DEVELOPMENT AND EVALUATION OF A NOVEL TIME AND PH-DEPENDENT COLON TARGETED DRUG DELIVERY OF ORNIDAZOLE

2021 ◽  
pp. 108-111
Author(s):  
SUSHMA M ◽  
PAVANI S
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
In Vitro Dissolution ◽  
Polymeric Coating ◽  
Delivery Method ◽  
Bulk Forming ◽  
Dissolution Tests ◽  
Inflammatory Bowel ◽  
Upper Gastrointestinal

Objective: The anti-amoebic drug Ornidazole was developed in this study as a novel colon-specific drug delivery method for the treatment of colonic diseases such as diverticulitis, inflammatory bowel syndrome, and Crohn’s disease. Pectin forms a matrix with a pH-sensitive polymeric coating that prevents drug release in the upper gastrointestinal tract, thereby addressing solubility issues. Pectin is sometimes used as an adsorbent, bulk-forming agent. Methods: Ornidazole-containing core tablets were directly compressed. Ornidazole compression coated tablets were formulated with varying polymer proportions in the coat. All the tablets were studied for weight uniformity, hardness, friability, drug content, and in vitro dissolution tests Results: All formulations demonstrated good Fourier-transform infrared compliance and no interaction between drug, polymer, and other excipients. The study’s findings show that the formulation F6 coated with Eudragit RS 100 had a drug release of 99.230.8 for 24 h. Conclusion: As a result, (F6) is regarded as the optimal formulation. The pH in the colon causes the release of Ornidazole from tablets.

scholarly journals Formulation and in-vitro evaluation of ciprofloxacin HCL floating matrix tablets

2020 ◽  
Vol 2 (1) ◽  
pp. 01-06
Author(s):  
Dhulipalla Mounika ◽  
I. Deepika Reddy ◽  
K. Sai Chandralekha ◽  
Kapu Harika ◽  
Ramarao Nadendla ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Drug Release ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Prolonged Release ◽  
Evaluation Parameters

Oral drug delivery is the most widely utilized route of administration among all the routes that have been explored for systemic delivery of drugs via pharmaceutical products of different dosage form. Oral route is considered most natural, uncomplicated, convenient and safe due to its ease of administration, patient acceptance and cost-effective manufacturing process. Gastroretentive drug delivery system was developed in pharmacy field and drug retention for a prolonged time has been achieved. The goal of this study was to formulate and in-vitro evaluate Ciprofloxacin HCl controlled release matrix floating tablets. Ciprofloxacin HCl floating matrix tablets were prepared by wet granulation method using two polymers such as HPMC K100M (hydrophilic polymer) and HPMC K15M. All the Evaluation parameters were within the acceptable limits. FTIR spectral analysis showed that there was no interaction between the drug and polymers. In-vitro dissolution study was carried out using USP dissolution test apparatus (paddle type) at 50 rpm. The test was carried out at 37 ± 0.5 0C in 900ml of the 0.1 N HCl buffer as the medium for eight hours. HPMC K100M shows a prolonged release when compared to HPMC K15M. These findings indicated that HPMC K100M can be used to develop novel gastroretentive controlled release drug delivery systems with the double advantage of controlled drug release at GIT pH. On comparing the major criteria in evaluation such as preformulation and in vitro drug release characteristics, the formulation F8 was selected as the best formulation, as it showed the drug content as 99±0.4% and swelling index ratio was 107.14, and in-vitro drug released 61.31±0.65% up to 8 hours. Results indicated that controlled Ciprofloxacin HCl release was directly proportional to the concentration of HPMC K100M and the release of drug followed non-Fickian diffusion. Based on all the above evaluation parameters it was concluded that the formulation batch F8 was found to be best formulation among the formulations F1 to F8 were prepared.

scholarly journals DESIGN AND EVALUATION OF SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEMS OF ALVERINE FOR ENHANCEMENT OF SOLUBILITY

2021 ◽  
Vol 12 (7) ◽  
pp. 25-31
Author(s):  
Pooja . ◽  
Pankaj Kumar Sharma ◽  
Viswanath Agrahari
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Ethyl Oleate ◽  
Spherical Shape ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Transmission Electron ◽  
The Stability

Background: The aim of this study is to develop a liquid self-nano emulsifying drug delivery system for alverine (liquid-SNEDDS).Excipients in the alverine SNEDDS include Ethyl oleate as the oil phase, Tween 80 as a surfactant, and PEG600, Propylene glycol as a cosurfactant.The prepared eleven formulations of alverine SNEDDS were performed for emulsification time, percentage transmittance, particle size, drug release, in vitro dissolution and stability studies.The optimised alverine liquid SNEDDS formulation (D1) was studied for drug-excipient compatibility using infrared spectroscopy, as well as particle size, zeta potential, transmission electron microscopy, and stability. Alverine SNEDDS have a spherical shape with uniform particle distribution, according to their morphology. D1's optimised formulation's drug release percentage (96.6). The stability data revealed no discernible changes in drug content, emulsifying properties, drug release, or appearance. As a result, a potential SNEDDS formulation of alverine with improved solubility, dissolution rate, and bioavailability was developed.

