Satisfactory Drug Release Research Articles

Tailored alginate sponges loaded with κ-carrageenan beads for controlled release of curcumin

This study presents an innovative approach to develop and characterize an alginate sponge containing κ-carrageenan (κ-CRG) beads loaded with curcumin. The beads were fabricated using varying concentrations of κ-CRG, and their properties were extensively evaluated using inverted phase-contrast microscopy, Scanning Electron Microscopy (SEM), FTIR, swelling behavior, mass distribution, encapsulation efficiency, in vitro drug release and kinetics of drug release. Beads formulated with specific concentrations of κ-CRG that exhibited optimal performance were then integrated into an alginate sponge matrix, which underwent similar comprehensive testing procedures as the individual beads. The characterized beads displayed a spherical morphology, a notable swelling degree of approximately 146 %, excellent mass uniformity, encapsulation efficiencies higher than 90 % and drug release rate exceeding 70 %. Moreover, the alginate sponge formulation demonstrated a satisfactory drug release profile of 67.9 ± 0.6 %. In terms of drug release kinetics, the Higuchi model was the most effective in explaining the release of curcumin from beads and sponge. These findings underscore the potential of both the beads and the sponge as effective vehicles for the controlled delivery of curcumin, positioning them as promising candidates for pharmaceutical applications across various fields.

Development and characterization of transdermal drug delivery system of ramosetron HCL using different polymers and their effect on In-vitro release

Transdermal Drug Delivery Systems (TDDS) offer a controlled and consistent release of medications, bypassing first-pass metabolism and minimizing side effects associated with traditional oral and intravenous therapies. This study focuses on the development and evaluation of Ramosetron HCl transdermal patches designed for sustained release to manage nausea and vomiting. Ramosetron HCl, a selective 5-HT₃ serotonin receptor antagonist, was incorporated into various formulations using different grades of Hydroxypropyl Methylcellulose (HPMC), Polyvinyl Pyrrolidone (PVP K30), and Polysorbate 80. The patches were prepared by solvent casting and evaluated for various parameters including thickness, weight variation, drug content, folding endurance, tensile strength, and in-vitro drug release. The calibration curve for Ramosetron HCl in 7.4 pH phosphate buffer was established with a λmax of 240 nm. Fourier Transform Infrared Spectroscopy (FTIR) was employed to ensure compatibility between the drug and excipients. Formulation F5 demonstrated optimal properties, including satisfactory drug release profiles and mechanical strength. Stability studies of F5 showed that the formulation maintained its release characteristics under accelerated storage conditions (40°C / 75% RH) for up to three months. This study confirms the potential of Ramosetron HCl transdermal patches as an effective alternative to oral dosage forms, providing sustained drug delivery and enhanced patient compliance.

Formulation, Optimization, and Evaluation of Ezetimibe for Chronotherapeutic Drug Delivery using Compression-Coating Technology

Objectives: The purpose of the present study was to Formulation, optimization and evaluation of drug for chronotherapeutic drug delivery using compression coating technology for hypercholesterolemia. Material and Methods: The drug delivery system was designed to deliver the drug at a time when it could be needed for the most in the early morning (4 to 6 a.m.) for patients in case of hypercholesterolemia. The pulsatile concept was applied to the dosage form by having a lag phase followed by an immediate release. The prepared system consisted of two parts: a core tablet containing the active ingredient and fracture outer shell with delay-release polymer having diffusion characteristics. Solid dispersion was carried out by screening of betacyclodextrin, Polyvinyl pyrrolidone (PVP K30), and HPMC using three different drug complex ratios 1:1, 1:2, and 1:3 by a solvent evaporation method through spray dryer. The immediate-release core tablet (IRCT) was prepared by using a superdisintegrant with active ingredients. Screening of IRCT was carried out by pre and post compression parameters, disintegration time and an in-vitro dissolution study. The pulsatile release tablet (PRT) of optimized IRCT was made by Glyceryl Behenate and Dibasic Calcium Phosphate. Optimization of polymer concentration of PRT was carried out by pre and post-compression parameters, pulsatile lag time, and an in-vitro dissolution study. A 32 factorial design was employed to optimize the PRT. The design consisted of two dependent variables R1, and R2 independent variables X1 and X2. The two independent formulation variables selected for the study including Concentration of coating polymer and Concentration of lubricant. The dependent variables are Lag Time and Thickness. Results: XRD, DSC and FTIR spectra showed that solid dispersion was formed by the drug and PVP K30 complex. IRCT batch RR1 containing 22mg croscarmellose sodium to achieve good 30sec disintegration time and 98.34% drug release at the end of 20 minutes of Ezetimibe respectively. PRT formulation DR6 showed good pre and post-compression parameters with a satisfactory drug release of 98.34% for Ezetimibe respectively with a lag time of 6 hours. The 32 factorial design was used for the optimization of PRT parameters. A total of 9 experiments were performed for two factors at three levels each. The optimized batch showed 98.27% DR for Ezetimibe in 6.2 hrs (within 20 min after lag time) with pulsatile lag time up to 6.0 hrs and thickness of 5.10 kp. Conclusion: It was concluded that tablet within the tablet, pulsatile drug delivery of Ezetimibe (BCS class-II drugs) was successfully formulated with the advantage of enhanced solubility, and pulsatile release behavior and had an added benefit of suitable for chronopharmacotherapy of diseases that show circadian rhythms in their pathophysiology.

