Drug Content Uniformity Research Articles

OPTIMASI BAHAN POLIMER PEMBENTUK MATRIKS TABLET SUSTAINED RELEASE Na. DIKLOFENAK

Sustained release tablet is one of drug delivery system with an extended release drugs which use polymer to control the release of drug from its dosage form. The advantages of this dosage form is can produce fixed blood levels are without repeat the administration of the unit dose. The aim of this study is to obtain the most optimum polymer as a matrix in sustained release tablets of Diclofenac Sodium. Sustained release tablets made by direct compression method from a mixture of three types of polymer combinations. F1 consists of a combination of HPMC polymer: Etilsellulosa, F2 is the combination of HPMC: Xanthan Gum and F3 consists of a combination of HPMC polymer: Na. Alginate. Each combination of polymer use the same ratio is 1: 2. Tablet evaluations include the weight uniformity of tablet, size,drug content and dissolution test. Result showed that the most optimum combination of polymer as a sustained release tablet matrix is F1 even F2 have an optimum dissolution.

OPTIMASI BAHAN POLIMER PEMBENTUK MATRIKS TABLET SUSTAINED RELEASE Na. DIKLOFENAK

Sustained release tablet is one of drug delivery system with an extended release drugs which use polymer to control the release of drug from its dosage form. The advantages of this dosage form is can produce fixed blood levels are without repeat the administration of the unit dose. The aim of this study is to obtain the most optimum polymer as a matrix in sustained release tablets of Diclofenac Sodium. Sustained release tablets made by direct compression method from a mixture of three types of polymer combinations. F1 consists of a combination of HPMC polymer: Etilsellulosa, F2 is the combination of HPMC: Xanthan Gum and F3 consists of a combination of HPMC polymer: Na. Alginate. Each combination of polymer use the same ratio is 1: 2. Tablet evaluations include the weight uniformity of tablet, size,drug content and dissolution test. Result showed that the most optimum combination of polymer as a sustained release tablet matrix is F1 even F2 have an optimum dissolution.

Natural Bioadhesive Biodegradable Nanoparticle-Based Topical Ophthalmic Formulations for Management of Glaucoma.

We prepared and characterized topical ophthalmic formulations containing brimonidine-loaded bioadhesive cationic chitosan or anionic alginate nanoparticles (NPs) for sustained release of brimonidine as once daily regimen for management of glaucoma. Nanoparticles were prepared using a spontaneous emulsification solvent diffusion method. Different concentrations of polymers, emulsifiers, and NPs stabilizers were used for formulation optimization. Nanoparticles were characterized regarding particle size, zeta potential, morphology, and drug content. Brimonidine-loaded NPs were incorporated into eye drops, a temperature-triggered in situ gelling system, and a preformed gel. They then were characterized regarding their pH, viscosity, uniformity of drug content, in vitro release characteristics, in vitro cytotoxicity, and in vivo intraocular pressure (IOP) lowering effects. Characteristics of optimized brimonidine-loaded chitosan and alginate NPs, respectively, are: particle size, 115.67 ± 3.58 and 157.67 ± 5.53 nm; zeta potential, +35.27 ± 3.39 and -37.8 ± 3.77 mV; encapsulation efficiency, 74.34% ± 2.05% and 70.40% ± 2.77%; drug loading, 11.81% ± 0.67% and 13.14% ± 0.90%; and yield, 87.91% ± 5.92% and 76.53% ± 3.32%. Transmission electron microscope (TEM) analyses revealed that NPs have spherical shapes with a dense core and distinct coat. Formulations possessed uniform drug content. Furthermore, pH and viscosity were compatible with the eye. Formulations showed a sustained release without any burst effect with a Higuchi non-Fickian diffusion mechanism. Cytotoxicity studies revealed that all formulations are biocompatible. Importantly, all formulations possessed a sustained IOP lowering effect compared to the marketed brimonidine tartrate eye drops. These formulations provide a great improvement in topical ocular brimonidine delivery. The application of a single drop is sufficient to provide extended IOP reduction, which should improve patient compliance. We have developed a novel biocompatible topical delivery system for brimonidine, a first line glaucoma medication. Once daily application should have positive effects on patient compliance and, therefore, preservation of vision.

