Coated Tablet Formulations Research Articles

Zileuton compression coated tablets : formulation development and in vitro evaluation

In the present research work Zileuton tablets were formulated by employing compression coating technology. Initially the core tablets were prepared by using various concentrations of super disintegrates, the formulated core tablets were coated with the polymers by using compression coating technology. All the core and compress coated tablet formulations were subjected to various physical and chemical evaluation tests for core and compress coated tablets. The thickness, hardness and weight variation shown by all the tablet formulations were found within the official pharmacopoeial limits. In vitro release of Zileuton of core tablet formulations ZF5 showed faster drug release after 15 min. Faster drug release can be correlated with the high disintegration and friability observed in this study.

Formulation of Coated Tablets Film of Jengkol Fruit Seeds (Pithecellobium lobatum Benth.) as A Selenium Herbal Supplement

The correlation between the high content of selenium (Se) in plasma and the low prevalence of cardiovascular disease has been published in previous epidemiological studies. The content of Se in the plasma is determined by daily intake. A preliminary surveillance of Se content of several plants showed that the seeds of jengkol (Pithecellobium lobatum Benth.) has the highest concentration of Se. This study aims to develop a pharmaceutical formulation of Se supplement for adjuvant therapy of cardiovascular disease. The jengkol seeds was made into film coated tablets with a wet granulation method. Optimization of the core tablet formula was carried out with variations of binder concentration and coating material. Evaluation was carried out on uniformity of size and weight, disintegration time, hardness and friability. The content evaluation was carried out including the levels of Se, water content, ash, fat, protein, carbohydrate and crude fiber. The results showed that the F3 had the lowest friability and highest hardness. The coating of tablets using PVA has covered the smell of jengkol seed. The evaluation results showed that film coated tablets contained the Se level content of 0.074 ± 0.004 µg/g, water content of 2.19%, ash content of 1.88%, fat content of 0.89%, protein content of 0.66%, carbohydrate content of 94.38% and crude fiber content 1.79%. The results showed that the jengkol seed film coated tablet formulation could be used as a supplement in additional therapy for cardiovascular disease.Keywords : Pithecellobium lobatum, film coated tablet, herbal supplement, selenium

Pharmacokinetic study of a novel oral formulation of S-adenosylmethionine (MSI-195) in healthy subjects: dose escalation, food effect and comparison to a commercial nutritional supplement product

BackgroundA novel, high bioavailability oral, enteric coated tablet formulation of S-adenosylmethionine (MSI-195) has been developed for life science application. The present research reports on a Phase 1 study to (i) determine the safety of single doses of MSI-195 (ii) to determine the dose proportionality of MSI-195 at doses of 400, 800 and 1600 mg (iii) determine the pharmacokinetics of MSI-195 compared with a commercial reference product (SAM-e Complete™) over 24 h and (iv) to determine the effect of food on the pharmacokinetic profile of MSI-195 in human subjects.MethodsThis study was a pharmacokinetic and safety evaluation of MSI-195 and a commercial comparator broken into two stages. The first stage was an exploratory single ascending dose design of MSI-195 in 8 healthy normal male volunteers. The second stage was a single dose evaluation, targeting 26 male and female volunteers at set doses of MSI-195 and commercial comparator in a cross-over design followed by a food effect study on MSI-195. Plasma samples were collected and assayed for S-adenosylmethionine using a validated HPLC method with MS/MS detection. The main absorption and disposition parameters were calculated using a non-compartmental approach with a log-linear terminal phase assumption. Statistical analysis was based on an ANOVA model or t test as appropriate.ResultsMSI-195 was found to be generally well tolerated with an adverse event profile similar to the SAM-e Complete™ comparator product. The relative bioavailability of MSI-195 was approximately 2.8-fold higher than SAM-e Complete based on area under the curve (AUC) ratios for the two products and the MSI-195 formulation exposure based on AUC was found to be approximately dose proportional. There was a significant food effect for MSI-195 with a delayed time to maximum absorption Tmax, going from 4.5 h under fasted conditions to 13 h under fed conditions, and area under the curve with food reduced to 55% of that seen under fasting conditions.ConclusionsThe overall conclusion was that MSI-195 was well tolerated and has markedly higher bioavailability compared with both the SAM-e Complete™ commercial product tested and, on a per mg basis, products reported in other literature.Trial registrationClinicalTrials.gov, identifier NCT04623034. Retrospectively registered Nov 9, 2020.

