Current Issue : October-December Volume : 2014 Issue Number : 4 Articles : 23 Articles
Drug delivery technology is one of the frontier areas of research in the field of science and technology. Considerable attention is focused on the development of controlled drug delivery systems offering the advantages of better therapeutic efficacy and easier to comply with than the conventional regimens requiring more frequent dosing. For many disease states, the ideal dosage regimen is one in which an acceptable therapeutic concentration of the drug is immediately attained at the site of action and is maintained constant for the desired duration of treatment. Thus for such dosage regimen, a biphasic drug delivery system is beneficial. Biphasic drug delivery comprise of 2 phases i.e. immediate release phase and Sustained release phase. Few approaches had been explored in this drug delivery system like Bilayer tablets, Matrix tablets, Floating matrix tablets etc. But the drawbacks are always been a definite problems for tablets while incorporating two different phases in one tablet. To overcome these problem biphasic drug delivery through capsule device is prescribed drug delivery system. Review focused on formulation aspect of Capsule-In-Capsule Technology. The purpose of this comprehensive review is to compile the work going on this delivery system. This article explains why the development and production of biphasic drug delivery system through capsule device needs to be carried out on purpose to overcome common bi-layer table and matrix tablets problems....
The distinctive anatomy and physiognomy of the eye presents obstacles and challenging endeavours to pharmaceutical and research scientists in ophthalmic drug delivery. The currently available formulations suffer with the limitations of increased tear dilution, high tear turnover rate, precorneal elimination leading to high frequency of administration, low drug bioavailability, poor drug permeability. Futhermore, various precorneal (lacrimation, tear production, nasolachrymal drainage) and corneal barriers control the rate and extent of drug permeation. Therapeutic entities can be delivered efficiently to their site of action by the use of penetration enhancers which act by different mechanisms either by altering the properties of the limiting membrane or the therapeutically active drug. The principal focus of the review is to present an insight on the effectiveness of penetration enhancers, their comparative studies, uses and limitations in medications designed for ocular targeting, promoting corneal permeation and eliminating drug loss from the eye....
Diltiazem hydrochloride is a calcium channel blocker which is used for the treatment of hypertension and angina pectoris. Fast dissolving films of diltiazem hydrochloride were prepared by using solvent casting technique by using hydrophilic polymers HPMCE5, HPMCE15 and NaCMC alone and in combination with poly vinyl pyrrolidine. The excipients such as mannitol (as a sweetening agent) and citric acid (as a saliva stimulating agent) and propylene glycol (as a plasticizer). The films were subjected for evaluation tests such as thickness, weight variation, folding endurance, content uniformity, percentage moisture loss, percentage moisture absorption, surface pH test, disintegration time and in-vitro drug release. The influence of plasticizer on the release rate was also evaluated. The film prepared with Glycerin as plasticizer offered relatively rapid release of drug when compared with Propylene glycol and Poly ethylene glycol 400 plasticizers. Based on the evaluation tests the formulations prepared with HPMCE5 and poly vinyl pyrrolidine as polymer and glycerin as plasticizer was selected as optimized formulation. The optimized formulation has uniform thickness, neutral pH, very short disintegration time and in-vitro drug release was found to be 99.33% within 8 min. The dissolution rate followed first-order kinetics. A statistically significant difference between dissolution efficiencies of films formulated with different plasticizers was calculated using a one-way analysis of variance (ANOVA). The P value was found to be less than 0.05, which indicates that there was a significant difference between different plasticizers with respect to dissolution efficiencies...
