HPMC E5 Research Articles

Formulating extended-release Meloxicam Pellets using the membrane coating technique

Background: Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) with potent anti-inflammatory and analgesic effects but is associated with various side effects such as inducing gastrointestinal ulcers. Extended-release meloxicam pellets offer several advantages, including reducing the frequency of daily medication intake and providing sustained drug release over time, thereby minimizing gastrointestinal side effects. The study was conducted to formulate and develop the manufacturing process for meloxicam pellets, while simultaneously evaluating the physicochemical properties of the formulated pellets. Materials and methods: Meloxicam, HPMC E5, and Ethyl Cellulose N7 were used in the study. Meloxicam pellets were formulated using the layering technique, initially depositing the drug onto inert pellets and subsequently extending the coating with Ethyl Cellulose N7. Results: The pellet formula utilizes EC N7 with the role of providing extended-release kinetics following zero-order kinetics. The pellets exhibit uniform and attractive appearance, with dimensions ranging from 0.7 - 1 mm. The drug content is 2.38% ± 0.11% (w/w), demonstrating the ability to release the drug according to a zero-order kinetic model. Conclusions: The study successfully formulated extended-release meloxicam pellets using a coating technique that involved a gradual deposition phase of the drug onto inert pellets, followed by an extended coating phase using a controlled-release excipient. Key words: Meloxicam, pellet, coating technology.

In Vitro and Biological Evaluation of Oral Fast-Disintegrating Films Containing Ranitidine HCl and Syloid® 244FP-Based Ternary Solid Dispersion of Flurbiprofen.

Flurbiprofen (FBP), a nonsteroidal anti-inflammatory drug (NSAID), is commonly used to treat the pain of rheumatoid arthritis, but in prolonged use it causes gastric irritation and ulcer. To avoid these adverse events of NSAIDs, the simultaneous administration of H2 receptor antagonists such as ranitidine hydrochloride (RHCl) is obligatory. Here, we developed composite oral fast-disintegrating films (ODFs) containing FBP along with RHCl to provide a gastroprotective effect as well as to enhance the solubility and bioavailability of FBP. The ternary solid dispersion (TSD) of FBP was fabricated with Syloid® 244FP and poloxamer® 188 using the solvent evaporation technique. The synthesized FBP-TSD (coded as TSD) was loaded alone (S1) and in combination with plain RHCl (S2) in the composite ODFs based on hydroxypropyl methyl cellulose E5 (HPMC E5). The synthesized composite ODFs were evaluated by in vitro (thickness, folding endurance, tensile strength, disintegration, SEM, FTIR, XRD and release study) and in vivo (analgesic, anti-inflammatory activity, pro-inflammatory cytokines and gastroprotective assay) studies. The in vitro characterization revealed that TSD preserved its integrity and was effectively loaded in S1 and S2 with optimal compatibility. The films were durable and flexible with a disintegration time ≈15 s. The release profile at pH 6.8 showed that the solid dispersion of FBP improved the drug solubility and release when compared with pure FBP. After in vitro studies, it was observed that the analgesic and anti-inflammatory activity of S2 was higher than that of pure FBP and other synthesized formulations (TSD and S1). Similarly, the level of cytokines (TNF-α and IL-6) was also markedly reduced by S2. Furthermore, a gastroprotective assay confirmed that S2 has a higher safety profile in comparison to pure FBP and other synthesized formulations (TSD and S1). Thus, composite ODF (S2) can effectively enhance the FBP solubility and its therapeutic efficacy, along with its gastroprotective effect.

Bioadhesive behaviors of HPMC E5: comparative analysis of various techniques, histological and human radiological evidence

Enhancing drug residence duration within the stomach offers distinct advantages for both localized and systemic effects. Numerous strategies have been proposed to extend drug residence time, with mucoadhesive polymers being a notable avenue. In this context, hydroxypropyl methylcellulose E5 has been employed as both a binding agent for granulating contrast metal powder and a mucoadhesive polymer, spanning various concentrations. The in vitro bioadhesion strength of the formulated tablets was gauged against the stomach lining of rabbits, for the quantification of bioadhesive forces. The temporal aspect of bioadhesion was evaluated through two approaches: one centered on gastric fluid dynamics and another proffered by the researchers, focusing on gastric wall kinetics. The results divulged a decline in bioadhesion force concomitant with high polymer concentrations. Histological examination of stained stomach sections revealed mucosal perturbations within the rabbit stomach. These disruptions exhibited an escalating trend in conjunction with elevated polymer concentrations, culminating in extensive disturbance at a 7.5% polymer concentration. The outcomes unveiled a direct relationship between polymer concentration increments and extended contact time. Subsequent radiological tracking of contrast metal behavior within a mature human stomach indicated a residence time of 6 h due to the entrapment of displaced components at disparate locations.

