Immediate Release Tablet Formulation Research Articles

Development and evaluation of physical and release properties of a tablet formulation containing dry hydroethanolic extract from Lippia alba leaves

The development of an immediate-release solid formulation which contains natural products is a challenge considering several variables. These include the physical properties of the drug, the complex composition of the herbal extracts, and its ability to be released in the body. The present study describes the development and characterization of an immediate-release tablet formulation of a hydroethanolic extract of Lippia alba (Mill.) N. E. Br. dried leaves which possess potential gastroprotective properties and sedative effects. L. alba is a Brazilian herb known as “cidreira,” and the ethnopharmacological use of the leaf infusion has been reported in many South and Central America countries. However, no study has considered phytotherapeutics containing extracts of this herb. To achieve this goal, 14 solid formulations were produced using direct compression, wet granulation, or dry granulation. These were characterized by physical tests, such as average weight, friability, hardness, and disintegration tests. The tablet formulation produced by the dry granulation of 100 mg of the L. alba extract exhibited better physical properties, and it was characterized using acteoside (verbascoside) as a chemical marker, presenting 6.9 % w/w of acteoside content per tablet, corresponding to 41.3 mg of this constituent per unit. This formulation dissolves rapidly in simulated gastric fluid without enzymes, achieving amounts >80 % after 20 min. Thus, an immediate-release tablet formulation with L. alba extract was successfully prepared.

Formulation, Characterisation and Evaluation of the Ethosuximide Oral Immediate Release Tablets

The present study is aimed to formulate, characterization, and evaluate oral immediate-release tablets of Ethosuximide. It is employed as an anti-epileptic agent used in the treatment of epilepsy, in all the age groups who were≥ 1 year. The dosage form is formulated by directly compressing the blend and granulating the powder blend by wet granulation methods. The optimized formulation is achieved by the trial and error method by changing the concentration of lactose monohydrate and di-basic calcium phosphate dehydrate as diluents, sodium starch glycolate as Super-dis-integrant, rice Starch as an intra-granular binder, hydroxypropyl cellulose as binder talc as a lubricant. Evaluation parameters such as micrometric properties, disintegration time along with in-vitro drug release studies were performed for characterizing the dosage form. In-vitro drug release studies were carried out using 0.1 N HCl as dissolution media with 75 rpm and temperature of 370C ± 50C by employing USP apparatus II (Paddle type). Estimation of the % drug release of the tablet was carried out using the UV method. The prepared formulation and the marketed formulation were tested for the in-vitro drug release profile and the prepared formulation was compared with the marketed formulation. All the evaluated result was found to be within the specifications. Therefore, from the obtained evaluation results F6 trail was selected as the best formulation.

Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method

To evaluate and compare the pharmacokinetic (PK) characteristics of a newly developed oral osmotically controlled drug delivery system of Eperisone 150 mg tablets with Eperisone immediate release (IR) marketed tablet brand as a reference formulation. It was a single dose, two treatment, two sequence, randomized, crossover study, involving 12 healthy human subjects. A modified, sensitive LC-ESI-MS/MS method was developed and validated as per FDA guidelines for estimation of Eperisone in plasma using a simple extraction and quick protein precipitation method. Non-compartmental pharmacokinetic model was used for PK analysis. Results were statistically compared using logarithmically transformed data, where p > 0.05 was considered as non-significant with 90% CI limit of 0.8–1.25. The bio-analytical method used for estimating drug plasma concentration was found to be simple, selective, linear, accurate and precise with 0.01 ng/ml as limit of detection. The comparative PK analysis revealed an insignificant difference in AUC0-∞, AUC0-t, Vz/F, Cl/F and t1/2λz, whereas a significant difference in Cmax, Tmax and MTTs were found. The relative bioavailability of Eperisone osmotic tablet was 109.7%. The osmotic controlled release drug formulation was found to release Eperisone for an extended period with less inter individual fluctuation in pharmacokinetic variables.

