Polymer Hydroxypropyl Methylcellulose Research Articles

Novel Solid Dispersions of Naphthoquinone Using Different Polymers for Improvement of Antichagasic Activity

IVS320 (3a,10b-dihydro-1H-cyclopenta[b]naphtho[2,3-d]furan-5,10-dione) is a naphthoquinone that has low solubility in aqueous medium, a physical behavior that limits its biological activities, considering that compounds from this class have several activities. In this work, solid dispersions (SDs) prepared between IVS320 and polymers hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG), and polyvinylpyrrolidone (PVP) were developed using physical mixture (PM), kneading (KN), and rotary evaporation (RE) methods. Dispersions were investigated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetry (TG), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). In addition, in vitro antiparasitic activity in Trypanosoma cruzi Y strains was evaluated. Physical-chemical characterization demonstrated the formation of SDs through the interaction of IVS320 with polymeric matrices. SDs of IVS320-polymer presented a significant potentiation of antichagasic activity, with inhibitory growth around 62% (IVS320-HPMC/RE), 55% (IVS320-PEG/RE), and 85% (IVS320-PVP/RE), while pure IVS320 showed a value of 48% for the highest concentrations evaluated (50 µg/mL).

Formulation and evaluation of gastro-retentive floating bilayer tablet for the treatment of hypertension

The paper aimed to progress an ideal gastro retentive drug delivery system intended for directing Losartan and Hydrochlorothiazide as a fixed-dose combination for anti-hypertensive therapy. The bilayer tablets were primed through direct compression method. Losartan was formulated by means of a floating layer expending hydrophilic swellable polymer Hydroxy Propyl Methyl Cellulose K4M, ethyl cellulose (4cps) as a buoyancy enhancer, sodium bicarbonate as a gas spawning agent. The amount of polymer blends remains optimized using 23 full factorial designs. The clout of experimental factors such as swelling agent concentration, buoyancy enhancer and gas generating agent on floating lag time, total floating time, T50% and % drug release remain investigated to get optimized formulation. The responses remain analyzed using Analysis of variance, and polynomial equation stood created for every retort using Multiple linear regression analysis. Entirely preparations floated for more than 12 h. The release pattern of losartan stood fitted to diverse models based on the coefficient of correlation (r). All the formulations, except F2, showed the Korsemeyer-Peppas model as the best fit model. Formulation F2 showed the zero-order model. Diffusion exponents (n) remained indomitable designed for entirely formulations (0.45–0.89), accordingly the chief drug discharge mechanism was non-fickian (anamolous) transport. Formulation F4 containing 20% w/w Hydroxy Propyl Methyl Cellulose K4M, 15% Sodium bicarbonate and 5% ethyl cellulose (4cps) was the best formulation as per the range of drug release remain institute to be more than 95 % in 12h and floating lag time was 20.15 s. The immediate-release layer stood optimized using crospovidone and Indion 414 as a super disintegrant. Formulation A8 containing 2% Indion 414 was considered as optimized formulation as it released 99% drug within 35 min and possessed less disintegration time. Optimized formulation F4 from the controlled-release layer and A8 from immediate-release layer was used to formulate bilayer tablet. The optimized formulation was imperilled to stability reading for three months at 40○C/75% relative humidity. The stability revision exhibited no substantial alteration in the appearance of tablets, floating characteristics, drug content and in-vitro drug dissolution. Consequently, a biphasic drug release design was effectively accomplished over the formulation of floating bilayer tablets.

Therapeutic Efficacy of Moxifloxacin Mucoadhesive Hydrogel for Bacterial Keratitis

Bacterial keratitis is a hypothetically devastating corneal infection due to the opportunity of fast development; corneal devastation either to be completed in 24–48 hours with even more contagious bacterial aetiological agents. Moxifloxacin mucoadhesive Hydrogel was prepared by using polymer Hydroxy Propyl Methyl Cellulose E50 LV by hydration method. Moxifloxacin was dissolved in small quantity of water and Benzalkonium Chloride was added to the Polymer solution. The formulations were evaluated for clarity, pH measurement, spread-ability test, drug content estimation, viscosity study, in vitro diffusion study and antibacterial activity. The developed formulation exhibits the sustained release over a period of 10 hour. The optimized formulation was further evaluated with antimicrobial activity. The results of the in-vitro antimicrobial activity of hydrogel were satisfactory.
 Keywords: Corneal Infection, Hydrogel, Moxifloxacin, invitro release

Development of Bioadhesive Buccal Tablets of Nicorandil Using a Factorial Approach.