The objective of the present work was to study the effect of different polymers on the solubility and dissolution rate of ibuprofen a poorly water soluble NSAIDs, by spherically agglomeration using methanol, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. The quasi-emulsion solvent diffusion technique was used as a method for spherical agglomeration. Spherical agglomeration of ibuprofen were prepared by using polyethylene glycol-4000, polyethylene glycol-6000 and PVP k-30 as water soluble carries proportions like 1:0.5,1:0.75,1:1. The agglomerates were subjected to various physicochemical evaluations such as practical yield, drug content, solubility, flow properities, average particle size, scanning electron microscopy and dissolution studies. The optical electron microscopy studies showed that the agglomerates posseeses a good spherical shape. This study, demonstrated that the successful development of directly compressible spherical agglomerates of ibuprofen prepared with hydrophilic polymers enhances the in-vitro dissolution property of ibuprofen, which could provide rapid onset of action and potentially increases oral bioavailability....
Microspheres are well accepted technique to control the drug release from the dosage form to improve bioavailability, reduce absorption difference in patients, reduce the dosing frequency and adverse effects during prolong treatment. The main objective of the present study was to prepare and evaluate ibuprofen microspheres by external ionic gelation method, with water soluble polymers such as sodium alginate and calcium chloride as crosslinking agent, using as carrier for oral administration in view to achieve oral sustained release of the drug. Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) used for relief of signs and symptoms of rheumatoid arthritis, osteoarthritis and is used in chronic and acute conditions of pain and inflammation. Its biological half-life is 2±0.5 hrs. Due to its low biological half-life (2 hrs), it requires frequent administration to maintain plasma concentration. This causes inconvenience to the patient and also leads fluctuations in plasma drug concentration that may cause inferior therapeutic effects or toxic effects. Therefore, development of controlled release dosage forms would clearly be beneficial in terms of decreased dosage requirements, thus increase patient compliance. The formulations were evaluated for particle size distribution analysis, flow properties like angle of repose, bulk density, tapped density, hausner’s ratio, carr’s index, encapsulation efficiency, scanning electron microscopy, optical electron microscopy and in-vitro release studies. The optimized formulation showed good in-vitro sustained release activity of the drug ibuprofen....
The purpose of the present research work was to develop ointment of Zaltoprofen with decreased systemic side effects and to create a more marked effect with lower doses of the drug. Ointment was developed using different bases like hydrocarbon bases, Absorption bases, and others exicipients. The ointment was prepared by simple fusion method in which the drug dissolve in ointment base. The ointment was evaluated for their physical appearance, pH evaluation, spreadability, viscosity, extruability, drug content, in-vitro permeation study and accelerated stability study (As per ICH guideline). Trial and error approach was used developing eighteen batches and finally six experimental batches were formulated and evaluated on the basis of physical parameters like (appearance, pH evaluation, spreadability, rheological study, drug content, in-vitro permeation study. No drug-excipients interaction was found. These ointment formulations showed acceptable physicochemical properties. In-vitro drug permeation studies were carried out using Franz diffusion cell for 6 experimental formulations (F1-F6). Results of all six batches showed that F2 batch was selected as optimized batch with desired pH (7.1), optimum viscosity (2585.5cps) and higher % drug release (85.12%). The stability study of F2 was carried out for 1 month. The result showed that there was no significant change in the ointment properties. The optimized formulations (F2) showed acceptable pH, good visual appearance, optimum viscosity, good spreadability, extruability, drug content uniformity and highest drug permeation as compared to other formulations. The optimized formulation was subjected to accelerated stability studies as per ICH guidelines and was concluded as a stable formulation....
Tolnaftate is a topically used antifungal agent, the aim of present research work was to develop an emulgel formulation of tolnaftate. Emulgel have emerged as one of the most interesting topical drug delivery systems as it has dual release control i.e. emulsion and gel. Thus in the present study efforts were made to formulate stable semisolid preparations containing 1% of tolnaftate. On the basis of solubility studies clove oil used as solubiliser of the drug to formulate microemulsion. The ternary diagram was plotted to identify microemulsion region. Various gelling agent were evaluated for their potential to gel of the tolnaftate microemulsion without affecting its structure. The effect of concentration of the gelling agent and emulsifying agent on the drug release was investigated using a 22 factorial design. The prepared emulgel were evaluated for their physical appearance, viscosity, drug release, globule size, spreadability skin irritation test, antifungal activity and stability study. The antifungal activity and drug release were found to be higher for optimized formulation. No irritation was observed on the skin of the white albino mice. Stability studies showed that the physical appearance, rheological study, in-vitro drug release and antifungal activity in all the prepared emulgel remained unchanged upon storage for 1 month....