Effects of water-soluble additive on the release profile and pharmacodynamics of triptorelin loaded in PLGA microspheres

A satisfactory drug release profile for gonadotropin-releasing hormone (GnRH) agonist drugs is high initial release followed by small amount of drug release per day. In the present study, three water-soluble additives (NaCl, CaCl2 and glucose) were selected to improve the drug release profile of a model GnRH agonist drug-triptorelin from PLGA microspheres. The pore manufacturing efficiency of the three additives was similar. The effects of three additives on drug release were evaluated. Under the optimal initial porosity, the initial release amount of microspheres containing different additives was comparable, this ensured a good inhibitory effect on testosterone secretion in the early stage. For NaCl or CaCl2 containing microspheres, the drug remaining in the microsphere depleted rapidly after the initial release. The testosterone concentration gradually returned to an uncontrolled level. However, for glucose containing microspheres, it was found that the addition of glucose could not only increase the initial release of the drug but also assist in the subsequent controlled drug release. A good and long-time inhibitory effect on testosterone secretion was observed in this formulation. The underlying cause why the incorporation of glucose delayed the subsequent drug release was investigated. SEM results showed that considerable pores in glucose containing microspheres were healed during the microspheres incubation. After thermal analysis, an obvious glass transition temperature (Tg) depression was observed in this formulation. As Tg decreased, polymer chains are able to rearrange at lower temperatures. This, morphologic change was reflected in the gradual closure of the pores, and is the likely reason that drug release slowed down after the initial release. HIGHLIGHTS The addition of glucose could not only increase the burst release of the drug but also delay the subsequent drug release. High initial burst and a sustained drug release helped obtain a good inhibitory effect on testosterone secretion. As Tg decreased, polymer chain was prone to rearrange. Morphologic change was reflected in the gradual closure of the pores. This was the reason that drug release slowed down after the initial burst.

Development of Resistant Starch-Pectin Microsphere for Improving Oral Colon-specific Drug Delivery of 5-Fluorouracil

Conventional chemotherapy is ineffective for colorectal cancer as the drug moiety does not reach its intended site. 5-Fluorouracil (5-FU) microspheres aimed at colon-specific drug delivery have been developed by using the solvent evaporation technique in this study. The influence of utilizing different percentages of resistant starch-pectin polymer on the drug loading, encapsulation efficiency, and release behavior of the drug was investigated. The characterization of prepared microspheres was done by shape, surface morphology, drug loading, encapsulation efficiency and in vitro drug release studies. Drug-polymer interactions and drug stability were investigated by Differential Scanning Calorimetry (DSC) and FTIR spectroscopy. The 5-Fluorouracil polymeric microspheres that were formulated utilizing a resistant starch (RS) and pectin polymer displayed ideal physicochemical properties and spherical particles. The targeted microspheres demonstrated a high drug loading, encapsulation efficiency, and a satisfactory drug release pattern over the time period of 8 hours. Studies on drug release conducted under conditions that simulate stomach to colon transit have demonstrated that the drug was prevented from being released in the physiological conditions of the stomach and small intestine. Creating a new multiparticulate system using RS-pectin microspheres in order to forecast the protection that the combination might provide to the dosage form that will ensure localized drug release in the colon. Finally, it was found that the 5-Fluorouracil polymeric microsphere is a suitable microcarrier for effective colon-specific drug delivery tools with increased chemotherapeutic efficacy. Bangladesh Pharmaceutical Journal 26(1): 36-44, 2023 (January)

