PVP K30 Research Articles

Development and Characterization of Gel-Based Buccoadhesive Bilayer Formulation of Nifedipine.

A promising controlled drug delivery system has been developed based on polymeric buccoadhesive bilayered formulation that uses a drug-free backing layer and a polymeric hydrophilic gel buccoadhesive core layer containing nifedipine. The DSC thermogravimetric analysis confirms the drug's entrapment in the gel layer and reveals no evidence of a potential interaction. Various ratios of bioadhesive polymers, including HPMC K100, PVP K30, SCMC, and CP 934, were combined with EC as an impermeable backing layer to ensure unidirectional drug release towards the buccal mucosa. The polymeric compositions of hydrophilic gel-natured HPMC, SCMC, and CP formed a matrix layer by surrounding the core nifedipine during compression. Preformulation studies were performed for all of the ingredients in order to evaluate their physical and flow characteristics. Ex vivo buccoadhesive strength, surface pH, swelling index, in vitro and in vivo drug release, and ex vivo permeation investigations were performed to evaluate the produced gel-based system. Rapid temperature variations had no appreciable impact on the substance's physical properties, pharmacological content, or buccoadhesive strength during stability testing using actual human saliva. It was clear from a histological examination of the ex vivo mucosa that the developed system did not cause any irritation or inflammation at the site of administration. The formulation NT5 was the best one, with a correlation coefficient of 0.9966. The in vitro and in vivo drug release profiles were well correlated, and they mimic the in vitro drug release pattern via the biological membrane. Thus, the developed gel-based formulation was found to be novel, stable, and useful for the targeted delivery of nifedipine.

Development of Fluoride-Loaded Chitosan Microparticles for Controlled Drug Delivery: A Comparative Study of PVP K17 and Eudragit® RS 30D as Coating Polymer

Development of Fluoride-Loaded Chitosan Microparticles for Controlled Drug Delivery: A Comparative Study of PVP K17 and Eudragit® RS 30D as Coating Polymer

Physiological adaptation in flagellar architecture improves Vibrio alginolyticus chemotaxis in complex environments

Bacteria navigate natural habitats with a wide range of mechanical properties, from the ocean to the digestive tract and soil, by rotating helical flagella like propellers. Species differ in the number, position, and shape of their flagella, but the adaptive value of these flagellar architectures is unclear. Many species traverse multiple types of environments, such as pathogens inside and outside a host. We investigate the hypothesis that flagellar architectures mediate environment-specific benefits in the marine pathogen Vibrio alginolyticus which exhibits physiological adaptation to the mechanical environment. In addition to its single polar flagellum, the bacterium produces lateral flagella in environments that differ mechanically from water. These are known to facilitate surface motility and attachment. We use high-throughput 3D bacterial tracking to quantify chemotactic performance of both flagellar architectures in three archetypes of mechanical environments relevant to the bacterium's native habitats: water, polymer solutions, and hydrogels. We reveal that lateral flagella impede chemotaxis in water by lowering the swimming speed but improve chemotaxis in both types of complex environments. Statistical trajectory analysis reveals two distinct underlying behavioral mechanisms: In viscous solutions of the polymer PVP K90, lateral flagella increase the swimming speed. In agar hydrogels, lateral flagella improve overall chemotactic performance, despite lowering the swimming speed, by preventing trapping in pores. Our findings show that lateral flagella are multipurpose tools with a wide range of applications beyond surfaces. They implicate flagellar architecture as a mediator of environment-specific benefits and point to a rich space of bacterial navigation behaviors in complex environments.

Cedrol-loaded dissolvable microneedles based on flexible backing for promoting hair growth

ABSTRACT Objectives The dissolvable microneedles loaded with cedrol based on flexible backing were developed to deliver cedrol directly and continuously to the dermis, where the drug concentration in the hair follicle can be increased locally. Methods The tip-layer matrix solution was prepared by mixing cedrol and polyvinylpyrrolidone K25 (PVP K25), and the pedestal matrix solution was prepared with aqueous hyaluronic acid. The cedrol-loaded dissolvable microneedles (cedrol-DMNs) were prepared under vacuum conditions. The mechanical properties, pig skin penetration efficiency, in vitro cutaneous permeation test, and the amount of drug in the skin and receptor chamber were evaluated. Pharmacodynamical studies were performed with C57BL/6 mice. Results The mechanical properties of cedrol-DMNs were good. In vitro cutaneous permeation tests and pharmacodynamical studies demonstrated that cedrol-DMN could efficiently deliver the drug to the deep dermis and effectively promote hair growth. Conclusions The cedrol-DMNs offer a promising strategy for treating patients suffering from hair loss.