Bioavailability study of two 81-mg coated tablet formulations of acetylsalicylic acid in fed healthy subjects

To perform a comparative bioavailability study between a test (re-formulation) and a reference acetylsalicylic acid formulation (Ecasil-81, 81mg coated tablet) in healthy subjects under fed condition. Healthy subjects (n=48) were included in this monocentric, open-label, randomized, two-way crossover pharmacokinetic study. They received a single 81-mg oral dose of a test or a reference formulation of acetylsalicylic acid under fed condition, with a 7-day washout period between the treatments. Blood samples were collected over a period of 36 hours. The salicylic acid plasma concentration was measured by liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). Pharmacokinetic analysis was performed using WinNonlin software. The geometric mean and 90% confidence interval of test/reference formulation ratios were 109.32% (102.54-116.54%) and 106.94% (102.97-111.07%) for salicylic acid Cmax and AUC0-last, respectively. Food decreased the AUC and Cmax (p<0.001) and delayed the tmax (p=0.0077). The investigated women presented higher AUC0-∞ and Cmax values (p<0.001) than men. The clinical and laboratory exams did not show significant alterations. The re-formulation is bioequivalent to the reference formulation regarding the absorption extent and rate in fed healthy subjects. The administration of acetylsalicylic acid with food decreased its bioavailability. Moreover, differences in salicylic acid disposition related to sex were observed. The treatments were well tolerated by the investigated subjects.

Formulation and In-Vitro Evaluation of Enteric Coated Tablet Incorporating Rabeprazole

The objective of the work is to try and assess the applicability and manufacturing possibilities to optimize an enteric coated tablet formulation containing Rabeprazole sodium as the drug aiming at the anti-acidity activity with desired drug release properties. Enteric coated tablet was chosen as dosage form being a cost-effective technology for pharmaceutical industry requiring fewer procedures. Before the implementation of the pharmaceutical technological aims, analysis of critical factors influencing the manufacture was carried out. Reproducible manufacturing processes are required to achieve suitability and tablets uniformity to achieve the uniform properties of tablets, which could influence experimental parameters. Rabeprazole in core content of tablet is blended with HPMC (different grades), xanthan gum, PVPK30, mannitol, crosspovidone, Sodium starch glycolate, Colloidal silicon dioxide to formulate the product. Prepared formulation was tested for weight and content uniformity, physical characteristics, in vitro dissolution behaviour, acid resistance and accelerated stability studies. All studies performed resulted and revealed for assurance of such enteric coated tablet formulation for drug Rabeprazole with optimum characteristics, concluding it as a promising approach to enhance drug release characteristics.&#x0D; Keywords: Rabeprazole, HPMC, enteric coated tablets, In Vitro evaluation.

Design and Evaluation of Time Dependent Delayed-Release Diclofenac Sodium Tablets for Chronopharmaceutical Drug Delivery

This research was aimed atformulatingand evaluating time dependent delayed-release diclofenac tablets forchronopharmaceutical drug delivery using press-coating technology. Rapiddisintegrating diclofenac core tablets were initially formulated using the directcompression method. Coats of powdered tragacanth or xanthan gum alone, and incombination in variousmixing ratios of 25:75, 40:60, 50:50 and 75:25 were compressed around the coretablet to form 3- layered tablets. Thepress-coated tablets were evaluated for post compression parameters such asweight variation, crushing strength, friability as well as, swelling index, lagtime and in vitro release studies in three different simulated gastro-intestinalfluids. The result revealed that thecore and compression coated tablet formulations were within the officialspecified limits. The release profile of the press coated tabletsexhibited lag times depending upon the type, amount and polymer combinationratio in the tablet coat. Optimizationwas done using analysis of variance (ANOVA). The optimizedbatch F6 which consisted of 40% xanthan and 60% tragacanth gave a lag time of 6h followed with burst release and complete drug release of 98.51%. Thisresearch shows that press-coated diclofenac tablets with 40:60% xanthan andtragacanth gum coat can be exploited in chronopharmaceutical delivery ofdiclofenac sodium.

