Percentage Of Drug Content Research Articles

Quality of different brands of metronidazole available in jimma town, south west Ethiopia; A cross- sectional pharmaceutical quality study

Background: WHO report of 2017 estimates that the rates of substandard and falsified medical products in low- and middle-income countries is approximately 10.5% with an estimated spend of US$ 30.5 billion.Objective: The purpose of the study is to assess the quality of different brands of metronidazole available in Jimma town, Oromia region, South West Ethiopia.Methods: Cross-sectional study was conducted in Jimma town, Oromia regional state, Ethiopia. The study was conducted from May 03 – July 30, 2018. Samples were collected using convenience sampling technique. The samples were analyzed using methods specified in British Pharmacopoeia 2013 and United States Pharmacopoeia 2015.Results: All the seven brands of Metronidazole analyzed for quality passed identity test specification of BP 2013. The three brands of Metronidazole capsules passed weight uniformity and dissolution test specification of USP 2015. The seven brands of Metronidazole passed assay (i.e. drug content) test specification of USP 2015. The highest percentage of drug content, 107.81% and 105.56%, obtained for Metronidazole (generic)(capsule) and Nirmet(injection) respectively. However, statistical comparison of assay of respective brands of the respectivedosage forms at 95% confidence interval indicates that there exists significant difference in assay within and among the brands of the respective dosage forms (p<0.05). All the four brands of Metronidazole injections passed USP 2015 limit for Endotoxin, Endotoxin limit ˂0.35Eu/ml. Two brands of Metronidazole injection, Aldezol and Metris, failed sterility test from the four brands of Metronidazole injections included in the study and hence of poor quality.

Formulation and evaluation of Olmesartan Medoxomil solid dispersions to enhance its solubility and dissolution characteristics

The objective of the present learns to improve solubility and dissolution of Olmesartan Medoxomil (OM) by improving water solubility by reliable dispersion methods using fusion method (FM) and solvent evaporation (SE) method via hydrophilic polymers PEG 6000 and PVP K30 in different ratios. Preformulation studies of OM: polymers were carried using DSC and FTIR proves that it is stable without any extra peaks, which implies no interaction among the drug and carrier. For OM in FM drug: polymer ratio was maintained in a range 1:1, 1:3, 1:5 and 1:7 w/w ratio of OM to PEG 6000 and coded as SDOM1, SDOM2, SDOM3 and SDOM4 whereas for SE method OM to PVP K30 ratio was maintained in a range of 1:1, 1:3, 1:5 and 1:7 w/w ratio and coded as SDOM5, SDOM6, SDOM7 and SDOM8. SDOM3 by FM and SDOM7 by SE method resulted in the highest production yield. The solubility studies have shown improved drug solubility compared with a pure drug in all medium. Percentage of drug content, flowability characters like the angle of repose and carr's index, bulk density, Hausner's, tapped density were within acceptable limits. In vitro drug release in the intestinal gastric medium of pH 1.2 was improved significantly when compared with pure drug. SDOM3 and SDOM7, selected for accelerated stability studies, had no significant change in physical parameters, drug content, with little changes in the in vitro drug release pattern. Hence solubility and dissolution rate of OM is increased by using the PEG 6000 and PVP K30 polymers.

Gastric floating pill enhances the bioavailability and drug efficacy of dihydromyricetin in vivo

Dihydromyricetin (DHM) is a natural flavonol compound that has shown significant pharmacological activities such as anti-atherosclerosis, anti-diabetes, anti-oxidation, and anti-inflammation, but its clinical application has been hindered by its poor stability and rapid metabolism that reduced its bioavailability in vivo. Since DHM is more stable under acidic conditions, selective and sustained absorption of DHM in the stomach via gastric floating drug carriers provide an attractive way to settle the problems. Previously, we reported a gastric floating tablet for DHM that demonstrated improved stability and bioavailability of the drug. However, the application of this drug carrier was still constrained by low drug content percentage, and short floating and drug releasing durations. Besides, the influences of dosage forms on the drug efficacy of DHM in vivo were not yet clear. In this study, gastric floating pill as a novel sustained-release dosage form for DHM (DHM-GFP) was developed using combined techniques of extrusion molding and freeze drying. The physicochemical properties of DHM-GFP could well meet the pharmacopoeial requirements for pills. Our data indicated that DHM-GFP had significantly higher drug content percentage, improved floating ability and more sustained drug release than the previously reported DHM tablet, and is promising to become a once-a-day dosing preparation. More importantly, this novel dosage form resulted in notably prolonged residence time, improved bioavailability, and enhanced anti-inflammatory effect of DHM in vivo, indicating its great potential to translate this natural compound into clinical application.