Formulation and Development of Solid Dispersion System for Enhancement of Solubility and Dissolution Rate of Lovastatin

The solubility and dissolution rate of Lovastatin, a drug used for the treatment of hyperlipidaemia. Lovastatin is a selective competitive inhibitor of HMG Co-A reductase. However, its absolute bioavailability is 5%. To increase the solubility of drug solid dispersion was prepared. Solid dispersion prepared with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. The present investigations showed that solubility of Lovastatin Sodium was markedly increased by its solid dispersion using PVP K30 as carrier. The formulation SDF8 containing (1:8) shows highest dissolution rate. Hence the solid dispersion a way is useful technique in providing fastest onset of action of Lovastatin Sodium as well as enhanced dissolution rate. The study also shows that dissolution rate of Lovastatin can be enhanced to considerable extent by solid dispersion technique with Polymer.

Design and Formulation for Enhancement of Solubility and Dissolution Rate of Atorvastatin using Solid Dispersion

The solubility and dissolution rate of Atorvastatin, a drug used for the treatment of hyperlipidaemia. Atorvastatin is a selective competitive inhibitor of HMG Co-A reductase. However its absolute bioavailability is 5%. To increase the solubility of drug solid dispersion was prepared. Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. Solid dispersion prepared with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. The present investigations showed that solubility of Atorvastatin Sodium was markedly increased by its solid dispersion using PVP K30 as carrier. The formulation SDF8 containing (1:8) shows highest dissolution rate. Hence the solid dispersion a way is useful technique in providing fastest onset of action of Atorvastatin Sodium as well as enhanced dissolution rate. The study also shows that dissolution rate of pravastatin can be enhanced to considerable extent by solid dispersion technique with Polymer.

Injectable systems of chitosan in situ forming composite gel incorporating linezolid-loaded biodegradable nanoparticles for long-term treatment of bone infections

The objective of the current study was to create an efficient, minimally invasive combined system comprising in situ forming hydrogel loaded with both spray-dried polymeric nanoparticles encapsulating linezolid and nanohydroxyapatite for local injection to bones or their close vicinity. The developed system was designed for a dual function namely releasing the drug in a sustained manner for long-term treatment of bone infections and supporting bone proliferation and new tissues generation. To achieve these objectives, two release sustainment systems for linezolid were optimized namely a composite in situ forming chitosan hydrogel and spray-dried PLGA/PLA solid nanoparticles. The composite, in situ forming hydrogel of chitosan was prepared using two different gelling agents namely glycerophosphate (GP) and sodium bicarbonate (NaHCO3) at 3 different concentrations each. The spray-dried linezolid-loaded PLGA/PLA nanoparticles were developed using a water-soluble carrier (PVP K30) and a lipid soluble one (cetyl alcohol) along with 3 types of dl-lactide and/or dl-lactide-co-glycolide copolymer using nano-spray-drying technique. Finally, the optimized spray-dried linezolid nanoparticles were incorporated into the optimized composite hydrogel containing nanohydroxy apatite (nHA). The combined hydrogel/nanoparticle systems displayed reasonable injectability with excellent gelation time at 37 °C. The optimum formulae sustained the release of linezolid for 7–10 days, which reveals its ability to reduce the frequency of injection during the course of treatment of bones infections and increase the patients’ compliance. They succeeded to alleviate the bone infections and the associated clinical, biochemical, radiological, and histopathological changes within 2–4 weeks of injection. As to the state of art in this study and to the best of our knowledge, no such complete and systematic study on this type of combined in situ forming hydrogel loaded with spray-dried nanoparticles of linezolid is available yet in literatures.Graphical

Development of canagliflozin nanocrystals sublingual tablets in the presence of sodium caprate permeability enhancer: formulation optimization, characterization, in-vitro, in silico, and in-vivo study

