Polyplasdone XL Research Articles

TASTE MASKING OF OXYBUTYNIN CHLORIDE USING LIPID EXCIPIENTS AND FORMULATION AS ORODISPERSIBLE TABLETS FOR GERIATRIC POPULATION

The aim of the present study was to mask the bitter taste of oxybutynin chloride by lipid excipients and to develop its fast disintegrating tablet. For this purpose, a blend of two lipids, glyceryl behenate and glyceryl palmitostearate was utilized for taste masking by solvent evaporation method. The evaporation of solvent was accomplished by freeze drying and taste masked granules were characterized for their micromeritic and rheological properties. The state of dispersion was analyzed by SEM and DSC. Orodispersible tablets were then formulated (F1- F6) using Polyplasdone XL as extragranular superdisintegrant and evaluated for hardness, disintegration time, in vitro dissolution time and in vivo disintegration time. Results indicated that the formulation F6 exhibited minimum in vivo disintegration time of 8 sec with effective taste masking. In vitro release analysis indicated %DE10 and %DE25 of 51.48 and 76.53 respectively. Conclusively, taste masked orodispersible formulation of oxybutynin chloride was developed that could be beneficial for geriatric population.

Formulation Development of Orodispersible Tablets of Mosapride citrate using different superdisintegrants and Their Evaluation

Mosapride is novel prokinetic agent which seems to exert its action via a high affinity and specifity for 5-HT 4 receptor. In addition the principal metabolite has high affinity for 5-HT 3 receptors and has proved to be potent 5-HT 3 antagonist. Mosapride has been used to treat gastroesophageal reflux disease, chronic gastritis, nonulcer dyspepsia and diabetic gastropathy. In the present study, an attempt has been made to formulate orodispersible tablets of Mosapride Citrate Dihydrate. The other objective of the study was to evaluate the performance of three different classes of superdisintegrants which are croscarmellose Sodium (Ac-Di-Sol), crospovidone (Polyplasdone XL), sodium starch glycolate (Primojel) in promoting disintegration and dissolution of Mosapride Citrate Dihydrate orodispersible tablets. At the optimum concentrations of 2% & 4% of selected superdisintegrants, their effect in the orodispersible tablet on the in vitro disintegration & in vitro dissolution was evaluated. It was concluded that, the formulation of Mosapride Citrate Dihydrate orodispersible tablets was made with functionality evaluation of selected superdisintegrants. KEYWORDS: Mosapride Citrate Dihydrate, Orodispersible tablets, Superdisintegrants, Crospovidone, Prokinetic agent.

Development and evaluation of ofloxacin orally disintegrating tablets

Bitter taste of ofloxacin, a broad spectrum bactericidal agent, is masked and orally disintegrating tablets were formulated. The bitter taste is masked by forming complex between drug and weak cation exchange resins, Tulsion 335 and Indion 204. Effect of pH and drug:resin ratio on the drug loading was studied. Maximum drug loading was observed at pH 6. Ratio of 1:2 of drug:resin masked almost complete bitterness of ofloxacin. Formation of complexes was confirmed by IR spectroscopy. Physical characterization of taste masked complexes was carried out. Present work envisages the taste masking of ofloxacin and development of orally disintegrating tablets. The effect of pH and resin quantities on drug loading were studied to find the optimum conditions of drug loading for complete taste masking. Effect of superdisintegrants like sodium starch glycolate, croscarmellose sodium and polyplasdone XL at varying level on physical parameters of compressed tablets was also assessed. The formulations containing 5 % w/w polyplasdone XL showed about 90 % of drug release within 5 minutes. No significant differences were observed in the physical parameters of resinates as well as tablets prepared from Tulsion 335 and Indion 204.

Novel oral delivery system of indomethacin by solidified mPEG-PDLLA micelles: in vivo study

To administer indomethacin (IND) orally using polymeric micelles, IND loaded solidified polymeric micelles (IND-SPM) were prepared and evaluated for their in vitro and in vivo characteristics. IND and methoxy-poly(ethylene glycol) poly(d, l-lactide) copolymer (mPEG-PDLLA) were dissolved in acetone followed by the addition of an equivalent amount of polyplasdone XL-10 and stirred to obtain a suspension. Afterwards, acetone was completely evaporated. It was found that IND-SPM generates small polymeric micelles of 18.1 nm. Moreover, the solubility of IND at pH 6.8 increased 4.6-folds, and more than 90% of IND in 20 mg of IND-SPM was dissolved in 250 mL SIF pH 6.8 within 30 min. Pharmacokinetic parameters in fasted rats showed that IND-SPM 1:3 resulted in 3-folds increase of AUC and Cmax compared to commercial IND. mPEG-PDLLA micelles were found to be efficient carriers for oral administration of IND as solid dosage forms by adsorption on polyplasdone XL-10.