Determination of Organic Volatile Impurities in Twenty-Three Different Coated Tablet Formulations Using Headspace Gas Chromatography with Flame Ionization Detection Technique

Organic solvents are extensively used in manufacturing processes of pharmaceutical formulations that cannot be completely eliminated from the product due to physical and chemical barriers. These solvents have no therapeutic value and may be toxic to human body if intake exceeds the permitted daily exposure. Therefore, a simple and sensitive method for simultaneous determination of methanol, acetonitrile, methylene chloride, n-hexane, cyclohexane, xylene, chloroform, nitromethane, toluene and pyridine was developed and validated. Separation was achieved on HP-Innowax polyethylene glycol gas chromatographic column (30 m × 250 μm × 0.25 μm) using Agilent 7890B gas chromatograph equipped with Agilent 7697A headspace auto-sampler and flame ionization detector. Twenty-three marketed coated tablet formulations (containing diclofenac sodium, Loratadine or montelukast sodium as active ingredient) were tested for the presence of volatile organic impurities using this method. Excellent results were obtained, within the globally accepted validation reference values, particularly taking into account the low concentration levels were investigated in twenty-three coated tablet formulations.

Design, Development and Evaluation of Enteric Coated Tablets of Glimepiride

The main objective of work was to develop pharmaceutically elegant and stable enteric coated tablet formulation for highly unstable drug in acidic environment using pH dependent polymer. Development of Enteric coated tablets were done for Controlled Release of drug. Coating was done by using methacrylic acid copolymer (Eudragit L 100). Characterization of Drug and Excipients was carried out including compatibility studies of drug and excipients. Solid dispersion of glimepiride was formulated using carrier PEG20000 was prepared by the Fusion method. Evaluation of Solid was carried out using suitable parameters like solubility, percentage yield, drug content, in-vitro drug release, FTIR and SEM. Further granules were formulated from the optimized batch of formulated SDs. Pre-compression studies of granules were carried out like Tapped density, Bulk density, Angle of repose, etc. of Granules. Four different batches were formulated of tablets. The tablets were evaluated for various parameters like weight variation, hardness, friability, thickness, disintegration and in-vitro drug release. For Dissolution studies, 7.4 phosphate buffer media was used. The optimized batch of tablets was further subjected to enteric coating using pan coating. Eudragit L100 was used as coating polymer and isopropyl alcohol, acetone and triethyl citrate were used as vehicle in solution. Eosine was used as colorant. The coating solution was prepared in three different concentrations viz., 1%, 2%, and 3%. The coating solution was sprayed on tablets using spray gun and after drying the tablets were evaluated for different parameters like in-vitro drug release and disintegration, Hardness, thickness, friability, drug content and weight variation. Here, as the tablet was enteric coated, 2 dissolution medias were used 7.4 phosphate buffer and 0.1 N HCl. Further Stability studies were carried out of optimized batch. Results obtained after the stability studies confirmed that prepared enteric coated tablets were stable at applied conditions and were complied with the initial results.

Comparative Bioavailability Study of Two 81 mg Coated Tablet Formulations of Acetylsalicylic Acid in Fasting Healthy Volunteers

