Post-compression Evaluation Research Articles

FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF DONEPEZIL HYDROCHLORIDE

Objective: The present study was aimed to develop the formulation and in vitro evaluation of Orodispersible tablets by wet granulation method using Donepezil HCl as a model drug to enhance patient compliance.
 Methods: In the wet granulation method, a mixture of microcrystalline cellulose and hydroxypropyl methylcellulose were used along with superdisintegrants, i.e., croscarmellose sodium and crospovidone. The prepared granules were subjected to both pre and post-compression evaluation parameters including; FTIR spectroscopy, micromeritics properties, tablet weight variation, hardness, friability, drug content, disintegration time and in vitro drug release.
 Results: FTIR studies indicated that there was nointeraction between the drug and the excipients used. The formulation containing high concentration of crospovidone and mixture as the best formulation F2 based on in vitro drug release characteristics of tablet formulation.
 Conclusion: The results of this work suggested that orodispersible tablets of Donepezil hydrochloride with rapid disintegration time, fast drug release and good hardness can be efficiently and successfully formulated by wet granulation method.

Formulation and Evaluation of Fast-disintegrating Tablets of Flurbiprofen and Metoclopramide

The present study was aimed to formulate and evaluate fast-disintegrating tablets (FDTs) having Flurbiprofen (FP) and Metoclopramide HCl (MHCl) in combination. Direct compression was used to formulate FDTs of FP and MHCl as a combination regimen in six formulations. FDTs are defined as solid oral dosage form that disintegrates rapidly within seconds when placed in the oral cavity. FDT-1, FDT-2, FDT-3, FDT-4, FDT-5, and FDT-6 were formulated using crospovidone, croscarmellose sodium, and sodium starch glycolate as superdisintegrants each in two formulations. Several pre-compression tests (angle of repose, bulk density, tapped density, Hausner’s ratio, and compressibility index), post-compression evaluation (weight variation, friability, hardness, disintegration time, wetting time, assay, in vitro dissolution study, release kinetics study, statistical analysis, and stability study), and drug compatibility study were done for all six formulations. Pre-compression evaluation showed good flow properties of powder blend. Drug compatibility study showed no interactions between active drugs and excipients. Disintegration and wetting time of all the formulations were in seconds indicating immediate release of drug. Optimized formulation (FDT-6) containing sodium starch glycolate in 15 mg gave 100% release in 15 min for MHCl and in 20 min for FP. Optimized formulation was found stable after being placed at accelerated stability conditions for 6 months. Release kinetics study showed that all formulations followed Korsmeyer-Peppas model indicating drug release from modified release dosage form. Statistical analysis revealed no significant difference statistically (p > 0.05) between drug release rate of all prepared formulations. FDTs improved the release rate that assured that this tactic may be beneficial to increase the dissolution rate of FP and MHCl in order to increase patient compliance.

Formulation and evaluation of dispersible isoniazid tablets for paediatric use: an extemporaneous model formulary application in a resource limited setting

Background: Tuberculosis (TB) remains a global burden and public health concern. Isoniazid, a principal anti-tubercular drug (ATD) though effectively used in TB preventive chemotherapy is preferentially available in adult formulations. Its use therefore in paediatric population is challenged with issues of high probability of inaccurate dose administrations, low patient compliance and adherence. This burden may be higher in resource limited settings, thus development of simple child friendly formulations is needful.Objectives: This study aimed to design, develop and evaluate an extemporaneous formulary model of a paediatric oral dispersible isoniazid tablet for use in a resource-limited setting.Method: Paediatric oral dispersible isoniazid granulation batches with varying concentrations (0.5 - 5.5 % w/w) of sodium carboxyl methylcellulose as superdisintegrant were prepared by wet granulation method and compressed. Granulation batches were subjected to pre and post compression evaluations respectively in accordance with established standard methods. Results were statistically analysed using one-way analysis of variance (ANOVA) with significance set at p < 0.05.Result: The outcome of the micromeritics variables for the granule batches were indicative of good flow properties. The tablet batches passed all the official tablet evaluation criteria, with no statistical significance between the batches. However, tablet batches that contained lower concentrations of carboxyl methylcellulose failed both the disintegration and dispersion tests. Optimal tablet formulation was obtained with 5.0 % w/w of the superdisintegrant.Conclusion: An optimized formulation of an oral paediatric dispersible isoniazid tablet that could be applied as an extemporaneous compounding model in a resource limited setting has been developed.Keywords: Paediatric Tuberculosis, Isoniazid, Dispersible Tablet, Extemporaneous Compounding

