Methylcellulose K4M Research Articles

Design of berberine hydrochloride sustained-release cold sol using hydroxypropyl methyl cellulose K100M to achieve superior drug dissolution and transdermal absorption

In this study, berberine hydrochloride (Ber) was used as model drug to prepare a sustained-release cold sol using hydroxypropyl methyl cellulose (HPMC) to achieve superior drug dissolution and transdermal absorption effects. For comparison, a Ber cold sol without HPMC was also prepared using the same method. The preparation process was optimized based on the in vitro release and transdermal permeability of the drug. The results indicated that 1.67 wt% Carbomer 940 and 1.33 wt% HPMC K100M were selected as matrix components with the best sustained-release effect, and drug dissolution of cold sol prepared by combination of these two matrices was significantly slower than the cold sol without HPMC. In addition, transdermal absorption result demonstrated that 0.67 wt% glycerin and 1.33 wt% peppermint oil were the best osmotic enhancers for the optimization of Ber sustained-release cold sol. Herein, HPMC K100M performed important functions in the external application of Ber.

Diltiazem Hydrochloride Floating Matrix Tablet: Formulation and in vitro-in vivo Evaluation.

Diltiazem hydrochloride is a calcium channel-blocker with a plasma elimination half-life of 4.4 ± 1.3 h and has a narrow absorption window. So, this work aimed to prepare a gastro-retentive floating matrix tablet. The direct compression method was used to manufacture tablets. 32 factorial design was applied for optimization, taking Hydroxypropyl Methylcellulose K100M (HPMC K 100M) and the amount of sodium bicarbonate as independent factors and cumulative percentage release at 1 h, at 6 h, and at 12 h and floating lag time as dependent variables. The high amount of HPMC K100M and sodium bicarbonate shows good results. The optimized preparation was evaluated for differential scanning calorimetry, in-vivo gastric retention in male albino rabbits, kinetic modeling, and stability study. An in vivo study revealed gastric retention of tablets up to 6 h in healthy male Albino rabbits. The stability study indicated no significant change in the buoyancy and release profiles of the drug. From this study, it can be concluded that the gastro-retentive diltiazem hydrochloride floating matrix tablet was successfully prepared and retained inside the rabbit stomach for up to 6 h and was stable under accelerated stability study.

3D printing of multi-unit gastro-retentive tablets for the pulsatile release of artesunate

Pulsatile drug delivery is hardly achieved by conventional gastro-retentive dosage forms. Artesunate as a typical anti-malaria medicine needs oral pulsatile release. Here, artesunate-loaded pulsatile-release multi-unit gastro-retentive tablets (APGTs) were prepared with a semi-solid extrusion three-dimensional (3D) printing method. An APGT was composed of three units: artesunate-loaded immediate and delayed release units and a block unit. The matrix of the immediate/delayed release units consisted of polyvinylpyrrolidone (PVP) K30 and croscarmellose sodium, which improved the rapid release of artesunate when contacting water. The block unit consisted of octadecanol, hydroxypropyl methyl cellulose K15M, PVP K30, and poloxamer F68. APGTs showed multi-phase release in simulated gastric liquids (SGLs). The first immediate release phase continued for 1 h followed by a long block phase for 7 h. The second rapid release phase was initiated when the eroded holes in the block unit extended to the inner delayed release unit, and this phase continued for about 14 h. Low-density APGTs could ensure their long-term floating in the stomach. Oral APGTs remained in the rabbit stomach for about 20 h. 3D printing provides a new strategy for the preparation of oral pulsatile-release tablets.

Establishment and Validation of a Transdermal Drug Delivery System for the Anti-Depressant Drug Citalopram Hydrobromide.

To enhance the bioavailability and antihypertensive effect of the anti-depressant drug citalopram hydrobromide (CTH) we developed a sustained-release transdermal delivery system containing CTH. A transdermal diffusion meter was first used to determine the optimal formulation of the CTH transdermal drug delivery system (TDDS). Then, based on the determined formulation, a sustained-release patch was prepared; its physical characteristics, including quality, stickiness, and appearance, were evaluated, and its pharmacokinetics and irritation to the skin were evaluated by applying it to rabbits and rats. The optimal formulation of the CTH TDDS was 49.2% hydroxypropyl methyl cellulose K100M, 32.8% polyvinylpyrrolidone K30, 16% oleic acid-azone, and 2% polyacrylic acid resin II. The system continuously released an effective dose of CTH for 24 h and significantly enhanced its bioavailability, with a higher area under the curve, good stability, and no skin irritation. The developed CTH TDDS possessed a sustained-release effect and good characteristics and pharmacokinetics; therefore, it has the potential for clinical application as an antidepressant.