A A COMPARATIVE STUDY OF QUALITY CONTROL TESTING ON CANDESARTAN CILEXETIL CONVENTIONAL TABLETS IN IRAQ

Objective: The present study was performed to compare the quality of conventional tablets loaded with candesartan cilexetil. The selected candesartan cilexetil tablets were commercialized in the Iraq market and produced by different companies. &#x0D; Methods: Different batches of candesartan cilexetil oral tablets (the concentration of candesartan was 8 mg) were subjected to quality control tests. Tests included weight variation, friability, hardness, drug content, disintegration time and in vitro release study. The protocols of these tests were performed according to USP pharmacopeia.&#x0D; Results: The results, in this study, revealed that all the used batches of candesartan cilexetil oral tablets complied with the specification of USP pharmacopeia for weight uniformity, friability value (% loss) was&lt;1. Hardness results of the tablets were 4.9-6.6 Kg/cm2, which was within the required limits (i.e. 4-8 Kg/cm2). Disintegration time was&lt;15 min in both Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF). The percentage of drug content in all marketed tablets was found between 96.2 % and 99.8 %, reflecting compliance with the pharmacopeia limits (i.e. 85-115 %). An in vitro release study indicated that the release of all marketed tablets exceeds 80 % within 15 min.&#x0D; Conclusion: All the studied tablets, loaded with candesartan cilexetil, were produced within the standard criteria of tablet production. The quality control analysis of the selected tablets, in this study, revealed satisfactory pharmaceutical properties (including safety and effectiveness) that comply within the limits of USP pharmacopeia.

In Vitro and In Vivo Assessment of Designed Melphalan Loaded Stealth Solid Lipid Nanoparticles for Parenteral Delivery

The aim of the present study is to develop the melphalan (MLN) loaded stealth solid lipid nanoparticles (SSLNs) for parenteral delivery by hot homogenization technique using central composite design. Amount of tristearin, soyalecithin, and DSPE-m-PEG-2000 is taken as independent factor whereas the particle size, % of encapsulation efficiency, and zeta potential are considered as dependent factors. Developed SSLNs were characterized through various physicochemical parameters, i.e., percentage of drug content, particle size, zeta potential, polydispersity, and percent encapsulation efficiency. The SSLNs were optimized using desirability and overlay plots, and optimized SSLNs were further characterized for various physicochemical parameters, i.e., in vitro drug release at pH 7.4, 6.5 and 5.5 by dialysis process, drug and excipient compatibility analysis (FTIR, DSC, TGA, SEM, and XRD), sterilization, in vitro cell viability and hematological studies, in vivo pharmacokinetics on rats, and stability, respectively. The % assay was found in the range 97.89 ± 0.9 to 101 ± 1.6%; particle size was found in the range of 106 ± 0.9 to 301 ± 1.2 nm whereas the zeta potential was found in the range of − 4 to -38 mV, respectively. The drug release of SSLN was found at around 100% at 28, 32, and 34 h for pH 7.4, 6.5 and 5.5 mediums, respectively. The lyophilized form of SSLNs showed better stability compared with SSLN suspension. The in vitro cell viability studies indicated that SSLNs showed superior results compared with their pure MLN solution. The in vivo pharmacokinetic studies revealed that SSLNs showed long circulation (t1/2), better residence time (MRT), and low elimination rate (Kel) compared with pure MLN solution. Melphalan loaded stealth solid lipid nanoparticles were successfully designed using central composite design by high-pressure homogenization with low particle size and high encapsulation efficiency (92%) and are able to release the drug in controlled manner.