Formulation and Evaluation of Oro dispersible Tablets of Fosinopril Sodium

The purpose of present research was to formulate and evaluate oro dispersible tablets (ODTs) of fosinopril sodium (FS). It has been developed at 20 mg dose and was prepared using different types of superdisintegrants such as (sodium starch glycolate, Ac-Di-Sol, crospovidone (CP), different types of subliming agents such as ammonium bicarbonate (AB) and camphor at different concentrations by direct compression method. The formulations were evaluated for uniformity of weight, content, hardness, friability, wetting time, in vitro dispersion time and dissolution rate. All formulations showed satisfactory mechanical strength, uniform weight, uniform drug content, and lesser wetting time and dispersion time. All the formulations showed more than 90% of drug release within 15 minutes. Among 10 formulations, formulation A5 (consisting of 2 % CP) and F4 (consisting of 15 % AB) were found to yield best results in terms of wetting time, in vitro dispersion time and dissolution rate.Dhaka Univ. J. Pharm. Sci. 14(1): 11-16, 2015 (June)

Formulation and Evaluation of Amoxicillin Trihydrate Lozenges

In the present investigation an attempt has been made to formulate medicated lozenges containing amoxicillin trihydrate. There are several amoxicillin trihydrate dosage forms in the market such as tablet, capsule, suspension and syrup. Still there is a need for more variant dosage forms which acts effectively and locally. The benefits of the present research work is to increase the retention of the dosage form in oral cavity for increased bioavailability, reduction in gastric irritation and bypassing first pass metabolism. The lozenges were prepared by heating and congealing method employing polyethylene glycol 1500 as matrix base, saccharin sodium (artificial sweetener), stevia (natural sweetener), xanthan gum (polymer), sodium carboxymethyl cellulose (polymer) as other exciepients. The prepared medicated lozenges were characterized for drug content uniformity, hardness, thickness, weight variation, friability and dissolution by standard pharmacopeal methods. The results of the evaluation tests obtained were within the limits. Accelerated stability studies were conducted as per ICH guidelines and found that there wasn’t any substantial interaction among the drug, flavour and colour and the prepared formulations were found to be stable. Formulations were tested for drug exciepients interactions subjecting to IR spectral and DSC analyses. The results revealed that there was no major interactions between the drug and polymers used for the preparation of lozenges.Dhaka Univ. J. Pharm. Sci. 14(1): 61-70, 2015 (June)

Novel use of superdisintegrants as viscosity enhancing agents in biocompatible polymer films containing griseofulvin nanoparticles

The advantages of using superdisintegrants, sodium starch glycolate (SSG), croscarmellose sodium (CCS) and crospovidone (CP) over traditional high molecular weight (MW) viscosity enhancing agents, guar gum (GG), xanthan gum (XG), pectin and high MW HPMC are examined for improving drug content uniformity without compromising dissolution of films containing nanoparticles of griseofulvin (GF), used as a model poorly water-soluble drug. Films were fabricated by preparing low MW HPMC solutions to which a fixed amount of viscosity enhancing agents was added and mixed with GF nanosuspensions produced via wet milling, followed by casting and drying. The addition of superdisintegrants and high MW HPMC led to an increase in viscosity of precursor suspensions without GF particle aggregation, and hence excellent drug content uniformity along with retention of the high surface area of the GF nanoparticles in dried films. In contrast, the addition of XG and pectin resulted in aggregation of GF particles in suspensions, leading to poor content uniformity and incomplete recovery of GF nanoparticles upon redispersion of dried films. In spite of their high precursor viscosity, the films containing superdisintegrants did not lead to increased mechanical strength and demonstrated fast drug release, suggesting faster matrix erosion. In contrast, films with high MW polymers (GG, XG, and pectin and high MW HPMC) had increased mechanical strength and their subsequent slow erosion/disintegration along with longer hydration times resulted in significant delay of drug release, which was found to be directly proportional to their MW. These results demonstrate novel use for superdisintegrants as economical and superior alternative to traditional viscosity enhancing agents in forming drug laden biocompatible polymer films.