A Study on Some Factors Affecting the Preparation of Piroxicam Nanosuspension Using Hydroxypropyl Methyl Cellulose (HPMC E5)

A Study on Some Factors Affecting the Preparation of Piroxicam Nanosuspension Using Hydroxypropyl Methyl Cellulose (HPMC E5)

In-vitro and In-vivo Evaluation of Cevimeline HCl Fast Dissolving Films

The primary aim and objective of the present work was to formulate the cevimeline HCl fast-dissolving films and assess the films, a pharmaceutical compound utilized for the management of xerostomia symptoms linked to Sjogren’s disease. Fast-dissolving films of cevimeline HCl were formulated by utilizing the solvent casting technique and the sodium carboxy methyl cellulose, HPMC E5, polyvinyl alcohol, and polyvinyl pyrrolidone were used as film-forming agents. Additionally, polyethylene glycol 600 and sodium starch glycolate were used as a super disintegrant and plasticizers. The formulation contains citric acid and stevia powder, which serve the purpose of stimulating saliva and providing sweetness, respectively. This study focused mainly on the development and assessment of cevimeline HCl fast-dissolving films, specifically examining parameters such as film thickness, folding resistance, drug content, air bubble entrapment, and film curling. The obtained results were found to be consistent with the preset ranges established for these parameters. The drug release from the fast-dissolving films formulated with PVP K30 was 99.91% released within 5 minutes timeframe. The results indicates that the films prepared with PVP K30 show enhanced solubility, rate of dissolution, flexibility, and tensile strength in comparison to the films formulated with sodium carboxy methyl cellulose, HPMC E5 and Polyvinyl alcohol. Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC) studies were done to characterize the pure drug, polymers and to C11 the optimized formulation. These findings indicated, no observed incompatibilities among the drug and polymers utilized in this study. Moreover, in-vivo investigations were conducted on optimized formulation C11, which demonstrated its notable stability.

Nano-calcium incorporated piscean collagen scaffolds: potential wound dressing material

BackgroundCollagen proteins extracted from piscean sources are alternatives to bovine and porcine collagen because of their abundance, low price, and skin compatibility and are being explored as suitable wound dressing materials. Intracellular calcium ions are crucial for wound healing, and studies have shown that calcium ion supplementation via an external medium is equally beneficial for speedy recovery. This study explores the wound healing potential of dressing materials that encompass the benefits of nano-calcium and piscean collagen. Nano-calcium sulphate (NCS)-integrated scaffolds were prepared with 100 ppm of NCS and varying concentrations of piscean collagen and HPMC E15 LV. The thickness, tensile strength, folding endurance, pH, expansion profile, and moisture vapour transmission properties of the scaffolds were determined. An in vitro scratch assay and an excision rat wound model were employed to evaluate the wound healing properties of the scaffolds.ResultsThe NCS particles had a mean particle size of 220.7 nm. The scaffolds demonstrated an acceptable thickness, mechanical strength, and flexibility. The scratch assay results revealed that at the end of 24 h of the study, there was an increased wound closure rate with collagen scaffolds in contrast to the control group. In the vivo wound healing studies, formulation CS6 showed 100.0% healing on day 12 as compared to other formulations.ConclusionsWounds treated with scaffolds contracted faster than those treated with a commercial collagen dressing and the control group. The current study thus demonstrates the wound healing ability of nano-calcium sulphate-incorporated piscean collagen scaffolds.