Canagliflozin (CFZ) is a sodium-glucose cotransporter-2 inhibitor (SGLT2) that lowers albuminuria in type-2 diabetic patients, cardiovascular, kidney, and liver disease. CFZ is classified as class IV in the Biopharmaceutical Classification System (BCS) and is characterized by low permeability, solubility, and bioavailability, most likely attributed to hepatic first-pass metabolism. Nanocrystal-based sublingual formulations were developed in the presence of sodium caprate, as a wetting agent, and as a permeability enhancer. This formulation is suitable for children and adults and could enhance solubility, permeability, and avoid enterohepatic circulation due to absorption through the sublingual mucosa. In the present study, formulations containing various surfactants (P237, P338, PVA, and PVP K30) were prepared by the Sono-homo-assisted precipitation ion technique. The optimized formula prepared with PVP-K30 showed the smallest particle size (157 ± 0.32 nm), Zeta-potential (−18 ± 0.01), and morphology by TEM analysis. The optimized formula was subsequently formulated into a sublingual tablet containing Pharma burst-V® with a shorter disintegration time (51s) for the in-vivo study. The selected sublingual tablet improved histological and biochemical markers (blood glucose, liver, and kidney function), AMP-activated protein kinase (AMPK), and protein kinase B (AKT) pathway compared to the market formula, increased CFZ’s antidiabetic potency in diabetic rabbits, boosted bioavailability by five-fold, and produced faster onset of action. These findings suggest successful treatment of diabetes with CFZ nanocrystal-sublingual tablets.

Formulation and Characterization of Olmesartan medoxomil as a Nanoparticle

Aim: The main object of this research work was the development and evaluation of olmesartan medoxomil nanoparticle for the solubility and bioavailability improvement. It is practically insoluble in water (class II, according to BCS). This work aims to improve the olmesartan medoxomil solubility as well as dissolution rate. Materials and methods: For the synthesis solvent evaporation technique was used, and many different types of stabilizers that used (PVP K30, poloxamer 188, HPMC E5, Soluplus, tween 80) in different ratio. Results: The particle size analysis indicated that the optimized formula 7 had a reduced nanoparticulate size of 86.38 nm, with more than 90 percent increase in in-vitro dissolution profile compared to 17 percent for the comparison olmesartan medoxomil powder in phosphate buffer PH 6.8. Conclusion: nanoparticle formulation of weakly water soluble olmesartan medoxomil greatly improved the drug's dissolving rate and increased its solubility.

Nano-suspension loaded mucoadhesive mouth dissolving film of meclizine hydrochloride

Meclizine Hydrochloride belongs to class H1 antagonist, antiemetic and anti-vertigo in nature, it is a Biopharmaceutical classification system (BCS) class II drug and is practically insoluble in water. The bottom-up approach was used in the formulation of nanosuspension in which methanol and millipore water was used as solvent and anti-solvent respectively, the stabilizers used for preparation were Polyvinylpyrrolidone K30 (PVP K30) and Hydroxypropyl Methylcellulose E15 (HPMC E15) which were found to be compatible with the formulation after Fourier Transform Infrared (FTIR) and Differential scanning calorimeter (DSC) studies. Mouth dissolving films were formulated by solvent casting method using glycerine lubricated petri dish and were kept for heating in a hot air oven at 45°C overnight. Characterization of nanosuspension-loaded mucoadhesive mouth dissolving films was done by evaluating various characteristics, the highest drug content was found to be 92.43±0.49% in Mouth dissolving film (MDF) 2. In-vitro drug release studies indicate that nanosuspension-loaded mucoadhesive mouth-dissolving film has a rapid drug release rate as compared to plain drug-loaded mouth-dissolving films and marketed tablet formulation.

Preparation of Loratadine Orally Disintegrating Tablets by Semi-solid Extrusion 3D Printing.

The orally disintegrating tablets (ODTs) are especially suitable for elders and children with dysphagia, who need to be given customized dosages. This study aimed to prepare orally disintegrating tablets (ODTs) which can be customized as drug content by using semi-solid 3D printing pressure extrusion technology, with water insoluble and thermally unstable drug loratadine. The influence of binder concentration, disintegrating agent dosage and ratio mannitol: cellulose on formability and disintegration time was investigated. The properties of orally disintegrating tablets were investigated by ATR-FTIR, XRPD, DSC and SEM. The correlation formula between tablet bottom area and drug content was established. The formulation was optimized, and contained loratadine 3 g, cellulose 4 g, mannitol 2 g, carboxy methyl starch sodium 1g, 6% PVP K30 16 ml. The disintegration time was less than 60 s with infilling percentage of 60%, and the disintegration time was less than 30 s with infilling percentage of 40%. There was no detectable interaction between loratadine and the selected excipients by the analysis of ATR-FTIR, DSC and XRPD. The structure of the tablets was porous, and the drug was dissolved completely within 10 min. The drug content (x) of the tablet and the bottom area (y) of the tablet showed a linear fitting relationship, y = 3.8603x - 0.7176, r2 = 0.9993. Semi-solid extrusion of 3D printing technology was applied to prepare loratadine orally disintegrating tablets with customized drug content, which provides an alternative method for the research of customized preparation.