Introduction: Low-dose acetylsalicylic acid is used as antithrombotic agent and the enteric-coated formulations are widely used to minimize the gastrointestinal side effects. Aim: To compare the bioavailability of two acetylsalicylic acid formulations (Ecasil-81®, 81 mg coated tablet) in fasting healthy volunteers. Methods: Healthy volunteers (n=16) were recruited to a monocentric, open label, randomized, two-way crossover pharmacokinetic study, with seven days washout period between the treatments. They received a single 81 mg oral dose of a test (new formulation) or a standard reference formulation of acetylsalicylic acid (Ecasil-81®) after about 8 h fasting. Blood samples were collected over a period of 36 h. The salicylic acid plasma concentration was evaluated by high-performance liquid chromatography coupled to tandem mass spectrometry (HPLC-MS/MS). Noncompartmental pharmacokinetic analysis was performed using the WinNonlin program. Results: The maximum plasma concentration (Cmax) of salicylic acid was 5433 and 5719 ng/mL reached in 3.66 and 4.02 h (tmax) for the test and the reference formulation, respectively. The 90% confidence interval of the ratios of geometric means of Cmax and area under curve of plasma concentration until the last concentration observed (AUC0- last) were within the interval 80-125%. Conclusion: The new acetylsalicylic acid formulation has a bioavailability equivalent to the reference formulation for the rate and the extent of absorption.

Chronotherapeutic Drug Delivery of Ezetimibe Using Press Coating Technology

In the present research work pulsatile drug delivery system of Ezetimibe tablets were formulated by employing compression coating technology. Initially the core tablets were prepared by using various concentrations of super disintegrants, the formulated core tablets were coated with the polymers by using compression coating technology. All the core and press coated tablet formulations were subjected to various evaluation tests. The inner core formulated with ethyl cellulose and outer core with Eudragit L- 100. Invitro release of Ezetimibe of core tablet formulations F4 was optimized and showed less amount of drug release during lag time. Time dependent pulsatile drug delivery system has been achieved from tablet of formulation F4 which meets demand of chronotherapeutic for drug delivery.

Formulation Development and Optimization of Febuxostat Tablets by Direct Compression Method

ABSTRACTThe aim of this study was to develop a simple and cost‐effective Febuxostat film coated tablet formulation by the direct compression method. To obtain the best optimized product, nine different formulations were developed using a central composite rotatable design. Avicel PH‐102, Magnesium stearate, and croscarmellose sodium were taken as independent variables. Micromeritic properties of powder blend showed excellent flow properties and were within USP limits. Tablets were compressed and before coating the core was tested for weight variations, hardness, thickness, friability disintegration, and dissolution. Tablets were film coated using hydroxypropyl methylcellulose 5cps, titanium dioxide, polyethylene glycol, and Instacoat blue, and again tested for the weight variations, assay, and single point dissolution. Three different dissolution media, i.e., 0.1 N HCl (pH 1.2) and phosphate buffer pH 4.5 and 6.8, were used for calculating the percentage release of Febuxostat and their release pattern was compared with an innovator brand by using the model‐independent methods such as similarity (f2), dissimilarity (f1), and model‐dependent methods such as first‐order, Hixson Crowell, and Weibull methods. The results revealed that Trial‐06 showed the maximum similarity, i.e., 81.18, 75.15, and 67.19 in three different pH dissolution media. Dissimilarity factor was also comparable in Trial 06, i.e., 5.21, 11.27, and 6.01 at pH 1.2, 4.5, and 6.8, respectively. Model‐dependent approaches showed the maximum r2 values for Trial 06, i.e., greater than 0.900 for all models in the above‐mentioned pH, whereas the overall release kinetics followed the Weibull model. Selected formulation was kept at 40 ± 5°C and 75 ± 2% relative humidity for accelerated stability studies, and no specific change was observed.

Formulation Development and Evaluation of Enteric Coated Tablets of Rabeprazole Sodium