Formulation and Evaluation of Metformin Hydrochloride Sustained Release Tablet

Metformin hydrochloride (MET) is an oral hypoglycemic agent which improves glucose tolerance in patients with type 2 diabetes and diminishes basal plasma levels of glucose. The aim of this study was to develop and optimize MET matrix tablets for SR application. The SR matrix tablet of MET was prepared by wet granulation technique using Polyvinyl pyrrolidone K30 and hydroxyl propyl methylcellulose of different viscosity grades (HPMC K4M, HPMC K15M, and HPMC K100M). The influence of varying the polymer ratios was evaluated. The excipients used in this study did not modify physicochemical properties of the drug. MET has relatively short plasma half-life, low absolute bioavailability. The need for the administration 2 to 3 times a day when larger doses are required can decrease patient fulfillment. SR formulation that would maintain plasma level for 8-12 h might be sufficient for daily dosing of MET. SR products are needed for MET to prolong its duration of action and to improve patient compliances. 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 F3 shows the best results. It has been observed that HPMC K100M alone cannot give satisfactory drug release profile but the blend of HPMC K100M and Polyvinyl pyrrolidone K30 together give the best drug release 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. Keywords: Metformin hydrochloride, SR matrix tablet, HPMC K100M, Wet granulation technique

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

Efficient Prediction of InVitro Piroxicam Release and Diffusion From Topical Films Based on Biopolymers Using Deep Learning Models and Generative Adversarial Networks.

The purpose of this study was to simultaneously predict the drug release and skin permeation of Piroxicam (PX) topical films based on Chitosan (CTS), Xanthan gum (XG) and its Carboxymethyl derivatives (CMXs) as matrix systems. These films were prepared by the solvent casting method, using Tween 80 (T80) as a permeation enhancer. All of the prepared films were assessed for their physicochemical parameters, their invitro drug release and exvivo skin permeation studies. Moreover, deep learning models and machine learning models were applied to predict the drug release and permeation rates. The results indicated that all of the films exhibited good consistency and physicochemical properties. Furthermore, it was noticed that when T80 was used in the optimal formulation (F8) based on CTS-CMX3, a satisfactory drug release pattern was found where 99.97% of PX was released and an amount of 1.18mg/cm2 was permeated after 48h. Moreover, Generative Adversarial Network (GAN) efficiently enhanced the performance of deep learning models and DNN was chosen as the best predictive approach with MSE values equal to 0.00098 and 0.00182 for the drug release and permeation kinetics, respectively. DNN precisely predicted PX dissolution profiles with f2 values equal to 99.99 for all the formulations.

Simulation of adsorption and release of doxepin onto ZIF-8 including in vitro cellular toxicity and viability

Doxepin hydrochloride is an antidepressant drug commonly used to treat mild to moderate depression. However, this drug has poor oral bioavailability, with the percentage of drug that can enter the bloodstream being weak and variable. The present study seeks to investigate the ZIF-8 nanoparticles for doxepin delivery and to assess this drug uptake and release in ZIF-8 frameworks using the Gibbs-ensemble Monte Carlo method in the Simulated Materials Studio. This study also adopted a model for showing surface adsorbent (ZIF-8S) capabilities. ZIF-8 nano-frameworks have many advantages such as easy flowing through capillaries leading to a satisfactory drug release into the systemic circulation and preventing high plasma concentration. Additionally, the study examined the diffusion of drug molecules using the simulated molecular dynamics with regard to the structural flexibility of the MOF. Proper loading of 8.6% and slow diffusion of 7.353 × 10−6 cm2/s doxepin molecules from ZIF-8 pores confirmed that this material could be recommended as an effective carrier for doxepin. Furthermore, the fixed ZIF-8S model is also used by keeping the opening of cavities fixed, thereby attaining a higher loading amount 12%. Moreover, since ethanol has been applied as a suitable solvent in many biological systems, of adsorption, diffusion processes are also repeated in this solvent. Thus, presence of such adsorption sites as zinc ions may facilitate the interaction of the framework with large molecules to provide desirable loading and diffusion amounts. Furthermore, more adsorption can be reached with less energy at the surface of the ZIF-8 in the presence of ethanol, which is due to the greater adsorption of solvent molecules. Finally, to ascertain the in vitro cellular toxicity and viability of the prepared nanoparticles, they are treated with PC3 human prostate cancer cells and the average growth curves are monitored via MTT assay. This study confirmed a decrease in the MTT signal compared to the untreated cells, so ZIF-8 can reduce the metabolic activity of the performed cancer cells. This study shows that this nanomaterial can be achieved as a vehicle for delivery of doxepin.