Formulation and Evaluation of Immediate Release Tablet of Simvastatin

Simvastatin is an Antilipidemic agent. The aim is to formulate and evaluate immediate release Simvastatin tablets prepared by wet granulation method. Sodium starch glycolate and crosscarmellose sodium were used as superdisintegrants. Formulations were prepared by Simvastatin with different concentration (1%, 2% and 3%) of crosscarmellose sodium and sodium starch glycolate. Formulations were evaluated for different pre and post compression parameter and in vitro drug release studies. The FTIR studies showed that there is no interaction between the drug and polymer. The results of pre compression parameters of batch I1 to I6 were compared with prescribed limits. It showed that batch I1 to I6 powder blend exhibit good flow property and compressibility property. In formulation I1-I6, disintegration time was observed 3–8 min and 100% drug released within 10–60 min time interval. Thus, based on evaluation of different parameters it was concluded that formulation of immediate release tablets of Simvastatin was successfully done and I2 showed almost 100% drug release at 10 min.

Formulation development and evaluation of immediate release tablet of terbinafine hydrochloride

The immediate release tablet of antifungal drug Terbinafine hydrochloride were prepared developed and evaluated to increase solubility and bioavailability of low soluble drug by using wet granulation method. The tablets were prepared by varying concentrations and compositions of microcrystalline cellulose, sodium starch glycolate, hydroxyl propyl methyl cellulose, magnesium stearate, and colloidal silicon dioxide for seven trial batches. The drug excipient compatability study was studied by photostability study. No significant changes were observed in photostability study. The tablets were evaluated for disintegration test, content uniformity, and friability. Invitro drug release profile Terbinafine hydrochloride was examined in four different media PH0.1N HCL, PH4.5 acidic buffers, PH6.8 phosphate buffer and PH3.0 citrate buffer for 45 minutes. The drug release for trial batch no.7 shows 100.4% of drug release and innovator shows 102% of drug release. The formulation trial no 6 and 7 showed no significant changes during the study period of accelerated stability study for 3 months. The result of all formulation 7 showed that good developed formulation of immediate release tablet containing Terbinafine hydrochloride drug was similar to the marketed product with all respect and stable to effect of temperature and humidity.

In Vitro Comparative Quality Evaluation of Non-Expired and 10 Years-Expired Lamotrigine Immediate-Release Tablet Formulations - Pilot Study

In Vitro Comparative Quality Evaluation of Non-Expired and 10 Years-Expired Lamotrigine Immediate-Release Tablet Formulations - Pilot Study

Formulation and Evaluation of Ritonavir Immediate Release Tablets by Hot Melt Extrusion Method

In the present work, an attempt has been made to develop immediate release coated tablets of Ritonavir by hot met extrusion method using 16 station rotary tablet punching machine. The blend of all the formulations showed good flow properties such as bulk density, tapped density. The prepared IR coated tablets of ritonavir shown good post compression parameters. They passed all the quality control evaluation parameters as per USP limits. Among all the formulations, F5 formulation showed maximum % drug release i.e., 99 % in 120 mins hence it is considered as optimized formulation. The optimized formulation was compared to innovator tablets. Keywords: Ritonavir, HPMC, Ethyl cellulose, Copovidone immediate release tablets.

Formulation and evaluation of immediate release tablet of zopiclone using wet granulation method

Zopiclone, a cyclopyrolone, is a non-benzodiazepine derivative used as a hypnotic agent in the treatment of short term insomnia. The main objective of the present investigation was to formulate a pharmaceutically active stable and bioequivalent immediate release (IR) tablets of zopiclone using wet granulation method. The prepared formulations were evaluated using various physical parameters, equipment, dissolution study and drug release profile. The basic approach used in development of zopiclone IR tablets was that the use of superdisintegrants as like Corn starch (maize) and Sodium starch glycolate which provide instant disintegration after administration. In-vitro dissolution testing study was carried out for 1 hours using 0.1N HCl in a dissolution apparatus for evaluation of Drug release. On the basis of the dissolution profile, F3 gives a better result and were found 100 % release in just 20 minutes and also found that as the polymer ratio were increases the drug release rate also increased from the formulation. Keywords: Hypnotic agent, immediate release, Wet granulation Method, Non-benzodiazepine derivative, Superdisintegrants, Zopiclone