Anti-psoriatic evaluation of aloe emodin-loaded topical hydrogel in an imiquimod-induced human plaque-type psoriasis in BALB/c mice

Aloe emodin, an anthraquinone derivative, mainly obtained from Aloe vera, possesses an extensive spectrum of pharmacological properties, including anti-proliferative, anticancer, wound healing, analgesic, anti-inflammatory, antibacterial, and antiviral properties. The objective of the present study was to prepare aloe emodin-loaded topical hydrogel formulations for managing plaque-type psoriasis. Different proportions of carbopol 940, chitosan, and hydroxyl propyl methyl cellulose K15M (HPMC K15M) were used as gelling agents. The prepared hydrogels were characterized for pH, viscosity, rheological behavior, spreadability, extrudability, swelling index, drug content, and accelerated stability. Based on physicochemical and in vitro permeation studies, PHGL1 containing aloe emodin (1%) and carbopol 940 (1%) was selected. The acute dermal toxicity study was also conducted as per the OECD guidelines 402. The mechanism of drug release followed Korsemeyer–Peppa’s model. The optimized batch showed a pH range from 6.867 ± 0.015 to 6.91 ± 0.254, drug content 94.6% ± 0.686% w/w of the active principle when studied in triplicate for drug content analysis, the measured viscosity of the formulation was 31402.33 ± 149.0783 mPaS exhibiting a shear thinning system along with thixotropic behavior at 25°C, and sustained drug release of 78% in 8 hours. An ex vivo permeation study demonstrated that 203.73 μg/ml/cm2 drug permeated through skin in 24 hours. Application of aloe emodin-loaded topical hydrogel to psoriatic skin resulted in a reduction of epidermal thickness, scaling, and ear thickness. The key inflammatory marker tissue necrosis factor (TNF-α) also showed a significant decrease. Compared with the marketed formulation, the test formulation showed no significant difference in the percentage reduction in ear thickness. No acute dermal toxicity was observed at the initial dose of 200 mg. The outcome suggests the promising potential of aloe emodin-loaded hydrogel in improving plaque-like psoriasis without dermal toxicity. Further studies are warranted to establish its efficacy in the management of psoriasis.

Formulation and Evaluation of Gastroretentive In Situ Gelling System of Ketoprofen

Abstract A revolutionary concept for achieving long-term medication release is the gastroretentive in situ gelling system. The goal of this research was to formulate and test a gastroretentive in situ gel for ketoprofen delivery to targeted site to increase the residence and delivery time. Ketoprofen gastroretentive in situ gels were synthesized using a cation-driven gelation approach using various combinations and concentrations of polymers such as gellan gum, sodium alginate, and hydroxypropyl methylcellulose (HPMC) K100M. Visual appearance, pH, viscosity, in vitro gelation, in vitro buoyancy, drug content, density measurement, gel strength measurement, water uptake, and in vitro drug release were all evaluated. The total floating time was more than 12 h, with a floating lag time of less than 2 min. The formulations showed pH ranging from 6.89 to 7.61 and drug content ranging from 82.01% to 95.53%. For 11 h, the percent cumulative drug release of formulations F5 and F14, which contained a greater concentration of polymer sodium alginate (1.5%) and a combination of gellan gum and HPMC K100M (0.175% and 0.2%), was 84.10% and 85.49%, respectively. In vitro dissolution experiments and stability investigations both revealed no significant changes in drug content. The findings revealed that the formulated in situ gels aided in extending gastric residence duration, allowing the drug to be released in the stomach.

Extraction, Characterization, and Evaluation of Lepidium sativum Linn. Mucilage as a Mucoadhesive Polymer.