Development of rapidly soluble mebendazole nanosuspension for colorectal cancer

Mebendazole (MBZ) has been proven as a repurposing molecule against colorectal cancer. Unfortunately, its clinical application is constrained by its extremely poor solubility and bioavailability. The aim of the current work was to augment the dissolution rate at colonic pH and the anticancer efficacy by formulating MBZ nanosuspension (NS). A robust MBZ NS was developed using a combination of Sodium Lauryl Sulphate (SLS) and Hydroxy Propyl Methyl Cellulose E5 (HPMC) as stabilizers through the dual centrifugation method. The prepared MBZ NS exhibited the smallest particle size (362.6 ± 12.3 nm) with unimodal particle size distribution and excellent short-term stability. DSC and FT-IR studies confirmed the crystallinity and the absence of interactions with the stabilizers used. The developed MBZ NS demonstrated ∼20 folds higher dissolution than MBZ alone in colonic pH. Cell experiments showed that HPMC E5 and SLS were safe on HT-29 and HT-116 cell lines. In addition, IC50 of MBZ-NS was found to be 1.028 ± 0.030 μM and 0.884 ± 0.050 μM in HT-29 and HT-116 cell lines, respectively. Furthermore, 1.5 folds and 1.8 folds reduction in 3D tumor spheroids after treatment with MBZ-NS was observed compared to the control and MBZ physical mixture. From the In Vitro Live/Dead Cell Assay higher amount of red fluorescence in treatment groups confirmed a large number of dead cells compared to the control. In a nutshell, the produced MBZ NS could be employed as a promising formulation to achieve a higher dissolution rate and anticancer efficacy against colorectal cancer of repurposing drug MBZ.

Comparison of Co-Processed Superdisintegrants with Superdisintegrants in Drug Release for Palatable Fast Disintegrating Oral Films of Metolazone

The present study was aimed to compare co-proceesed superdisentigrant with superdisentigrants in drug release and formulate a palatable fast disintegrating oral films of metolazone and compare with standard market solid oral dosage forms. The drug was incorporated as solid dispersion to mask the bitter taste of the drug with different polymers in different ratios (PEG 4000 & Poloxomer 407) and was assessed for its taste. Metalazone with Poloxomer 407 (M-SD 5) in the ratio of 1:2 was better masked. The films were prepared by solvent casting method. HPMC E15 & Pullulan were chosen as the film forming polymers and sodium starch glycolate and crosscaramellose sodium were chosen as superdisentigrant for formulation. Pullulan (80mg) and crosscaramellose sodium (0.6%) showed the highest % drug release (99.49±0.15 within 15 min.). Therefore, this composition was chosen to prepare the film having co-processed superdisintegrants (SSG+CCS in 1:1) MF-10. MF-10 showed better disintegration (10 sec) and dissolution rate (99.12% drug release within 10 minutes.) when compared with the best formulation of superdisintigrant. All the evaluations of the optimized formulation were found to be satisfactory and within limits. MF-10 was subjected to stability studies and compared with marketed oral formulation and was found to be satisfactory.
 Keywords: Metolazone, Fast disintegrating oral films (FDOFs), patient compliance, taste mask, rapidly disintegrate, co-processed superdisintegrants.

Topical delivery of extracted curcumin as curcumin loaded spanlastics anti-aging gel: Optimization using experimental design and ex-vivo evaluation

