Wet Granulation Method Research Articles

Compressional Physics of Binary Mixture of Dried Andrographis paniculata and Moringa oleifera Leaves

Traditionally, the leafy part of Andrographis paniculata and Moringa oleifera have been widely reported to manage hypertension. Investigation of its pharmacological actions justifies its use. As part of formulation studies to standardize them, this study focused on their compaction and compression properties. Compacts equivalent to 250 mg of A. paniculata and M. oleifera were produced by compressing powders and granules at various compression pressure. Results show that M. oleifera met the WHO limit for ash values. Relative density values for granulated batches were higher, while their moisture content values were lower when compared to those of direct compression. The result from Heckel plots shows that batches deform mainly by plastic flow. For Kawakita plots, values of 1/b show that batches containing microcrystalline cellulose were less cohesive. The plot of tensile strength signifies that granulated batches achieved maximum crushing strength faster at low pressure. Formulations containing maize starch were shown to have higher percent porosity, and granulated batches gave higher values for apparent density-pressure relationship and lower friability values. Tablets produced by the wet granulation method showed better compression and compaction properties than those formulated by direct compression.

Formulation of Moringa oleifera Leaf Cereal Granules with Variation Types of Binder and Xanthan Gum Concentration

Moringa leaves contain macronutrients and micronutrients, potential to be developed into cereal products in the form of granules using the wet granulation method. The type of binder and the concentration of the suspending agent are the main factors that affect the physical characteristics and proximate content of cereals. In this research, 6 formulas of cereal granules were optimized with various types of binders (arrowroot flour, sorghum flour, cornstarch) and variations in the concentration of xanthan gum (0.5% and 1.0%). This study aims to obtain a granule formula of Moringa leaf cereal that meets the requirements of physical, chemical, proximate, and heavy metal characteristics. The results of the evaluation of the granule characteristics showed that all Moringa leaf cereal formulas had good flow characteristics. The results of the evaluation of cereal characteristics after reconstitution showed that cereal granules dispersed quickly (12.58–16.45 seconds), viscosity 73.75 -245 cps, pseudoplastic flow characteristics, and met the pH requirements of food products (5.00-6.00). The results of proximate analysis and metal content showed that all cereal formulas met the SNI requirements for cereal milk (SNI 01-4270-1996) in terms of protein, carbohydrate, ash, lead (Pb), and copper (Cu) content parameters. The most optimal cereal formula is formula 2 because it shows physical characteristics, fat content, carbohydrates, protein, and heavy metals that meet the requirements, as well as crude fiber content (0.76%) which is closest to the requirements (0.7%).

Formulation and Evaluation of Tablets Containing Fenugreek Extract Using Sodium Starch Glycolate as Super Disintegrant

The present work is aimed to formulate the tablets containing fenugreek extract as drug by wet granulation method. Further the effect of Sodium Starch Glycolate as super disintegrant on disintegration and drug release was studied. Fenugreek extract contains mucilage which retards the disintegration of tablets and hence shows slower drug release. Hence in order to improve disintegration and thereby in vitro drug release, Sodium Starch Glycolate was used as super disintegrant.
 Tablet formulations were prepared without the SSG (Conventional-F1) and also with sodium starch glycolate (F2-F4) by wet granulation method. Assessment of flow properties of granules, physicochemical characterization of tablet formulations was carried out. Fenugreek is widely used for its antidiabetic activity which is attributed to mainly to the presence of an alkaloid Trigonelline. Hence in vitro release study of trigonelline was carried out which showed that the percentage release from F1 and F2 was found to be 58.12±4.49 and 99.08±0.01 respectively after 6 hrs. This study concludes that tablet formulation of fenugreek seed extracts with super disintegrants will be more desirable, advantageous and therapeutically more beneficial than incorporating the direct plant materials for the treatment of diabetes for faster onset of action.