Exploration of novel co-processed multifunctional diluent for the development of tablet dosage form

The aim of this investigation was to develop a novel multifunctional co-processed diluent consisting of microcrystalline cellulose (Avicel PH 102), crospovidone (Polyplasdone XL) and polyethylene glycol 4000. Colloidal silicon dioxide and talc were also incorporated as minor components in the diluent to improve tableting properties. Melt granulation was adopted for preparation of co-processed diluent. Percentage of Avicel PH 102, Polyplasdone XL and polyethylene glycol 4000 were selected as independent variables and disintegration time was chosen as a dependent variable in simplex lattice design. The co-processed diluent was characterised for angle of repose, bulk density, tapped density, Carr's index, percentage of fines and dilution potential study. Acetaminophen and metformin were used as poorly compressible model drugs for preparation of tablets. The blend of granules of drug and extra-granular co-processed diluent exhibited better flow as compared to the blend of drug granules and physical mixture of diluents blend. The diluent exhibited satisfactory tableting properties. The tablets exhibited fairly rapid drug release. In conclusion, melt granulation is proposed as a method of preparing co-processed diluent. The concept can be used to bypass patents on excipient manufacturing.

Formulation and in vivo evaluation of ondansetron orally disintegrating tablets using different superdisintegrants

The aim of this study was to formulate cost effective taste-masked orally disintegrating tablets of ondansetron, a bitter drug using different superdisintegrants by a wet granulation technique. Microcrystalline cellulose (Avicel) as a diluent and disintegrant in addition to aspartame as a sweetener were used in all formulations. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. The tablets' hardness was maintained in the range of 2-3 kg and friability was <1% for all batches. All tablet formulations disintegrated rapidly in vitro within 5.83 to 33.0 sec. The optimized formulation containing 15% Polyplasdone XL-10 released more than 90% of drug within 5 min and the release was comparable to that of a commercial product. In human volunteers, optimized formulation was found to have a pleasant taste and mouth feel and they disintegrated in the oral cavity within 12 sec. The stability results were also satisfactory. A pharmacokinetic study with the optimized formulation was performed in comparison with a reference (Zofer MD 8®) and they were found to be bioequivalent. In conclusion, a cost effective ondansetron orally disintegrating tablet was successfully prepared with acceptable hardness, desirable taste and rapid disintegration in the oral cavity.

Formulation, development, and performance evaluation of metoclopramide HCl oro-dispersible sustained release tablet

The present study was undertaken to develop and evaluate an oro-dispersible, sustained release tablet of metoclopramide HCl. The technology was comprised of developing sustained release microparticles, and compression of resultant microspheres into a fast dispersible tablet by direct compression. The microspheres of metoclopramide HCl were prepared by an emulsification-solvent evaporation method using ethylcellulose as the matrix polymer. The prepared microspheres were evaluated for morphology, particle size, entrapment efficiency, and in vitro drug release characteristics. Scanning electron microscopy demonstrated spherical particles with a mean diameter of 81.27 ± 5.87 μm and the drug encapsulation efficiency was found to be 70.15 ± 3.06%. The process and formulation variables such as rotation speed, polymer concentration, and drug concentration influenced the drug encapsulation efficiency and in vitro drug release. Optimized microspheres were compressed into tablets which were comprised of metoclopramide HCl microspheres, 53% (w/v) of D-mannitol granules, 7% (w/w) of Polyplasdone XL 10, and 0.5% (w/w) of calcium stearate. The tablets demonstrated a hardness of 59 ± 3 N, friability of 0.21% and disintegration time of 27 ± 3 sec. The formulations were subjected to stability studies as per ICH guidelines and were found to be stable after a 6 month study. In vivo experiments conducted in rats demonstrated that a constant level of metoclopramide HCl in plasma could be maintained for up to 20 h at a suitable concentration for antiemetic activity. An appropriate combination of excipients made it possible to obtain orally disintegrating sustained release tablets of metoclopramide HCl using simple and conventional techniques.

Compatibility study between acetylcysteine and some commonly used tablet excipients.