Zidovudine sustained release matrix tablets were prepared by using two natural polymers and one semi-synthetic polymer. Three different ratios of polymers were selected for the fabrication of tablets, natural gums like (Hupugum, Sterculia gum) and semi-synthetic polymer like HPMCk100 at different ratios (5%, 10% and 15%) by direct compression method. The fabricated tablets were characterized for hardness, friability, drug content. In-vitro drug release studies were carried out in pH 1.2 buffer for 2 hrs and then in PH 6.8 phosphate buffer for 10 h. Dissolution studies were conducted for 12 hrs by the three polymers among them HPMCk100m showed more sustained nature with 96% efficiency compared to hupugum and sterculia gum. Order of release for all the formulations fitted zero order except F5, F7, F8 formulations followed first order kinetics. The mechanism of drug release from all the formulations followed anomalous mechanism....
In the present work, an attempt has been made to enhancement solubility and dissolution rate of poorly water soluble drug, naproxen by preparing ternary solid dispersions using combination of two hydrophilic polymers namely PVP K30 and PEG 4000. Drug carrier solid dispersions were prepared by solvent evaporation method using ethanol as a solvent. Solid dispersions of naproxen with PVP K30 and PEG 4000 having ratio of 1:0.5:0.5 markedly increase the solubility and dissolution rate of solid dispersion compared to the free form of naproxen. The characterization of ternary solid dispersion carried out using saturated solubility studies, FTIR spectroscopy, x-ray diffraction and differential scanning calorimetry, in-vitro dissolution study. X-ray diffraction and differential scanning calorimetry resulting the transformation of crystalline to amorphous naproxen. The optimized batch of solid dispersed naproxen formulated into conventional tablet dosage form by applying factorial design. Evaluation of solid dispersed naproxen conventional tablet was performed. In-vitro release of optimized naproxen conventional tablet shows better release as compare to marketed naproxen tablet (Naprosyn®250)....
The present study describe about selection of diluents to formulate successful tablet of glimepiride. Glimepiride is chosen as drug for which dissolution minima is prescribed in literature. In the present study three diluents are studied either alone or in combination to formulate tablet dosage form. All other ingredients are used commonly in present study and thus eight formulations are prepared. While granulating in some formulations, organic solvent dichloromethane or combination of dichloromethane and isopropylalcohol (1:1) are used, thus alteration in diluents (s) or organic solvents used in method are made. Deliberately name of diluent(s), intragranular disintegrant, binder, extragranular disintegrant, lubricant, glidant and colour are not given in present study. All ingredients are very commonly used in tablet formulation as well as they are economically viable. In two formulations where all ingredients are same as well as they are almost similar in evaluations, one of them only differ in using dichloromethane for dispersion of drug. The method, where dichloromethane was used, was discarded on the basis of economy and ecofriendly alternative. Present study is highly illustrative for selection of diluent (s) and method for manufacture of tablet as dosage form. The successful tablet formulation was compared with two marketed product and found superior. The successful formulated tablets were packed in PVC aluminium blister pack and subjected to stability study at 40°C2°C/75% +5% RH and 25 2C/60% + 5% RH for 2 months. Results showed that product in stable....
The aim of the present investigation was to develop a pulsatile drug delivery system based on an insoluble capsule body filled with glibenclamide microspheres and sealed with hydrogel plug. The microspheres were prepared by solvent evaporation. The plugs of varying thickness and hardness were prepared by direct compression which was then placed in the capsule opening. The drug delivery system was designed to deliver the drug at such a time when it was needed (early hours in morning). Dissolution studies of pulsatile capsule device in media with different pH (1.2, 7.4 and 6.8) showed that drug release in colon could be modulated by optimizing the concentration of polymers in the plug and also the position of plug. The study showed that, lag time prior to drug release was highly affected by the plug position. The dissolution data revealed that the plug position and the composition of plug were very important to achieve an optimum formulation. Drug– polymer interaction studies indicated no interaction or complexation in between the drug and the polymer....