DESIGN AND DEVELOPMENT OF LOSARTAN POTASSIUM FLOATING DRUG DELIVERY SYSTEMS

Objective: The current study was projected to prepare a losartan potassium gastroretentive drug delivery system (GRDDS) of floating tablets was planned to enhance the gastric residence time, thus prolong the drug release.Methods: Effervescent floating matrix tablets of losartan potassium were prepared by direct compression technique using polymers like HPMC k4m, guar gum, and gum karaya, with lubricants magnesium stearate and talc. In the present study, sodium bicarbonate was incorporated as a gas generating agent. Total nine formulations were designed and evaluated for pre-compression parameters known as the angle of repose, bulk density, tapped density, Hausner’s ratio, compressibility index, and post-compression parameters are uniformity of weight, hardness, and drug content percentage, variability, in vitro buoyancy, dissolution studies, and Fourier transform infrared spectroscopy (FTIR).Results: An in vitro dissolution study was carried out by using buffer pH 1.2. From in vitro dissolution studies, it has been found that an increase in polymer concentration diminishes the drug release profile. The in vitro drug release percentage from F4-F9 formulations ranged from 60.28%-98.66% at the closing of 12 h and buoyancy found over 12 h.Conclusion: The in vitro drug release from F1-F3 and F7-F9 followed zero-order, F4 followed Higuchi order, F5 and F6 followed Hixon-Crowell release kinetics. The drug release mechanism was set up to be F1-F8 non-Fickian (anomalous behavior) and F9 having Fickian diffusion type.

FORMULATION AND CHARACTERIZATION OF SUSTAINED RELEASE COATED MATRIX GRANULES OF METFORMIN HYDROCHLORIDE

Objective: Metformin hydrochloride is a biguanide antihyperglycemic agent which is a generally recommended first-line drug for the treatment of diabetes mellitus (Type II). The purpose of this investigation is to prepare sustained release matrix granules of metformin hydrochloride which are coated to extend the drug release over a longer time period.Methods: Metformin hydrochloride granules were prepared by mixing all the dry powders in a V-cone blender and wetting the powder mix with aqueous solution of hydroxypropyl methyl cellulose K100. The prepared granules (MG1-MG5) were investigated for drug release. The batch of granules which exhibited extended release for up to 4 h was coated in a standard coating pan with blends of Eudragit RS and RL to further enhance release period. These were marked as coated metformin granules (CMG3) and CMG4 which were later filled into empty capsules. The granules were characterized for micromeritic properties, percentage yield, particle size distribution, percentage of drug content, and in vitro release of the drug.Results: All the formulations showed percentage yield in the range of 77.66–82.86% and drug content in the range of 78.23–96.62%. CMG3 showed drug release of 97.02% for 12 h. Fourier-transform infrared spectroscopy and differential scanning calorimetry studies indicated that no possible interaction existed between the drug and the polymers used. Scanning electron microscopy images revealed that the granules were spherical in shape with smooth surface and completely covered with a coating of polymer. Kinetic analysis of drug release confirmed that drug release followed zero-order kinetics where it is independent of the concentration.Conclusion: From the results, it was analyzed that design of coated granules employing the polymers used in the present work can produce a sustained release of the drug over a period of 12 h.

DEVELOPMENT AND EVALUATION OF BILAYER TABLETS FOR IMMEDIATE AND CONTROLLED RELEASE OF METFORMIN HYDROCHLORIDE

Objective: The purpose of this study was to develop and evaluate bi-layer tablets for the immediate and controlled release of Metformin Hydrochloride for effective treatment of type 2 Diabetes mellitus.Methods: The immediate release layer was prepared by using super disintegrants like cross carmellose sodium, sodium starch glycolate and sustained release layer was prepared by using hydrophilic polymer like HPMC K 100 and PVP. Various proportions of super disintegrants and polymer were used to select the best formulation composition. Bilayer tablet of metformin was prepared by wet granulation method and was evaluated for physical characteristics like hardness, weight variation, and friability. In vitro release of drug was performed in USP type II dissolution test apparatus using phosphate buffer (pH 6.8) as dissolution media and dissolution was continued for 9 h for the sustained release layer. For immediate release layer, readings were recorded in each 10 min time interval for the first 1h.Results: From the obtained result it was found that all the formulations were within the limit of the standard. The hardness was found to be in the ranges from 5.1 to 5.5 kg/cm2, weight variation was in the range 0.53% to 0.83%, friability of all the formulations was within the range (&lt;1%)and percentage of drug content was more than 97%. The drug release of the tablet was in the range of 85%-91% in 9 h.Conclusion: From the result obtained, it is found that the formulation F6 satisfies all the criteria as sustained release tablet for the effective treatment of type 2Diabetes mellitus. Â

Formulation and evaluation of ileo-colonic targeted matrix-mini-tablets of Naproxen for chronotherapeutic treatment of rheumatoid arthritis