Differential scanning calorimetry (DSC), Fourier transform infra-red spectroscopy (FT-IR), HPLC and TLC were used to investigate the interactions between the mucolytic drug acetylcysteine and a number of commonly used tablet and capsule excipients. Acetylcysteine was found to be compatible with microcrystalline cellulose (Avicel PH 101), sodium carboxymethylcellulose, amorphous silicon dioxide (Aerosil), PVP, cross-linked PVP (Polyplasdone XL), corn starch, saccharose and magnesium stearate. Acetylcysteine thermal stability (onset degradation temperature) was decreased in mixtures with corn starch, magnesium stearate, saccharose and lactose. Interactions of acetylcysteine with lactose, PEG 4000 and 6000, glycine, adipic acid and saccharin sodium were found using DSC and studied in detail with FT-IR, HPLC and TLC. The results suggest that acetylcysteine in mixtures with PEG 4000, glycine or saccharin sodium is degraded during storage at conditions of high temperature and humidity.

Development, characterization and performance evaluation of oro-dispersible tablet containing aceclofenac hydroxypropyl-β-cyclodextrin binary system

The purpose of this research was to mask the intensely bitter taste of aceclofenac (ACF) and to formulate oro dispersible tablet (ODT) of the taste-masked drug. Taste masking was done by complexing aceclofenac with Hydroxypropyl-β-Cyclodextrin (HPβCD) by different methods. Phase solubility studies indicated complex with possible stoichiometry of 1:1 and a stability constant of 221.11 M−1. The complexes were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, and differential scanning calorimetry studies. The characterization studies confirmed inclusion of the ACF within the nonpolar cavity of HPβCD in the neutralization method (NM). Remarkable improvement in the in vitro drug release profiles in pH 6.8 phosphate buffer was observed with all complexes, especially the neutralization. The complexes of ACF–HPβCD (1:1) was compressed into tablet and properties of tablets such as tensile strength, wetting time, in vitro disintegration time, and disintegration in the oral cavity were investigated to elucidate the wetting and disintegration characteristics of tablets. Polyplasdone XL-10 7% wt/wt gave the minimum disintegration time. Tablets of batch F4 containing Avicel 200 and 7% wt/wt Polyplasdone XL-10 showed faster disintegration, within 12 s, than the marketed tablet (128 s). Good correlation between in vitro disintegration with in-house developed method and in the oral cavity was recognized. Taste evaluation of ODT in human volunteers revealed considerable taste masking with the degree of bitterness below threshold value. Thus, results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated tablets in the oral cavity.

Effect of bioadhesion on initial in vitro buoyancy of effervescent floating matrix tablets of ciprofloxacin HCL

The purpose of this study was to investigate effect of bioadhesion on the initial in vitro buoyancy behaviour of effervescent matrix tablets of ciprofloxacin HCl (CIPRO). Tablets were prepared by direct compression using HPMC K4M and Carbopol 971P as hydrophilic-controlled release polymers, sodium bicarbonate (NaHCO3) as gas-generating agent, polyplasdone XL, Explotab and Ac-Di-Sol as swelling agents. Tablets were evaluated for normal and modified initial in vitro floating behavior, floating duration, swelling behavior and in vitro drug release studies. A modified buoyancy lag time for tablets was determined in order to include the effect of bioadhesion on initial buoyancy. The initial buoyancy was found depended on bioadhesion ability of tablets. The lowest modified buoyancy lag time of 20 seconds was obtained for Formulation F7 having both NaHCO3 and polyplasdone XL. The floating duration was also found dependent on concentration of NaHCO3 and swelling agents. The drug release of F7 was also sustained up to 12-hr duration with anomalous drug transport mechanism.

FORMULATION AND EVALUATION OF TASTE MASKED MOUTH DISSOLVING TABLETS OF ONDANSETRON HYDROCHLORIDE

To overcome difficulty in swallowing tablets or capsules, formulators have considerably dedicated their effort to develop novel drug delivery systems which enhance safety and efficacy of drug molecule and to achieve better patient compliance. One such approach is ‘Mouth Dissolving Tablets’. The purpose of this research was to mask the intensely bitter taste of ondansetron Hcl by complexing with indion204 Resin by the solvent evaporation and to formulate a mouth dissolving tablets of the taste-masked drug. Tablets were formulated by direct compression method using different superdisintegrants like Polyplasdone XL-10 & Sodium starch glycolate (SSG) in different concentration, diluents like Mannitol, Microcrystalline cellulose (MCC 112), sweetening agent Aspartame, Flavoring agents like peppermint and vanilla, lubricant Magnesium Stearate & glidant aerosil. All formulations were evaluated for disintegration time, wetting time, % friability, Content uniformity and in vitro dissolution rate. Formulations with 7% Polyplasdone XL-10 showed the disintegration time 14 seconds and wetting time 25 seconds. In vitro drug release study of taste masked tablet showed complete drug release within 10 minutes & successful masking of taste and rapid disintegration of the formulated tablets in the oral cavity.