Formulation and Evaluation of Ethionamide Immediate Release Tablets

Due to the lack of complexities of production and introduction schedule for the patient, solid dosage form i.e. tablets are very popular all over the globe. Most of the prescriber prefers solid dosage form in their prescription and 50% of total prescription contains compressed tablets. Immediate release tablets are those which separate promptly and get dissolved to release the medicaments based on a single or multiple-unit reservoir or matrix system, in a little period of time. This research was conducted with the primary objective of formulation and evaluation of immediate release tablet of Ethionamide 250mg. Immediate release tablets of Ethionamide were formulated by using wet granulation and direct compression method using microcrystalline cellulose as diluents, povidone as the binder, Croscarmellose sodium as a disintegrant, colloidal silicon dioxide as glidant/disintegrant and Mg(C18 H35O2)2 as a lubricant. Characterizations of blends were done by using different parameters. The compressed tablets were analyzed for physicochemical parameters. Thicknesses of all tablets were almost similar in all formulations and were found in a range of 5.11 to 5.20 mm. Hardness of tablets of each batch ranges between 9.28 to 10.32 KP. The Friability values of each formulation were less than 1% i.e. considered as satisfactory value and the values were 0.393 to 0.28%. Percentage of active ingredient in all formulation ranges from 96.7 to 99.8%. The results obtained confirmed that formulation F10 containing Ethionamide-250mg, microcrystalline cellulose-281mg, povidone-30mg, colloidal silicon dioxide-3mg, Croscarmellose sodium-30mg and Mg(C18 H35 O2)2-6mg was the best amongst the rest. The best prepared formulation i.e. F10 was again compared with Trecator, a marketed tablet containing Ethionamide. The dissolution profile of the formulation F10 was found to possess an equivalent quantity of drug release when compared to the innovator product.

Formulation and Evaluation of Immediate Release Tablet of Efavirenz by Micellar Solubilization Technique

Formulation and Evaluation of Immediate Release Tablet of Efavirenz by Micellar Solubilization Technique

Formulation and Evaluation of Immediate release tablets of Topiramate using Sodium starch glycolate

The aim of the current study was to develop immediate release tablets (IRT) of topiramate using different concentrations of sodium starch glycolate (SSG) as super disintegrant. Four different formulations of IRT were prepared using wet granulation method. Different pre compression and post compression characterization of tablet was carried out. In vitro drug release studies were carried out in USP II paddle type dissolution apparatus for different formulation and the batch containing 7.5 mg of SSG per tablet gave maximum amount of drug release of 90.76% at the end of 50 mins. Drug and excipients compatibility studies were carried out through FTIR spectroscopy. FTIR spectroscopy studies revelled that there is no interaction between drug and different excipients used in formulation. Short term stability studies (at 40±2oC/75±5% RH) on the best formulation indicated that there were no significant changes in release profile and drug content after a period of one to three month. Among all the formulations, F4 formulation was finally optimized.

SOLUBILITY ENHANCEMENT, FORMULATION DEVELOPMENT AND EVALUATION OF IMMEDIATE RELEASE TABLET OF ANTIHYPERTENSIVE DRUG TADALAFIL