Rizatriptan benzoate is a selective 5-hydroxytriptamine1B/1D receptor agonist that was launched in 1988 for the acute treatment of migraine in adults. Rizatriptan undergoes hepatic first pass metabolism, hence it shows poor bioavailability. The motive of the study is to formulate a buccalmucoadhesive dosage form using biocompatible polymers with rizatriptan to circumvent the first pass metabolism and to increase the bioavailability. This study was designed to develop a buccalmucoadhesive tablet containing rizatriptan benzoate using primary and secondary bioadhesive polymeric combinations such as carbopol 934 with HPMC K-4M, PVP and chitosan in different concentrations using direct compression technique. Tablets were subjected to physico-chemical parameters along with Swelling index, surface pH, bioadhesion strength, in-vitro drug release. Satisfactory results were obtained in all evaluated parameters. The drug release of all formulations follows zero order kinetics. All the prepared tablets are weighing between 144 mg to 154 mg. The thickness of the tablet was in the range of 3.5 to 3.7 mm. Hardness was in the range of 3.0 to 6.0 kg/cm2. Swelling index is in the range of 44% to 81%. Surface pH was in the range of 5.9 to 6.19. Drug content uniformity study showed drug was dispersed equally throughout the formulation and is in the range of 97.46% to 99.02%. FT-IR studies revealed that, there was no incompatibility of drug with the excipients used. Formulations F1 and F8 showed 92% drug release at 8th hr. Release of rizatriptan from all the tablets followed zero order kinetics and showed controlled release. From the current study it was concluded that rizatriptan benzoate buccal mucoadhesive tablets showed better swelling property, good bioadhesive strength, residence time and drug release to improve the bioavailability and greater therapeutic efficacy....
Nateglinide is an anti diabetic drug. Nateglinide fast dissolving tablet have been prepared by direct compression method. Effect of superdisintegrants (such as crosscarmellose sodium, sodium starch glycolate and crospovidone) on wetting time, disintegration time, drug content, in-vitro release and stability parameters has been studied. Disintegration time and dissolution parameters which increase in case of combination of croscarmellose sodium and sodium starch glycolate. Stability studies indicated that tablets containing super disintegrants were sensitive to high humidity conditions. It was concluded that the faster disintegration of crospovidone tablets may attributed to its rapid capillary activity and pronounced hydration with little tendency to gel formation....
In the present investigation preparation of FDT of model drug (telmisartan) by using direct compression. Telmisartan was complexed with β-CD by physical mixture, kneading and microwave method to improve the solubility and dissolution rate before formulating into a dosage form. Drug: ß-CD (molar ratio of 1:1) complexed by microwave method which gives marked increased in solubility and selected for formulation of FDT. The prepared complex (TELMW) was characterized by DSC, FTIR and XRD studies. Fast dissolving tablet of solubility enhanced telmisartan was prepared by direct compression technique because of its ease of access and contain limited number of unit operations. FDT was formulated with various concentration of excipients like superdisintegrants, binder and diluents which were screened to find the best formulation with good friability, disintegration values and % cumulative drug release. Employing a 23 factorial design, the joint influence of two variables like amount of superdisintegrants (CCNa) and binder (maltodextrin) on the disintegration time and % CDR. The formulation batches were evaluated for pre-compressional and post-compressional parameters like weight variation, hardness, friability, thickness, disintegration time and dissolution at gastric pH. The values were of post-compressional parameter were in the prescribed limit and results were within IP acceptable limits. The study reveals that the formulation F3 (5% of CCNa and 6% of maltodextrin) is found to be optimized formulation with 95.98% drug release within 5 min. The kinetic study shows that the fast dissolving formulation follows the first order kinetic for the drug release mechanism....