In this present research work, the aim was to develop ileo-colonic targeted matrix-mini-tablets-filled capsule system of Naproxen for chronotherapeutic treatment of Rheumatoid Arthritis. So Matrix-mini-tablets of Naproxen were prepared using microsomal enzyme dependent and pH-sensitive polymers by direct compression method which were further filled into an empty HPMC capsule. The compatibility was assessed using FT-IR and DSC studies for pure drug, polymers and their physical mixtures. The prepared batches were subjected to physicochemical studies, drug content estimation, in-vitro drug release and stability studies. When FTIR and DSC studies were performed, it was found that there was no interaction between Naproxen and polymers used. The physicochemical properties of all the prepared matrix-mini-tablets batches were found to be in limits. The drug content percentage in the optimized formulation F18 was found to be 99.24±0.10%. Our optimized matrix-mini-tablets-filled-capsule formulation F18 releases Naproxen after a lag time of 2.45±0.97h and 27.30±0.86%, 92.59±0.47%, 99.38±0.69% at the end of 5, 8, 12h respectively. This formulation was also found to be stable as per the guidelines of International Conference on Harmonisation of Technical Requirements of Pharmaceuticals for Human Use. Thus, a novel ileo-colonic targeted delivery system of Naproxen was successfully developed by filling matrix-mini-tablets into an empty HPMC capsule shell for targeting early morning peak symptoms of rheumatoid arthritis.

Potency and Antibacterial Efficacy of Degraded Chloramphenicol in Marketed Eye Drop Preparations

This study was done to evaluate the antibacterial activity of chloramphenicol eye drops after exposure to sunlight as well as to measure the percentage of drug content. Chloramphenicol eye drops manufactured by four different companies were collected from local market and exposed to sunlight and their antimicrobial activity was determined against Salmonella typhi and Staphylococcus aureus. Each product was exposed to sunlight for fourteen hours in three different ways with or without of their packaging. The percentage of chloramphenicol contents in eye drop samples was also measured by UV-spectrophotometric method. Significant differences in the inhibitory zones were observed among different set of samples. An inverse correlation between percentage of chloramphenicol content and their antibacterial activity was observed. The results indicate that the UVspectrophotometric method cannot distinguish between chloramphenicol and its degraded products and thus gives incorrect high values of drug content in the preparations, therefore, it should not be considered as an appropriate method to analyze chloramphenicol preparation with its degradation products. DOI: http://dx.doi.org/10.3329/bpj.v16i2.22299 Bangladesh Pharmaceutical Journal 16(2): 165-169, 2013

Microspheres Embedded In Microbeads: A Novel Approach to Improve Various Controlled Release Characteristics of Highly Water Soluble Drug through Ionic Gelation Method

Abstract: The major hindrance behind the preparation of gellan microbeads by simple ionic gelation technique with aqueous soluble drugs is their low entrapment efficiency and sometimes its faster dissolution characteristics. This limits the employment of such a simple method for the preparation of microbeads of water-soluble drugs like stavudine. In the present study a novel attempt has been undertaken by embedding stavudine loaded Eudragit RSPO microspheres into gellan microbeads by ionotropic gelation method with an aim to improve its controlled drug delivery characteristics. The prepared microbeads were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, and optical microscopy for surface topography, drug polymer interaction and particle size analysis respectively. Other studies like drug content, encapsulation efficiency and drug release studies were also carried out. The resulting microspheres embedded in microbeads were free flowing in nature with mean particle size ranging from 544.2-564.2 μm. SEM photomicrographs distinctly shows the microspheres embedded within the microbeads effectively with a smooth surface topography and the gellan microbeads containing D4T only are spherical in nature with rough surface. The FTIR study ascertained the compatibility of the drug within the formulation. The microspheres embedded in microbeads had enhanced percentage of drug content, drug entrapment efficiency and controlled release characteristics as compared to beads containing stavudine only. The mechanism of drug release from the formulations were found to follow non Fickian type diffusion with “n” value between 0.5 to 1but in case of stavudine loaded Eudragit RSPO microspheresit was found to be Fickian type. Key words: Gellan gum, Stavudine, Microbeads, Microsphere embedded in Microbeads, Entrapment efficiency, and Controlled release.

Matrix-mini-tablets of lornoxicam for targeting early morning peak symptoms of rheumatoid arthritis.