Melt-in-Mouth Pellets of Fexofenadine Hydrochloride Using Crospovidone as an Extrusion–Spheronisation Aid

Microcrystalline cellulose (MCC) is well established as an extrusion spheronisation aid for the preparation of pellets. Crospovidone (Polyplasdone XL-10) is compared with microcrystalline cellulose for the preparation of melt-in-mouth pellets. Taste-masked fexofenadine hydrochloride was incorporated in the melt-in-mouth formulation. Crospovidone was found to be well suited as extrusion-spheronisation aid for the preparation of melt-in-mouth pellets. The great advantage of crospovidone is, however, the disintegrating properties of the pellets after only a short time of exposure to liquid. Crospovidone was successfully employed as an extrusion-spheronisation aid to produce melt-in-mouth pellets obviating the need of a traditional extrusion-spheronisation aid, MCC. Dual properties of Crospovidone were explored viz. as an extrusion-spheronisation aid and a disintegrant.

Effect of auxiliary substances on complexation efficiency and intrinsic dissolution rate of gemfibrozil-beta-CD complexes.

The studies reported in this work are aimed to elucidate the ternary inclusion complex formation of gemfibrozil (GFZ), a poorly water-soluble drug, with beta-cyclodextrin (beta-CD) with the aid of auxiliary substances like different grades of povidone(s) (viz. PVP K-29/32, PVP K-40, Plasdone S-630, and Polyplasdone XL), organic base (viz. triethanolamine), and metal ion (viz. MgCl(2).6H(2)O), by investigating their interactions in solution and solid state. Phase solubility studies were carried out to evaluate the solubilizing power of beta-cyclodextrin, in association with various auxiliary substances, to determine the apparent stability constant (K (C)) and complexation efficiency (CE) of complexes. Improvement in K (C) values for ternary complexes clearly proves the benefit of the addition of auxiliary substances to promote CE. Of all the approaches used, the use of polymer Plasdone S-630 was found to be the most promising approach in terms of optimum CE and K (C). GFZ-beta-CD (1:1) binary and ternary systems were prepared by kneading and lyophilization methods. The ternary systems clearly signified superiority over binary systems in terms of CE, solubility, K (C), and reduction in the formulation bulk. Optimized ternary system of GFZ-beta-CD-Plasdone S-630 prepared by using lyophilization method indicated a significant improvement in intrinsic dissolution rate when compared with ternary kneaded system. Differential scanning calorimetry, X-ray diffraction, Fourier transform infrared, scanning electron microscopy, and proton nuclear magnetic resonance were carried out to characterize the binary and optimized ternary complex. The results suggested the formation of new solid phases, eliciting strong evidences of ternary inclusion complex formation between GFZ, beta-CD, and Plasdone S-630, particularly for lyophilized products.

Design and evaluation of the fast dissolving tablet of terbutaline sulfate

Asthma is an inflammatory disorder that results in the obstruction of air pathways and causes difficulty in breathing. Oral dosage forms associated with lag time and delayed onset of action are among the available means of treatment. However, aerosols and parenterals have a rapid onset of action but strongly affect the patient compliance.Thus, an attempt was made to improve the onset of action of bronchodilator used commonly in the treatment of asthma. Fast dissolving tablets of terbutaline sulfate were prepared by the direct compression method after incorporating superdisintegrants such as Explotab, Ac-Di-Sol and Polyplasdone XL in different concentrations.The prepared tablets were evaluated for weight variation, thickness, hardness, friability, wetting time, drug content, water absorption ratio, in vitro dispersion time, in vitro disintegration time and in vitro drug release. Among all, the formulation F9 (containing 5% w/w concentration of Polyplasdone XL) was considered to be the best formulation, which releases up to 99.33% of the drug in 10 min.