Vaginal delivery of clotrimazole by mucoadhesion for treatment of candidiasis

The aim of this study was to prepare mucoadhesive vaginal tablets of clotrimazole for treatment of vaginal candidiasis. A combination of mucoadhesive polymers like HPMC K100M, Sodium CMC, and Eudragit L100 were used in different ratios prepare solid dispersions to enhance its solubility. Tablets were prepared by the wet granulation method. Solid dispersions were evaluated for saturation solubility. All tablet batches were evaluated for weight variation, hardness, friability, drug content, swelling index, in vitro drug release study, ex vivo diffusion and mucoadhesive strength. FTIR spectra showed there was no interaction between the drug and the excipients. HPMC K100 M increased the solubility of clotrimazole in simulated vaginal fluid at pH 4.5. Eudragit L100 was shown to increase the swelling and mucoadhesive strength of the tablet, i.e., 3.03 and 3.29 g. The in vitro and ex vivo release of all 9 batches showed between 61 to 78% release in 8h. Ex vivo diffusion studies using sheep vaginal membrane showed 43 to 59% in 6h in simulated vaginal fluid. The release and flux were nearly comparable to marketed tablet i.e., Candid-V6. The drug release of all batches followed the Korsmeyer-Peppas kinetic model, and the mechanism was found to be non‐Fickian/anomalous.
 Keywords: Clotrimazole, solid dispersion, HPMC K100M, Eudragit L100, Sodium CMC.

Detailed Research on a Comparative Evaluation of Diclofenac Sodium Tablets Manufactured by Using DC Grade Excipients and Wet Granulation Methods

Detailed Research on a Comparative Evaluation of Diclofenac Sodium Tablets Manufactured by Using DC Grade Excipients and Wet Granulation Methods

Analysis of Flow Characteristics and Paracetamol Tablet Hardness Using 2D Double Mixer of Design Drum Type with Rotation and Mixing Time Variations

One of the tablet manufacturing processes using the wet granulation method is the process of mixing the active ingredient granules, fillers, binders and pelicans. The parameters of the mixing process are important to study because they will affect the physical properties of the tablet. This study studied the effect of the variable duration and the size of the mixing cycle on the physical properties of paracetamol tablets using a 2D double mixer. The results of the analysis and testing showed that the variation of mixing time and the size of the rotation had a significant effect on the flow properties of the granules and the hardness of the tablets. In addition, the optimal parameter results to obtain optimal tablet hardness occurred at 15 minutes of mixing process and 50 rpm of rotation.

Development of novel lozenges tablets containing chloroform root extract of Adenodolichos paniculatus (hua) Hutch. & Dalz (Fabaceae)

Medicinal plants have been widely used as a source of medicine to combat ailments including infectious disease and may constitute a reservoir of new antimicrobial substances to be developed. Adenodolichos paniculatus is a medicinal plant widely used for the traditional remedy of coughs, dysentery, diarrhea and sore throat infections. The aim of this study was to formulate Adenodolichos paniculatus chloroform root extract as a novel lozenge tablet and to evaluate their antibacterial and tablet parameters. Streptococcus pyogenes, Staphylococcus aureus and Pseudomonas aeruginosa were used as the test bacteria. The extract was formulated into Lozenge tablets using wet granulation method with gelatin and sucrose as binder and diluent respectively. Uniformity of weight, hardness, friability, bacterial susceptibility tests were conducted on two batches of formulated Lozenges of 25 and 50 mg and a reference standard formulation, StrepsilsR, containing Amylmetacresol (0.6 mg) and 2,4-dichlorobenzyl alcohol (2 mg). Results showed that both batches passed the tablet weight uniformity test with mean crushing strengths of 10.4 and 13.1 KgF, respectively. S. pyogenes, S. aureus and P. aeruginosa were susceptible to both batches with inhibition zones ranging from 18.00-25.50, 16.00-21.50 and 9.00-12.00 mm and 22.00-26.50, 20.50-23.00 and 10.00-13.00 mm respectively. The bacterial susceptibility compared favorably with the standard formulation as the difference between the inhibition zone diameters of each test bacteria and the standard formulation was not statistically significant (p˃0.05). The result indicated that there was a delayed release of the extract from the test lozenges with batch 1 (25 mg) being from 30 minutes and batch 2 (50 mg) from 60 minutes compared to that of the standard formulation which had immediate drug release at 5 minutes. The method used for the formulation and the sticky nature of the extract might not allow and promote the immediate release of the antibacterial extract from the dosage form.