The objective of the study was to enhance the solubility and dissolution rate of Tadalafil using hydrophilic carriers such as PVP K-30, Poloxamer 188, Sodium starch glycolate and compatibility study of Tadalafil with different polymers by FTIR. Characterization of solid dispersion-FTIR, DSC and phase solubility analysis was study to improve the oral bioavailability. Formulation and evaluation of immediate release tablets prepare from solubility enhanced Tadalafil. Among the various approaches Solvent evaporation has gained good acceptance in recent years in the industry for enhancing the solubility and dissolution rate of poorly soluble drugs. Poloxamer 188 used as polymer as it is good solubilizing agent. As per the phase solubility studies, a 32 factorial study were used to prepare the immediate release tablet and evaluated for the interactions and in vitro drug release. Sodium Starch Glycolate and PVP used as superdisintegrants. The solubility of tadalafil in selected ratios containing tadalafil and Poloxamer 188 solid dispersion prepared by solvent evaporation was determined. From the various ratios 1:0.5 was resulted in a much higher enhancement (9.75folds). Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) studies conducted, explain overall drug and excipients compatibility. More than 90% of tadalafil was released from IR tablet within 30 min. There is enhancement of the solubility rate if tadalafil by solid dispersion with Poloxamer 188 prepared by solvent evaporation method. The compatibility studies of the drug and polymers showed that there was no incompatibility between them. Wet granulation method showed that, the desired flow properties for the compression into tablets. Tablets were prepared using wet granulation method resulted into simple, cheap, more suitable method for the manufacturing immediate release dosage form.

EVALUATION OF A MODIFIED BIOMATERIAL OF TYMPANOTONUS FUSCATA SHELL POWDER II: FORMULATION OF PYRIMETHAMINE AND PYRIDOXINE HYDROCHLORIDE TABLETS

A novel modified biomaterial of periwinkle shell powder, MBPSP was developed from Tympanotonus fuscata . It was assessed as a bulking agent in the formulation of pyrimethamine and pyridoxine hydrochloride tablets adopting dicalcium phosphate dihydrate (DCP) as a standard. A 100 g of the ground periwinkle shell was broken down in 166.0 ml of 2 M hydrochloric acid, clarified and treated with 5 M sodium hydroxide. The thick white precipitate obtained was washed severally and to it, ortho-phosphoric acid was dropped in bits until a thick, dehydrated bulk was attained which was dried at 60 o C and classified with 250 μm sieve. The product was coded MBPSP. Two batches of granules containing pyrimethamine (25 mg) and pyridoxine hydrochloride (50 mg) were generated by the wet granulation employing MBPSP alongside DCP. The granules were lubricated with magnesium stearate and talc and compacted into tablets at 7.55kN using a 10.50 mm diameter die and flat-faced punch fixed in a hydraulic hand press. The tablet produced were evaluated using the British Pharmacopoeia specifications. The weight variation for the pyrimethamine or pyridoxine hydrochloride tablets containing MBPSP or DCP were 0.06, 0.1, 0.097 and 0.143 % respectively. The total drug content for the individual lots of tablets for either pyrimethamine or pyridoxine hydrochloride was within 85.00-115.00 % of their label claim. Higher mechanical strength were noted for the batch of tablets manufactured with DCP and containing pyrimethamine and pyridoxine hydrochloride than MBPSP. Though the entire batches of tablets for the two drugs manufactured with either MBPSP or DCP disintegrated in less than 5.00 min with no significant difference in their individual disintegrating time (p>0.05), pyridoxine hydrochloride tablets prepared with DCP disintegrated in lesser time when compared to MBPSP (p<0.05). Only the pyrimethamine tablets prepared with MBPSP attained 75.00 % drug release in 45.00 min in line with the United States Pharmacopoeia (USP) criteria. Therefore, MBPSP could be another very useful bulking agent in the formulation of pyrimethamine immediate-release tablets by the wet granulation technique. Keywords : Modified biomaterial, Tympanotonus fuscata, periwinkle, shell, pyrimethamine, pyridoxine hydrochloride, tablet.

EVALUATION OF A MODIFIED BIOMATERIAL OF TYMPANOTONUS FUSCATA SHELL POWDER I: FORMULATION OF THEOPHYLLINE HYDRATE AND HYDROCHLOROTHIAZIDE TABLETS.