Being biocompatible, less toxic, cheap, easily available, and environmentally friendly, there is an increased trust in natural polymers in the drug delivery system. Mucilages, among the natural polymers, are the primary metabolites of plants that have been widely utilized in pharmaceutical manufacturing for different purposes, and mucoadhesive is one among them. The present study was designed to investigate the use of LSM as a mucoadhesive polymer using ibuprofen as a model drug. The mucilage was extracted following an aqueous extraction method and its percentage yield was found to be 13.2% w/w. Besides, three microsphere formulations of ibuprofen were prepared using synthetic polymer hydroxyl propyl methyl cellulose (HPMC) K100M and the LSM in polymer to drug ratios of 1 : 1, 1 : 5, and 3 : 5 by applying ionotropic gelation followed by solvent evaporation methods. The microspheres were evaluated for various micromeritic properties and all the formulations exhibited free-flowing properties. Optical microscopic pictures of almost all the microspheres except F3 and F6 (which had more or less spherical shapes) were found to have irregular and discrete shapes. Besides, the surfaces of all the formulations were rough in texture. The drug entrapment efficiency of the microspheres was found to be between 52.08% ± 0.80 and 87.97% ± 0.72. The in-vitrowash-off test evidenced that almost 50 percent (especially F3) of the microspheres were able to adhere up to 18 h and showed remarkable bioadhesion properties. The in-vitro drug release profile indicated that all the formulations were able to prolong their drug release up to 12 h with a non-fickian release mechanism, except for F4, which followed a fickian release. Therefore, based on the findings of this study, LSM can be used as a potential alternative mucoadhesive excipient for sustained release formulations.

Buccal spray of standardized Berberis aristata extract causes tumour regression, chemoprotection and downregulation of inflammatory mediators in oral cancer hamster model

Ethnopharmacological relevanceBerberis aristata (BA) has been described in Ayurveda in formulations for treating conditions related to the buccal cavity, including tumours and inflammation. Oral cancer (OC) is a major global health problem with high rates of recurrence and metastasis. Natural product based therapies are being explored as safer therapeutic strategies for OC. Aim of the studyEvaluating the potential of standardized BA extract loaded buccal spray formulation in OC. Material and methodsBA stem bark extract was prepared using sonication and standardized with respect to Berberine. The standardized extract was characterized and formulated as a buccal spray (SBAE-BS) using hydroxyl propyl methyl cellulose K15M, polyethylglycol 400, Miglyol®812N and ethanol. The SBAE-BS was characterized and evaluated in vitro in KB cell line and in vivo in OC hamster model. ResultsThe SBAE-BS had pH, viscosity, mucoadhesive strength and BBR content corresponding to 6.8, 25.9 cP, 345 dyne/cm2 and 0.6 mg/mL respectively. In vitro cytotoxicity of SBAE-BS was comparable to 5 fluorouracil (5FU). In hamsters, SBAE-BS treatment lead to tumour regression (p = 0.0345), improved body weights (p < 0.0001), no organ toxicity, downregulation of inflammatory mediators and improved survival outcomes as compared to standard systemic 5FU. ConclusionThus, SBAE-BS showed cytotoxic and chemo-protective effects in the OC hamster model, evidencing its ethnopharmacological use and demonstrating translational potential to be developed as therapy for OC.

Optimised neem oil-bilayer tablets: A safe, effective and stable tool for the prevention of vector-borne disease outbreaks by Aedes albopictus

The control of mosquito breeding is an essential step towards the reduction of vector-borne disease outbreaks. Synthetic larvicidal agents produce resistance in vectors and cause safety concerns in humans, animals and aquatic species. The drawback of synthetic larvicides opened a new avenue for natural larvicidal agents, but poor dosage accuracy, need for frequent applications, low stability and sustainability are the major challenges with them. Hence, this investigation aimed to overcome those drawbacks by developing bilayer tablets loaded with neem oil to prevent mosquito breeding in stagnant water. The optimised batch of neem oil-bilayer tablets (ONBT) had 65%w/w hydroxypropyl methylcellulose K100M and 80%w/w ethylcellulose in its composition. After the completion of 4th week, 91.98 ± 0.871% azadirachtin was released from the ONBT, which was followed by a subsequent drop in the in vitro release. ONBT reported long-term larvicidal efficacy (>75%) and a good deterrent effect which was better than neem oil-based marketed products. The acute toxicity study on a non-target fish model (Poecilia reticulata), OECD Test No.203 confirmed the safety of the ONBT on non-target aquatic species. The accelerated stability studies predicted a good stability profile for the ONBT. The neem oil-based bilayer tablets can be used as an effective tool for the control of vector-borne diseases in society. The product may be a safe, effective and eco-friendly replacement for the existing synthetic as well as natural products in the market.