DESIGN, DEVELOPMENT & CHARACTERIZATION OF FAST DISSOLVING TABLET OF CARVEDILOL

Fast dissolving tablets are developed as an alternative to tablet, capsule and syrup for the paediatric and geriatric patient suffering from disease who feels difficulty in swallowing the oral solid dosage form. Carvedilol is practically insoluble in water, slightly soluble in an alcohol, practically insoluble in dilute acids. Carvedilol is a non-cardioselective beta blocker. It has vasodilating properties, which are attributed mainly to its blocking activity at alpha1 receptors; at higher doses calcium-channel blocking activity may contribute. Carvedilol competitively blocks receptors. The elimination half-life is about 6 to 10 hours. The main objective of this research work was to formulate and evaluate fast dissolving tablet of carvedilol using excipients like Croscarmellose sodium, Crospovidone, Microcrystalline Cellulose, magnesium stearate, PVP etc. Formulation of fast dissolving tablets of Carvedilol by direct compression method using different types of polymer in different percentages. The tablets with drug were also evaluated for uniformity of drug content, in-vitro drug release and stability studies. The drug content in the fast dissolving tablets was found to be uniform and with low correlation of variation. The tablets prepared with solid dispersion in combination with super disintegrate showed better release profile as compared to only incorporation of super disintegrates. The tablets prepared by effervescent and pore forming technology provides satisfactory drug release. The release of drug followed first order kinetics and mechanism of drug release was found to be diffusion controlled.
 The stability data at different temperature and humidity showed no significant degradation of Carvedilol and shelf life found to be more than 520 days. Fast dissolving tablets prepared by the Ac – Di – Sol in 4% concentration are promising for rapid release of Carvedilol. Incorporation of solid dispersion (PEG 4000 : CARVEDILOL) (4:1) into Ac – Di – Sol in 2 % concentration enhanced the release rate of Carvedilol and thus therapeutic levels of the drug could be achieved through fast dissolving tablets. Tablets prepared by effervescent and pore forming technologies are also very promising for stable and rapid release of Carvedilol.
 Keywords: Carvedilol, FDDS, solid dispersion, tablets, Sodium, Crospovidone, Microcrystalline Cellulose, magnesium stearate, PVP.

Hollow MnO2/GNPs serving as a multiresponsive nanocarrier for controlled drug release

In this work, hollow manganese dioxide/gold nanoparticle (MnO 2 /GNPs) hybrid drug nanocarriers were prepared by coupling the gold nanoparticles (GNPs) with hollow structure manganese dioxide (MnO 2 ). Among them, GNPs have been used as near-infrared (NIR)-responsive element for photothermal effect under NIR laser irradiation. The glutathione (GSH)-responsive and pH-responsive performances of drug release were derived from hollow MnO 2 . Particularly, Doxorubicin hydrochloride (DOX) can be loaded into hollow MnO 2 /GNPs with the drug loading efficiency up to 82.0%. Moreover, the photothermal effect and GSH-/pH-responsive properties of hollow MnO 2 /GNPs were investigated. The hollow MnO 2 /GNPs possessed satisfactory drug release efficiency ( ca. 87.4% of loaded drug released in 12 h) and have high photothermal conversion efficiency, multiresponsive properties, and degradability. Finally, the kinetics of drug release was discussed in detail. Thus, our finding highlights that the multiresponsive nanocarriers are of great potential in the field of drug controlled release.