FORMULATION AND EVALUATION OF MUCOADHESIVE CLOTRIMAZOLE VAGINAL TABLET USING LIQUISOLID TECHNOLOGY

Liquisolid technology is very effective technique for improving the solubility and dissolution properties of poorly water soluble drug formulations like Clotrimazole. Clotrimazole is a BCS Class II, antifungal drug used for treatment for Vaginal Candidiasis. In this liquisolid technique the drug soluble in non volatile solvents and then it converted into free flowing, non adherent powder, which can be compressed into tablet. Here N-methyle-2-pyrrolidone and propylene glycol is used in the ratio of 1:1 as a solvent. Neusilin US2 and Aerosil 200 used as Coating and Carrier material respectively. For mucoadhesion on vaginal wall Sodium carboxymethyle cellulose used as a mucoadhesive agent. Mucoadhesive tablets were prepared using direct compression technique. Magnesium Stearate used as a glidant. Mucoadhesive liquisolid tablets were evaluated as precompression evalutions and post compression evaluations. Future tablets were evaluated as In vitro and Ex vivo evaluations. The optimized batch showed that In vitro release in simulated vaginal fluid pH 4.5 in 6 hr was 99%. Ex vivo diffusion studies of optimized batch showed 80% of drug diffusion in 6 hr. Mucoadhesive strength showed high mucoadhesion of optimized batch that is 36 gm. From this study it was concluded that liquisolid technology is an effective technique to improve solubility and dissolution properties of poorly water soluble drug formulations like Clotrimazole.

FORMULATION OF ORALLY DISINTEGRATING TABLETS OF CINNARIZINE BY USING DIRECT COMPRESSION METHOD

Objective: The aim of this work was to formulate and evaluate orally disintegrating tablets of cinnarizine that were prepared by direct compression method using different types of diluents and super disintegrants. The rationale behind this work was to accelerate the disintegration of the tablet to provide rapid dissolution, quick action and enhanced bioavailability of the drug.Methods: The tablets were prepared by direct compression method using different types of diluents as mannitol, microcrystalline cellulose (MCC), and lactose. Different super disintegrants were used such as crospovidone (CP), sodium starch glycolate (SSG) and Kyron T-314; Kyron T-314 was used in different concentrations of 5%, 6%, 7%, and 8%. The prepared formulae (F1-F9c) were subjected to flowability studies and post-compression evaluation studies. The optimized formula was selected depending on the time of disintegration and dissolution; then it was subjected to drug-excipient compatibility study and stability study.Results: Flowability results were ranging from excellent, excellent to good, and good to fair according to the type of the diluent used. All of the prepared tablets showed acceptable hardness, friability, drug content, and disintegration. A rapid disintegration of 11.66±2.25 s with the highest percentage 2 min-drug release of 74.55±3.01% was obtained by using the diluent lactose and the super disintegrant Kyron T-314 (8%) in the formula F9c. The infrared spectroscopic studies of the formula F9c showed no drug-excipient interaction. In addition, the stability study indicated that the optimized formula is a stable formula.Conclusion: Formula F9c of a rapidly disintegrating tablet was easy to be manufactured, and the results showed that this formula had a rapid disintegration, high dissolution profile, no noticeable chemical incompatibility and it was stable upon storage.

Design, Development and Evaluation of Fast Dissolving Tablet of Antiasthmatic Drug

The aim of the work is an attempt to design, development and evaluation of fast dissolving tablets of Levosalbutamol sulphate by direct compression method with the aid of superdisintegrant addition. Levosalbutamol (LS) is the R – enantiomer of short acting beta2 adrenergic receptor agonist of salbutamol used to treat asthma and Chronic obstructive pulmonary disease. Nine formulations were prepared by using three different superdisintegrants in varying concentration in such way that total weight of the tablet remains same. The drug-polymer incompatibility was analysed by FTIR studies. All the formulated tablets were subjected for pre and post-compression evaluation parameters. From the FTIR studies the drug-polymer compatibility were confirmed. The pre-compression parameters like bulk density, tapped density, Carr’s index and angle of repose was determined. The optimized formulation showed acceptable flow properties. The post-compression parameters like the thickness, hardness, friability and in vitro dispersion time, wetting time, water absorption ratio and in- vitro drug release were carried out and the values were found to be within IP limits. Among the nine formulations, the formulation containing Kyron T 314 (F9) showed highest drug release of 97.71 % than other formulations.