In the present investigation, bioadhesive buccal tablets were prepared using the sustained-release polymer hydroxypropyl methylcellulose (HPMC) K100M, bioadhesive polymer neem gum, and an impervious backing layer of ethyl cellulose. Nicorandil is sensitive to the first-pass effect; therefore, a buccal-adhesive dosage form can avoid this effect. We used the direct compression technique to prepare the tablet formulation. A 32 full factorial design was composed in which the amounts of HPMC K100M (X1) and neem gum (X2) were chosen as the independent variables and the dependent variables were the percentage drug release at 6 h (Y1) and mucoadhesive strength in grams (Y2). Various in vitro parameters, i.e. thickness, friability, hardness, weight variation, surface pH, moisture absorption ratio, dissolution studies, and drug release kinetics, and ex vivo parameters like mucoadhesive strength and mucoadhesion time were determined for the prepared tablets. We subjected the optimized batch to a comparison with the marketed formulation and stability studies were performed. The formulation containing a 50:50 ratio of neem gum and HPMC K100M (F5) was considered optimum. The zero-order release kinetics model best fitted the optimized batch release profile, suggesting the system would release the drug at a constant rate. The release by the optimized formulation of the drug at a sustained rate along with its bioadhesive nature showed that the buccal route can be an option for the administration of nicorandil.

Development and Evaluation of Curcumin Floating Tablets

In the present study, curcumin an anti-inflammatory agent, was first complexed with the soluplus by hot melt extrusion machine to enhance the solubility of curcumin and was formulated into floating tablets by direct compression method. Tablets were formulated using various grades of Hydroxypropyl methylcellulose (HPMC) polymers and sodium bicarbonate as gas generating agent. Preformulation and micromeritic studies were performed. The floating tablets were evaluated for their physico-chemical properties, in-vitro release, in-vivo floating property, pharmacokinetic and stability studies. Formulations were found uniform with respect to thickness (5.11 to 5.27 mm) and hardness (4.4 to 4.8 kg/cm2). The friability (0.27 to 0.53 %), weight variation (1.28-1.89%) and Drug content (97.84 to 99.46 %). The order of swelling index of HPMC was found to be K100M > K15M > K4M. Sodium bicarbonate at the concentration of 16% w/w was found to be sufficient in attaining the buoyancy. The buoyancy lag time was found to be less than 1 minute for all the prepared tablets. The total floating time for different formulations was in the range of 12-24 hours. The optimized formulation F4, and F6 showed 98.85 and 98.10 % drug release at the end of 20 and 24 hrs respectively. The in-vivo floating study was carried out by X-ray imaging showed floating of the tablet in the stomach. The pharmacokinetic study showed, Cmax-260 ng/ml, Tmax-12 hrs, AUC -738.33 ng/hr/ml Kel as 0.061 and t1/2 was found to be 11.36 hrs. FT-IR, XRD and DSC studies revealed no chemical interaction between drug and polymers. During the stability period selected tablets were found to be stable with respect to floating behaviour and drug release characteristics.

Dataset on applying HPMC polymer to improve encapsulation efficiency and stability of the fish oil: In vitro evaluation.

Data examines the effect of hydroxypropyl methylcellulose (HPMC) HPMC15 cP, and HPMC 5 cP polymer composition on the physicochemical traits of encapsulated oil made using lab scale spray drying (180 °C). The data found showed that the properties of the reconstituted fish oil powder are significantly affected by the polymer's composition and ratio (p < 0.05). In this experiment, powder with the particle sizes below 60 μm was produced and it was observed that HPMC is a good emulsifier for all formulations and the encapsulation efficiency is high with 75.21% for AF1 formulation. It was also observed that the process of fish oil encapsulation employed by HPMC 5 cP produce a more volatile oil powder, while encapsulation with HPMC 15 cP produced a more stable fish oil powder. These finding shows that the utilisation of HPMC as a polymer to encapsulate fish oil can produce a more efficient and stable compound.