Design and development of fluoxetine hydrochloride oro flash films to alleviate major depressive disorder

The current research concerns the development of the formulation of fluoxetine HCl (anti-depressant) oro flashes the new prospective by using solvent casting method. Oro flashes are quick dissolving oral films and the materials used were hydrophilic. Fluoxetine HCl formulations were developed since oro flashes improves bioavailability to attain onset of action, along with the patient compliance. Fluoxetine HCl is used to treat major depressive disorder, bulimia nervosa (an eating disorder), obsessive–compulsive disorder, panic disorder, and premenstrual dysphoric disorder. Polyvinyl alcohol (PVA) undergoes polymerization and forms oro flash film. Five different formulations were developed by using different polymeric concentrations of PVA. Polyvinyl pyrollidone K30 (PVP K30) used as super disintegrating agent and plasticizer, whereas menthol and mannitol were used as sweetener, flavoring agent respectively and water as a solvent system. In the study five formulations (F1, F2, F3, F4, and F5) were evaluated for the properties such as thickness, folding endurance, drug content uniformity, surface pH, in vitro disintegration time, dissolution studies, % moisture loss, % moisture uptake, weight variation test, conductivity test. Results revealed that, F3 formulation can be considered as best, which has morphological features are homogenous and transparent with optimum thickness 0.23 ± 0.02 µm, folding endurance (>250 times number of folds on the same crease), drug content uniformity (λ max at 225 nm) 97.60 ± 1.28, surface pH 6.654 ± 0.020, in vitro disintegration time 11 ± 1.20 s, in vitro dissolution studies 97.30 ± 0.75 %, % moisture loss 5.021 ± 0.052 %, % moisture uptake 3.634 ± 0.102 %, weight variation test 48.74 ± 1.0, conductivity test 61 µS which has maximum drug release (97.3 %) which facilitates maximum bioavailability.

Tadalafil oral disintegrating tablets: an approach to enhance tadalafil dissolution

Improvement of the dissolution behavior of poorly water soluble tadalafil using solid dispersion technique was investigated. Polyvinylpyrollidone (PVP) was used to prepare solid dispersions (SDs) based on different ratios; 1:1 (SD1,), 1:2 (SD2,), 1:3 (SD3), 1:4 (SD4,) respectively. Tadalafil/PVP/Avicel® in a ratio of 1:2:2 respectively (SD5) was also prepared. SD5 was selected to formulate orally disintegrating tablets (ODTs). Five formulae were prepared (F1–F5) and characterized with respect to drug content uniformity, breaking strength, % friability, wetting behavior, oral disintegration time. Results revealed that SD2 exhibited the highest dissolution rate improvement, where mean dissolution time was 8.22 min compared to 60.12 min for free tadalafil. X-ray powder diffraction spectroscopy and differential scanning calorimetry showed partial drug amorphization in the tested SDs sample which was further confirmed by scanning electron microscope. Moreover, particle size analysis showed the presence of nanocrystals combined with microcrystals dispersed in the prepared SDs. Among the studied solid SDs, SD2 showed the most satisfactory results. In order to improve % yield of SD2 (70.14 %), avicel® was added and the resulting tertiary combination (SD5) showed better flow and higher % yield value (94.22 %). % tadalfil released from SD2 & SD5 differ insignificantly (p ≥ 0.05). F3 (48 % mannitol, 16 % avicel®, 16 % croscarmellose) showed superior wetting time (30.1 s), excellent oral disintegration time (20 s) with an accepted hardness (3.6 kg) & % friability (0.7). Additionally, F3 exhibited a significant improvement of tadalafil dissolution compared to that of pure drug and test commercial tablet brand (p ≤ 0.05).

FORMULATION AND EVALUATION OF FLOATING TABLETS OF NIZATIDINE

The present investigation is concerned with formulation and evaluation of floating tablet of Nizatidine using the hydrophilic polymer hydroxypropyl methylcellulose a nd gas generating agent sodium bicarbonate and citric acid by wet granulation method. Nizatidine is H 2 receptor antagonist and antiulcer having dose 150 mg twice daily. The drug - excipient compatibility studies were conducted by using FTIR, DSC and visual o bservations. The granules were prepared by wet granulation method and evaluate d for their granules properties. A 3 2 factorial design was applied to systematically optimize the drug release profile. The amount of citric acid (X1) and concentration of polyme r HPMC K100M (X2) were selected as independent variables. The % drug release at 6 hour (Q6) and drug release at 12 hour (Q12), and t 50 % were selected as dependent variables. The results of factorial design indicated that low level of HPMC K100M favors the preparation of floating controlled release of Nizatidine tablets. The tablets were compressed by tablet compression machine and evaluated with different par ameter like thickness, hardness and weight variation, in - vitro buoyancy study swelling index, drug content uniform ity, and in - vitro drug release. Effect of hardness on floating tablet revealed that increase in hardness affect buoyancy lag time due to reduction in porosity of compact mass. Formulations of NFT7 provided sustain release of Nizatidine o ver the period of 12 h .