Formulation and evaluation of orodispersible tablets of dimenhydrinate by using co-processed superdisintegrants

The main objective of this study was to formulate orodispersible tablets of Dimenhydrinate for quick relief of emesis. Orodispersible tablets were prepared by direct compression method using co-processed super-disintegrants. Co-processed super-disintegrants are the mixture of crospovidone and guar gum in different ratios. The powder mixtures and tablets were subjected to various pre-compression and post-compression evaluations. IR spectroscopy showed no interaction between drug and other excipients. Angle of repose and Carr’s index was found in the range of 23.89°-28.27° and 23.29-15.48 respectively. These results indicated that powder mixtures showed good to acceptable flow properties. All formulations containing co-processed super-disintegrant showed short disintegration time (38.23-17.67 s) and maximum water absorption ratio 73.39%-91.35% compared to control formulation (3.54 min wetting time). Among all formulation F7 containing crospovidone: guar gum in 1:3 ratio showed highest percentage of drug release (98.89%) in 30 min, which is due to high degree of swelling caused by guar gum along with rapid hydration of tablets by crospovidone. Formulation F7 was subjected for 3 months of stability studies; results reviled that the tablet formulation was stable throughout the study period. In conclusion the obtained results suggested that orodispersible tablets of Dimenhydrinate with rapid disintegration and fast drug release can be successfully formulated by employing co-processed super-disintegrants. Kathmandu University Journal of Science, Engineering and TechnologyVol. 12, No. I, June, 2016 Page: 23-33

PREPARATION AND EVALUATION OF DROTAVERINE HCL ORAL DISINTEGRATING TABLETS USING SOLID MIXTURE TECHNIQUE

Objective: The objective of this study is to formulate orally disintegrating taste masked tablets of drotaverine HCl using solid mixture technique.Methods: Taste masked drug-polymer solid mixtures of drotaverine HCl were prepared by using hydroxypropyl methylcellulose (HPMC) 3 cps and rxcipient® FM1000/calcium silicate (rxcipient) as carriers employing kneading method using varying drug-polymer ratios of 1:1, 1:5, 1:7.5, and 1:9. Prepared drug-polymer mixtures evaluated for taste masking, and the ratio of drug-polymer is optimized. The granules and tablets prepared with optimized drug-polymer ratio were evaluated for pre- and post-compression parameters, in vitro dissolution studies, Fourier-transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD) studies.Results: The drug:polymer ratios 1:7.5 with rxcipient and 1:9 with HPMC were optimized based on taste evaluation. The pre-compression results showed that all the formulae have good flow properties. The post-compression evaluations showed that all the formulae met the specifications of orally disintegrating tablets. From all the prepared taste masked drotaverine HCl tablets, R10 formulation consisting of 4% croscarmellose sodium and H9 formulation consisting of 3% croscarmellose sodium, 3% sodium starch glycolate, and 2% microcrystalline cellulose shown more than 99% drug release in 60 min, and both the formulations showed better taste masking and were meting oral disintegrating tablet (ODT) parameters. The optimized formulation was characterized by FTIR, DSC, and XRD studies and found no incompatibility.Conclusion: The results demonstrated that the prepared drotaverine HCl ODT showed better taste masking and meeting the parameters of ODT formulations R10 and H9. The present solid mixture technique can be effectively used for taste masking.

PREPARATION AND EVALUATION OF ORALLY DISINTEGRATING TABLETS OF DROTAVERINE HYDROCHLORIDE USING SUBLIMATION TECHNIQUE

Objective: To formulate orally disintegrating taste masked tablets of drotaverine hydrochloride (HCl) by sublimation technique.Methods: Initially superdisintegrant was selected and its concentration was optimized by pre-compression and post-compression parametric evaluation. Camphor and menthol were used as sublimating agents alone and in combination to mask the taste of drotaverine hydrochloride. Prepared tablets were evaluated for physicochemical evaluation, in vitro dissolution studies and fourier transformation-infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry studies.Results: The optimised formulation DCM2 prepared with a mixture of camphor and menthol was characterised by fourier transformation-infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry studies and found no incompatibility and no major shifts were noticed.Conclusion: The results demonstrated that the prepared drotaverine HCl orally disintegrating tablets showed better taste masking. The present sublimation technique can be effectively used for taste masking and also for orally disintegrating tablets.