Enhancing Oral Absorption of Orlistat through Gastroretentive Mucoadhesive Pellets: Formulation and Evaluation

Aim: The aim of this study was to develop gastroretentive mucoadhesive pellets of Orlistat to improve its oral bioavailability and enhance its absorption.&#x0D; Methods: Orlistat pellets were prepared using Hydroxy Propyl Methyl Cellulose (HPMC) K100M, Sodium Carboxy Methyl Cellulose (NaCMC), Carbopol 934P, and Polyvinyl Pyrrollidone (PVP) K30 in varying ratios. Physical characteristics of the tablets were evaluated, and compatibility studies were performed between Orlistat and the excipients. Swelling index, mucoadhesion strength and drug release were measured for each formulation. Drug release kinetics and stability studies were carried out.&#x0D; Results: The combination of HPMC K100M, NaCMC, Carbopol 934P and PVP K30 provided balanced release and mucoadhesion with F13 showing sustained release up to 16 hours. The calibration curve demonstrated a good linear relationship between Orlistat concentration and absorbance over the range of 10 to 50 ?g/ml. Swelling index increased with time and polymer concentration and mucoadhesion strength increased with polymer viscosity and concentration. Drug release from formulations containing HPMC K100M, NaCMC and Carbopol 934P were 12-14 hours, 10-12 hours and 8-11 hours, respectively. Combination polymers in F10-F13 provided balanced release and mucoadhesion, with F13 showing sustained release up to 16 hours. The drug release followed zero order kinetics with non-Fickian diffusion. Stability studies on the optimized F13 formulation showed no significant changes in appearance, hardness, mucoadhesion or drug release over 3 months.&#x0D; Conclusion: The combination of HPMC K100M, NaCMC, Carbopol 934P and PVP K30 improved the oral bioavailability and absorption of Orlistat. The study demonstrated the importance of compatibility studies and the use of calibration curves for quantitative analysis. The findings provide valuable insights into the development of drug delivery systems for poorly bioavailable drugs.

Design, preparation, and in vitro evaluation of gastroretentive floating matrix tablet of mitiglinide.

The present research is focused on developing floating matrix tablets of mitiglinide to prolong its gastric residence time for better absorption. Gastroretentive tablets were prepared using a direct compression technique with hydroxypropyl methylcellulose K15M (HPMC K15M) and sodium alginate as matrix-forming polymers and sodium bicarbonate as the gas-forming agent. A 32 full factorial design was adopted to optimize the flotation and release profile of the drug. The concentration of HPMC K15M and sodium alginate were taken as the independent variables, and the floating lag time, time required for 50% drug release, and time required for 90% drug release were taken as dependent variables. The compatibility between drug and excipients was assessed by Fourier transform infrared (FTIR) spectroscopy. The prepared tablets were evaluated for different parameters such as hardness, friability, drug content, floating time, in vitro dissolution, and stability. Dissolution data were analyzed using various kinetic models to ascertain the mechanism of drug release. Finally, a radiographic study was conducted to estimate the retention time of the optimized floating matrix tablets of mitiglinide inside the body. The results revealed that all the physical properties of the developed formulations were within standard limits. The formulation M3, with the maximum amount of both independent variables, was considered to be the optimized formulation based on the desirability value. In addition, the optimized M3 formulation showed stability for over 6months, as evidenced by insignificant changes in lag time, drug release pattern, and other physical properties. Furthermore, radiographic examination indicated that the tablets remained afloat in gastric fluid for up to 12h in the rabbit's stomach. In conclusion, the developed floating matrix tablet of mitiglinide could be regarded as a promising formulation that could release the drug in the stomach at a controlled rate and, hence, offer better management of type II diabetes.

Formulation and Development of β-glucan Hydrogel using Design of Experiments (DOE)

β-Glucan, an endogenous carbohydrate, is a key functional ingredient found in barley and oats and a major component of microbiological and plant cell walls. With no severe adverse effects, it has anti-tumor, diabetic lowering, wound healing, anti-aging and anticholesteremic effects. Twenty formulations were prepared using different polymers like carbapol 934, hydroxypropyl methylcellulose (HPMC) K100M, HPMC K15M, guar gum and xantham gum. F1 formulation exhibited satisfactory results with respect to in-vitro drug release, spreadability, extrudability viscosity and drug content. In order to optimize the concentration of polymers used in F1 formulation, design 13 was opted. All the above 8 runs were subjected to evaluation tests, out of which F28 exhibited maximum drug release with optimum viscosity, spreadability and extrudability. The results correlated with the design with less percentage relative error. F28 formulation was observed to have positive correlation for ex-vivo drug release. Comparable wound healing activity was observed when performed on HaCaT cell lines.