Formulation and Development of Dendrimer-Based Transdermal Patches of Meloxicam for the Management of Arthritis

Purpose: To develop transdermal patches of meloxicam (MLX) using chitosan and hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA) as hydrophilic polymers, polyamido amine (PAMAM) dendrimer as a permeation enhancer, and dibutyl pthalate as a plasticizerMethods: The patches were prepared by solvent casting evaporation technique using 3-factor, 3-level Box-Behnken design. The patches were evaluated for physical appearance, thickness, weight variation, folding endurance, drug content uniformity, tensile strength, moisture absorption and moisture loss, in vitro drug release, as well as by field-emission scanning electron microscopy (FESEM) and x-ray diffraction (XRD). A specially designed glass diffusion cell was used for the in vitro drug release study. The effect of concentrations of dependent variables (PAMAM G3, chitosan and dibutyl pthalate) on drug release was investigated.Results: The patches demonstrated satisfactory characteristics. PAMAM dendrimer significantly enhanced (p < 0.5) the permeation of MLX. A maximum of 85.7 % drug release was achieved in 24 h.Conclusion: Dendrimer increased the release of MLX by increasing its solubility and permeation through the membrane. Thus, dendrimer patches are a potentially suitable transdermal drug delivery system for the management of some diseased conditions.Keywords: Dendrimers, Transdermal patches, Skin permeation, Permeation enhancer, Chitosan, Hydroxypropyl methyl cellulose, Meloxicam, Plasticizer

Influence of the Component Excipients on the Quality and Functionality of a Transdermal Film Formulation.

The influence of formulation variables, i.e., a hydrophilic polymer (Methocel(®) E15) and a film-forming polymer (Eudragit(®) RL 100 and Eudragit(®) RS 100), on the physicochemical and functional properties of a transdermal film formulation was assessed. Several terpenes were initially evaluated for their drug permeation enhancement effects on the transdermal film formulations. D-Limonene was found to be the most efficient permeation enhancer among the tested terpenes. Transdermal film formulations containing granisetron (GRN) as a model drug, D-limonene as a permeation enhancer, and different ratios of a hydrophilic polymer (Methocel(®) E15) and a film-forming polymer (Eudragit(®) RL 100 or Eudragit(®) RS 100) were prepared. The prepared films were evaluated for their physicochemical properties such as weight variation, thickness, tensile strength, folding endurance, elongation (%), flatness, moisture content, moisture uptake, and the drug content uniformity. The films were also evaluated for the in vitro drug release and ex vivo drug permeation. The increasing ratios of Methocel(®):Eudragit(®) polymers in the formulation linearly and significantly increased the moisture content, moisture uptake, water vapor transmission rate (WVTR), and the transdermal flux of GRN from the film formulations. Increasing levels of Methocel(®) in the formulations also increased the rate and extent of the GRN release and the GRN permeation from the prepared films.

Development and evaluation of natural gum-based extended release matrix tablets of two model drugs of different water solubilities by direct compression