PENGARUH KONSENTRASI HYDROXYPROPYL METHYLCELLULOSE SEBAGAI BAHAN PENGIKAT PADA SEDIAAN TABLET EKSTRAK RIMPANG JAHE MERAH (zingiber officinale Var. Rubrum.)

Lozenges are solid preparations made from aromatic and sweet taste that can dissolve slowly in the mouth, which are intended to treat infections in the mouth and throat. Hydroxypropyl Methylcellulose (HPMC) is a binder that can be used in lozenges.This study attempted to examine the effect of the concentration of HPMC as a binder in the tablet preparation of red ginger rhizome extract (Zingiber officinale Var Rubrum) by wet granulation method. This study was a laboratory experimental study by comparing the three concentrations of HPMC binder used in each formula i.e., FI (4%), FII (5%), FIII (6%).The resulting tablets were tested for physical properties including organoleptic tests, weight uniformity, tablet hardness, tablet friability and hedonic tests. Based on the results of the study, it was shown that with an increase in the concentration of the HPMC binder, the physical quality of the resulting tablet also increased. The higher the concentration of HPMC used, the better the uniformity of weight and the high level of tablet hardness. However, tablet friability will decrease. The results showed that the concentrations of 4%, 5%, and 6% had an effect on the tablet physical properties whichwas fragility. Further, formula II with a concentration of 5% had better tablet physical quality and was preferred by respondentsbased on hedonic tests.

Design of Solid Dosage Form using Isolated Mucilage from Cassia fistula

The present study was aimed to isolate and characterize mucilage obtained from the leaves of Amaltas (Cassia fistula) and to check the binding efficiency by comparing with gum acacia. Isolation of mucilage was done by hot maceration process and investigated for various physicochemical characterization and in vitro dissolution profile to check mucilage as a binding agent. Different batches (KF1 – KF4) of paracetamol tablets of different concentration of mucilage (3%, 5%, 10% and 15% w/v) were prepared by wet granulation method. All the parameters of uncoated tablets were performed and compared with tablets prepared with gum acacia in the same concentration. SEM indicated irregular shape and size of mucilage particles. Good thermal stability of mucilage was indicated by TGA and amorphous nature by P-XRD and DSC. FTIR and NMR confirmed the presence of polysaccharide. From the results, formulations KF2 and KF3 were found to be optimized as they showed 99% drug release within 20-25 min and better results were obtained when compared with existing binder gum acacia. According to the studies, mucilage isolated from the leaves of Cassia fistula showed interesting results suggesting that amaltas mucilage can be used as a promising natural excipient (binder) in preparation of conventional uncoated tablet dosage form.

Formulation, Evaluation of Physical Properties, Anti-Cholesterol Activity from Ficus carica L. Leaves Extract Tablet

Figs knew playing vital roles in reducing cholesterol, strengthening the heart, and controlling respiration. Figs leaves extract with a dose of 50 mg/kg and 100 mg/kg can reduce triglyceride levels and can increase HDL cholesterol levels. This study aims to determine the effect of Ficus carica L. (fig) leaves extract on tablet dosage forms to reducing total cholesterol in rats induced with pork fat feed. Tablets were made by the wet granulation method in three formulas, there are F1 (extract dose 50 mg), F2 (extract dose 100 mg), and F3 (extract dose 150 mg), and compared with simvastatin tablets. The rats used in this study were 40 animals which were divided into 8 groups. Negative control group (induced of pork oil), F1 group, F2 group, F3 group, F4 group (placebo), positive control group (simvastatin 10 mg), base suspending agent group, and normal group.The average weight (mg) of F1 tablets (605.96 ± 9.94%), F2 (611.81 ± 12.33%), and F3 (639.09 ± 4.65%). As for the uniformity of size, all formulas have a diameter of 0.9 ± 0.0 (cm). for the hardness values of F1 (6.54 kg), F2 (5.31 kg), and F3 (5.43 kg). The value of friability F1 (0.8%), F2 (1.38%), and F3 (0.77%). While the disintegration time of F1 (13.31 minutes), F2 (19.48 minutes), and F3 (21.11 minutes). Whereas the dissolution rate (DE45) of each formulation decreased with increasing dose of extract, F1 (69.43%), F2 (64.95%), and F3 (60.04%). Extract contain quercetin as flavonoid, saponin, polyphenol, alkaloid, and tannin. Based on the results of statistical analysis, extract tablets did not differ significantly from simvastatin tablets in reducing total cholesterol levels. Tablet formulation of fig leaves extract with a dose variant has been shown to reduce total cholesterol in the blood between 18.3% until 37.98%.