ObjectiveThis study aimed to extract and separate the organic coloring agent known as Curcumin from the rhizomes of Curcuma longa, and then to create Spanlastics that were loaded with curcumin using the ethanol injection technique. The optimized Spanlastic dispersions were then incorporated into a gel preparation for topical anti-aging use. The Spanlastic dispersions were analyzed for particle size, zeta potential, drug loading efficiency, and in vitro release profile. Furthermore, the rheological properties of the gel preparation were assessed, and a skin penetration study was conducted using confocal microscopy. MethodsTwelve different Curcumin-loaded Spanlastic dispersions using the ethanol injection method with Span® 60 as a surfactant and Tween® 80 as an edge activator in varying ratios. The dispersions were then subjected to various tests, such as particle size analysis, zeta potential measurement, drug entrapment efficiency assessment, and in vitro release profiling. The optimized formula was selected using Design-Expert® software version 13, then used to create a gel preparation, which utilized 2% HPMC E50 as a gelling polymer. The gel was evaluated for its rheological properties and analyzed using confocal microscopy. Additionally, Raman analysis was performed to ensure that the polymers used in the gel were compatible with the drug substance. ResultsF5 formula, (that contains 10 mg Curcumin, and mixture 5 of span-tween mixtures that consist of 120 mg Span® 60 with 80 mg Tween® 80) was selected as the optimized formula with a desirability produced by Design Expert® software equal to 0.761, based on its particle size (212.8 ± 4.76), zeta potential (−29.4 ± 2.11), drug loading efficiency (99.788 ± 1.34), and in vitro release profile evaluations at Q 6hr equal to almost 100 %. Statistical significance (P < 0.05) was obtained using one-way ANOVA. Then F5 was used to formulate HPMC E50 gel-based preparations. The gel formula that was created and analyzed using Raman spectroscopy demonstrated no signs of incompatibility between the Curcumin and the polymers that were utilized.The confocal spectroscopy found that the anti-aging gel preparation showed promising results in terms of skin penetration. Also, images revealed that the gel could penetrate the layers of the skin (reached a depth of about 112.5 μm), where it could potentially target and reduce the appearance of fine lines and wrinkles. The gel also appeared to be well-tolerated by the skin, with no signs of irritation or inflammation observed in the images. ConclusionThe obtained results successfully confirmed the potential of the promising (F5) formula to produce sustained release action and its ability to be incorporated into 2% HPMC E50 anti-aging gel. The confocal microscopy study suggested that the anti-aging gel had the potential to be an effective and safe topical treatment for aging skin.

Formulation and evaluation of topical gels incorporated with solid dispersions of an antiinflammatory drug

Formulation and development of a most effective product from poorly soluble drugs is one of the most challenging tasks in pharmaceutical industries. Solid dispersion is an efficient solubility enhancement method to overcome the solubility problem. The aim of this study was to formulate topical gels incorporated with solid dispersion of Aceclofenac to enhance permeability through the skin. Aceclofenac solid dispersions were prepared using suitable hydrophilic carriers to increase its aqueous solubility. In this study, solid dispersions of Aceclofenac were prepared by solvent evaporation and co-grinding method with two different hydrophilic carriers such as polyvinyl pyrrolidone (PVPk-30), and HPMC E15 LV. These were used in the ratio of (drug: carrier) 1: 1, 1:2 &amp; 1:3 respectively. Evaluation parameters for formulation optimization were drug content, percentage practical yield, DSC, , in-vitro dissolution studies &amp; FTIR. The optimized SD (F3) solid dispersion is incorporated in topical gels of different concentrations prepared by using two gelling agents such as Carbopol 934 and HPMC K100M. From the results of in-vitro dissolution studies it was found that formulation F3 containing PVP k30 (1 : 3 ratio of drug: PVP k30) shows a higher dissolution rate compared with other formulations and pure drug. Optimized solid dispersion was incorporated into topical gels prepared by using two gelling agents in different concentrations. From the stability data obtained, no significant changes in physical appearance, viscosity, pH, and drug contents were seen. The present research work could be concluded as a successful production of topical gels incorporated with Aceclofenac solid dispersion. Improvement in aqueous solubility and thereby greater skin permeation is expected

Study on Improving the Performance of Traditional Medicine Extracts with High Drug Loading Based on Co-spray Drying Technology.

The purpose of this study is to develop modified particles with different structures to improve the flowability and compactibility of Liuwei Dihuang (LWDH) powder using co-spray drying technology, and to investigate the preparation mechanism of modified particles and their modified direct compaction (DC) properties. Moreover, tablets with high drug loading contents were also prepared. Particles were designed using polyvinylpyrrolidone (PVP K30) and hydroxypropyl methylcellulose (HPMC E3) as shell materials, and sodium bicarbonate (NaHCO3) and ammonium bicarbonate (NH4HCO3) as pore-forming agents. The porous particles (Ps), core-shell particles (CPs), and porous core-shell particles (PCPs) were prepared by co-spray drying technology. The key DC properties and texture properties of all the particles were measured and compared. The properties of co-spray drying liquid were also determined and analyzed. According to the results, Ps showed the least improvement in DC properties, followed by CPs, and PCPs showed a significant improvement. The modifier, because of its low surface tension, was wrapped in the outer layer to form a shell, and the pore-forming agent was thermally decomposed to produce pores, forming core-shell, porous, and porous core-shell composite structures. The smooth surface of the shell structure enhances fluidity, while the porous structure allows for greater compaction space, thereby improving DC properties during the compaction process.