The investigation was concerned with design and characterization of oral immediate release tablets of Efavirenz, in order to improve efficacy and better patient compliance. Efavirenz is an antiretro viral drug a NNRTI of HIV-1. Efavirenz is a non-competitive inhibitor of HIV-1 reverse transcriptase (RT) and does not significantly inhibit HIV-2 RT or cellular DNA polymerases (α, β, γ or δ). Immediate Release tablet of Efavirenz drug was formulated by direct compression using super disintegrants like croscarmellose sodium, sodium starch glycolate, Crospovidone and microcrystalline cellulose.The drug-excipients interaction was investigated by FTIR. The granules and tablets of Efavirenz were evaluated for various pre and post compression parameters like Angle of repose, Compressibility index, Hausner’s ratio, Tablet hardness, Friability, Weight variation, Drug content and in-vitro dissolution. During the course of study it was found that the formula F7 containing croscarmellose sodium as disintegrant exhibited acceptable disintegration time, percentage drug content per tablet and in vitro drug release. Later they were subjected to stability studies after packing in amber colored PVC-PVDC blister packing which showed acceptable results....
The present study was aimed to develop in-situ gel of carvedilol for improved bioavailability by circumventing the hepatic first pass metabolism and patient compliance. The carvedilol in-situ gelling system was formulated by using carbopol 934 in combination with HPMC K4M by cold technique to reduce the mucociliary clearance and thereby it will increase the contact of formulation with nasal mucosa and hence improving drug absorption. The prepared gels were characterized by viscosity, pH, drug content, gel strength, in-vitro diffusion study, permeation studies, stability study etc. In this formulation the release profile depend on the concentration of carbopol 934 and HPMC K4M. A 32 factorial was applied to see the effect of varying the concentration variables carbopol 934 (X1) and HPMC K4M (X2). In-vitro release data were fitted to various models to ascertain kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. Formulation containing carbopol 934p (0.3%) and HPMC K4M (0.1%) was found to be optimum. The optimized formulation showed a drug release of 98.75% in 480 min. The biopolymers used and their compositions in the in-situ gels preparation greatly affected the drug release which allows absorption in the nasal mucosa....
Tolnaftate is a topically used antifungal agent, having specific and significant fungicidal effect on trichophyton, microsporum and epidermophyton. It has a history of 50 years of usage and still remains one of the most potent drugs for treatment of Tinea Pedis, which affects approximately 10% of the population. Tolnaftate is a BCS class IV drug. It possesses poor water solubility and high hydrophobicity which leads to low permeability. Such drugs pose a challenge in development of topical drug delivery system. Hence, for solubilization of tolnaftate, formulation of emulsion appeared to be a viable approach. Emulsions have gained lot of attention for delivery of hydrophobic agents for local treatment; because of its ability to increase solubility, permeability of drug. In the global market tolnaftate is available in the form of solutions, aerosols, powders and creams (in form of suspension); while no emulgel dosage forms with dissolved tolnaftate are available till date. Thus the present work was done with an objective to formulate tolnaftate (1% w/w) in the form of emulgel, containing emulsion of the drug, with a view to achieve main objective, To design a stable topical dosage form of tolnaftate that will effectively release drug for prolong period time. Tolnaftate emulgel was prepared by dispersing carbopol 934 in purified water with constant stirring at moderate speed, the pH was adjusted to 6-6.5 using tri ethanol amine (TEA). 32 factorial design was applied for the formulation of emulgel. Evaluation of tolnaftate emulgel was carried out for physical appearance, pH, spreadability, Rheological study, drug content, in-vitro release study of all formulation F1-F9. Optimization was done by design expert software trial version 8.0.0.6. % Drug release and viscosity was consider as response for this and according to design expert F3 batch was selected as optimized batch and optimized batch was evaluated for the skin irritation test, antifungal study (zone of inhibition), stability study and fitting result into different kinetic equations was also carried out. From this study it was concluded that optimized batch having good release and no skin irritation on rats skin, drug release follow zero order kinetic and the formulation was stable at room temperature....