Floating Microspheres Based Nizatidine Gastro Retentive Formulation to Control the Release of Drug

Present research aimed at formulation development and characterization of the floating drug delivery system of Nizatidine, a H2-receptor antagonist, widely prescribed in gastric ulcers and duodenal ulcers. Nizatidine loaded floating microspheres were developed by the solvent diffusion-evaporation method using polymers hydroxypropyl methylcellulose (HPMC) and microcrystalline cellulose (MCC) to prolong the gastric retention time of the drug for the therapeutic management of gastric disorders like ulcers. Further, the developed formulations were characterized for percentage yield, drug entrapment, floating behavior, shape and surface morphology, in vitro drug release, determination of particle size and Zeta potential, in vitro stability studies, and antimicrobial activity. The percentage yield of the different formulation was found to be a range of 75.65– 81.25%, drug entrapment efficacies of different formulations were in the range of 65.56- 75.65% w/w, formulation F4 of floating microsphere was found to be 178.5 nm, Zeta potential of optimized formulation F4 of floating microsphere was found -33.6 Mv, Surface morphology of formulation examines at two different magnification 55X which illustrate the smooth surface of Microspheres. The in vitro drug release pattern of Nizatidine loaded optimized floating microsphere was subjected to the goodness of fit test by linear regression analysis, and it was observed that ‘r’ values of microsphere were maximum for zero-order, i.e., 0.969 hence indicating drug release from formulations follow zero-order kinetics with non-fickian diffusion mechanism which in turn prolonged drug release. The antimicrobial activity of the optimized formulation showed clear fluid with no development of turbidity. It inferred better clearance from infection than plain drug solution at the same doses. Floating microspheres of Nizatidine as gastro retentive dosage forms precisely control the release rate of Nizatidine to a peculiar site and expedite an immense impact on health care.

The Effect of Combination of Hydroxypropylmethylcellulose and Carboxymethylcellulose Sodium Polymers to The Physical Properties of Celery (Apium graveolens L.) Ethanolic Extract Patch

Celery herbs (Apium graveolens L.) contain apigenin compounds (flavonoids) that are effective as antihypertensiv. Celery herbs used in the form of decoction and oral preparations have a deficiency that is voluminous and can cause gastric irritation. Patches were chosen because it can prevent gastric irritation and reduce the frequency of drug administration because the drug is delivered over the skin with a long duration. This study aimed to know the effect of variations in the ratio of the concentrations of hydroxypropyl methylcellulose (HPMC) and carboxymethylcellulose sodium (CMC sodium) polymers to the physical properties of celery herbs ethanol extract patch.This study was conducted with maceration of celery herbs using 96% ethanol and then dispersed in patch made with variations in the concentrations ratio of HPMC and CMC sodium polymers of 3:1, 1:1, and 1:3. Patches were tested for physical properties including organoleptic, pH, thickness, weight, folding endurance, and moisture content. Statistical analysis of test data used One Way ANOVA and Paired Samples T Test.The results of statistical analysis showed that the increase concentrations ratio of CMC sodium polymer in the combination of HPMC and CMC sodium polymers could increase the thickness, weight, and moisture content of celery herbs ethanol extract patch. The best patch was formula 2 with the same concentration ratio of HPMC and CMC sodium polymers because it showed the best results with a pH 6,12-6,29, thickness 1,37-1,53 mm, weighting 2,24-2,52 gram, folding endurance more than 300 times, and the moisture content was quite stable.

Transformation of essential minerals into tablet formulation with enhanced stability

Essential minerals play a very important role in maintaining our physical well-being. In this work, essential minerals; copper sulphate, zinc sulphate, selenium dioxide, chromium picolinate, sodium molybdate and potassium iodide were prepared into tablet formulation with enhanced stability. These minerals are prepared in a coated or as an adsorbate form so as to increase the stability of the minerals. The coated/adsorbate form was formulated into matrix tablets using hydroxypropyl methyl cellulose (HPMC) by the direct compression technique. The distinctively formed tablet was assessed for its physicochemical properties, in-vitro release, microbiological and stability studies. SEM analysis showed that the surface topography of the tablet displayed mechanical interlocking between the trace elements and polymer. During dissolution, the hydrated tablet shows highly porous network of the polymer matrix. Afterwards, they undergo surface erosion from the porous network and the trace minerals gets released. The in-vitro release of zinc sulphate with polymer HPMC K4M showed a sustained release behaviour and fits into the first order and Korsemeyer-Peppas model. The formulation of the trace mineral tablet shows a sustained release profile with increased stability. This trace element matrix tablet supplements is expected to gain acceptance than the marketed products owing to its sustained release behaviour.