The study was aimed at developing extended release matrix tablets of poorly water-soluble diclofenac sodium and highly water-soluble metformin hydrochloride by direct compression using cashew gum, xanthan gum and hydroxypropylmethylcellulose (HPMC) as release retardants. The suitability of light grade cashew gum as a direct compression excipient was studied using the SeDeM Diagram Expert System. Thirteen tablet formulations of diclofenac sodium (∼100mg) and metformin hydrochloride (∼200mg) were prepared with varying amounts of cashew gum, xanthan gum and HPMC by direct compression. The flow properties of blended powders and the uniformity of weight, crushing strength, friability, swelling index and drug content of compressed tablets were determined. In vitro drug release studies of the matrix tablets were conducted in phosphate buffer (diclofenac: pH 7.4; metformin: pH 6.8) and the kinetics of drug release was determined by fitting the release data to five kinetic models. Cashew gum was found to be suitable for direct compression, having a good compressibility index (ICG) value of 5.173. The diclofenac and metformin matrix tablets produced generally possessed fairly good physical properties. Tablet swelling and drug release in aqueous medium were dependent on the type and amount of release retarding polymer and the solubility of drug used. Extended release of diclofenac (∼24h) and metformin (∼8–12h) from the matrix tablets in aqueous medium was achieved using various blends of the polymers. Drug release from diclofenac tablets fitted zero order, first order or Higuchi model while release from metformin tablets followed Higuchi or Hixson-Crowell model. The mechanism of release of the two drugs was mostly through Fickian diffusion and anomalous non-Fickian diffusion. The study has demonstrated the potential of blended hydrophilic polymers in the design and optimization of extended release matrix tablets for soluble and poorly soluble drugs by direct compression.

Development of biofilm-targeted antimicrobial wound dressing for the treatment of chronic wound infections

It has been established that microbial biofilms are largely responsible for the recalcitrance of many wound infections to conventional antibiotics. It was proposed that the efficacy of antibiotics could be optimized via the inhibition of bacterial biofilm growth in wounds. The combination of antibiofilm agent and antibiotics into a wound dressing may be a plausible strategy in wound infection management. Xylitol is an antibiofilm agent that has been shown to inhibit the biofilm formation. The purpose of this study was to develop an alginate film containing xylitol and gentamicin for the treatment of wound infection. Three films, i.e. blank alginate film (SA), alginate film with xylitol (F5) and alginate film with xylitol and gentamicin (AG), were prepared. The films were studied for their physical properties, swelling ratio, moisture absorption, moisture vapor transmission rate (MVTR), mechanical and rheology properties, drug content uniformity as well as in vitro drug release properties. Antimicrobial and antibiofilm in vitro studies on Staphylococcus aureus and Pseudomonas aeruginosa were also performed. The results showed that AG demonstrates superior mechanical properties, rheological properties and a higher MVTR compared with SA and F5. The drug flux of AG was higher than that of commercial gentamicin cream. Furthermore, antimicrobial studies showed that AG is effective against both S. aureus and P. aeruginosa, and the antibiofilm assays demonstrated that the combination was effective against biofilm bacteria. In summary, alginate films containing xylitol and gentamicin may potentially be used as new dressings for the treatment of wound infection.

BIOADHESIVE BUCCAL DISCS OF FLUVASTATIN SODIUM

Fluvastatin sodium (FVS) is a cholesterol lowering agent (HMG-CoA reductase inhibitor) which undergoes extensive hepatic first pass metabolism causing an absolute bioavailability of ~30%. The aim of this work was to formulate a buccoadhesive disc of FVS to be applied to the buccal mucosa, releasing the drug in a unidirectional manner, in order to improve the bioavailability of the drug and lower the dose-dependent side effects. The bioadhesive discs were prepared by direct compression method using several polymers such as: guar gum, sodium alginate, sodium carboxymethyl cellulose, carbopol 934P, and hydroxypropylmethyl cellulose. Impermeable ethyl cellulose was applied as the backing layer. Different permeation enhancers such as bile salts, surfactants, fatty acids, chitosan, dimethyl sulfoxide, and polyethylene glycol 6000 (PEG 6000) were tested to improve the permeability of buccal mucosal membranes. The optimized formulation contained FVS, guar gum, PEG 6000, and sodium deoxycholate (permeation enhancer, 4%). It showed a drug release of 95.4% in 80 min, drug permeation through chicken pouch membrane (flux (Jss) = 3.74 mg cm-2 h-1), ex vivo bioadhesion strength of 2.543 g, along with satisfactory bioadhesion time of 4.87 h. Physicochemical characteristics of the buccal discs such as drug content uniformity, disc thickness, disc hardness, surface pH, and swelling index were also evaluated.

Formulation development and evaluation of fast disintegrating tablets of salbutamol sulphate, cetirizine hydrochloride in combined pharmaceutical dosage form: a new era in novel drug delivery for pediatrics and geriatrics.