Microspheres are well accepted technique to control the drug release from the dosage form to improve bioavailability, reduce absorption difference in patients, reduce the dosing frequency and adverse effects during prolong treatment. The main objective of the present study is to prepare and evaluate glibenclamide microspheres by solvent evaporation method, with water insoluble polymers such as ethyl cellulose, eudragit RS100, cellulose acetate and carboxy methyl cellulose sodium 200-300cps as suspending agent, using as carrier for oral administration in view to achieve oral controlled release of the drug. Glibenclamide is an oral antidiabetic agent which is widely used in the management of non-insulin dependent diabetes mellitus (type II). It is a second generation sulphonyl urea which is more potent than the first generation drugs in this class. Its biological half-life is 4-6 hrs. Due to its low biological half-life (5 hrs), it requires frequent administration to maintain plasma concentration. This causes inconvenience to the patient and also leads fluctuations in plasma drug concentration that may cause inferior therapeutic effects or toxic effects. There-fore, development of controlled release dosage forms would clearly be beneficial in terms of decreased dosage requirements, thus increase patient compliance. Compatibility studies revealed there was no interaction between the drug and polymers. The formulations were evaluated for particle size distribution analysis, flow properties like angle of repose, bulk density, tapped density, hausner’s ratio, carr’s index, encapsulation efficiency, scanning electron microscopy and in-vitro release studies. The optimized formulation showed good in-vitro controlled release activity of the drug glibenclamide....
The objective of present study is to formulate and optimize the self emulsifying drug formulations systems of nevirapine by use of 22 factorial designs to enhance the oral absorption of nevirapine by improving its stability, solubility, dissolution rate and diffusion profile. SEFS are the isotropic mixtures of oil, surfactant, co-surfactant and drug that form oil in water micro emulsion when introduced into aqueous phase under gentle agitation. Solubility of nevirapine in different oils, surfactants and co-surfactants was determined for the screening of excipients. Pseudo-ternary phase diagrams were constructed by the aqueous titration method and formulations were developed based on the optimum excipient combinations with the help of data obtained through the maximum micro emulsion region containing combinations of oil, surfactant and co-surfactant. The formulations of SEFS were optimized by 22 factorial designs. The optimum formulation of SEFS contains 32.5% oleic acid, 44.16% tween 20 and 11.9% PEG 600 as oil, surfactant and co-surfactant respectively. The SEFS were evaluated for the following drug content, self-emulsification time, rheological properties, zeta potential, in-vitro diffusion studies, thermodynamic stability studies and in-vitro dissolution studies. An increase in dissolution was achieved by SEFS compared to pure form of nevirapine. Overall, this study suggests that dissolution and oral bioavailability of nevirapine could be improved by SEFS technology....
The aim of present research work was at formulation, evaluation and taste masking ofmouth dissolving filmof Phenylephrine Hydrochloride to provide rapid onset of action with improved patientcompliance. Phenylephrine Hydrochloride is a NasalDecongestants and Vasoconstrictor drug. Solventcasting method was adopted for preparation of mouth dissolving film using HPMCE5 LV aspolymer, PEG 400 as a plasticizer, Aspartame as sweetener, Menthol as Flavour, Ethanol (95%) as a solvent and distilled water as a vehicle. Bitter taste of drug was evaluated by electronic tongue. A 32 full factorial design wasapplied systematically to optimize mouth dissolving film. The concentration of HPMCE5 LV (X1)andconcentration of PEG 400 (X2) were selected as independent variables. The effects of these factors were observed on dependent variables % drug release (Y1) and tensile strength (Y2). Theprepared films were evaluated for weight variation, Thickness, Folding endurance,Tensile Strength, Disintegration time, and% Drug release. FT-IR and DSC studies proved no chemical interaction betweendrug and Excipients. The prepared Phenylephrine Hydrochloridemouth dissolving films werefound to be of good quality fulfilling all the requirements for films. The resultsrevealed that concentration of polymer HPMCE5 LV and concentration of plasticizer PEG 400significantly affected % drug release and tensile strength. Dependentvariableswere increased with increase in the amount of HPMCE5 LV(X1) andconcentration of PEG 400 (X2). Regression analysis and numerical optimization wereperformed to identify the best formulation. The optimized formulation F10 preparedwith HPMCE5 LV 484.59 mg and PEG-400 18.62% (% of polymer) was found to be the bestformulation with 94.98% drug release and 1.66 N/cm2tensile strength. Acceleratedstability studies on the promising formulations indicatedthat there were no significant changes in evaluation parameters. Thus, the mouth dissolving film of Phenylephrine Hydrochloride was successfully formulated by solvent casting technique with immediate onset ofaction & improved patient compliance....