Rabeprazole sodium is highly acid-labile and presents many formulation challenges and to protect it from acidic environment of the stomach an enteric coated tablet formulation is tried in the present study. This study is aimed to develop pharmaceutically equivalent and stable enteric-coated tablets of Rabeprazole sodium comparable to innovator product. Different Formulations of Rabeprazole core tablets were developed using mannitol as diluent and croscarmellose as super disintegrant in different proportions. Further optimized formulation was coated with varying the compositions of sub coating and enteric coating using opadry white and enteric yellow. Compatibility studies were performed for drug, physical mixture tablet which shows no interaction. From the dissolution the formulation F6 shows highest percentage of drug release. The kinetics of drug release for F6 & Innovator followed first order and ‘n’ value ( 0.5>n<1) shows that the mechanism may be erosion control rate release. The f1 and f2 were found to be 3.03 and 72.01 respectively for formulation F6 and innovator product. Hence these two products were considered similar and comparable. In the accelerated stability testing carried out at 40°c and 75% RH for three months, no significant change in the physical properties, drug content, and dissolution rate of formulation F6 was observed. From this it can be concluded that formulation F6 developed is found to be an efficient delayed release formulations of Rabeprazole comparable to the innovator product. Thus the study fulfilled the objective of developing efficient Rabeprazole delayed release tablets.

Bioavailability of Two Different Coated-Tablet Formulations of Valacyclovir of Two Different Strengths (500 mg and 1000 mg) in Healthy Mexican Adult Volunteers

Valacyclovir is a prodrug of acyclovir. In Mexico, it is indicated for the treatment of herpes zoster and herpes simplex infections. The aims of these 2 studies were to compare the bioavailability and to determine the bioequivalence of 2- test formulations containing 500 mg and 1000 mg of oral valacyclovir. Two separate, single-dose, open-label, randomized, 2-period, crossover studies were conducted. For each study a different set of 26 subjects of both genders was enrolled, with a 7-day washout period. In both studies, the study formulations were administered after a 10-hour overnight fast. For pharmacokinetic analysis, blood samples were drawn at baseline, 0.25, 0.50, 0.75, 1, 1.25, 1.50, 1.75, 2, 3, 4, 6, 8, 12 and 24 hours after administration. Plasma concentrations of acyclovir were determined using HPLC coupled to a fluorescence detector. The test and reference formulations were to be considered bioequivalent if the 90% CI for the geometric mean test/reference ratios were within a predetermined range of 80% to 125%. In the study with valacyclovir 500 mg, the 90% CI were 95.24% - 115.33% for Cmax, 96.20% - 103.55% for AUC0-t, 97.12% - 104.34% for AUC0-∞. In the study with valacyclovir 1000 mg the 90% CI were 86.22%- 100.87% for Cmax, 89.11% - 98.50% for AUC0-t, 89.00% - 98.34% for AUC0-∞. In both studies, a single dose of the test formulation met the regulatory requirements to assume bioequivalence, based on the rate and extent of absorption.

Bioequivalence Study of Two Different Coated Tablet Formulations of Finasteride in Healthy Volunteers

This study was conducted in order to assess the bioequivalence of two different coated tablet formulations containing 5 mg finasteride (CAS 98319-26-7). Twenty-six healthy volunteers were enrolled in an open, randomised, crossover single dose study with 2 periods x 2 sequences and a minimum washout period of 7 days. Plasma samples were obtained over 24 h (at baseline, +0.5 h, +1 h, +1.5 h, +2 h, +2.5 h, +3 h, 3.5 h, +4 h, +4.5 h, +5 h, +6 h, +8 h, +10 h, +12 h, +16 h and +24 h after administration). Finasteride levels were determined by high-pressure liquid chromatography with tandem mass detection, HPLC-MS/ MS, (LOQ 0.50 ng/mL). Pharmacokinetic parameters used for bioequivalence assessment (AUClast and Cmax were main evaluation criteria, however, AUCinf was also analysed) were determined from the finasteride concentration data using non-compartmental analysis. The 90 % confidence intervals (obtained by ANOVA) were 86.31-98.69 for Cmax, 95.40-104.88 for AUClast and 96.20-105.81 for AUCinf that is, they were all within the predefined ranges. It may be therefore concluded that the evaluated formulations are bioequivalent in terms of rate and extent of absorption.