DESIGN AND IN VITRO EVALUATION OF EXTENDED RELEASE TABLET OF NATEGLINIDE

The aim of present study is to formulate and evaluate extended release matrix tablet of Nateglinide by direct compression method using different polymer like HPMC K4 and HPMC K15. Matrix tablet of nateglidine were prepared in combination with the polymer HPMC K4, HPMC K15, along with the excipients and the formulations were evaluated for tablet properties and in vitro drug release studies. Nateglinide matrix tablet prepared by using polymer such as HPMC K4 and HPMC K15, it was found that HPMC K15 having higher viscosity as compare to HPMC K4 therefore different concentration of polymer were studied to extend the drug release up to 12 h. The tablets of Nateglinide prepared by direct compression had acceptable physical characteristics and satisfactory drug release. The study demonstrated that as far as the formulations were concerned, the selected polymers proved to have an acceptable flexibility in terms of in-vitro release profile. In present the study the percent drug release for optimize batch was found to 94.62%. Hence it can be conclude that Nateglinide extended release matrix tablet can prepared by using HPMC. The swollen tablet also maintains its physical integrity during the drug release study
 Keywords: Tablet, in-vitro drug release, Nateglinide, HPMC

FORMULATION, IN VITRO AND EX VIVO CHARACTERIZATION OF MUCOADHESIVE BUCCAL TABLETS FOR ANTIHYPERTENSIVE DRUG

Objective: Olmesartan belongs to a class of angiotensin II receptor blockers. It is used in the treatment of hypertension. However, it undergoes extensive hepatic first-pass metabolism, resulting in low oral bioavailability is about 26%. The aim of this study was to prepare and evaluate the mucoadhesive buccal tablets of olmesartan with a goal to increase the bioavailability and improve the patient compliance.Methods: Mucoadhesive buccal tablets were prepared by a direct compression technique using mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC K4M), sodium carboxymethylcellulose (SCMC), and Carbopol 934P. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, ex vivo mucoadhesive strength, ex vivo mucoadhesive time, and ex vivo permeation studies. The release kinetics was calculated to determine the drug release mechanism. Results: The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets F2, F7, and F11 showed satisfactory drug release rates with the diffusion controlled mechanism. Optimized buccal tablets developed for olmesartan possess reasonable mucoadhesive strength, mucoadhesive time, and surface pH was in an acceptable salivary pH 6.76±0.28–6.89±0.34. The ex vivo permeation studies for optimized tablets were shown satisfactory drug permeation and could meet the target flux 0.991 mg h−1cm−2.Conclusion: The obtained results could be used as a platform to develop the buccal delivery of this drug, which bypasses the first-pass metabolism and results in the improvement of bioavailability. Hence, the present study concludes that the olmesartan could be delivered through the buccal route.

Design of antihistaminic transdermal films based on alginate–chitosan polyelectrolyte complexes: characterization and permeation studies

The purpose of this study was to develop suitable matrix-type transdermal drug delivery systems of Ketotifen fumarate (KF) as antiasthmatic drugs. Chitosan–alginate polyelectrolyte complex (PEC) films were used as drug release regulators for KF. Antihistaminic films with variable PEC compositions were prepared using different ratios of chitosan (CTS) to sodium alginate (ALG). Propylene glycol (PG) was used as plasticizer; Tween 80 (T80) and Span 20 (S20) were used as permeability enhancers. Nine formulations were obtained by film casting method and characterized in terms of weight uniformity, thickness, folding endurance, moisture lost, and moisture absorption. In addition, drug release and permeation through rat abdominal skin mounted in Franz cell were investigated. All formulations were found to be suitable in terms of physicochemical characteristics, and there was no significant interaction between the used drug and polymers. It was noticed that when T20 is used as permeation enhancer, a satisfactory drug release pattern was found where 99.88% of drug was released and an amount of 2.121 mg/cm2 of KF was permeated after 24 h. For the optimal formulation, a permeability coefficient of 14.00 ± 0.001 cm h−1 and a latency time of 0.35 ± 0.02 h were found. The in-vitro analysis showed controlled release profile which was fitted by Korsmeyer–Peppas model (R2 = 0.998). The obtained results suggested that new controlled release transdermal formulations of asthmatic drugs could be suitably designed as an alternative to the common forms.