scholarly journals Formulation and Evaluation of Floating Matrix Tablets of Sacubitril and Valsartan

2019 ◽  
Vol 9 (4-s) ◽  
pp. 298-309
Author(s):  
Sudhakar Pathak ◽  
Harish Pandey ◽  
Sunil Kumar Shah
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Potential Candidate ◽  
In Vitro Drug Release ◽  
Gastric Emptying Rate ◽  
Floating Tablets

Floating Drug Delivery Systems (FDDS) have a bulk density lower than gastric fluids and thus remain buoyant in the stomach for a prolonged period of time, without affecting the gastric emptying rate. While the system is floating on the gastric contents, the drug is released slowly at a desired rate from the system. These floating tablets mainly prepared for reduction of lag time and release the drug up to 12 hours and may also increase the bioavailability of the drugs by utilizing the drug to full extent avoiding unnecessary frequency of dosing. The purpose of this research was to develop and evaluated floating matrix tablets of sacubitril and valsartan. The floating matrix tablets of sacubitril and valsartan were prepared by direct compression method using altered concentrations of HPMC K4M, HPMC K100M, sodium alginate as polymers and sodium bicarbonate, citric acid as gas generating agent. FTIR, DSC studies conformed that there was no incompatibility between the polymers and the drug. Tablet preformulation parameters were within the pharmacopoeias limit. Tablets were evaluated by different parameters such as weight uniformity, content uniformity, thickness, hardness, in vitro release studies, buoyancy determination and kinetic analysis of dissolution data. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. Tablet showed ≤ 1min lag time, continuance of buoyancy for >12 h. The in-vitro drug release pattern of sacubitril and valsartan optimized floating tablets (F16) was fitted to different kinetic models which showed highest regression (r2 = 0.9838) for Higuchi model. The Optimized formulation (F16) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months.  Prepared floating tablets of sacubitril and valsartan may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.  

scholarly journals FORMULATION AND EVALUATION OF FLOATING MATRIX TABLETS OF LEVOFLOXACIN HEMIHYDRATE USING HYDROXYPROPYL METHYLCELLULOSE K4M TO TREAT HELICOBACTER PYLORI INFECTION

2018 ◽  
Vol 11 (6) ◽  
pp. 148
Author(s):  
Srinivasa Rao Baratam ◽  
Vijayaratna J
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Linear Regression Method ◽  
In Vitro Drug Release ◽  
Sustained Drug Delivery

Objective: The aim of the study was to develop a floating drug delivery system of levofloxacin (LVF) hemihydrate for sustained drug delivery to improve the extended retention in the stomach, oral bioavailability, and local site-specific action in the stomach. Methods: Preparation of LVF tablets using melt granulation method using hydroxypropyl methylcellulose (HPMC) K4M with sodium bicarbonate as gas generating agent. From LFTA1 to LFTA5, formulations were developed and evaluated for floating properties for swelling characteristics and in vitro drug release studies. In vitro dissolution was carried out using USP II paddle method using 0.1N HCI pH buffer at 50 rpm and samples were measured at 294 nm using ultraviolet-visible spectroscopy. Results: Obtained Fourier-transform infrared charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. In vitro drug release was performed and drug release kinetics were evaluated using the linear regression method and were found to be followed the zero-order release by diffusion controlled release. Optimized formula was found to be LFTA4 with 20% of a polymer with 99.03% of drug release with 12 h of floating time and 32 s floating lag time. Conclusion: Matrix tablets (LFTA4) formulated employing 20% HPMC K4M are best suited to be used for gastroretentive dosage form of LVF.

Formulation development and in vitro Evaluation of sustained release matrix tablets of Cefpodoxime proxetil

2021 ◽  
pp. 273-278
Author(s):  
A. Bhavani ◽  
B. Hemalatha ◽  
K. Padmalatha
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
Oral Dosage ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Formulation Development ◽  
Cefpodoxime Proxetil

The present focus is on the development of sustained release formulations due to its inherent boons. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance, reduction in fluctuation and increased safety margin of potent drug. The present study was aimed to prepare a sustained drug delivery system to design a controlled release oral dosage form of Cefpodoxime proxetil. The sustained release matrix tablets of Cefpodoxime proxetil were prepared by wet granulation and evaluated for different parameters such as weight variation, drug content, thickness, hardness, friability and In vitro release studies. The in vitro dissolution study was carried out for 12 hours using USP (Type- II) paddle apparatus in hydrochloride (0.1N) as dissolution media for first 2 hours and phosphate buffer (pH 6.8) for next 10 hours. Based on the in vitro dissolution data, formulation F8 was selected as the best formulation from Cefpodoxime proxetil formulations (F1 – F9) as the drug release was retarded up to 12 hours with 96.29 % and followed zero order release kinetics & drug release mechanism was diffusion.