Formulation and evaluation of bi-layer tablet of metoclopramide hydrochloride and ibuprofen.

The aim of this study was to prepare bi-layer tablet of Metoclopramide Hydrochloride (MTH) and Ibuprofen (IB) for the effective treatment of migraine. MTH and IB were formulated as immediate and sustained release layer respectively. MTH was formulated as immediate release layer by using various disintegrants like Ac-Di-Sol, Polyplasdone XL, Explotab, Agar and Gellan Gum. Treated form of gellan gum and agar was prepared and compared for their disintegrant efficiency with other disintegrants. IB was formulated as sustained release layer using hydrophilic matrix (hydroxypropylmethylcellulose [HPMC K(4)M]). The effect of concentration of hydrophilic matrix (HPMC K(4)M), binder (polyvinylpyrollidone [PVP K(30)]) and buffer (sodium bicarbonate) on IB release was studied. The dissolution study of sustained release layer showed that an increasing amount of HPMC or PVP K(30) results in reduced IB release. The inclusion of buffer (sodium bicarbonate) enhanced the release of IB from sustained release layer. The rational for formulation of bi-layer tablet of these two drugs in combination was (1) MTH increases the absorption of acidic non-steroidal anti-inflammatory drug (NSAID) by increasing gastric motility. So sequential release of MTH (as immediate release) and IB (as sustained release) was suitable for treatment of migraine. (2) MTH was degraded when prolonged contact with acidic NSAID. Bi-layer tablet was suitable for preventing direct contact of these two drugs and thus to maximize the efficacy of combination of two drugs for migraine.

Immediate Release Tablets of Telmisartan Using Superdisintegrant-Formulation, Evaluation and Stability Studies

Telmisartan (anti-hypertensive) is insoluble in water; hence the drug may be slowly or incompletely dissolved in the gastro intestinal tract. So the rate of dissolution and therefore its bioavailability is less (bioavailability 42%). In the present study an attempt has been made to prepare immediate release tablets of telmisartan by using Polyplasdone XL-10 (Crosspovidone) at intragranular, extragranular and partly intra and extragranular level of addition to increase the rate of drug release from dosage form to increase the dissolution rate and hence its bioavailability. The prepared granules and tablets were evaluated for their physiochemical properties and in-vitro dissolution study was conducted for the prepared tablets. It was concluded that the immediate release tablets with proper hardness, disintegration time and with increase rate of dissolution can be made using Polyplasdone XL-10. Formuation-10 (F10) was selected for stability study and the in-vitro dissolution study showed that was no difference in percent of drug released between initial and sixth month sample.

Development of a rapidly dispersing tablet of a poorly wettable compound—formulation DOE and mechanistic study of effect of formulation excipients on wetting of celecoxib

Celecoxib has extremely poor aqueous wettability and dispersibility. A dispersibility method was developed to study the effects of formulation excipients and processing methods on wetting of celecoxib. In this method, a tablet or powder was placed in water and the turbidity of the resulting “dynamic” suspension was measured. Higher turbidity values reflect better dispersibility. Results show that wet granulation facilitates better drug dispersion than does dry granulation or direct compression. Results from a screening formulation statistical design of experiments (DOE) show that sodium lauryl sulfate (SLS), an anionic surfactant, gives higher celecoxib dispersibility than polysorbate 80, a neutral surfactant. Polyplasdone XL as a disintegrant results in better celecoxib dispersibility than sodium starch glycolate. The binder Kollidon 30 leads to better dispersibility, but slower disintegration than Kollidon 12. Jet-milling celecoxib with excipients not only improves dispersibility of the drug but also the ease of material handling. The method of microcrystalline cellulose addition does not significantly impact tablet properties. The effect of critical formulation variables on the wettability of celecoxib was further examined in prototype formulations. It is found that ionic surfactant resulted in better dispersibility than a neutral surfactant, probably due to charge dispersion. Kollidon 30 gives better drug dispersion than hydroxypropylmethyl cellulose and hydroxypropyl cellulose. This may be explained through a surface energy calculation, where the spreading coefficients between Kollidon 30 and celecoxib indicate formation of open porous granules in which pores can facilitate water uptake. The mode of disintegrant addition also impacts dispersibility of the drug. Dense granules were formed when the disintegrant, Polyplasdone, was added intra-granularly. As the extra-granular portion of the disintegrant increases, the dispersibility of the drug increases as well. The drug initial dispersibility (turbidity at 5 min during the dispersibility test) increases as the tablet porosity increases. A 3-factor face-centered experimental design was conducted to optimize the levels of surfactant (SLS), binder (Kollidon 30) and disintegrant (Polyplasdone). Within the range that was studied, the dispersibility of micronized drug increases as the amount of SLS and Kollidon 30 increases. The level of Polyplasdone has no significant impact on the dispersibility of micronized drug; however, higher levels of Polyplasdone lead to significantly harder tablets.