Formulation and Evaluation of Sustained Release Floating Tablets of an Antihypertensive Diltiazem

The aim of the present study was to develop and evaluate sustained release floating tablets of Diltiazem hydro-chloride, an antihypertensive agent. The sustained release floating tablets were prepared by direct compression method and formulated using different polymer combinations, formulations such as F1 to F9. Natural polymer Sodium alginate and synthetic polymer HPMC K4M were used. Developed formulations were evaluated for the pre compression parameters i.e., drug- excipients compatibility by FTIR, bulk density, compressibility, and angle of repose etc. Post compression parameters i.e. weight variation; full factorial design was applied to optimize the developed formulation. SA and HPMC K4M were selected as independent variable at three different concentrations. The in-vitro drug release study revealed that formulation F8 combination of both synthetic (HPMC) and natural polymers (sodium alginate) was the most successful formulation of the study, all tablets but one exhibited gradual and near complete sustained release for diltiazem HCl (90-100%) that extended the drug release up to 8 hours, with satisfactory drug release in the initial hours, and the total release pattern was close to the theoretical release profile. Model equations of zero and first order, Higuchi, Hixson-Crowell and Peppas, intended to elucidate the drug release mechanism, and were fitted to the release data. Mathematical modelling of in-vitro dissolution data indicated the best-fit release kinetics was achieved with Higuchi model with r2 vales of 0.994 in its semi log plot. The ‘n’ value in Higuchi model was >0.89 which indicated, Super Case-II transport of drug from polymer sustained, i.e., diffusion with relaxation of polymeric chain. In conclusion, the results indicated that the prepared sustained-release tablets of Diltiazem hydrochloride could perform therapeutically better than conventional tablets with improved efficacy and better patient compliance. 

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 and In-vitro Evaluation of Sublingual Tablets of Ondansetron Hydrochloride using Coprocessed Excipients

Abstract: The formulation of sublingual tablets of Ondansetron HCl was carried out by using direct compression technique and evaluation tests were carried out as per pharmacopoeial specifications. Poor compressibility problem of Mannitol was overcome by coprocessing it with maltose and corn starch in varying ratios. The results of evaluation tests indicate that the ratio of Mannitol: Maltose: Corn starch: 19:2:1 gave better tableting performance with respect to precompression & postcompression parameters. It was also observed that increase in maltose content, increased the hardness but negatively affects disintegration and drug release and vice versa. Furthermore the study on effect of superdisintgrants shows that Crospovidone gives faster disintegration and satisfactory drug release in concentration of 4% compared to that of Sodium starch glycolate & Croscarmelose sodium. Formulation using a bioadhesive polymer PVP K 30 in ratio of 0.5% showed uniform release of drug over a period of 20 minutes with complete solubilization of tablet compared to that of gelatin and carbopol 934. On numerical optimization of prepared formulations, three formulations were suggested by Design Expert 8.0.7.1(Trial Version), among that Formulation B gave better correlation between predicted value and observed value. Thus Formulation B was chosen as global best formulation. Key words: Sublingual Tablet, Direct Compression, Co-processing of excipients, Historical Data Optimization, Ondansetron HCl.

Development of Controlled Release Osmotic Pump Tablet of Glipizide Solid Dispersion

To develop controlled release osmotic pump tablets (COPT) of glipizide (GZ) solid dispersion (SD). In elementary osmotic pump (EOP) tablets, an osmotic core with the drug is surrounded by a semi-permeable membrane which is drilled with a delivery orifice. COPT tablets eliminate the need of drilling process as controlled release can be achieved by the presence of osmogen in the coating. Poorly water soluble drug molecule cannot give satisfactory drug release hence GZ solid dispersion was prepared in the present study. The SDs having different ratio of drug to Poloxamer (PXM) 188 were prepared by hot melt method and optimized by solubility study, drug content estimation and in vitro dissolution study. Effect of two independent variables, amount of osmogen (potassium chloride) and hydrophilic polymer (polyethylene oxide WSR 303), were investigated using 3(2) factorial design. Core and coated tablets were evaluated for pharmacotechnical parameters. In-vitro drug release profiles of COPT tablets were compared with marketed with push-pull osmotic pump tablet, Glucotrol XL. Prepared core and coated tablets showed acceptable pharmacotechnical parameters. Drug release was directly proportional to initial level of hydrophilic polymer, but inversely related to the osmogen, confirming osmotic mechanism. Zero order drug release pattern was achieved which was comparable to marketed product. Novel oral controlled release of glipizide was successfully achieved by incorporating glipizide solid dispersion into osmotic system.