A universal natural hydroxy propyl methyl cellulose polymer additive for modifying lignocellulose-based gel polymer electrolytes and stabilizing lithium metal anodes

Defects in gel polymer electrolytes (GPEs) limit the comprehensive performance of lithium-ion batteries (LIBs). Even using an excellent lignocellulose (LC)-based GPE is not sufficient for practical applications due to its poor mechanical properties, low liquid absorption and ionic conductivity. To eliminate these limitations, in this work, a novel biodegradable hydroxy propyl methyl cellulose (HPMC) polymer with a remarkable swelling effect was added to an LC-based polymer matrix. The LC/HPMC (LCH) membrane prepared by the phase transfer method retains the excellent performance of the LC membrane. A large amount of free volume is formed in the corresponding GPE due to the swelling effect, which can remarkably improve the physical and electrochemical properties, including the absorption of the liquid electrolyte (1168 wt%), mechanical property (14.45 MPa), ionic conductivity (6.14 × 10−3 S cm−1, 25 °C), lithium ion transfer number (tLi+ = 0.75), charge/discharge performance (162 mA h g−1 at 0.2C), and excellent regulation ability of Li deposition. Moreover, the overpotential of the Li/LCH-based GPE/Li symmetric battery is stable for more than 1000 h, which illustrates that the addition of the HPMC can provide long-term protection for lithium metal electrodes.

Advancement Of Changed Pulsincap Medicate Conveyance Arrangement Of Metronidazole For Tranquilize Focusing

A changed Pulsincap measurements type of metronidazole was created to target tranquilize discharge in the colon. Groups of hard gelatin cases were treated with formaldehyde keeping the tops in that capacity. Metronidazole pellets arranged by expulsion spheronization technique were consolidated into these particular container shells and stopped with polymers guar gum, hydroxypropylmethylcellulose 10K, carboxymethylcellulose sodium and sodium alginate independently at fixations 20 mg, 30 mg and 40 mg. The filled cases were totally covered with 5% cellulose acetic acid derivation phthalate to forestall variable gastric purging. All the definitions were tested to decide sedate substance and the capacity of the adjusted Pulsincap to give colon-explicit medication conveyance was surveyed by in vitro tranquilize discharge concentrates in cushion pH 1.2 for 2 h, pH 7.4 (reproduced intestinal liquid) for 3 h and pH 6.8 (animated colonic liquid) for 7 h. The outcomes showed that critical medication discharge happened simply after 5 h from the beginning of analysis.

Development of indigenous Streptococcus salivarius TUCC 1253-fermented soy oral strip using Box-Behnken design for oral health

The study was to develop Streptococcus salivarius TUCC 1253-fermented soy oral strip that exhibits antimicrobial activity against oral pathogens. Indigenous S. salivarius TUCC 1253 isolated from healthy human saliva grew well in soy protein isolate after 24 hrs fermentation. Oral strip was developed using hydroxypropyl methylcellulose polymer, propylene glycol plasticizer, S. salivarius TUCC 1253-fermented soy, peppermint flavouring and distilled water. The formulation was successfully optimized which gives characteristics such as low moisture uptake, high percent elongation and high tensile strength. The formulation was successfully optimized with a percentage error of not greater than 4.22%. The optimized S. salivarius TUCC 1253-fermented soy oral strip (20% v/v inoculum) contains more than 108 CFU/g of live cells. The optimized S. salivarius TUCC 1253-fermented soy oral strip was able to inhibit all studied oral pathogens (Enterococcus faecalis, Streptococcus pyogenes and Staphylococcus aureus) in both aerobic and anaerobic conditions. Up to our knowledge, this is the first available oral strips containing indigenous oral probiotic-fermented soy which serve as a new alternative for oral health.