Influence of polymers on oxaprozin dissolution kinetics and mechanisms

In this work, the influences of polymers (HPMC E3, PEG 6000, PVP K25, PVP K30), temperature, stirring speed and polymer mass fraction on the oxaprozin (OXA) dissolution profiles were measured by a United States Pharmacopeia (USP) Ⅱ dissolution apparatus. The two-step chemical potential gradient model combined with the interfacial steady-state mass transfer model as well as PC-SAFT (perturbed-chain statistical associating fluid theory) were used to analyze the dissolution mechanism of OXA under different conditions. The presence of polymer could promote the surface reaction of OXA while temperature and stirring speed have different influences on the surface reaction and diffusion. The diffusion boundary layer thickness δ of OXA tablets increases with the increase of temperature and decreases with the increase of stirring speed. Based on the obtained surface reaction rate constant ks and diffusion rate constant kd, the dissolution profiles with high accuracy compared with the experimental data.

Incorporation of exemestane into ternary nanosponge system for enhanced anti-tumor potential in breast cancer

The present investigation reports the potential of exemestane loaded cyclodextrin based nanosponges for the treatment of breast cancer. Fourier transform infrared, and nuclear magnetic resonance (NMR) spectroscopic analysis confirmed the encapsulation of ring B, C, and D of exemestane in the nanosponge cavity. In vitro studies demonstrated a 6.58-folds increase in the aqueous solubility and a 1.76-folds increase in the dissolution of exemestane in the optimized nanosponge formulation EF2. It also exhibited enhanced cytotoxicity in MCF-7 cell line. Pharmacokinetic studies revealed a 1.37-fold increase in C max and a 2.10-fold increase in oral bioavailability of EF2, as compared to its marketed product Aromasin®. Concomitantly, this nano-formulation reduced the tumor burden to 45.71% in a DMBA-induced breast cancer rat model. This EF2-treatment also improved the hematological parameters of the animals. Histopathology of breast tissue also presented reduction in characteristic cytoarchitectural features of breast tumor. In vivo toxicity studies demonstrated reduced hepatotoxicity of the nanosponge formulation when compared with Aromasin®. These results were further supported by histological studies of excised liver tissues, where the size of hepatocytes in EF2-treated animals was like the normal hepatocyte size. In conclusion, the encapsulation of exemestane in β-cyclodextrin nanosponge along-with HPMC E5 improved its aqueous solubility, bioavailability, and ultimately therapeutic efficacy for the treatment of breast cancer.

Development and optimization of mouth-dissolving strips of L-methyl folate: A modern approach for patient compliance

The goal of this study is to create a mouth-melting strip of L-methyl folate calcium, which will dissolve and disintegrate more quickly when given orally for the onset of action. : Solvent casting was used to create a calcium L-methyl folate film that dissolves in the mouth. Polymer, plasticizer, and flavouring agents were chosen after early experiments. Once the excipients were chosen, 3 complete factorial designs were used to improve the formulation. Folding endurance (Y1), tensile strength (Y2), and disintegration time (Y3) were chosen as dependent variables, whereas HPMC E5 concentration (X1) and glycerine concentration (X2) were chosen as independent variables. The film's physicochemical parameters, including SEM, thickness, percent elongation, percent cumulative drug release, and palatability, were measured for the optimized batch and compared to those of the commercial product. The formulation of the mouth-dissolving strip took into account outcomes from the trial batch, including transparency, stickiness, and brittleness. The optimal batch has 55% HPMC E5 and 14.9% glycerine, with a folding endurance of 59±0.23, a tensile strength of 4.18±0.07 N/m, and a disintegration time of 40±0.12 seconds. The optimized film has dimensions of 0.08±0.01 mm in thickness, 60±1.58 mg in mass, 15.33±0.25% in elongation, and 98.33±0.27% in content uniformity. The SEM results validate the uniform film with uniform drug distribution. After 3 minutes, the L-methyl folate calcium mouth-dissolving strip had a %CDR of 99.42%. Findings of f2=52.85 and f1=12.5 for the similarity factor suggest that the medication release is clinically and commercially equivalent. One month of stability at 30°C and 65%RH was observed for the improved batch. The results of the created mouth-dissolving strip test are satisfactory, indicating the intended medication release. When compared to pills that dissolve in the mouth, it is clear that it is more patient-friendly.