The objective of the present study was to prepare the fast disintegrating tablet of Salbutamol Sulphate, Cetirizine Hydrochloride in combined tablet dosage form for respiratory disorders such as bronchitis, asthma, and coughing for pediatrics and geriatrics. The tablets were prepared by direct compression technique. Superdisintegrant such as Sodium Starch Glycolate was optimized as 4% on the basis of least disintegration time. Different binders such as MCC and PVP K-30 were optimized along with optimized superdisintegrant concentration. 1% MCC was selected as optimum binder concentration on the basis of least disintegration time. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time, and drug content uniformity. Optimized formulation was further evaluated by in vitro dissolution test, drug-excipient compatibility, and accelerated stability study. Percent weight variation and content uniformity were within the acceptable limit. The friability was less than 1%. The wetting time and disintegration time were practically good for all formulations. FTIR studies and accelerated stability study showed that there was no interaction between the drug and excipients. It was concluded that, by employing commonly available pharmaceutical excipients such as superdisintegrants, hydrophilic and swellable excipients and proper filler, a fast disintegrating tablet of Salbutamol Sulphate, Cetirizine Hydrochloride in combined tablet dosage form, were formulated successfully with desired characteristics.

Formulation and Evaluation of Mucoadhesive Buccal Tablets of Repaglinide

Objective: Delivery of the desired drug as mucoadhesive drug delivery systems has been subject of interest since 1980s. The various advantages associated with these systems made the buccal drug delivery as a novel route of drug administration. Buccal region offers an attractive route for the administration of systemic drug delivery. The objective of the study was to develop mucoadhesive buccal tablets of repaglinide. Methodology: The tablets were prepared by wet granulation method using a combination of mucoadhesive polymers like chitosan, hydroxyethyl cellulose, guar gum and carbopol 934P in different ratios. Results: Buccal tablets were evaluated by different methods for parameters such as thickness, hardness, weight uniformity, drug content uniformity, surface pH, ex vivo mucoadhesive strength, ex vivo residence time, in vitro drug release, ex vivo drug permeation. The tablets were evaluated for in vitro release in phosphate buffer of pH 6.8 for 12 h. In order to determine the mode of release, the data was subjected to zero order, first order, Higuchi and Korsmeyer-Peppas model. The mucoadhesive strength was evaluated by measuring the force required to detach the tablets from sheep buccal mucosal membrane. Carbopol 934P showed maximum mucoadhesion and required maximum force for detachment; the force required for detachment was directly proportional to its content. DSC and XRD study of the pure drug indicated that the drug is in the crystalline form. But in the formulations, peaks indicated that the drug is in the amorphous form. FTIR spectroscopic studies indicated that there is no drug-excipient interaction. Conclusion: The prepared formulations showed good mucoadhesive strength and ability to sustain the drug release over 12 h; hence, these are the versatile drug delivery systems for repaglinide.

Skin permeation of buflomedil form adhesive matrix patches

The main objective of this research work was to fabricate and evaluate adhesive matrix-type transdermal patches of buflomedil hydrochloride, employing different ratios of pressure sensitive adhesives (PSAs) by solvent casting technique. The adhesive matrix-type transdermal patches were evaluated by their in vitro physicochemical properties such as thickness, moisture content, weight variation, drug content uniformity, etc. The effects of PSAs ratio, drug loading, and concentration of permeation enhancer were evaluated thoroughly. Ex vivo skin permeation studies with kinetic modeling of adhesive matrix patches were systematically evaluated. Based on the above observations, the best optimized buflomedil hydrochloride-loaded adhesive matrix-type transdermal patch was further characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, X-ray diffraction study, and differential scanning calorimetry analyses. Drug containing adhesive matrix patches showed sustained release property without showing any incompatibility in adhesive matrix system. Hence, adhesive matrix-type transdermal patches of buflomedil hydrochloride can be used as a potential carrier for sustained transdermal delivery of hydrophilic drugs like buflomedil hydrochloride.