Processing of Polyvinyl Acetate Phthalate in Hot-Melt Extrusion-Preparation of Amorphous Solid Dispersions.

The preparation of amorphous solid dispersions (ASDs) is a suitable approach to overcome solubility-limited absorption of poorly soluble drugs. In particular, pH-dependent soluble polymers have proven to be an excellently suitable carrier material for ASDs. Polyvinyl acetate phthalate (PVAP) is a polymer with a pH-dependent solubility, which is as yet not thoroughly characterized regarding its suitability for a hot-melt extrusion process. The objective of this study was to assess the processability of PVAP within a hot-melt extrusion process with the aim of preparing an ASD. Therefore, the influence of different process parameters (temperature, feed-rate) on the degree of degradation, solid-state and dissolution time of the neat polymer was studied. Subsequently, drug-containing ASDs with indomethacin (IND) and dipyridamole (DPD) were prepared, respectively, and analyzed regarding drug content, solid-state, non-sink dissolution performance and storage stability. PVAP was extrudable in combination with 10% (w/w) PEG 3000 as plasticizer. The dissolution time of PVAP was only slightly influenced by different process parameters. For IND no degradation occurred in combination with PVAP and single phased ASDs could be generated. The dissolution performance of the IND-PVAP ASD at pH 5.5 was superior and at pH 6.8 equivalent compared to commonly used polymers hydroxypropylmethylcellulose acetate succinate (HPMCAS) and Eudragit L100-55.

Gelatin Nanoparticles-HPMC Hybrid System for Effective Ocular Topical Administration of Antihypertensive Agents.

The increment in ocular drug bioavailability after topical administration is one of the main challenges in pharmaceutical technology. For several years, different strategies based on nanotechnology, hydrogels or implants have been evaluated. Nowadays, the tolerance of ophthalmic preparations has become a critical issue and it is essential to the use of well tolerated excipients. In the present work, we have explored the potential of gelatin nanoparticles (GNPs) loaded with timolol maleate (TM), a beta-adrenergic blocker widely used in the clinic for glaucoma treatment and a hybrid system of TM-GNPs included in a hydroxypropyl methylcellulose (HPMC) viscous solution. The TM- loaded nanoparticles (mean particle size of 193 ± 20 nm and drug loading of 0.291 ± 0.019 mg TM/mg GNPs) were well tolerated both in vitro (human corneal cells) and in vivo. The in vivo efficacy studies performed in normotensive rabbits demonstrated that these gelatin nanoparticles were able to achieve the same hypotensive effect as a marketed formulation (0.5% TM) containing a 5-fold lower concentration of the drug. When comparing commercial and TM-GNPs formulations with the same TM dose, nanoparticles generated an increased efficacy with a significant (p < 0.05) reduction of intraocular pressure (IOP) (from 21% to 30%) and an augmentation of 1.7-fold in the area under the curve (AUC)(0–12h). On the other hand, the combination of timolol-loaded nanoparticles (TM 0.1%) and the viscous polymer HPMC 0.3%, statistically improved the IOP reduction up to 30% (4.65 mmHg) accompanied by a faster time of maximum effect (tmax = 1 h). Furthermore, the hypotensive effect was extended for four additional hours, reaching a pharmacological activity that lasted 12 h after a single instillation of this combination, and leading to an AUC(0–12h) 2.5-fold higher than the one observed for the marketed formulation. According to the data presented in this work, the use of hybrid systems that combine well tolerated gelatin nanoparticles and a viscous agent could be a promising alternative in the management of high intraocular pressure in glaucoma.

Solid state nuclear magnetic resonance studies of hydroxypropylmethylcellulose acetyl succinate polymer, a useful carrier in pharmaceutical solid dispersions.