Bioequivalence study of two oral tablet formulations containing saquinavir mesylate boosted with ritonavir in healthy male subjects

Saquinavir (SAQ) mesylate (CAS 149845-06-7) is a potent inhibitor of the HIV-1 protease indicated in combination with other antiretrovirals for the management of HIV-1 infection. The objective of this study was to compare rate and extent of absorption and to assess the bioequivalence between a new pharmaceutical equivalent tablet formulation containing 500 mg of SAQ mesylate and the innovator film coated tablet formulation. A randomized, single-center, open-label, two-treatment, two-sequence, three-period, replicated crossover bioequivalence study in 40 healthy male subjects was conducted. All subjects received 100 mg ritonavir (CAS 155213-67-5) twice daily for a run-in period of 3 days before treatment. Dosing was separated by a wash-out period of 14 days. Blood samples were collected over 72 h and plasma levels of SAQ were determined by a validated HPLC/UV assay. The 90% confidence interval (CI) of the ratio of the geometric means for log-transformed C(max), AUC(last) and AUC(inf) values were used to assess bioequivalence using the equivalence interval of 80-125%. Point estimate and 90% CI of the ratios of C(max), AUC(last) and AUC(inf) values were 94.9 (80.9-111.3), 97.4 (82.4-115.4) and 97.4 (82.5-115.0), respectively. Both treatments exhibited similar tolerability and safety. It was concluded that the new pharmaceutical product was bioequivalent to the innovator.

Tabletability assessment of conventional formulations containing Vitamin E tocopheryl polyethylene glycol succinate

Vitamin E tocopheryl polyethylene glycol succinate (TPGS) is known to enhance the bioavailability of poorly water-soluble drugs via solubility and permeability enhancement. Few studies have evaluated feasibility of formulating TPGS in conventional solid dosage forms such as tablets due to processing challenges resulting from its waxy nature and low melting point (∼37 °C). The objective of this study is to systematically investigate the tabletability of conventional high shear wet granulation (WG) formulations incorporated with Vitamin E TPGS. Impact of critical formulation variables such as levels of TPGS, hydroxypropyl cellulose (binder) and Prosolv (extragranular filler) on product quality attributes was studied using a full factorial experimental design. The potential influence of temperature elevation during processing was assessed through a heated die fitted onto a compaction simulator. Bilayer tabletability of the TPGS formulation was also assessed in combination with a secondary non-TPGS formulation. TPGS levels significantly impacted tensile strength (TS), disintegration time and dissolution. Heat sensitivity studies indicated that TS reduction upon exposure to heat was minimized by higher levels of extragranular fillers. Acceptable interfacial strength of bilayer tablets was achieved and tablets could be coated without the need for hydroalcoholic solutions. The study demonstrates preliminary feasibility to develop monolithic and bilayer coated tablet formulations containing up to 10% (w/w) TPGS for the given compound and drug load. Further studies are required to validate these findings at larger scales.

Topical formulations of serratiopeptidase: development and pharmacodynamic evaluation

Serratiopeptidase, an enzyme derived from Serratia marcescences strain E-15 (ATCC 21074), present in the gut wall of the silk worm possesses anti-inflammatory properties, and can prove to be a suitable alternative to commonly used non steroidal antiinflammatory agents. Being sensitive to gastric degradation, serratiopeptidase is conventionally given orally in the form of enteric coated tablet formulations. Topical formulations of serratiopeptidase would be useful to treat local inflammations and may prove to be more effective compared to non steroidal antiinflammatory agents. The present study investigates the feasibility of developing topical preparations of serratiopeptidase in the form of ointments and gels. Excipient compatibility of serratiopeptidase with various excipients and polymers, formulation development, characterization and stability studies have been carried out. Stable formulation was evaluated for anti-inflammatory activity by oxazolone induced ear edema method in mice and allergenic potential by passive cutaneous anaphylaxis.

Relative bioavailability of imipramine (Tofranil) coated tablets in healthy volunteers

Imipramine is a tricyclic antidepressant drug with a considerable hepatic first-pass metabolism resulting in highly variable pharmacokinetic characteristics and desipramine as active major metabolite. This study describes the bioavailability of 3 formulations of imipramine. In a randomized, three-period crossover study, 18 healthy male Caucasian subjects received single oral doses of Tofranil 25, Tofranil mite (10 mg) and an aqueous solution containing 25 mg imipramine-HCl. Serum concentrations of imipramine-HCl and its main metabolite desipramine were measured. The pharmacokinetic characteristics, Cmax, AUC, t1/2 and tmax were determined and the relative bioavailability of the two coated tablet formulations was calculated with the aqueous solution as reference. Safety and tolerability were assessed using vital signs, ECG, clinical laboratory and adverse event recording. The relative bioavailabilities of Tofranil 25 and Tofranil mite were 97% and 81%, respectively. The study medication was well tolerated. A sufficiently high extent of absorption was found for the test formulations ensuring therapeutic efficacy.

