolterodine Tartrate ◽

Vitro Release

The present study is based on preparation of sustained release matrix tablets of tolterodine tartrate (for overactive bladder treatment) using guggul resin. Tolterodine tartrate is a highly soluble drug, to increase the duration of action the release of the drug has to be sustained. Natural resin is used as a polymer to sustain the release of drug, which was isolated from guggul gum by petroleum ether. Natural polymers are economical, biodegradable and can be chemically modified. Different ratios of drug and guggul resin were tried in the formulation of sustained release matrix tablets of tolterodine tartrate. Wet granulation technique was adopted for preparation of tolterodine tartrate granules, showed good flow properties and compressibility. The fabricated tablets were evaluated for various physicochemical characteristics and in vitro release studies like hardness, thickness, weight variation, friability, drug content and content uniformity were found to be within the limits. The drug release of optimized formulation (F6) was fitted to various kinetic models and the R2 value is 0.988 and the n value of drug release is 0.787. Therefore, the drug release follows zero order with non-fickian diffusion. The mechanism of drug release involves erosion and diffusion. Stability studies were performed for the optimized formulation as per ICH guidelines climatic zone III and were found to be stable with insignificant changes in physicochemical characteristics and in vitro release studies.Bangladesh Pharmaceutical Journal 21(1): 24-34, 2018

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