IN VITRO AND IN VIVO EVALUATION OF EZETIMIBE FAST-DISSOLVING FILMS

Objective: The goal of this investigation was to develop and evaluate Ezetimibe fast-dissolving films, which are used to treat hyperlipidemia and prevent cholesterol absorption. Methods: The fast-dissolving Ezetimibe films were developed using the solvent casting method and included the following ingredients sodium carboxy methyl cellulose, HPMC E5, Polyvinyl Alcohol, Polyvinyl pyrrolidone which act as film-forming agents polyethylene glycol 600 and sodium starch glycolate, which acts as a superdisintegrant and plasticizer;, citric acid and stevia powder, which serves as a saliva stimulant and sweetener. Results: The fast-dissolving films of Ezetimibe prepared with PVP K30 released the drug up to 99.87% within 5 min, which showed the increased solubility, dissolution rate, flexibility and tensile strength of the films when compared to formulation prepared with sodium carboxy methyl cellulose, HPMC E5, Polyvinyl Alcohol. The FTIR and DSC studies were conducted for pure drug, polymers and optimized formulation E11, which indicated that were no incompatibilities found between the drug and polymers used in the present studies. Scanning electron microscopy analysis was performed for pure drug, and optimized formulation E11 showed that they were no surface fractures and cracks in the films. The optimized formulation E11 was subjected to in vivo studies by using New Zealand Rabbits, and accelerated stability studies revealed that all the formulation is stable. Conclusion: The current study reveals that fast-dissolving films formulated as a novel drug delivery technology can increase the solubility and dissolution rate of poorly water-soluble drug Ezetimibe.

SOLID DISPERSION SYSTEMS OF POORLY WATER SOLUBLE DRUG FEBUXOSTAT: PREPARATION, CHARACTERIZATION AND OPTIMIZATION

Febuxostat is a poor soluble drug used in the management of hyperuricemia and gout. The present study aims at increasing the solubility of febuxostat by solid dispersion technique with the aid of various polymers (Beta cyclodextrin, Soluplus®, HPMC E5, and Kolliphor® P 407) in various drug: carrier ratios employing the solvent evaporation method. Solid dispersions were evaluated for physical appearance, percentage yield, drug content, saturation solubility and dissolution properties. Saturation solubility data of the study depict an increased solubility of the solid dispersion compared to the pure drug. In in vitro release profiles revealed that formulation SD20, having drug: Kolliphor® P 407 in 1:9 ratio exhibited highest dissolution rate. The powder X-ray diffraction study and scanning electron microscopy (SEM) exhibited a crystalline to an amorphous transformation in the solid dispersion. The study demonstrated that solid dispersions are a highly effective technique to increase solubility and bioavailability of febuxostat.

The impact of polymer mixture composition on the properties of electrospun membranes for drug delivery applications

Orally dispersible films (ODFs) prepared by an electrospinning are a novel type of pharmaceutical formulation. This dosage form has the potential to be beneficial for small children and the elderly, who can have problems with administration of classical tablets due to the increased risk of choking and difficulty with swallowing. Due to the highly porous nanofiber morphology, the ODFs examined in this study achieve rapid disintegration into drug microparticles when in contact with saliva. The suspension is then easier to swallow. In this study, we focus on the impact of film composition (polymer matrix composition) on the properties of electrospun membranes. In particular, we prepared ODFs composed of a mixture of PEG 100 000 with HPMC E5 and PVP k90 with HPMC E5. We found significant differences in the structure of electrospinned membranes, where samples containing PEG 100 000 and HPMC E5 exhibited much narrower distribution of fibers. Furthermore, nanofibers containing PVP k90 exhibit a faster disintegration rate, while dissolution of the drug was faster in the case of PEG 100 000 containing ODFs. The improvement was caused by both the structure and composition of the membranes.