Formulation and evaluation of gastroretentive drug delivery system of eprosartanmesylate

It had became a challenging experience and effort for a formulator to develop and innovate a drug with maximum bioavailability. Objective: In the present study the focus of research is in the treatment of Hypertension, which is one of the most prevalent cardiovascular diseases in the world, affecting a big proportion of the adult and old age population. Eprosartan mesylate(EPM) is angiotensin-II receptor antagonist used for the treatment of high blood pressure. The drug has poor bioavailability due to limited oral absorption and maximum absorption at proximal intestine. This warrants and offers the use of Gastro Retentive Drug Delivery System (GRDDS) for sustained release formulation in order to achieve prolonged action and to improve patients compliance. Method: Wet granulation technique was selected for preparation of tablets and the drug is formulated with hydroxyl propyl methyl cellulose K100m, hydroxyl propyl methyl cellulose K15m, polyox WSR coagulant, polyox WSR301,polyox WSR N80, Lactose Monohydrate, Micro crystalline cellulose(Avicel), magnesium sterate, ethylcellulose, sodium bicarbonate, tromethamine, etc. Results: For around twenty formulations were made and evaluated for General appearance, Thickness, Hardness or Crushing strength Test, Friability Test, Estimation of drug content.

Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers

Gastroretentive raft-forming formulations were developed in liquid and chewable tablet dosage forms to achieve prolonged delivery of quercetin in the stomach. The formulations contained a solid dispersion of quercetin and polyvinylpyrrolidone (PVP K 30) at a 1:10 w/w ratio to improve the solubility of the flavonoid. The formulations also contained sodium alginate as a gel forming agent, calcium carbonate as a calcium source and carbon dioxide producer and hydroxypropyl methylcellulose K100M as a drug release retarding polymer. The chewable tablets incorporated mannitol as a diluent. Both liquid and chewable tablet formulations exhibited rapid floating behaviour (lag time < 1 min) and long floating duration (>24 h) in 0.1 N HCl. The optimized liquid formulation showed superior characteristics based on high raft strength (10.4 g) and sustained release of quercetin (93 % over 8 h) whereas the optimized chewable tablet formulation exhibited lower raft strength (7.2 g) and lower drug release (79 % in 8 h). The optimized liquid and chewable tablet formulations were found to induce anti-inflammatory activity in cell culture using RAW 264.7 cells macrophages and enhance the migration of human gastric adenocarcinoma (AGS) epithelial cells in vitro, indicating wound healing potential for treatment of gastric ulcers.

DoE-Based Design of a Simple but Efficient Preparation Method for a Non-Effervescent Gastro-Retentive Floating Tablet Containing Metformin HCl.

A sustained-release non-effervescent floating matrix tablet was prepared using a simple and efficient direct compression of spray-dried granules containing metformin hydrochloride and cetyl alcohol with hydroxypropyl methylcellulose K15M (HPMC K15M). The design of experiments was employed to explore the optimal composition of the tablet. The similarity factor was employed to evaluate the equivalence in dissolution profiles between the test tablets and Glucophage XR as a reference. Bootstrap analysis was used to eliminate the formulations for which the dissolution profile was potentially inequivalent to that of the reference. The optimized tablet consisting of 150 mg of cetyl alcohol and 17% HPMC K15M showed a dissolution profile comparable with that of the reference with a similarity factor of 52.41, exhibited a floating lag time of less than 3 s in buffer media, remained floating for 24 h, and reduced the tablet weight by about 20% compared to that of the reference. The current study sheds light on the potential use of non-effervescent gastro-retentive extended-release tablets for high-dose drugs using a simple and efficient direct compression method, and as a potential alternative treatment for Glucophage XR. This study also highlights the importance of a systematic approach to formulation optimization and the evaluation of the dissolution profile.