Design and In Vitro Evaluation of Pentoxifylline- Polyelectrolyte Complex Tablets

Abstract: The purpose of present study was to develop once a day sustain release enteric coated tablet of Fluoxetine HCl by direct compression method. Design was prepared for nine batch using fenugreek mucilage at 40%, 50% and 60% concentration ; HPMC at 10%, 15% and 20%; compritol ATO 888 at 10%, 15% and 20% and ethyl cellulose at 2%, 3% and 4% concentration. Fenugreek mucilage was extracted from dried ripe seeds of Trigonella foenum-graecum (Fabaceae). Cellulose acetate phthalate was used as enteric coating agent. The tablets were characterized for weight variation, crushing strength, friability, drug content and in vitro drug release study. All the formulations were complied with standard specifications. The Drug excipients compatibility study was performed by DSC and IR Spectroscopy and no incompatibility was found. The results of in vitro dissolution studies indicated that formulations X2, X5 and X8 released 7.03%, 7.03%, 4.75% of Fluoxetine respectively at the end of 2 hour and 98.17%, 78.12%, 65.45% of Fluoxetine respectively at the end of 24 hour. Drug release rate was increased in polymer order HPMC K 100M > ethyl cellulose > compritol ATO 888. Formulation X2 (50% fenugreek mucilage and 15% HPMC K 100M) could extend drug release up to 24 hour and it exhibited satisfactory drug release within first 2 hours and total release pattern was very close to marketed product. The mechanism of drug release was found to be diffusion coupled with erosion. Optimized formulation was found to be stable when exposed to 400C/75 % of relative humidity. Keywords: Delayed release, Fluoxetine HCl, HPMC K 100M, Fenugreek mucilage.

Pioglitazone Solid Dispersion System Prepared by Spray Drying Method: In Vitro and In Vivo Evaluation

Pioglitazone is a thiazolidinedion antidiabetic agent which decreases insulin resistance in the periphery and in the liver, resulting in increased insulin-dependent glucose disposal and decreased hepatic glucose output. Pioglitazone is insoluble in water and has a low dissolution rate. The objective of the current work was to improve aqueous solubility of pioglitazone by the solid dispersion approach using the spray drying technique. In this study, various hydrophilic polymers such as PVP K17, PVP K30, and HPMC E3 were used to prepare pioglitazone solid dispersion by the spray drying method. Characterization of solid dispersion included solubility, particle size, surface area analysis, differential scanning calorimetry, infrared spectroscopy, x-ray diffraction, and dissolution test. In vivo hypoglycaemic activity was studied in Swiss albino mice. RESULTS showed that there was significant improvement in solubility and dissolution rate in solid dispersion containing PVP K17 than in that of the pure drug. This in turn resulted in improved pharmacodynamic activity, giving 2 fold mean percentage glucose inhibition as compared to the pure drug; thus the solid dispersion strategy proved to be potentially beneficial for improving the in vivo hypoglycaemic activity of pioglitazone. Increase in pioglitazone solubility and in vitro dissolution in solid dispersion was followed by improved in vivo hypoglycaemic activity. The aim of the present study was to prepare and evaluate solid dispersion of pioglitazone by the spray drying method. Various hydrophilic polymers were used for preparation of solid dispersion. Pioglitazone is an oral antidiabetic agent effective for reactive hypoglycaemia and aggravated glycaemic metabolism associated with insulin resistance. The prepared solid dispersion was evaluated for saturation solubility, drug content, differential scanning calorimetry, x-ray diffraction, infrared spectroscopy, and stability as per International Conference on Harmonisation guidelines. The glucose-lowering response of the optimized formulation was also studied in Alloxan-induced diabetic Swiss Albino mice. The formulation containing hydrophilic polymers showed a satisfactory drug release pattern compared to the pure drug. Further, when in vivo hypoglycaemic response of pure drug, prepared solid dispersion, and marketed formulation was compared, the optimized solid dispersion batch revealed significant improvement in hypoglycaemic activity. Hence, the present study reveals that the formulation of solid dispersion of pioglitazone with hydrophilic polymer exhibits good release properties as well as in vivo antihyperglycemic activity.