Hydroxypropylmethylcellulose (HPMC) acetyl succinate (HPMC-AS) is a key polymer used for the enablement of amorphous solid dispersions (ASDs) in oral solid dosage forms. Choice of the appropriate grade within the material is often made empirically by the manufacturer of small-scale formulations, followed by extensive real time stability. A key factor in understanding and predicting the performance of an ASD is related to the presence of hydrogen (or other) bonds between the polymer and active pharmaceutical ingredient (API), which will increase stability over the parameters captured by miscibility and predicted by the Gordon-Taylor equation. Solid state nuclear magnetic resonance (NMR) is particularly well equipped to probe spatial proximities, for example, between polymer and API; however, in the case of HPMC-AS, these interactions have been sometimes difficult to identity as the carbon-13 NMR spectra assignment is yet to be firmly established. Using feedstock, selectively substituted HPMC polymers, and NMR editing experiments, we propose here a comprehensive understanding of the chemical structure of HPMC-AS and a definitive spectral assignment of the 13 C NMR spectra of this polymer. The NMR data also capture the molar ratios of the acetate and succinate moieties present in HPMC-AS of various grades without the need for post treatment required by chromatography methods commonly use in pharmacopoeia. This knowledge will allow the prediction and measurement of interactions between polymers and APIs and therefore a rational choice of polymer grade to enhance the solid state stability of ASDs.

Fast Dissolving Sublingual Strips: A Novel Approach for the Delivery of Isosorbide Dinitrate

Background: Isosorbide dinitrate (ISDN) is used for treating the angina attacks. In addition, oral ISDN is available in immediate and sustained release formulations and the bioavailability of ISDN is about 20-25% when taken orally. Further, the ISDN films are developed for sublingual drug delivery by improving drug bioavailability. The present study aimed to design and evaluate the physicochemical properties of the film formulation for sublingual delivery of ISDN. Methods: In the present study, sublingual films were prepared by the solvent casting technique using the hydroxypropyl methylcellulose (HPMC) polymers (i.e., 100, 150 and 200 mg) with a different drug to polymer ratios (i.e., 1:5, 1:7.5 and 1:10). Then, ISDN was evaluated for the film appearance, drug content, surface pH, mucoadhesion force, differential scanning calorimetry (DSC), in vitro drug release, and ex vivo permeability. Results: Based on the results, F3 formulation (1:10 ISDN to HPMC ratio) showed acceptable thickness (0.93 mm), weight (11.14 mg), surface pH (7.82), moisture absorption capacity (6.08%), elasticity (&gt;200), mucoadhesion force (18.05 N/cm2), and drug content (6.22%). Furthermore, the results demonstrated that HPMC polymer improved the characteristics of the films, modified the bioadhesiveness, and finally, enhanced elasticity. However, DSC thermogram failed to show any crystalline drug substance in the films except for F1 (immediate release) and the endothermic peak of ISDN was absent in F2 and F3 films. Therefore, the drug which was entrapped into the film was in an amorphous or disturbed-crystalline phase of the molecular dispersion or dissolved in the melted polymer in the polymeric matrix. Moreover, the drug release from the films was faster compared to the tablet® (P&lt;0.05). Conclusion: In general, the formulation of F1 was observed to be an appropriate candidate for developing the sublingual film for the remedial use.

Application of cellulose-based polymers in oil well cementing

Cellulose-based polymers have been successfully used in many areas of petroleum engineering especially in enhanced oil recovery drilling fluid, fracturing and cementing. This paper presents the application of cellulose-based polymer in oil well cementing. These polymers work as multifunctional additive in cement slurry that reduce the quantity of additives and lessen the operational cost of cementing operation. The viscosity of cellulose polymers such as hydroxyethyl cellulose (HEC), carboxymethylcellulose (CMC) and hydroxypropyl methylcellulose (HPMC) has been determined at various temperatures to evaluate the thermal degradation. Moreover, polymers are incorporated in cement slurry to evaluate the properties and affect in cement slurry at 90 °C. The API properties like rheology, free water separation, fluid loss and compressive strength of slurries with and without polymer have been determined at 90 °C. The experimental results showed that the viscosity of HPMC polymer was enhanced at 90 °C than other cellulose-based polymers. The comparative and experimental analyses showed that the implementation of cellulose-based polymers improves the API properties of cement slurry at 90 °C. The increased viscosity of these polymers showed high rheology that was adjusted by adding dispersant which optimizes the rheology of slurry. Further, improved API properties, i.e., zero free water separation, none sedimentation, less than 50 ml/30 min fluid loss and high compressive strength, were obtained through HEC, CMC and HPMC polymer. It is concluded that cellulose-based polymers are efficient and effective in cement slurry that work as multifunctional additive and improve API properties and cement durability. The cellulose-based polymers work as multifunctional additive that reduces the quantity of other additives in cement slurry and ultimately reduces the operational cost of cementing operation. The comparative analysis of this study opens the window for petroleum industry for proper selection of cellulose-based polymer in designing of cement slurry.