Formulation and in vitro Evaluation of Effervescent Bilayer Floating Controlled Release Tablets of Clarithromycin and Famotidine

The development of floating tablets with required buoyancy, lag time, and controlling release behaviour of drugs at target site is truly interesting and challenging task for researchers. Current study is concerned with the designing of effervescent floating controlled release tablets of clarithromycin and famotidine to treat peptic ulcer due to Helicobacter pylori (H. pylori) infection. Five formulations (F1-F5) were prepared, among which three formulations were of bilayered tablets while the remaining were included as plain tablets. These tablets were prepared by direct compression method using hydroxypropyl methylcellulose (HPMC) K100M, HPMC K4M and sodium bicarbonate as swelling and floating agents respectively. The qualitative tests such as thickness, hardness, weight variation, friability and uniformity of content were performed to ensure the quality of prepared tablets. The floating lag time of all formulations ranged from 14 to 20 seconds. The effervescent floating tablets with HPMC K4M (F1, F3 &amp; F5) attained the total floating time of more than 12 hours, while tablets prepared with HPMC K100M (F2 &amp; F4) achieved the total floating time of less than 7 hours. This difference in floating behaviour could be due to the variation in compaction and flow properties of the two polymers. The formulations with HPMC K100M (F2 &amp; F4) have comparatively more sustained drug release properties when compared to F1, F3 and F4 using HPMC K4M as swelling and floating polymers. This could be attributed to better compaction of HPMC K100M. The prepared tablets follow non-Fickian diffusion kinetics. Overall, these floating controlled release effervescent bilayer and plain tablets may enhance the compliance and therapeutic outcomes of clarithromycin and famotidine in treatment of H. pylori.

ENHANCEMENT OF THERAPEUTIC WINDOW OF METFORMIN HYDROCHLORIDE BY FABRICATION OF MICROSPHERES COMPRISING POLYMERIC INCULCATION WITH SEMI-SYNTHETIC AND SYNTHETIC POLYMERS BY IMPLEMENTATION OF BOX-BEHNKEN DESIGN

Objective: Innovative enhancement of therapeutic window of Metformin hydrochloride (MFH) and bioavailability through mucoadhesive microspheres by polymeric inculcation of hydroxypropyl methylcellulose K4M grade (HPMC K4M), hydroxypropyl methylcellulose K100M grade (HPMC K100M) and Kollidon SR grade (KS).&#x0D; Methods: Controlled release system was developed by incorporating semi-synthetic and synthetic polymers by modified solvent evaporation technique. Fabrication of mucoadhesive microspheres was designed by the implementation of experimental designs to obtain most optimum concentration of selected factors. The method was optimized by Box Behnken design (BBD) with selected factors as concentrations of semi-synthetic and synthetic polymer with stirring speed influence for the obtained responses that were mean particle size (Y1) entrapment efficiency of drug (Y2) and percent mucoadhesion (Y3). Microspheres were characterized for particle size, entrapment efficiency of drug, ex-vivo mucoadhesion study, in vitro study, Fourier transform infrared spectroscopy (FTIR), x-ray diffraction (XRD) detection and H1 Nuclear magnetic resonance (NMR) quantification for optimized formulation.&#x0D; Results: Implementation of response surface method software for BBD yielded stable microspheres with mean particle size 274 µm, entrapment efficiency of drug 85.07% and percent mucoadhesion 67.03% for optimized formulation F5.&#x0D; Conclusion: Bridging of MFH with the highly innovative combination of semi-synthetic and synthetic polymers yielded stable, cost-effective microspheres with improved bioavailability with controlled-release effect as till date no literature is available that provide information with selected polymeric combination and analytical characterization.

DESIGN AND IN VITRO EVALUATION OF FLOATING DRUG DELIVERY SYSTEM OF GLIPIZIDE USING COMBINATION OF NATURAL MUCILAGES AND SYNTHETIC POLYMERS