THE EFFECT OF COPROCESSED SUPERDISINTEGRANTS RATIO (CROSPOVIDONE-SODIUM STARCH GLYCOLATE) TO THE PHYSICOCHEMICAL CHARACTERISTICS OF ATENOLOL ORALLY DISINTEGRATING TABLETS

Objective: The objective of this study was to evaluate the effect of coprocessed superdisintegrants (crospovidone-sodium starch glycolate) ratio 1:1; 1:2; and 1:3 to the physicochemical characteristics of atenolol orally disintegrating tablets.Methods: Orally disintegrating tablets of atenolol were prepared by direct compression method. There were three formulas which using three different ratios of coprocessed superdisintegrants (crospovidone-sodium starch glycolate). The ratio of coprocessed superdisintegrants were, 1:1 (formula 1); 1:2 (formula 2); and 1:3 (formula 3). Evaluation of the formulas was conducted before compression (pre-compression evaluation) and after compression (post-compression evaluation).Results: The results of pre-compression evaluation showed that all the formulas have good flowability and excellent angle of repose. The results of post-compression evaluation showed that all the formulas met the specification of orally disintegrating tablets. The different ratio of coprocessed crospovidone-sodium starch glycolate (1:1; 1:2; and 1:3) caused significant differences in tablet dispersion time (p<0.05). Dissolution test showed that all the formulas met the specification of dissolution from atenolol tablet (not <85% of atenolol was dissolved in 30 min). Formula 1 showed the highest dissolution efficiency (92.91±0.11)% and area under the curve value (11149.13±13.15) compared to formula 2 and formula 3.Conclusion: The results from this study showed that coprocessed superdisintegrants (crospovidone-sodium starch glycolate) ratio affect the physicochemical characteristics of atenolol orally disintegrating tablet. Based on pre-compression evaluation and post-compression evaluation, formula 1 was the best formula.

DESIGN ZOLMITRIPTAN LIQUISOLID ORODISPERSIBLE TABLETS AND THEIR IN VITRO EVALUATION

<p><strong>Objective: </strong>The objective of present study is to develop orodispersible tablets (ODTs) of zolmitriptan by liquisolid technique using different types of super disintegrants to enhance the disintegration and dissolution of zolmitriptan to improve the bioavailability of the drug.</p><p><strong>Methods: </strong>Liquisolid ODTs of zolmitriptan were prepared from; microcrystalline cellulose (Avicel PH-102) as carrier, colloidal silicon dioxide (Aerosil 200) as a coating material, croscarmellose sodium (CSS), sodium starch glycolate (SSG), and crospovidone (CP) as super disintegrants, and propylene glycol as liquid vehicle. The ratio of carrier to coating material was kept constant in all formulations at 35:1, this ratio was chosen after testing the ratios 10:1, 15:1, 20:1, 25:1,30:1, and 35:1. The ratio 35:1 give optimal results relative to other ratios. The pre-compression evaluation includes: flow properties were measured using the angle of repose and the compressibility index and FT-IR. The prepared liquid-solid system compacts were evaluated for their post-compression evaluation which includes: hardness, friability, wetting time, <em>in vitro</em> disintegration time, drug content and <em>in vitro</em> drug release.</p><p><strong>Results: </strong>The tabletting properties of the liquid-solid ODTs were within the acceptable limits. Among the three super disintegrants, CP found to be the best in term of showing the fastest disintegration time. The optimized selected formula (F11) was prepared using 5% w/w crospovidone, by direct compression showed the shortest disintegration time (24 s), superior drug release profile [ the time required for 80% of the drug to be released (T<sub>80</sub>%) and percent drug dissolved in 2 min (D<sub>2 </sub>min) 1.84 min and 87.59%, respectively]. In addition to that, the selected formula had an acceptable hardness and friability, so it was selected as the best formula.</p><p><strong>Conclusion: </strong>The overall results showed that CP was the best super disintegrant of showing the shortest disintegration time while loading factor of 0.125 was the best in the preparing of zolmitriptan liquid-solid ODTs, and this suggested the possibility of utilizing the selected best formula (F11) in the preparation of zolmitriptan ODTs as a new dosage form for oral administration. </p>