SUSTAINED RELEASE MATRIX DRUG DELIVERY SYSTEM: AN OVERVIEW

Oral delivery of drugs is the most preferable route of drug delivery due to the ease of administration, patient compliance and flexibility in formulation, etc. Sustained release constitutes are the dosage form that provides medication over an extended time or denotes that the system is able to provide some actual therapeutic control whether this is of a temporal nature, spatial nature or both. The objective of the study was to explore the necessity, advantages and various techniques of extended release matrix tablet to get a constant drug delivery rate and reproducible kinetics for advance delivery. Matrix tablets are the type of controlled drug delivery systems, which release the drug in continuous manner by dissolution controlled as well as diffusion controlled mechanisms. To control the release of the drugs, which are having different solubility properties, the drug is dispersed in swellable hydrophilic substances, an insoluble matrix of rigid non swellable hydrophobic materials or plastic materials. Matrix tablets can be formulated by either direct compression or wet granulation method by using a variety of hydrophilic or hydrophobic polymers. The extended release matrix tablets can assure better patient compliance through reduction in total dose and dosage regimen, which can be great help to treat chronic diseases. This review highlights the types of matrices, mechanisms involved and evaluation studies.

Extraction and Evaluation of Lepidium Sativum and Flax Seeds Mucilage as a Pharmaceutical Granulation Binder

The powders are held together by a binder to form granules. Some excipients are of natural origins are currently available as an alternative over the synthetic ones in pharmaceutical formulation. The aim of this study was to isolate the mucilage from different plant seeds and compare them to evaluate the binding effects. In the present study, an effort was made to investigate the efficacy of mucilage obtained from Lepidiumsativum and flax seeds as granules excipients. The mucilage was extracted from selected seeds by the conventional method by precipitation of soaked and blended seeds in acetone. The dried mucilages were subjected to several phytochemical and physicochemical properties. Granules were formulated by wet granulation method by using extracted mucilage as a binding agent and comparisons were made against the granules prepared with standard binder as PVP. The granules are evaluated by various physical properties such as (bulk and tapped densities, Hausner’sratio, Carr’s index, angle of repose and friability). The results showed that the granules prepared from extracted mucilage as a binder had good flow and mechanical properties, all evaluated parameters were within the permissible limits. Thus, mucilage could be used as an alternative binding agent in pharmaceutical granules.

FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE SUSTAINED RELEASE MATRIX TABLETS

Objective: Now a days as very few antidiabetic drugs are coming out of research and development and some existing drugs are showing several side effects when administered orally, multiple times in a day, hence change in the operation is a suitable and optimized way to make some drug more effective by slight alteration in the drug delivery. Matrix type drug delivery systems of an antidiabetic drug like Metformin Hydrochloride, is an interesting and promising option when developing an oral sustained release system
 Methods: An appropriately designed controlled release drug delivery system can be a major advance towards solving problems concerning the targeting of a drug to a specific organ or tissue and controlling the rate of drug delivery to the target sites. This research work is made in designing of sustained release dosage form of Metformin Hydrochloride by wet granulation method employing both Xanthan Gum and Hydroxy Propyl Methyl Cellulose (HPMC K4M) as a rate controlling polymer.
 Results: The development of oral sustained release systems has been a challenge to formulation scientists due to their inability to restrain and localize the system at targeted areas of the gastrointestinal tract. From all the formulation trial batches, formulation F7 shows the best results. It has been observed that HPMC K4M alone cannot give satisfactory drug release profile but the blend of HPMC K4M and Xanthan gum together give the best drug release kinetics.
 Conclusion: The drug release mechanism from the matrix tablets follows Fickian diffusion with first order kinetics. Thus, sustained release matrix tablets of metformin hydrochloride can be expected to reduce the frequency of administration and decrease the dose dependent side effects

The Possible Antidiabetic Effect of Ficus carica L. Tablet on lloxan-Induced Diabetes Model in Rats