The aim of present research was to develop matrix-mini-tablets of lornoxicam filled in capsule for targeting early morning peak symptoms of rheumatoid arthritis. Matrix-mini-tablets of lornoxicam were prepared by direct compression method using microsomal enzyme dependent and pH-sensitive polymers which were further filled into an empty HPMC capsule. To assess the compatibility, FT-IR and DSC studies for pure drug, polymers and their physical mixture were performed. The formulated batches were subjected to physicochemical studies, estimation of drug content, in vitro drug release, drug release kinetics, and stability studies. When FTIR and DSC studies were performed it was found that there was no interaction between lornoxicam and polymers which used. All the physicochemical properties of prepared matrix-mini-tablets were found to be in normal limits. The percentage of drug content was found to be 99.60±0.07%. Our optimized matrix mini-tablets-filled-capsule formulation F30 released lornoxicam after a lag time of 5.02±0.92 hr, 95.48±0.65 % at the end of 8 hr and 99.90±0.83 % at the end of 12 hr. Stability was also found for this formulation as per the guidelines of International Conference on Harmonisation of Technical Requirements of Pharmaceuticals for Human Use. A novel colon targeted delivery system of lornoxicam was successfully developed by filling matrix-mini-tablets into an empty HPMC capsule shell for targeting early morning peak symptoms of rheumatoid arthritis.

Preparation and Evaluation of Valsartan Liquid Filling Formulations for Soft Gels.

The present investigation includes the preparation of liquid filling formulations for soft gels using an antihypertensive drug, valsartan (VAL), in order to improve its dissolution properties and thereby its bioavailability. Formulations were prepared using excipients like polyethylene glycol 400 (PEG 400), propylene glycol (PG), polyvinylpyrrolidone (PVP K-30), antioxidants, ethanol, and purified water. Prepared formulations were evaluated for appearance, pH, drug content percentage, viscosity, stability, and in vitro dissolution studies. The compatibility between the drug and excipients in formulations was confirmed by FTIR spectra. The drug contents were in the range of 99.62-99.63 and the viscosity was in the range of 60.9–591.7 cps with all the formulations developed. Formulations containing 10 mg PVP K 30 gave better dissolution properties when compared to formulations without PVP K 30, and a complete drug dissolution was observed within 10 min and followed the first-order release kinetics. Stability studies were conducted for selected formulations (F4–F9) for a period of 6 months at room temperature (~30°C/65% RH). From the studies, it can be concluded that VAL liquid filling formulations for soft gels were successfully prepared with in vitro dissolution properties superior when compared to VAL itself.

Characteristics of Drug Release from Gel Beads Formed by Hydrolysis of Alginic Acid into Guluronic Acid Blocks

Alginic acid (Alg) is a natural anionic polysaccharide, which consists of α-L-guluronic acid (G) and β-D-mannuronic acid (M). G-G sequence-rich chain regions, known as G-blocks (GB), are important regions for gelation of Alg using divalent cations. In this study, calcium-induced GB gel beads were prepared, and drug release profiles and degradation properties of the GB gel beads were investigated in aqueous media. The GB gel beads swelled slightly in JP XVI 1st fluid (pH 1.2), and only slight release of sodium diclofenac (DF) from the GB gel beads was observed. Disintegration of the GB gel beads was not observed in the 1st fluid. On the other hand, the GB gel beads disintegrated in JP XVI 2nd fluid (pH 6.8), and the rate of disintegration depended on the concentration of calcium chloride used to prepare the GB gel beads. The DF release profiles of the GB gel beads in the 2nd fluid could be controlled by the concentration of CaCl2 used to prepare the GB gel beads. The initial release profile of DF from GB gel beads was not consistent with the profile of disintegration. According to the Higuchi-plot of the percentage of drug content released against the square root of time, gel disintegration did not affect the release of DF from GB gel beads. It appears that a diffusion-type mechanism was responsible for DF release. We propose that the GB gel bead gel matrix is an effective medium by which to control the release of drug within the gastrointestinal tract.

Mucoadhesive slow-release tablets of theophylline: Design and evaluation

Mucoadhesive tablets were prepared to evaluate the adhesive property of the gum obtained from seeds of Ceaselpinia pulcherrima (CP) by comparing it with carbopol, hydroxy propyl methylcellulose (HPMC), and Chitosan. Physical parameters such as bulk density, tapped density, compressibility index, and Hausner’s ratio values indicate good flow, the percentage of drug content was in the range of 96.4±0.97%, and various adhesive evaluation results reveal a good mucoadhesive property.The barium sulphate loaded tablet possesses strong mucoadhesive property, which was evident from prolonged adhesion in the same location of the stomach up to a period of 10 h, whereas the duration of adhesion found to be comparatively less with other polymers. From the results of in vitro and in vivo adhesive tests and in vitro release study the test agent (Gum) appears to exhibit considerable mucoadhesive property and mean residence time values when compared with tablets of carbopol, HPMC, and Chitosan.