Formulation, development and evaluation of colon-specific ketorolac tromethamine compression coated tablets

The major intention to formulate and develop colon targeted tablets is to improve the therapeutic efficacy by increasing therapeutic drug concentrations in colon. The present study was aimed to develop guar gum compression coated tablets ketorolac tromethamine to achieve the colon-specific drug release. In this study, both core and compression coated tablets were prepared by direct compression method. The prepared colon targeted tablets were characterized for different pre-compression and post-compression evaluations. In vitro drug release studies were performed by using USP XXIV Type II dissolution apparatus in simulated gastrointestinal fluids. From the in vitro dissolution studies, the formulation F4 showed 4.72±0.76% drug release in 5 h and it was progressively increased to 99.12±0.42% in 24 h that indicates retardation of drug release in stomach and small intestine and significant amount of drug release was observed in colonic environment. The accelerated stability studies proved the stability of guar gum compression coated tablets. From the above results, achievement of colon specific drug release might be due to substantial integrity of the compression coated guar gum in the upper gastrointestinal trac , but microbial degradation in the colon. In conclusion, development of microbial degradation compression coated tablets was suitable to target the ketorolac tromethamine to colon. Further the efficacy of the developed formulations has to be assessed by pharmacokinetic studies.Keywords: In vitro drug release, Microbial degradation, Pre-compression, Post-compression, Simulated gastrointestinal fluids, Upper gastrointestinal tract

Isolation and preliminary evaluation of Mulva Neglecta mucilage: a novel tablet binder

ABSTRACT The aim of this study was to evaluate binding potential of Mulva neglecta mucilage (MNM) with subsequent comparison to PVP K30. Eight batches of Diclofenac sodium tablets were prepared by wet granulation technique keeping different concentrations (4, 6, 8 & 10% w/w) of Mulva neglecta mucilage (extracted from leaves of Mulva neglecta) and PVP K30 as standard binder. The granules of formulated batches showed bulk density (g/mL) 0.49 ± 0.00 to 0.57 ± 0.00, tapped density (g/mL) 0.59 ± 0.01 to 0.70 ± 0.01, Carr's index 09.27 ± 0.95 to 19.65 ± 0.59, Hausner's ratio 1.12 ± 0.00 to 1.24 ± 0.01 and angle of repose 30.37 ± 2.90 °C to 36.86 ± 0.94 °C. Tablets were compressed to hardness 7.50 to 7.95 kg/cm2. The tablets showed 0.39 ± 0.02 to 0.39 ± 0.01% friability and 7:20 to 14:00 min disintegration time. Granules and post-compression evaluation revealed that parameters assessed were all found to be within the pharmacopoeial limits. The results (hardness, disintegration and dissolution) proved that Mulva neglecta mucilage has better binding capacity for preparation of uncoated tablet dosage form as compared to PVP K30. Among all the formulations, MN-1 to MN-4 showed slow release as compared to PV-1 to PV-4 and thereby Mulva neglecta mucilage exhibited satisfactory drug release phenomenon tablets of diclofenac sodium.

Formulation Approach to Improve the Gastric Residence Time of Bisoprolol Fumarate by Gastro-Retentive Tablets

Purpose: Gastric retentive drug delivery devices can be used for controlled drug delivery systems containing drugs, which are degraded in the colon. The main objective of the present study is to design and formulate gastric retentive controlled release dosage form of bisoprolol fumarate in order to improve the gastric residence time, which in turn increases its bioavailability. Approach: Floating dosage form of bisoprolol fumarate was prepared by direct compression method using different concentration and grades of hydroxypropyl methylcellulose and sodium bicarbonate. Prepared powder mixtures and tablets were subjected to various pre-compression and post-compression evaluations respectively. Findings: Powder mixture showed good flow properties for uniform die filling. The SEM analysis showed minimum number of pores and erosion on the surface of the tablet. The optimized formulation F8 gave floating lag time less than 3 min with a floating time of 12 h, and an in vitro release profile very near to the desired release. The prepared dosage form reported to follow the zero order release and non-Fickian mechanism. Best formulations were subjected to accelerated stability studies. The assay results showed that the drug was stable for 3 months without any change in the drug content. Conclusion: Finally it can be concluded that the gastric retentive time of bisoprolol can be increased by formulating it in a floating dosage form.