A modified biomaterial of periwinkle shell powder, MBPSP derivative of Tympanotonus fuscata shell was applied as a diluent in theophylline hydrate (TPH) and hydrochlorothiazide (HCTZ) tablets. A 100 g of the pulverized periwinkle shell was digested with 166.0 ml of 2 M hydrochloric acid, filtered and neutralized with 5 M sodium hydroxide. Ortho-phosphoric acid was added drop wise until a thick, dehydrated mass was obtained. It was dried at 60 o C and milled to 250 I¼m size and designated as MBPSP. Using this, batches of granules containing TPH (100 mg) and HCTZ (50 mg) were produced by the wet granulation technique alongside lactose and dicalcium phosphate dihydrate (DCP). They were tableted at 7.55kN using a 10.50 mm diameter die and flat-faced punch on a hydraulic hand press. Tablet properties were evaluated. The weight variation for the TPH or HCTZ tablets produced from MBPSP, lactose or DCP were between 0.03- 0.32 %. The total drug content for the respective batches of tablets was within 85-118 % of the claimed label potency. Though the respective batches of tablets of TPH and HCTZ containing MBPSP, lactose or DCP maintained significantly high values of mechanical strength, the tablets of TPH and HCTZ prepared with DCP generally showed significantly higher values of mechanical strength than those of MBPSP and lactose. Dissolution profile showed that at 45.00 min, 73.13, 87.72 and 87.45 % of TPH was released from the tablets containing lactose, MBPSP and DCP respectively while at 60.00 min, 64.58, 57.84 and 66.00 % of HCTZ was dissolved from the tablets having lactose, MBPSP and DCP respectively. Though MBPSP compared significantly favourably with lactose and DCP in the various tablet parameters evaluated, the tablets of TPH or HCTZ comprising MBPSP displayed very significant shorter tablet disintegration time and also maintained a significantly greater mechanical strength in comparison to lactose and DCP. Therefore, MBPSP could be a very useful excipient in the formulation of TPH and HCTZ immediate-release tablets. Keywords: Modified biomaterial, Tympanotonus fuscata, periwinkle, shell, theophylline hydrate, hydrochlorothiazide, tablet.Â

Formulation and evaluation of immediate release tablet of risperidone

The main objective of the present investigation was to formulate Risperidone immediate release tablet. Risperidone, an antipsychotic drug mainly act as a D2 and 5HT2A receptor antagonist. Superdisintegrants agents like kollidon and citric acid were used and compressed into tablet by direct compression method. Risperidone is mainly used to treat schizophrenia bipolar disorder. The six formulations having different concentration of superdisintegrants were prepared and formulation blend was examined for angle of repose, bulk density tapped density and compressibility. The tablet were evaluated for various parameters like hardness, thickness, friability, weight variation, disintegration time and invitro dissolution time, all the parameter were found within limits.

Correlation of dissolution and disintegration results for an immediate-release tablet

The drug release rate of a rapidly dissolving immediate-release tablet formulation with a highly soluble drug is proposed to be controlled by the disintegration rate of the tablet. Disintegration and dissolution test methods used to evaluate the tablets were shown to discriminate manufacturing process differences and compositionally variant tablets. In addition, a correlation was established between disintegration and dissolution. In accordance with ICH Q6A, this work demonstrates that disintegration in lieu of dissolution is suitable as the drug product quality control method for evaluating this drug product.

Formulation and Evaluation of Immediate release Tablets of Dasatinib using Croscarmelose Sodium

The objective of the present study was to develop an immediate release tablet of Dasatinib using different concentrations of cross carmelose sodium (CCS) as superdisintegrant with a view to gain rapid disintegration in gastric pH for treatment of chronic myeloid leukemia (CML) and acute myeloid leukemia (AML).Five different formulations of Dasatinib immediate release tablets were prepared using wet granulation method. Different pre compression and post compression characterization of tablet was carried out. In vitro drug release studies were carried out in USP II paddle type dissolution apparatus for different formulation and the batch containing 5% CCS gave maximum amount of drug release of 99.14%.Drug and excipients compatibility studies were carried out through FTIR spectroscopy. FTIR spectroscopy studies reveled that there is no interaction between drug and different excipients used in formulation. Short term stability studies (at 40±2oC/75±5% RH) on the best formulation indicated that there no significant changes in drug content.