Formulation and Pharmaceutical Quality Evaluation of Tablets Containing Extract of Cinnamomum burmannii BARK and Colocasia esculenta (L) Schott Leaves

Cinnamon bark (Cinnamomum burmannii) is used traditionally and has an ingredient containing cinnamic acid compounds. Colocasia esculenta (L) Schott leaves contains of flavonoids, alkaloids, tannins, saponins, steroids, and terpenoids. Both of the plants C. esculenta and C. burmannii plants have the potential as anti-diabetics because they can lower blood glucose levels. This study aims to make combination tablets of C. burmannii bark and C. esculenta leaves extract with various concentrations of PVP K30 binder. This research made four formulas with the concentration of PVP K30, namely F1 (2%), F2 (3%), F3 (4%), and F4 (5%). Tablet preparations were prepared by the wet granulation method. Tablet analysis used flavonoids quercetin and cinnamic acid as markers. The results showed that the tablets were flat, round in shape, light green, had a slightly bitter taste, and had a distinctive aromatic odor. The differences in the concentration of PVP K30 binder 2-5% could affect the hardness, friability, disintegration time, and tablet dissolution (p<0.05). The tablet's hardness was 3.65-5.01 KP; friability was 0.705%, disintegration time was <15 minutes, and dissolution was 84.61% in 40 minutes. The levels of the flavonoid quercetin in the tablets were 4.21% and 8.03% cinnamic acid. A tablet combination of C. burmannii bark and C. esculenta leaves extract with a PVP K30 concentration of 5% (F4) has the best quality.

Polymorphs of a 1:1 salt of sulfadiazine and piperazine–relative stability, dissolution studies, pharmacokinetics and anti-meningitis efficiency

Two new salt forms of sulfadiazine (SDZ) and piperazine (PIP) were synthesized and characterized. Out of the two polymorphs (SDZ-PIP Ⅰ and SDZ-PIP II), SDZ-PIP Ⅱ is the more stable form at low temperature, room temperature and high temperature. The solution-mediated phase transformation result shows that SDZ-PIP II can transform into pure SDZ within 15 s in phosphate buffer at 37 °C, which leads to a loss in solubility advantage. The addition of 2 mg/mL PVP K30, a polymeric crystallization inhibitor, maintains the solubility advantage and permits supersaturation for a longer period of time. SDZ-PIP II showed 2.5 times the solubility of SDZ alone. The area under the curve (AUC) of SDZ-PIP II with 2 mg/mL PVP K30 was approximately 165% of that of SDZ alone. Moreover, SDZ-PIP II with PVP K30 was more effective than SDZ alone in treating meningitis. Therefore, the SDZ-PIP II salt improves the solubility, bioavailability, and anti-meningitis activity of SDZ.

Preparation, Characterization and Optimization of Sustained Release Matrix Tablets of Repaglinide using Box–Behnken Design

The aim of this investigation was to develop and optimize the Sustained release Matrix formulations of Repaglinide (RLD) using response surface methodology by employing a 3-factor, 3-level Box–Behnken statistical design. The independent variables studied were the amount of hydroxypropyl methylcellulose (HPMC K4M), Ethyl cellulose (EC) and PVP K30. The Swelling index (Y1), drug release at 8 hr and 12hr were the target responses. The response surface methodology and multiple response optimizations utilizing a polynomial equation were used to search for the optimal formulation with a specific release rate at different time intervals. The results showed that the effect of combination of HPMC K4M and EC was the most influencing factor on the drug release from ER matrix tablets. The mechanism of drug release from RLD Matrix tablets was dependent on the added amount of EC. Validation of the optimization technique demonstrated the reliability of the model. The optimized formulation containing 50mg of HPMC K4, 35mg of EC, and 30mg of PVP K30 was prepared according to the software determined levels. DSC and FTIR studies combined with the stability study of the optimized formulation proved the integrity of the developed formulation. The Box–Behnken experimental design facilitated the formulation and optimization of extended release hydrophilic matrix systems of RLD in a short period of time and with the fewest number of experiments. The optimized Matrix tablet of Repaglinide showed good pharmacokinetic result over conventional formulation.