Hibiscus Rosa-Sinesis Leaves Polysaccharide as Solubility Enhancing Agent for Poorly Soluble Drug

The main purpose of this research was to use hydrophilic Hibiscus Rosa-sinesis (HRS) dry leaves mucilage as functionality solubility enhancing agent for the design and development of solid dispersion of the drug Telmisartan (TS) to formulate tablets and to study its in vitro quality control tests. The mucilage was extracted, isolated, purified and prepared solid dispersions with different ratio of drug: mucilage (1:0.5, 1:1.0, 1:1.5, 1:2.0 and 1:2.5) using solvent evaporation method and another. Two formulations were prepared using drug: mucilage ratio of 1:1.0 as co-grinding method (GM) and physical mixture (PM). The solubility study showed a significant enhancement in the aqueous solubility of the drug where the solubility rate was increased with the increment in ratio of the mucilage. The formulation giving the best solubility enhancement of Telmisartan in aqueous media was in the order of SD > GM > PM > API. Then, the dispersions were compressed into tablets where it passed the precompression and post-compression evaluation parameters. Swelling index increased as the amount of mucilage added to each formulation (SD1 to SD3). Nevertheless as the amount of mucilage is increased for formulation SD4 and SD5 (1:2.0 and 1:2.5 ratio of drug: mucilage) the swelling index were decreased. The in-vitro dissolution study revealed that there is marked decrease in the dissolution rate of Telmisartan for all the solid dispersion containing tablets when compared to Telmisartan API tablets. This proves with the increase in mucilage ratio, the drug release from the solid dispersion tablet got retarded because of the formation of highly viscous barrier layer at the interface of the tablet and dissolution medium. In conclusion, the solubility of the drug has been greatly enhanced by the solid dispersion technique incorporating HRS mucilage using solvent evaporation method. Therefore, it is suggested that the drug Telmisartan can be converted to solid dispersion using Hibiscus Rosa-sinesis dry leaves mucilage as solubility enhancing agent and the solid dispersion granules can be filled in capsules as a dosage form.

Preparation and Evaluation of Ketoprofen Enteric Coated Mini Tablets for Prevention of Chronic Inflammatory Disease

Preparation and Evaluation of Ketoprofen Enteric Coated Mini Tablets for Prevention of Chronic Inflammatory Disease Ketoprofen is the propionic acid derivative used to treat chronic inflammatory disease like rheumatoid/Osteoarthritis. Here, the delivery of the drug based on the mini tablets approach, the few reasons for the mini tablets to avoid the drug release related fluctuations in the body and greater surface area leads to improve the bioavailability when compared with the single tablet dosage form. The tablets were prepared with two different polymers POLYOX WSR and HPMC K4M used individually. The evaluation parameters include preformulation studies, like DSC, solubility and flow properties of powder and post compression evaluation parameters includes hardness, weight variation, content uniformity, Friability, in vitro dissolution, SEM and in vivo radio graphic studies were successfully performed. The tablets were compressed with 3 mm punches by direct compression technique. The results of In vitro release studies of ketoprofen optimized core tablets in pH 6.8 phosphate buffer have shown 98.2% with HPMC K4M and 94% with POLYOX WSR within 12h time period and enteric coated optimized formulation has shown 97.79 ± 1.77. In vivo radio graphic studies showed that the tablets reached the intestinal region within 3 h after administration and was visually observed for 9h in the colonic region after that no tablet was found, total radiographic study was carried out with a single mini tablet due to effect of motility problem.

Lemon Peel as a Potential Source of Pectin and it's use as Application of Pectin as Binder in the Formulation of Tablets

Present study was aimed to study the use of pectin isolated from the lemon peels and assess its binding property in tablets using febuxostat as a model drug. The lemon peel which is waste part of lemon (Citrus limonis) remained after squeezing and taking the juice, are the potential source of pectin. The peels were shade dried and ground to get powder. The powder was subjected to simple water based blending and pectin was isolated using ethanol. Pectin was analyzed for confirmation. It has shown better binding properties. Tablets of febuxostat were formulated using pectin in different proportions (10, 20, 30 mg) and to compare the binding property of pectin, a reference batch was also formulated using starch as a binding agent instead of isolated pectin. Precompression and post-compression evaluation studies were performed for all formulations and found to be within the range as prescribed in the pharmacopoeias. Friability and disintegrating time of formulation F3 (30 mg of pectin) showed better results when compared to other formulations. In vitro dissolution studies revealed that formulation F3 containing 30 mg of pectin showed 82% drug release. In view of natural origin, better friability, hardness, disintegration time and drug release properties of the pectin formulation, lemon peel pectin can serve as an excellent binder in tablet dosage form.