Lidocaine Loaded Ca/P Scaffolds for Bone Regeneration and Local Drug Delivery

2011 ◽  
Vol 222 ◽  
pp. 289-292 ◽  
Author(s):  
Dagnija Loca ◽  
Janis Locs ◽  
Juris Gulbis ◽  
Ilze Salma ◽  
Liga Berzina-Cimdina
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Bone Regeneration ◽  
Pore Size ◽  
Clinical Importance ◽  
Local Drug Delivery ◽  
In Vitro Dissolution ◽  
Poly Lactic Acid ◽  
Porous Scaffolds

Local drug delivery devices especially based on osteoconductive porous calcium phosphate ceramics are of clinical importance. However, the brittleness, pore structure, porosity and pore size should be controlled for their wider applications in hard tissue implants and load bearing compartments. An approach to the fabrication of the bone graft exhibiting bone regeneration function as well as the local drug delivery was made. Hydroxyapatite (HAp)/β-tricalcium phosphate (β-TCP) porous scaffolds were prepared and mechanical properties (compression strength 20MPa), porosity (>50%), pore size (60-350µm) and structure as well as interconnectivity of pores were investigated. Porous scaffolds were impregnated with 4-5 mg of lidocaine hydrochloride (LidHCl) and drug release rate was evaluated and compared for scaffolds with and without poly lactic acid (PLA), poly(-caprolactone) (PCL) and polyvinyl alcohol (PVA) coatings. From in vitro dissolution tests it was seen that biopolymer coatings sustained the drug release up to 12h.

scholarly journals Development and in vitro evaluation of pulsatile drug delivery system of enalapril maleate

2015 ◽  
Vol 18 (1) ◽  
pp. 66-71 ◽  
Author(s):  
Sumaiya Mehjabin Tosha ◽  
Ashima Aziz ◽  
Sharmin Jahan Chisty ◽  
Md Asaduzzaman ◽  
Mohiuddin Ahmed Bhuiyan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Cube Root ◽  
Physical Parameters ◽  
Type I ◽  
Enalapril Maleate ◽  
Pulsatile Drug Delivery

Pulsatile drug delivery of enalapril maleate is one such system that, by delivering drug at the right time, right place and in right amounts, holds good promises of benefit to the patients suffering from hypertension. The basic design involves the preparation of cross linked hard gelatin capsules using formaldehyde. Then the drug diluent mixtures were prepared and loaded which was separated by using hydrogel plug of polymers of different grades such as HPMC 50 cps, HPMC 100 cps, HPMC K4M, HPMC K15M, HPMC K100M, xanthan gum, carbopol 971 and sodium CMC at different amount (100 and 120 mg). Prepared formulations were subjected to evaluation of various physical parameters and in vitro drug release studies. Dissolution tests were performed using the USP type I basket method at 50 rpm in 6.8 phosphate buffer. From the in vitro dissolution studies it was found that by increasing the amount of polymers, release rate was decreased. Here, 100 mg of HPMC K100M showed 80% drug release in 8 hours whereas 120 mg showed 78.87% drug release in 10 hours. Similar decrease in the release rates were found with the increase of other polymers used in this study. The release data was fitted to various mathematical models such as zero order, first order, Higuchi, Korsmeyer Peppas and Hixson Crowell cube root law. The drug release follows mixed order kinetics and mechanism was found to be non-Fickian diffusion.Bangladesh Pharmaceutical Journal 18(1): 66-71, 2015

scholarly journals Development and optimization of self microemulsifying drug delivery of domperidone

2014 ◽  
Vol 50 (1) ◽  
pp. 91-100 ◽  
Author(s):  
Pankaj Laddha ◽  
Vrunda Suthar ◽  
Shital Butani
Keyword(s):  
Drug Delivery ◽  
Oleic Acid ◽  
Drug Release ◽  
Droplet Size ◽  
Stability Study ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Solubility Study ◽  
Mixture Experimental Design