Granulation by Roller Compaction and Enteric Coated Tablet Formulation of the Extract of the Seeds of Glinus Lotoides Loaded on Aeroperl® 300 Pharma

The purpose of this research was to improve the hygroscopicity and poor flow properties of the crude dry extract of the seeds of Glinus lotoides and improve the disintegration time of the core-tablets for enteric coated formulation thereof. The liquid crude extract of the plant was adsorbed on granulated colloidal silicon dioxide (Aeroperl 300 Pharma) at 30% w/w and the dry extract preparation (DEP) was dry-granulated with roller-compaction using Micro-Pactor. Hygroscopicity, flow property and disintegration time were improved significantly due to the adsorption and granulation processes. Moreover, the DEP does not become mucilaginous even at higher relative humidity levels (above 65%). Oblong tablets (20 x 8.25 mm) containing 947 mg of the granulated DEP (equivalent to the traditional dose), 363 mg of Avicel PH101 and 90 mg of Ac-di-Sol as disintegrant were formulated using an instrumented eccentric tablet machine at 20 kN. The tablets showed a crushing strength of 195 N, a friability of 0.4% and disintegrated within 9 min. The tablets were then enteric coated using polymethacrylate co-polymers (Eudragit L 100-55 and Kollicoat MAE 100P). The coated tablets resisted disintegration or softening in simulated gastric fluid for a minimum of 2 h and disintegrated within 15 min in intestine simulated fluid at pH 6.8. In addition to controlling the release of the active agents, the enteric coating improved the strength and decreased friability of the core-tablets.

Effect Of Formulating Additives On The Properties Of Ibuprofen Tablets

A study of the comparative effects of different formulating additives and film coating on the properties of ibuprofen tablets was made. The tested properties were hardeness (H), friability (F), the disintegration time (D) and dissolution characteristics of ibuprofen tablets. The hardeness, friability, the hardeness friability ratio (HFR) and the disintegration time were affected by diluent-binder ratio and binder concentration. The ranking for the values of HFR for different coated tablet formulations and commercial tablet formulation )FC) was FVI>FV>FI>FII>FIV>FC>FIII. The ranking for disintegration times D of uncoated tablet formulations were FI>FII>FVI>FV>FIV>FIII and that of coated formulations and commercial formula was FI>FVI>FII>FV>FC>FIV>FIII. The ranking for the dissolution rates of uncoated tablet formulations after one hour were FIV>FV>FIII>FVI>FII>FI whereas those of coated formulations and commercial tablet formulation (FC) were FIV>FC>FV>FVI>FIII>FII>FI. It was found that, Film coating has a remarkable effect on both mechanical strength and drug release from different ibuprofen formulations. The results suggest that hydroxypropyl methylcellulose (HPMC) could be selected as a binding agent and film coating material. It produces tablets with acceptable mechanical properties and drug release pattern. Formula FIV gave the most acceptable properties and drug release profile compared to other tested formulations. The oral absorption profile of the selected formula (FIV) was studied and compared to that of the commercial tablet formulation (FC). The AUC of FIV was not significantly larger than that of FC. The maximum biological half life (tmax) of FIV was the same as that of FC. Statistical comparison of the biological half-life parameter did not indicate a significant difference between results from FIV tablets and FC tablets. Cmax of FIV was higher than that of FC. The results indicated that the adopted formulation technique gave ibuprofen tablets with acceptable properties. These results were comparable with FC.Egyptian Journal of Biomedical Sciences Vol. 23 (1) 2007: pp. 60-72