Formulation for Enhancement of Solubility and Dissolution Rate of Simvastatin using Solid Dispersion

Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. The solubility and dissolution rate of Simvastatin, a drug used for the treatment of hyperlipidaemia. Simvastatin is a selective competitive inhibitor of HMG Co-A reductase. However its absolute bioavailability is 5%. To increase the solubility of drug solid dispersion was prepared. Solid dispersion prepared with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. The present investigations showed that solubility of Simvastatin Sodium was markedly increased by its solid dispersion using PVP K30 as carrier. The formulation SDF8 containing (1:8) shows highest dissolution rate. Hence the solid dispersion a way is useful technique in providing fastest onset of action of Simvastatin Sodium as well as enhanced dissolution rate. The study also shows that dissolution rate of Simvastatin can be enhanced to considerable extent by solid dispersion technique with Polymer.

Bulk Flow Optimisation of Amorphous Solid Dispersion Excipient Powders through Surface Modification.

Particulate amorphous solid dispersions (ASDs) have been recognised for their potential to enhance the performance of various solid dose forms, especially oral bioavailability and macromolecule stability. However, the inherent nature of spray-dried ASDs leads to their surface cohesion/adhesion, including hygroscopicity, which hinders their bulk flow and affects their utility and viability in terms of powder production, processing, and function. This study explores the effectiveness of L-leucine (L-leu) coprocessing in modifying the particle surface of ASD-forming materials. Various contrasting prototype coprocessed ASD excipients from both the food and pharmaceutical industries were examined for their effective coformulation with L-leu. The model/prototype materials included maltodextrin, polyvinylpyrrolidone (PVP K10 and K90), trehalose, gum arabic, and hydroxypropyl methylcellulose (HPMC E5LV and K100M). The spray-drying conditions were set such that the particle size difference was minimised, so that it did not play a substantial role in influencing powder cohesion. Scanning electron microscopy was used to evaluate the morphology of each formulation. A combination of previously reported morphological progression typical of L-leu surface modification and previously unreported physical characteristics was observed. The bulk characteristics of these powders were assessed using a powder rheometer to evaluate their flowability under confined and unconfined stresses, flow rate sensitivities, and compactability. The data showed a general improvement in maltodextrin, PVP K10, trehalose and gum arabic flowability measures as L-leu concentrations increased. In contrast, PVP K90 and HPMC formulations experienced unique challenges that provided insight into the mechanistic behaviour of L-leu. Therefore, this study recommends further investigations into the interplay between L-leu and the physico-chemical properties of coformulated excipients in future amorphous powder design. This also revealed the need to enhance bulk characterisation tools to unpack the multifactorial impact of L-leu surface modification.

A proof-of-concept study of coupled supercritical CO2-assisted processes to produce solid self-assembled drug delivery systems (S-SADDS)

The development of innovative drug delivery systems is currently under intense consideration to overcome bioavailability issues of poorly water-soluble drugs. Among the many existing delivery systems, self-assembled drug delivery systems (SADDS) are of great interest. Solid Lipid Nanoparticles (SLN), which are part of SADDS, have been widely studied in the pharmaceutical field since they are biodegradables and biocompatibles. However, stability of SLN suspension over time is limited and quick drug released were frequently observed. The development of solid SADDS (S- SADDS), to produce an on-demand delivery system, through a one-step production process has been designed to overcome these issues. The coupling of both Supercritical Carbon Dioxide (scCO2) assisted RESS and SAS processes (RESS/SAS) have been proposed as a proof-of-concept. This study was carried out in three steps: (i) the development and adjustment of operating conditions to produce SLN suspension using solvent injection process, (ii) the optimization of the formulation to produce SLN with a mean particle size diameter close to 100 nm and stable at least 24 h, (iii) the transposition of the SLN formulation composition into the RESS/SAS coupled process for the production of S-SADDS. SLN composed of stearic acid, PVP K30, phosphatidylcholine and nifedipine, with an average size under 100 nm and a zeta potential about −35 mV were obtained from the preliminary study. These results allowed the transposition of the optimal formulation into RESS/SAS crystallization process. The developed RESS/SAS scCO2-assisted processes demonstrate the simultaneous crystallization of a self-assembled formulation in a one step process. A control of operating conditions was also demonstrated through the generation of S- SADDS containing desired amount of nifedipine. The proof-of-concept process studied, seems to be very promising tool for the generation of complex solids, intermediate products or for the development of innovative drug delivery systems.