Evaluation of Luffa aegyptica mill Powder: A Novel Superdisintegrant in Delayed Release Tablets

2full factorial design was employed for the optimization of developed formulation. The developed formulations showed uniform appearance, average weight, drug content and adequate hardness. The increase in lag time was observed with an increase in HPMC concentration and decreased concentration of a superdisintegrant. Further comparison of Luffa aegyptica mill powder in the concentration suggested in the optimized formulation with pharmaceutically acceptable superdisintegrant in same concentration showed equivalent drug release behavior. It can be concluded from the outcome of the present research that Luffa aegyptica mill powder, a natural superdisintegrant, can prove to be best alternative to the existing superdisintegrants.

Tablet splitting: is it worthwhile? Analysis of drug content and weight uniformity for half tablets of 16 commonly used medications in the outpatient setting.

Tablet splitting is a well-established medical practice in clinical settings for multiple reasons, including cost savings and ease of swallowing. However, it does not necessarily result in weight-uniform half tablets. To (a) investigate the effect of tablet characteristics on weight and content uniformity of half tablets, resulting from splitting 16 commonly used medications in the outpatient setting and (b) provide recommendations for safe tablet-splitting prescribing practices. Ten random tablets from each of the selected medications were weighed and split by 5 volunteers (2 men and 3 women aged 25-44 years) using a knife. The selected medications were mirtazapine 30 mg, bromazepam 3 mg, oxcarbazepin 150 mg, sertraline 50 mg, carvedilol 25 mg, bisoprolol fumarate 10 mg, losartan 50 mg, digoxin 0.25 mg, amiodarone HCl 200 mg, metformin HCl 1,000 mg, glimepiride 4 mg, montelukast 10 mg, ibuprofen 600 mg, celecoxib 200 mg, meloxicam 15 mg, and sildenafil citrate 50 mg. The resulting half tablets were evaluated for weight and drug content uniformity in accordance with proxy United States Pharmacopeia (USP) specification (95%-105% for digoxin and 90%-110% for the other 15 drugs). Weight and drug content uniformity were assessed by comparing weight or drug content of the half tablets with one-half of the mean weight or drug content for all whole tablets in the sample. The percentages by which the weight and drug content of each whole tablet or half tablet differed from sample mean values were calculated. Other relevant physical characteristics of the 16 products were measured. A total of 52 of 320 half tablets (16.2%) and 48 of 320 half tablets (15.0%) fell outside of the proxy USP specification for weight and drug content, respectively. Bromazepam, carvedilol, bisoprolol, losartan, digoxin, and meloxicam half tablets failed the weight and content uniformity test; however, the half tablets for the rest of the medications passed the test. Mean percent weight loss after splitting was less than 1.5% for all drugs. Bromazepam, carvedilol, and digoxin showed the highest powdering loss during the tablet-splitting process. Tablet splitting could be safer and easier when drug- and patient-specific criteria have been met. Tablet size, shape, and hardness may also play a role in the decision to split a tablet or not. Tablets containing drugs with a wide therapeutic index and long half-life might be more suitable candidates for division. Dose variation exceeded a proxy USP specification for more than one-third of sampled half tablets of bromazepam, carvedilol, bisoprolol, and digoxin. Drug content variation in half tablets appeared to be attributed to weight variation due to fragment or powder loss during the splitting process.

Studies on Formulation and Evaluation of Transdermal Drug Delivery System of Nicorandil

In the present study, attempts were made to prepare and evaluate the matrix type transdermal patch of Nicorandil, an antianginal and antihypertensive drug using different ratios of polymer concentration of Eudragit RS100, Eudragit RL100, and Ethyl cellulose by the solvent evaporation technique by using 30% w/w of di-butyl phthalate, incorporated as plasticizer. In preformulation studies were determined. The transdermal patches were prepared and evaluated for appearance, weight uniformity, thickness, DSC, XRD, FTIR, Scanning electron microscopy, Water vapor transmission, tensile strength, swelling index, drug content uniformity, in-vitro permeation study through rat skin, skin irritation and stability studies. All the patches were thin, smooth, elastic and transparent/translucent, uniformity in drug content; weight and thickness were observed with their low SD values. The XRD analysis confirmed the amorphous dispersion of the drug. SEM analysis showed surface morphology. The prepared patches were permeable to water vapors. In-vitro drug permeation studies showed formulation UD11 has maximum permeation at the end of 24 hrs. It shown that drug release follows zero order. All the formulations were found to be stable with respect to drug content and physical changes at 400C and 75% RH.