BACKGROUND: Fig leaves are reported to have an effect on reducing blood glucose levels. However, the use of fresh leaves makes the effects obtained is not measurable and efficient. AIM: The purpose of this research was to determine the antidiabetic potential of ethanol extract of fig leaves and to optimize tablet dosage formulations. METHODS: Four tablet formulas were made using the wet granulation method. Formula I (FI), Formula I (FII), and Formula III (FIII) groups to give a tablet of ethanol extract of fig leaves with a dose of 40 mg, 60 mg, and 80 mg and placebo treatment group. There were eight groups of male rats strain Wistar treated as follows: Normal control, negative control, positive control (metformin tablets), basis group, placebo treatment group, F1, F2, and F3 groups. The antidiabetic activity was evaluated from a decrease in rat blood glucose levels. Previously, rats were induced first using alloxan 150 mg/kg intraperitoneally to damage β-pancreatic cells so that the rats could experience increased blood glucose levels. After giving treatment to each group for 14 days, a rat blood sample was then taken on days 9 and 14, which were then analyzed by the GOD PAP method with readings carried out using a spectrophotometer with a wavelength of 500 nm. RESULTS: The average weight (mg) of FI tablets (617.8 ± 3.21%), FII (629.35 ± 8.16%), and FIII (643.6 ± 6.21%), and placebo tablet (666.45 ± 4.36%). As for the uniformity of size, all formulas have a diameter of 0.9 ± 0.0 (cm). For the hardness values of FI (5.7 kg), FII (1.31 kg), and FIII (3.09 kg), placebo tablet (2.98%). The value of friability FI (1.42%), FII (11.8%), and FIII (0.84%), placebo tablet (1.16%). While the disintegration time of FI (11.02 min), FII (10.10 min), and FIII (17.00 min), placebo tablet (12.23%). As for the uniformity of size, all formulas have a diameter of 0.9 ± 0.0 (cm). Whereas the dissolution rate (DE45) of each formulation decreased with increasing dose of extract, FI (73.73%), FII (74.80%), and FIII (69.80%). The treatment group of the ethanol extract of fig leaves at a dose of 40 mg, ethanol extract of fig leaves at a dose of 60 mg, and ethanol extract of fig leaves at a dose of 80 mg could reduce rats’ blood glucose levels with statistically significant results (p < 0.05) compared to negative group. When it was compared to the positive group, it had significant results with a statistical value (p < 0.05). CONCLUSION: Ethanol extract of fig leaf tablets had a significant effect on lowering rats’ blood glucose levels.

FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE AND GLICLAZIDE SUSTAINED RELEASE BILAYER TABLETS: A COMBINATION THERAPY IN MANAGEMENT OF DIABETES

Objective: The main objective of the present investigation is to develop a sustained-release (SR) formulation to optimize the postprandial elevation of glucose level in type 2 Diabetic subjects using combination therapy. In the present research work, bilayer sustained release formulation of metformin hydrochloride (MFH) and gliclazide (GLZ), based on monolithic-matrix technology was developed and evaluated. Methods: The formulations of metformin hydrochloride layer and gliclazide layer that contain polyox WSR coagulant and different viscosity grades of hydroxyl propyl methylcellulose (HPMC) as sustained-release matrix were prepared by direct compression and wet granulation method respectively. The bilayer tablets were prepared after carrying out the optimization of metformin layer and evaluated for various pre-compression and post-compression parameters. For the best formulation selected on basis of in vitro evaluation of tablets, Fourier-transform infrared spectroscopy (FT-IR) studies and comparison of in vitro dissolution profile of developed formulation with the innovator were performed. Results: Metformin hydrochloride and gliclazide showed sustained release of drug by diffusion mechanism and followed first-order kinetics. The best formulation of metformin hydrochloride (M7) and gliclazide (G8) show 99.93% and 99.65% of drug release in 24 h respectively. The similarity factor (f2) was 79.95 for metformin hydrochloride and 73.62 for gliclazide when compared with the innovator. Conclusion: The monolith diffusion-controlled bilayer tablets of metformin hydrochloride and gliclazide offer improved patient compliance and convenience with better postprandial hyperglycemic control with once-a-day dosing. The sustained release of the drug up to 24 h regulate antidiabetic activity round the clock with minimal side effects.