Single-dose Pharmacokinetic Properties and Relative Bioavailability of a Novel Methylphenidate Extended-release Chewable Tablet Compared With Immediate-release Methylphenidate Chewable Tablet

PurposeA novel methylphenidate hydrochloride extended-release chewable tablet (MPH ERCT) was developed to potentially address an unmet need for patients with attention-deficit/hyperactivity disorder, especially children, who cannot or will not swallow tablets or would prefer the convenience of a chewable tablet. This randomized, open-label, crossover trial compared the pharmacokinetic properties and relative bioavailability of MPH ERCT with an MPH chewable immediate-release tablet (IR MPH) formulation in healthy adults. MethodsHealthy men and women 18 to 55 years of age were randomly assigned to MPH ERCT 40 mg or 40 mg IR MPH administered in 2 equal doses of 20 mg 6 hours apart with a 7-day washout period. Plasma concentrations of MPH at selected time points up to 24 hours were measured, and pharmacokinetic parameters were determined using a noncompartmental approach in the SAS (Version 9.2) PROC general linear model procedure. FindingsA total of 33 participants were enrolled in the study; 31 participants were included in the pharmacokinetic analysis. The exposure ratios for MPH ERCT and IR MPH (MPH ERCT/IR MPH) for area under the analyte concentration versus time curves (AUC) from time zero to the last measurable analyte concentration (AUC0–last) (87.64%; 95% CI, 84.96–90.41) and AUC0–∞ (89.11%; 95% CI, 86.57–91.73) were within the standard 80% to 125% bioequivalence acceptance criteria. Mean Cmax for MPH ERCT and IR MPH was 12.51 ng/mL and 15.57 ng/mL, respectively; mean time to Cmax was 4.16 hours and 6.43 hours, respectively. The mean Cmax of MPH ERCT was 80% of the Cmax of IR MPH due to a higher peak concentration that occurs after the second dose of IR MPH. All adverse events were mild in severity. ImplicationsThe relative bioavailability of MPH ERCT 40 mg, based on the exposure (AUC), was comparable to that of IR MPH 40 mg administered in 2 equal doses of 20 mg 6 hours apart. Both formulations were generally well tolerated.

English

English

Onset of analgesia and efficacy of ibuprofen sodium in postsurgical dental pain: a randomized, placebo-controlled study versus standard ibuprofen.

Objectives:A novel, immediate-release tablet formulation of ibuprofen (IBU) sodium dihydrate, Advil Film Coated Tablets (IBUNa), has been developed that is absorbed faster than standard IBU tablets. The objective of the current study was to compare the efficacy and onset of analgesia of this new formulation with standard IBU tablets after a single dose.Materials and Methods:Patients (N=316) with at least moderate baseline postsurgical dental pain were randomized to 400 mg IBUNa, Advil (IBUAdv), Motrin (IBUMot), or placebo. Primary endpoints were time-weighted sum of pain relief (PR) and pain intensity differences over 8 hours (SPRID 0-8) and time to onset of meaningful pain relief (TMPR) measured by the double-stopwatch method.Results:SPRID 0-8 was significantly greater for IBUNa and the other active treatments versus placebo (P<0.001). IBUNa had a significantly earlier TMPR versus placebo, pooled IBUAdv/IBUMot, and IBUMot (P<0.001 for all), and a marginally faster TMPR (P=0.075) versus IBUAdv. Results for secondary endpoints were similar. Adverse events were comparable across treatment groups, with gastrointestinal disorders being most frequently reported. Most adverse events were mild or moderate.Discussion:This novel formulation of IBUNa provided superior overall PR compared with placebo and more rapid onset of analgesic effect compared with standard IBU tablets. Rapid PR is important in the treatment of acute pain, including dental pain, and this IBUNa formulation represents a new treatment option for rapid PR.