Objective: The objective of the study is to explore polysaccharide mucilages of Colocasia esculenta (CE), and Fenugreek (FG) as buoyancy enhancing agents, and mucoadhesive agents by developing gastroretentive floating tablets of Glipizide.&#x0D; Methods: Glipizide loaded floating tablets were developed with CE, and FG alone and in combination of Guar gum (GG), and Hydroxypropyl methylcellulose (HPMC) K4M using direct compression technique. The developed formulations have been subjected to evaluation of in vitro buoyancy study, in vitro drug release study (pH 1.2), and in vitro bioadhesiveness study. Therefore, the final optimized formulation was subjected to Fourier Transform Infrared Spectroscopy (FTIR), Differential scanning calorimetry (DSC), and X-ray powder diffraction (XRD) study.&#x0D; Results: The results of the buoyancy study for formulation F1, F2, and F5 revealed that the instant floating lag time, floating time duration of 1 h, and exhibited 100% drug release in 4 h. Therefore, the formulations developed with GG (F3), and HPMC K4M (F4) have been exhibited slow floating lag time, prolonged floating duration and drug released up to 100 % in 12 h, while; formulations F6, F7, F8, and F9 have been exhibited shortest floating lag time, longest floating time duration, the best drug released up to 12 h, and better in vitro bioadhesiveness properties. Furthermore, F7 exhibited good bioadhesive property as compared to F6, F8-F9. The results of the FTIR, DSC, and XRD study for F7 revealed that the presence of functional groups and amorphous.&#x0D; Conclusion: Owing to the anticipated properties like biocompatibility, biodegradability, swelling ability, and cost-effectiveness of CE; it could be the potential macromolecule for the replacement of synthetic polymers.

Three-dimensional printing of gastro-floating tablets using polyethylene glycol diacrylate-based photocurable printing material

Extruded three-dimensional (3D) printing based on photocurable materials has shown good application prospects in the medical field. This has been attributed to the operational aspect that can be performed at room temperature and the high mechanical strength of the extrudate and final product. However, the commonly used photocurable polymer, polyethylene glycol diacrylate (PEGDA), has a low viscosity and exhibits a long crosslinking time. Therefore, additives are added to improve the printability of the extrudate. In this study, various hydrogels were used to improve the mixing uniformity and rheological behavior of PEGDA-based printing materials. Printing accuracy and mechanical strength were evaluated to optimize print material composition and process parameters. Hydroxypropyl methylcellulose K100M was found to improve the shear thinning and self-supporting properties of printing materials, which were essential for printability. Although the storage modulus of the photocured material proportionally increased with curing time in the range of 20–80 s, the minimal layer time of the 3D samples remained at 65 s, ensuring interlayer adhesion. Gastro-floating tablets with different infill densities were printed to illustrate the application of 3D extrusion printing in personalized medicine. The weight, crushing strength, and floating time were regulated by the infill density of the models. Overall, this study demonstrates that extrusion printing with a photocurable material is an easy way to prepare customized oral preparations with complex internal structures and tunable properties.

The Formulation and Evaluation of Gastro-Bilayer Floating Tablets of Losartan Potassium as Immediate Release Layer and Ramipril Hydrochloride as Sustained Release Floating Layer

Objectives: A sustained release Gastro-bilayer floating tablets with reduced dosing frequency and increased drug bioavailability is developed. The dosage form is suitable for the release of two drugs simultaneously in a single dosage unit i.e. Losartan Potassium and Ramipril Hydrochloride. The SeDeM system for selection of powder blend for direct compression gave the parameter index value of ≥0.5 which is considered as best in terms of compression properties. The prepared dosage form provided sustained effect of the drug for 12 hr by Non-Fickian, controlled diffusion and swollen matrix. Peppa’s release model is best suited for the final formulation of batches. Optimized formulation exhibited floating time of 12 hr and floating lag time of less than 1 min. In-vitro dissolution studies shows 96% of the both the drugs release. The swelling and erosion of polymers is studied by Scanning Electron Microscopy. The data obtained from Analysis of variance demonstrated the significance of the model with a P-value of less than 0.05. Methods: SeDeM system was adopted on powder blend before direct compression for preparation of tablet, the hydroxyl propyl methyl cellulose was used as a rate-controlling polymer and a mixture of citric acid and Sodium bicarbonate formed the floating layer. Results: Radius values through SeDeM diagram was plotted and index values are calculated and resulted in an index value of ≥0.5. The pre-compression and post compressional parameters are as per Indian Pharmacopeia specifications. The best formulation for gastric bilayer tablet had a combination of Hydroxy propyl methyl cellulose K15M and Sodium Carboxy methyl cellulose which gave 99.57% drug dissolution within 12 hr. Conclusion: Gastro-Bilayer Floating Tablets of Losartan as Immediate Release layer and Ramipril as sustained-release floating layer are successfully developed. The problem of poor solubility of drugs can be solved by optimization of blend through SeDeM expert System. Hydroxy propyl methyl cellulose K15M, K4M and Carbopol 934 are helpful in achieving the sustained effect of the drug for 12 hr by Non-Fickian, controlled diffusion and swollen matrix. Peppa’s release model is best suited for the final formulation batches based on the drug release mechanisms.