FORMULATION, IN VITRO, AND IN VIVO EVALUATION OF TASTE-MASKED ORAL DISINTEGRATING TABLETS OF FEXOFENADINE HYDROCHLORIDE USING SEMISYNTHETIC AND NATURAL SUPERDISINTEGRANTS

Objective: The aim of the present research work was to prepare and evaluate taste-masked oral disintegrating tablets (ODT) of Fexofenadine hydrochloride. Methods: In the present work, Eudragit EPO, a taste masking agent and Karaya gum (GK) (natural), Sodium starch glycolate, and Croscarmellose sodium (CCS) (semi-synthetic) super disintegrants in three ratios (3, 6,9%) were used. Taste masked granules were prepared by different ratios of the drug: Eudragit EPO (1:1, 1:1.5, 1:2) by wet granulation method. The optimized taste-masked granules (1:2) were selected by sensory evaluation test to prepare 9 Fexofenadine ODT (FH1-FH9) formulations. These were evaluated for different parameters. Then desirability function (DF) was calculated for all formulations using disintegration time (DT), time taken for the tablet to release 90% of the drug (t 90%), and % drug dissolved in 10 min (Q10) as significant parameters. Results: The best formulation (FH6) showed the highest DF value due to less DT and 100% in vitro drug release within 15 min. Thus, FH6 formulation containing 9% CCS was selected as the best among the prepared formulations to which in vivo studies were performed on rabbits to find maximum plasma concentration (Cmax), time taken to reach maximum concentration (tmax), area under the curve (AUC), rate of elimination (Kel), absorption rate (Ka) and half-life(t1/2) and compared with Fexofenadine (Allegra) marketed tablets. Total bioavailability was increased for the test formulation compared to the reference formulation. Conclusion: Fexofenadine was successfully prepared as ODT with increased AUC and decreased tmax to which stability studies were conducted which were found to be stable.

Scaling of the Granulation Process in the Conditions of GMP Training Center and Assessment of Possible Risks

Introduction. The stage of wet granulation is often used in the technology of solids. The method of wet granulation in a mixer-granulator with high shear force can be regarded as the most complicated method of its implementation from the engineering and technological point of view. The mixer-granulator has two mixers located in mutually perpendicular planes. Using an impeller, dry components are mixed, and the chopper, turning on when spraying a humidifier, ensures the formation of granules. By setting different chopper rotational speed, granules of different sizes can be obtained. This granulator has the following advantages: it provides a high product yield (≥ 99 %), takes up small workspaces, and the closed design ensures environmental protection.Aim. The aim of the research is to scale the granulation process, on the example of the solids production technology, using the wet granulation stage - in a mixer-granulator with high shear force.Materials and methods. Dry extract «N» and auxiliary substances were used as a pharmaceutical substance: lactose monohydrate, microcrystalline cellulose (MCC) (MICROCEL® MC-102), potato starch, povidone (Plasdone™ K-29/32), calcium stearate. Granulate under scaling conditions was produced in a mixer-granulator with high shear force. Technological properties of dry extract «N» and granulate were determined by the methods described in National pharmacopeia XIV.Results and discussion. On the basis of experimental studies, it was found that the resulting granulate, both when obtained under laboratory conditions and under scaling conditions, has good flowability, and also has a homogeneous fractional composition. The presence of a grinder in the mixer-granulator made it possible to obtain a more uniform fractional composition of the granulate. A 10-fold increase in loading did not affect the composition of the granulate. When scaling the pelletizing process, a risk analysis was carried out, factors influencing the technological process were identified and structured. It turned out that the most important stages are mixing and the actual granulation. To obtain a homogeneous mixture, additional equipment was used - a mixer.Conclusion. As a result of scaling up the granulation process, the parameters of wet granulation in the mixer-granulator (optimal loading, impeller and grinder rotation frequency), technological properties of the resulting granulate, and risks affecting the technological process were selected. were evaluated and a causal diagram (Ishikawa diagram) was drawn.