Formulation and Evaluation of Bilayer Anti-Diabetic Tablet of Murayya Koeinigii and Spinach Olaracea

The purpose of this study was to develop and evaluate bilayer tablet for the immediate and controlled release of murayya koeinigii and spinach oleracea for effective treatment of diabeties (Type 2). The immediate release layer was prepared by using super disintegrants- starch powder and the sustained release layer was prepared by using polymer like acaia, HPMC E5 and Methyl cellulose. Before preparation of the tablets, all the preformulation parameters were checked and the tablet of murayya koeinigii and spinach oleracea were prepared by direct compression method and was evaluated for physical characteristics like hardness, weight variation, drug content and friability. In vitro release of drug was performed USP type II dissolution test apparatus using distilled water buffer as dissolution media and dissolution was continued for 10 hrs for the sustained release layer. It was found that all the formulations were within the limit of the standard. The drug release of the tablet was in the range of 67%-99% in 10 h. The drug release pattern of formulation F5 was fitted in different kinetic models which showed highest regression for zero order kinetics with Koresmeyer Peppas through non-fickian type of drug release mechanism. Hence It was concluded that the F5 formulation showed the optimum result as a bilayer tablet for the effective treatment of diabeties (Type 2).

DEVELOPMENT AND EVALUATION OF RAMOSETRON HYDROCHLORIDE MOUTH DISSOLVING THIN FILM FOR ENHANCED THERAPEUTIC EFFICACY AND PALATABILITY

Objective: Many people have difficulties in swallowing traditional dosage forms such as tablets and capsules. The goal of this study was to develop the mouth-dissolving thin film of Ramosetron HCl (RH) for quick onset of action in the treatment of vomiting and irritable bowel syndrome, with the added benefit of disguising the bitter taste of RH. Methods: The solvent-casting approach was employed to formulate mouth dissolving thin film. The effect of variable concentrations and different grades of hydrophilic polymer HPMC (E5, E15 and E50), and plasticizers like glycerol and PEG 400 on disintegration time, drug release, thickness, tensile strength, percent elongation, folding endurance, and on appearance were studied. The optimized batch was kept for stability study at40±2 °C/75±5% RH for 30 d. Results: The formed films were transparent with a smooth surface texture. The thickness, weight variation, drug content and pH of the surface were within acceptable limits. Tensile strength and folding endurance values demonstrated adequate mechanical strength. In 45 seconds, the formulation F6 comprising HPMC E5 (150 mg) and HPMC E15 (150 mg) with PEG 400 (0.4 ml) disintegrated. The F6 formulation released 98.78±0.96 %drug in 8 min and considered as optimal formulation. The taste masking of drug was evaluated by a taste perception study using volunteers. The optimized batch was found to be stable at 40±2 °C/75±5% RH for 30 d. Conclusion: The concentration of hydrophilic polymers and plasticizers had a significant effect on the formulation and assessment characteristics of thin film. Mannitol assisted in masking the bitter taste of RH.

Formulation development and characterization of Lecarnidipine hydrochloride niosomal transdermal patches

The bioavailability of Lercanidipine Hydrochloride (LCP) is about 44% and half-life of the drug is about 4.6 hours. LCP due to its low therapeutic dose range of 2.5 to 20mg and substantial biotransformation in liver becomes it ideal molecule in development of transdermal therapeutic system. The primary objective of the present research work was to develop Niosomal transdermal patch (NP) of Lecarnidipine. The LCP nanoparticles were prepared by solvent evaporation method and the optimized Nanoparticles formulation has shown 225nm particle size with a polydispersity index (PDI) of 0.120. LCP patches were prepared by incorporating nanoparticles dispersion, using varying concentrations of polymers HPMC E5, HPMC 5cps, HPMC 15cps, Carbopol 734 and Sodium alginate using solvent casting techniques and further optimized by central composite design(CCD) the effect of polymer on the various physico-chemical characteristics and in-vitro drug release studies, ex-vivo skin permeation studies is studied. On the basis of in-vitro drug release and ex-vivo skin permeation studies, the formulation containing (HPMC 15cps and HPMC 5cps) has shown sustained and extended drug release over a period of 24 hrs.&#x0D; Keywords: Lecarnidipine; Niosomes; Transdermal patch; Central composite Design, Controlled release; Bioavailability etc.