Fast dissolving tablets are useful in patients such as paediatric, geriatric, bedridden or developmentally disabled who face difficulty in swallowing conventional tablets or capsules leading to ineffective therapy. Ketorolac tromethamine is a non-selective COX Inhibitor used as an analgesic in moderately severe acute pain. Ketorolac tromethamine tends to cause severe gastric irritation within short course of therapy. Hence the present study is aimed at developing and evaluating fast dissolving tablets of ketorolac tromethamine using superdisintegrants like agar, sodium starch glycolate and crosspovidone to reduce gastric irritation and enhance the patients’ compliance during administration. Ketorolac tromethamine fast dissolving tablets were prepared by direct compression method. Tablets were evaluated for their physicochemical properties and in-vitro release studies. The hardness (5-7 kg/cm2), friability (0.1-0.4%), drug content (81-100%) and disintegration time (29 - 62 seconds) of fast dissolving tablets were found to be uniform and reproducible. Dissolution of tablets was not directly proportional to the concentration of superdisintegrants but showed varying response according to the nature of superdisintegrants used. The formulations prepared with 10% SSG were found to be better in terms of disintegration and in-vitro drug release profile compared to other formulations....
About 40% of active pharmaceutical ingredients (API) in development pipelines are poorly water soluble drugs which limit clinical application, formulation approaches and marketability. Solid dispersion is a promising approach to improve solubility and dissolution properties of water insoluble drugs. In this technique, one or more API is dispersed in an inert carrier or matrix at the solid state prepared by solvent, melting or solvent-melting method. In solid dispersions solubility is increased by reducing particle size possibly to molecular level, enhancing wettability and porosity, as well as changing drug crystalline state preferably into amorphous state. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. This review shade light on need of solubility enhancement, basic concept, advantages, classification, mechanism drug release and characterization techniques of solid dispersion....
The objective of present study was to formulate deflocculated and flocculated suspensions of metronidazole benzoate and evaluate various parameters of suspensions. Six deflocculated suspension formulations D1 to D6 were prepared having common humectants, preservatives 1 and 2, sweetener, pH adjusting agent and purified water. Among all six, one different in wetting agent, two differed in flocculating agents, one differed in complexing agent. There were two flocculating agents; one differed in concentration of 0.02% w/v to 0.1% w/v for two separate formulations. Seven flocculated suspension formulations (F1 to F7) were prepared in which wetting agent and flocculating agent were common to all but flocculating agent different in three concentration 0.02% w/v, 0.05 5 w/v and 0.1 w/v for three separate formulations. Viscosity enhancers and one complexing agent were used and they different not in all formulations but in some of formulations. Humectants, preservatives 1 and 2 sweetener, pH adjusting agent and purified water were common to all seven formulations. 100 g of metronidazole benzoate was suspended in 250 ml of volume in all 13 formulations. After evaluation of particle size distribution, sedimentation volume, degree of flocculation, resuspendability, drainage/ adherence test, photo-microscope study and assay, it was found that formulation with 0.05% flocculating agent is successful....
Loading....