Impact of Solubility Enhancement Methods on the Dissolution Rate of Valsartan Sachet

The oral drug delivery is the most generally used route of administration that has been explored for the delivery of drugs through various pharmaceutical products. Solubility of drug plays critical role in achieving the optimum therapeutic levels of the drug in blood and thus bioavailability. There are many drugs of various therapeutic categories fall in Biopharmaceutics Classification System Classes II and IV as they lack solubility. For all these drugs, dissolution is the big issue for the absorption process. Valsartan is an effective antihypertensive agent and it can be used for the treatment of hypertension in most cases. The objective of this study is to prepare Valsartan as an oral sachet which can be used as an alternative dosage form after improvement of drug solubility using solubilizing agents such as sodium lauryl sulfate and tween 80. Three different formulas of Valsartan sachet were prepared by conventional technique of wet granulation method named conventional formula (Fc), sodium lauryl sulfate formula (Fs), and tween 80 formula (Ft) then compared with the available marketed product of Valsartan tablet (Fd) as a reference. The preformulations studies were conducted to exclude drug excipients interaction. Evaluation was performed in terms of weight variation, dose content uniformity, and drug release study using dissolution test apparatus. Fourier Transforms Infrared Spectroscopy reveals no drug excipient interaction and the drug release profile for Fs and Ft formulas within 30 min was 100.16% and 104.16%, respectively, while for Fc only 57.55% of the drug was released. This difference in the release profile was statistically significant (P < 0.05) between Fs and Ft with Fc, but a non- significant difference (P > 0.05) was observed between Fs and Ft with the marketed Valsartan tablet (Fd). The results support the possibility of using the prepared formulas Fs and Ft as a Valsartan sachet for the oral administration alternative to conventional Valsartan tablets Fd.

Formulation and in vitro Evaluation of Matrix tablets containing Repaglinide

The aim of this project was to develop sustained release matrix tablets of Repaglinide. Sustained release matrix tablets of Repaglinide were prepared by the wet granulation method using polymers like Hydroxy propyl methyl cellulose, Microcrystalline cellulose, Eudragit RS-100 in different ratios. The matrix tablets of Repaglinide were evaluated for hardness, weight variation, friability, drug content uniformity, and in-vitro drug release. In order to determine the drug release mechanisms and kinetics, the data was subjected to zero order, first order, and higuchi and peppas diffusion model. Twelve batches of sustained release matrix tablets of Repaglinide were developed. Among these formulations F4, F8 and F12 formulation showed satisfactory physicochemical properties and drug content uniformity and sustained release of drug for 12 hours with maximum release of 86.95%, 84.91% and 84.91%. The optimized formulations were characterized for Differential scanning calorimetric analysis; Fourier transforms infrared spectroscopy and scanning electron microscopic studies. IR spectroscopic studies indicated that there were no drug-excipient interactions. The prepared sustained release matrix tablets of Repaglinide were successfully developed and evaluated.

The development of Moringa leaves effervescent granules with effervescent agent of citric acid and sodium bicarbonate

Moringa leaves are part of Moringa Oleifera, which have a high antioxidant content, therefore, it is beneficial for overcoming free radicals in the body. Furthermore, the leaves contents have the potential to be developed into a functional drink in the form of effervescent granules. The important aspects influencing the physical characteristics, stability, and acceptability of granule is the type and ratio of the effervescent agent. In this study, citric acid and sodium bicarbonate were used as effervescent agents because they both provide acceptable texture and mouthfeel. This study aimed to develop an effervescent granule formula of Moringa leaves and to optimize the molar ratio of citric acid and sodium bicarbonate as the effervescent agent. Three molar ratios of citric acid and sodium bicarbonate were optimized, namely 1:3.11 (Formulation 1), 1:3 (Formulation 2), and 1:2.93 (Formulation 3). These formulations were developed using the wet granulation method. The results showed effervescent granules of the three formulations exhibited good flowability and uniform particle size distribution. Furthermore, formulation 3 showed better granule flow characteristics than the others. The results after reconstitution showed the granules were quickly dispersed within 207-234 secs, the pH of the preparation ranged between 5.74-5.92 (neutral pH), the viscosity was between 326-333 cps, and exhibited dilatant flow characteristics. Also, the organoleptic and sensory evaluation results showed formulation 3 was the most acceptable in terms of color, taste, aroma, and texture. Based on these findings, it was concluded that formulation 3 which used (citric acid ratio, sodium bicarbonate 1:2.93) was the optimal formulation.