The present investigation is aimed to develop self-microemulsifying drug delivery system (SMEDDS) to improve the in vitro dissolution of a BCS (Biopharmaceutical Classification System) class II anti emetic agent, domperidone. Solubility study was performed to identify the ingredients showing highest solubility of domperidone. The ternary phase diagrams were plotted for selected components to identify the area of microemulsion existence. D-optimal mixture experimental design was applied to optimize a liquid SMEDDS using formulation variables; the oil phase X1 (Oleic acid), the surfactant X2 (Labrasol) and the co-surfactant X3 (Transcutol HP). The liquid SMEDDS were evaluated for droplet size, emulsification time, % transmittance and drug release. Stability study was performed at 40 °C/75% RH. Liquid formulation was solidified by adsorption on carrier Aerosil 300. Solid SMEDDS was evaluated and compared with liquid SMEDDS and marketed formulation. Oleic acid was selected as oil, Labrasol as surfactant and Transcutol HP as co-surfactant for formulation of SMEDDS. The optimized batch showed best results in terms of smaller droplet size (<170 nm), emulsification time (<40 s) and drug release (>85% in 15 min) and was stable for 3 months. Solid SMEDDS containing Aerosil 300 showed good flow properties and uniform drug content. XRPD study revealed that the crystalline drug was converted to amorphous form in solid SMEDDS. The rate and extent of drug dissolution from solid SMEDDS was significantly higher than pure drug and commercial tablet formulation. The results demonstrate the potential of SMEDDS as a means of improving solubility, dissolution and hence the bioavailability.

scholarly journals PREPARATION AND EVALUATION OF PARECOXIB MICROSPONGE HYDROGEL SUSTAINED RELEASED TABLET

2019 ◽  
Vol 8 (3) ◽  
Author(s):  
Maruthi. N ◽  
Lakshmi Radhika G
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Production Yield ◽  
In Vitro Dissolution ◽  
Diffusion Method ◽  
Solvent Diffusion ◽  
Dissolution Studies ◽  
Emulsion Solvent Diffusion Method

Microsponges are the polymeric drug delivery systems composed of porous microspheres. They are tiny sponge like spherical particles that consists of myriad of inter-connecting voids within a non-collapsible structure with a large porous surface. The present work is to formulate and evaluate the Parecoxib Microsponge Hydrogel Sustained Release Tablet. The Microsponges of Parecoxib is prepared by Quasi-emulsion solvent diffusion method using Ethyl cellulose and Eudragit RS100 as polymers and Di-butyl phthalate as Plasticizer. And they are characterized for FTIR studies, production yield, particle size analysis, DSC and SEM. The production yield of formulations was from 77.77 to 82.75. FTIR and DSC studies are revealed that the drug and polymer are compatible with each other during preparation. The average diameter of Microsponge is ranged from 536.9 nm to 489.7. Parecoxib Microsponge hydrogel were prepared as sustained release tablets by using sustained release polymers like MCC, Magnesium stearate, Lactose and talc. Preformulation of Microsponge granules were carried out by various parameters and post formulation were carried out by In-vitro dissolution studies, hardness, friability and weight variation tests. Formulation F3 shows good results for the drug release kinetics as controlled release and F6 formulation shows good results for the in-vitro dissolution studies for sustained release. Key words: Microsponge hydrogel drug delivery, Parecoxib, Sustained drug release tablets, quasi emulsion solvent diffusion method.

scholarly journals F FORMULATION DEVELOPMENT AND EVALUATION OF CARBOPOL-INCORPORATED THERMOREVERSIBLE GELS OF PSEUDOEPHEDRINE FOR RECTAL DRUG DELIVERY

2019 ◽  
pp. 231-235 ◽  
Author(s):  
FIROZ S ◽  
PADMINI K ◽  
PADMASREE K ◽  
SRAVANI N ◽  
HEMALATHA A ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Drug Content ◽  
Ir Studies ◽  
Thermoreversible Gels ◽  
Rectal Drug Delivery

Objectives: The present study describes the preparation and evaluation of a Poloxamer 188 (P188)-based thermoreversible gel using Carbopol 934P (C934P) as a mucoadhesive polymer of pseudoephedrine for enhancing the bioavailability and to avoid the first-pass metabolism. Materials and Methods: Five formulations (F1-F5) were prepared using cold method. The prepared gels were characterized by pH, drug content, spreadability, mucoadhesive force, gelation temperature, and drug release profile. Thermoreversibility of P188/C934P gel was demonstrated by rheological studies. The drug-polymer compatibility was studied using Fourier transform infrared (FTIR). Results: The incorporation of carbopol into P188 gel also reduced the amounts of drug released from the gel formulations. FT-IR studies revealed that there are no interactions between the drug and polymers. Drug content of gels was estimated and the results were found to be satisfactory. In vitro dissolution studies revealed a good drug release from the gels. The drug release was higher in formulations F4 and F5 and lower in F1, F2, and F3 formulations. The order of drug release was found to be F5>F4>F3>F2>F1. Conclusion: These findings suggested that developed thermoreversible gels could be used as promising dosage forms to rectal drug delivery for prolonged periods in the management of hemorrhoids.

Sign in / Sign up

Export Citation Format

Share Document