The Effect of Crospovidone on the Dissolution Profile of Amlodipine Besylate from Fast Orally Dissolving Film.

BACKGROUND:Fast Orally Dissolving Film preparation can be used for patients with problems in ingesting solid dosage forms, such as mentally ill, elderly, geriatric and patients who are reducing fluid intake or nausea.AIM:This study aimed to formulate and evaluate the rapid dissolution of amlodipine besylate.METHODS:Amlodipine besylate film was prepared by solvent casting method by using hydroxypropyl methylcellulose (HPMC) as film formers, crospovidone as superdisintegrant with Varian concentration F1 (2%), F2 (4%), F3 (6%) and F4 (8%), PEG 400 as plasticizer, sucralose and sorbitol as sweetener, citric acid as saliva stimulation, and grape essence as flavoring and coloring agent. Characteristics of films include organoleptic, weight uniformity, film thickness, surface pH, swelling, uniformity of content, time of disintegration, and dissolution.RESULTS:All formulated films produced a good film, smooth, transparent and uniform physical properties. F2 with polymer HPMC and the 4% concentration of crospovidone was the best formula with 31.50 seconds of disintegration time, the index expanding at the 15 second by 242.29% and the cumulative percent of the drug at 80 seconds by 98.08%.CONCLUSION:Amlodipine besylate can be formulated into fast orally dissolving film preparations using HPMC and crospovidone polymers so that they may be considered for use in the treatment of hypertension for patients with drug-induced problems in tablet or capsule form.

Partial depolymerization of hydroxypropylmethyl cellulose for production of low molar mass polymer chains

Low molar mass (LMM) biopolymers are highly required to design functional nanomaterials, which mainly find application in biomedical fields. However, the synthesis of LMM polymer is a challenging task. In this work, we report a partial enzymatic depolymerization process which allows to produce a series of LMM hydroxypropylmethyl cellulose (HPMC) polymer, with a weight average molar mass (Mw) under and over 10,000 g mol−1 and low dispersity (Ɖ < 1.5). Variation of the starting HPMC grade, reaction time, and enzyme concentration were the key parameters to control the Mw and yield of the target molecules. This approach provides a versatile way of producing LMM HPMCs with varying degrees of substitution, and having a single reactive aldehyde function at one chain extremity. LMM HPMC can find for instance application as building blocks for the development of new functional molecular architectures.

DEVELOPMENT AND EVALUATION OF FLOATING TABLET OF METOPROLOL SUCCINATE FOR INCREASED BIOAVAILABILITY VIA IN VIVO STUDY

Objective: This study was performed to formulate a floating tablet using hydrophobic glyceryl behenate (GB) and hydrophilic hydroxypropyl methylcellulose polymers, optimization of the same for retention in stomach and sustained drug delivery over a period of 20 h from upper gastrointestinal tract so as to increase its oral bioavailability.&#x0D; Methods: Granules of GB with the metoprolol succinate (MS) was formulated and compressed with the other ingredients to formulate a floating tablet. Physiochemical parameters of an optimized formulation along with its in vitro buoyancy study, dissolution study, in vivo studies in rabbit, and stability studies were performed.&#x0D; Results: Differential scanning calorimetry data show no interaction between polymers and the drug MS. A 32 factorial design was applied for optimization purpose, and from ANOVA and surface response plot the best formulation (F3) was obtained. In vitro dissolution study shows sustained drug release for 20 h for all the formulations and in vivo studies using rabbit model show increased bioavailability of an optimized formulation F3 as compared to the marketed sustained release formulation of MS (25 mg). Stability study shows no comparable differences in physical parameters and the drug release of initial formulation and the one which is kept for accelerated stability testing.&#x0D; Conclusion: Hence, we can conclude that a floating tablet containing a combination of hydrophilic and hydrophobic polymers can be used for gastric retention for more than 20 h which will increase the oral bioavailability of MS.