Preparation and In-Vitro Evaluation of Donepezil Hydrochloride Sustained Release Matrix Tablets Using Non-Gelling Polymer

The aim of the current investigation was to develop a Sustained release tablet of Donepezil Hydrochloride using non- gelling polymer in order to overcome the problem of dose dumping. Viscarin GP-209 was used as a non-gelling release modifying agent. The formulated granule blends were evaluated for powder properties. Prepared tablets were subjected to post compression evaluations. In-vitro dissolution studies were carried out in 3 different dissolution profiles. Profile1: 0.1 N Hcl medium, Profile 2: pH 5.5 sodium phosphate buffer medium and Profile3: in 0.1 N Hcl for 2hrs and in 6.8 pH sodium phosphate buffer medium using the USP Type 2 apparatus as per the FDA guidelines. The dissolution data was fitted into various kinetic models to determine the release mechanism and mean dissolution time. Formulation F6 was considered as optimized as it showed similar drug release pattern with that of innovator immediate release formulation and similarity factor (f2) of 82. F6 formulation was found to be stable up to 3 months of stability testing at 40 o c / 75%RH.

Formulation and optimization of orodispersible tablets of flutamide

The present study aimed to formulate orodispersible tablets of flutamide (FTM) to increase its bioavailability. Orodispersible tablets were prepared by direct compression technique using three different approaches namely; super-disintegration, effervescence and sublimation. Different combined approaches were proposed and evaluated to optimize tablet characteristics. Sodium starch glycolate (SSG) was used as the superdisintegrant. The prepared powder mixtures were subjected to both pre and post compression evaluation parameters including; IR spectroscopy, micromeritics properties, tablet hardness, friability, wetting time, disintegration time and in-vitro drug release. IR studies indicated that there was no interaction between the drug and the excipients used except Ludipress. The results of micromeritics studies revealed that all formulations were of acceptable to good flowability. Tablet hardness and friability indicated good mechanical strength. Wetting and dispersion times decreased from 46 to 38s by increasing the SSG concentration from 3.33 to 6.66%w/w in tablets prepared by superdisintegration method. The F8 formulation which was prepared by combined approaches of effervescence and superdisintegrant addition gave promising results for tablet disintegration and wetting times but failed to give faster dissolution rate. The incorporation of 1:5 solid dispersion of FTM: PEG 6000 instead of the pure drug in the same formulation increased the drug release rate from 73.12 to 96.99% after 15min. This increase in the dissolution rate may be due to the amorphization of the drug during the solid dispersion preparation. The presence of the amorphous form of the drug was shown in the IR spectra.

Bioadhesive Controlled Release Clotrimazole Vaginal Tablets

Purpose: To formulate bioadhesive clotrimazole vaginal tablets using natural polymers in order to provide long-term therapeutic action at the site of infection. Methods: The tablets were prepared by direct compression using bioadhesive polymer mixtures: hydroxypropyl methylcellulose/sodium carboxymethylcellulose (HPMC/NaCMC) and HPMC/Guar gum (GG) in different ratios. Differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) spectroscopic evaluations were carried out to assess compatibility between the drug and the excipients. The tablets were subjected to various pre- and post-compression evaluations, including in vitro drug release, in vitro bioadhesive strength, swelling and stability studies. Results: The results show that all the formulations satisfied Indian Pharmacopoeial specifications for tablet parameters. DSC and FT-IR data indicate there was no interaction between the drug and the excipients. Drug dissolution rate at pH 6.0 followed the rank order: HPMC)/NaCMC > HPMC/GG. There was increase in swelling index with time at 37 0C. The combination of HPMC with NaCMC showed greater mucoadhesive strength and superior controlled drug release to the formulations prepared with GG polymer mixture. Furthermore, the release properties of the former in pH 6.0 buffer, as well as release mechanism (n values), were negligibly affected by ageing. Conclusion: This study indicates the possible use of suitable mixtures of natural and semi-synthetic cellulosic polymers for the preparation of clotrimazole mucoadhesive tablets for application as a vaginal controlled delivery system. Keywords: Clotrimazole, Swelling, Cellulosic polymers, Guar gum, Bioadhesion, Release properties