Mechanistic Insight of Polymer Effects on the Kinetic of Solution-Mediated Phase Transformation of Nitrofurantoin Anhydrate to Monohydrate.

Nitrofurantoin is an effective antibacterial drug for the treatment of lower urinary tract infection. However, the anhydrate form can easily transform to the less soluble hydrate form (monohydrate) during dissolution, resulting in a reduction of dissolution rate and oral bioavailability. Therefore, inhibition of phase transformation is vital to stabilize the quality of drugs. In this work, the potential of polyethylene glycol (PEG 8000), polyvinyl pyrrolidone (PVP K30), poloxamer 188 and hydroxypropyl methylcellulose (HPMC) to inhibit the hydration of nitrofurantoin during dissolution was investigated by experimental and simulation approaches. The rates of phase transformation were decreased in the presence of PEG 8000 and poloxamer 188, and PVP K30 and HPMC completely inhibited the phase transformation of anhydrate. The abundant hydrogen bond donor and acceptor groups of PVP and HPMC may easily establish intermolecular interactions with nitrofurantoin molecules, accounting for stronger inhibition of nucleation. Besides, the molecular dynamic simulation further indicated the formation of more extensive interactions between PVP K30 (or HPMC) and the (111) face of monohydrate, suggesting that the strong absorption of polymers on the surface and thus block the sites for incorporation of new growth. This study provides a mechanistic insight into the inhibition of nitrofurantoin hydration by polymeric additives, which helps design formulations and improve the physical stability of anhydrate.

Development and in Vitro/In Vivo Evaluation of Itopride Hydrochloride Expanding Tablets

PurposeGastroretentive drug delivery systems (GRDDS) have attracted interest for enhancement of absorption and bioavailability of some drugs. Itopride hydrochloride (ITOP) is a drug used for treatment of gastroesophageal reflux and other gastric motility disorders, but is characterized by narrow absorption window and short in vivo half-life. Therefore, it is expected that its formulation in expanding gastroretentive tablets would increase its gastric residence, thus leading to decreased frequency of administration and increased patient compliance.MethodsThe direct compression method was used for formulation of tablets. Four different hydrophilic polymers (xanthan gum, sodium alginate, gellan gum, pectin) were screened separately with Avicel 102 and PVP k30 as excipients. The effect of different factors (polymer type and amount, and excipient amount) on the tablet properties such as hardness, friability, thickness, diameter, weight variation, swelling, and in vitro drug dissolution was studied. In addition, swelling test, accelerated stability test, and in vivo study were performed on the optimized formulation.ResultsTablets prepared using xanthan gum exhibited favorable properties compared to tablets prepared using the other gums, however increasing the polymer amount led to increased tablet friability. The selected formulation exhibited obvious expansion reaching 17.45 mm and lasting for 24 h, coupled with a sustained release behavior. X-ray scans in human volunteers suggested the residence of the tablet in the stomach for a period of 6 h in fed state.ConclusionSuccessful preparation of directly compressible ITOP expanding tablets was achieved in this study, which is expected to result in better therapeutic outcome in gastroesophageal reflux.

IMPROVEMENT OF DISSOLUTION RATE OF REPAGLINIDE BY UTILIZING SOLID DISPERSION TECHNIQUE

The recent study's objective was to prepare and evaluate the Repaglinide (RG) solid dispersion. RG is poorly water soluble, BCS class II drug. Repaglinide solid dispersion (RG-SD) was prepared by solvent evaporation method using different proportion of PVP K30. The prepared RG-SD was evaluated for solubility studies, drug content, in vitro dissolution, DSC studies and XRD studies. DSC and XRD studies results indicate that RG exists in amorphous form in solid dispersion. The solubility of pure RG was enhanced from 34.41±0.68 to 370.3±1.52 μg/mL in distilled water at 370 C. RG-SD (RG:PVP K30) (1:10) showed high burst release (65%) in the first 30 min. Current research concludes that Repaglinide solid dispersions using PVP-K30 (1:10) as a carrier in solid dispersions showed promising results in enhancement of repaglinide properties. KEYWORDS: Repaglinide, Solid Dispersion, PVK K30, Dissolution Rate, Solvent evaporation