Taste masking of ondansetron hydrochloride by polymer carrier system and formulation of rapid-disintegrating tablets

The purpose of this research was to mask the intensely bitter taste of ondansetron HCl and to formulate a rapid-disintegrating tablet (RDT) of the taste-masked drug. Taste masking was done by complexing ondansetron HCl with aminoalkyl methacrylate copolymer (Eudragit EPO) in different ratios by the precipitation method. Drug-polymer complexes (DPCs) were tested for drug content, in vitro taste in simulated salivary fluid (SSF) of pH 6.2, and molecular property. Complex that did not release drug in SSF was considered taste-masked and selected for formulation RDTs. The complex with drug-polymer ratio of 8:2 did not show drug release in SSF; therefore, it was selected. The properties of tablets such as tensile strength, wetting time, water absorption ratio, in vitro disintegration time, and disintegration in the oral cavity were investigated to elucidate the wetting and disintegration characteristics of tablets. Polyplasdone XL-10 7% wt/wt gave the minimum disintegration time. Tablets of batch F4 containing spray-dried mannitol and microcrystalline cellulose in the ratio 1:1 and 7% wt/wt Polyplasdone XL-10 showed faster disintegration, within 12.5 seconds, than the marketed tablet (112 seconds). Good correlation between in vitro disintegration behavior and in the oral cavity was recognized. Taste evaluation of RDT in human volunteers revealed considerable taste masking with the degree of bitterness below threshold value (0.5) ultimately reaching to 0 within 15 minutes, whereas ondansetron HCl was rated intensely bitter with a score of 3 for 10 minutes. Tablets of batch F4 also revealed rapid drug release (t(90), 60 seconds) in SGF compared with marketed formulation (t(90), 240 seconds; P < .01). Thus, results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated tablets in the oral cavity.

Design and evaluation of silymarin-HP-β-CD solid dispersion tablets

Since solubility is the main constraint for oral bioavailability of silymarin, an attempt has been made to design tablet formulations of silymarin-HP-β -CD solid dispersion in order to improve oral bioavailability. Tablet formulations were prepared by direct compression technique using superdisintegrants such as crosscarmellose sodium, sodium starch glycolate and polyplasdone XL in different concentrations. Developed formulations were evaluated for various pharmaceutical characteristics viz. hardness, % friability, weight variation, drug content, disintegration time and in vitro dissolution profiles. Amongst different batches, formulations containing crosscarmellose sodium showed superior disintegration and dissolution profiles compared to other formulations. However all the formulations showed improved dissolution over marketed formulation reflecting vital role of HP-β -CD dispersion in promotion of silymarin oral bioavailability. Moreover, optimized formulation showed stability at varying temperature and relative humidity.

FACTORIAL DESIGN USED IN OPTIMIZATION IMMEDIATE RELEASE SOLID DOSAGE RANITIDINE HYDROCHLORIC

The aims of this study were to develop a predictive immediate release tablet formulation system for soluble drugs. Ranitidine hydrochloride, silicifiedmicrocrystallinecellulose (SMCC), polyplasdone XL and hydroxyprophylmethylcellulose (HPMC) E6 were evaluated for powder properties. The effects of binder (HPMC E6) and disintegrant (Polyplasdone XL) were investigated. A 32 factorial design was applied to optimize the drug release profile. The amount of binder and disintegrant were selected as independent variables. The times required for 50% (t50) and 80% (t80) drug dissolution and similarity factor (f2) were chosen as dependent variables. The results of factorial design indicated that a high amount of binder and low amount of disintegrate favored the preparation of drug release. The difference (f1) and similarity (f2) factors were used to measure the relative error and the closeness (similarity) between the factorial design batches and brand name drugs. No significant difference was observed between the brand drug and ranitidine batches F1, F2, F5, F6 and F9. Ranitidine batch F2 yielded the highest value of f2(71%)and the lowest of f1(10%). This research indicates that the proper amount of binder and disintegrant can produce drug dissolution profiles comparable to their brands.