Excipient Compatibility Studies Research Articles

Colon Targeted Protein Nanoparticles Loaded Suppositories : Effective against Intestinal Parasites.

Purpose: The aim of the present investigation was to formulate protein nanoparticles (PNPs) loaded suppositories for colon targeting of metronidazole (MZ), to achieve sustain release effect. Methods: PNPs were formulated via desolvation technique by utilizing 23 factorial design which results into eight formulations. The synthesized PNPs were characterized for different physicochemical and in vitro parameters viz. particle size, surface morphology, entrapment efficiency and zeta potential, drug- excipients compatibility studies.Results: The formulated PNPs were found to be spherical in shape and have an average size in the range of 300.7 nm to 504.8 nm. Based on the results obtained, F7 was found to be the optimized formulation that was loaded into the suppository base. Furthermore, suppositories were also characterized for several parameters like content uniformity, weight variation and liquefaction time.Conclusion: Resultant, suppositories were free from pits, fissures and cracks. The in-vitro release data of MZ-PNPs loaded suppositories were compared with the suppositories loaded with active ingredient only i.e. MZ. Screening against Pheretima posthuma was also conducted. The results of in vitro drug release testing proved that protein nanoparticle loaded suppositories is a better approach, compared to pure MZ loaded suppositories. Release kinetic study concluded that the formulation follows Higuchi’s equation i.e. having a biphasic release pattern. The efficiency of the formulated dosage form was evaluated using Indian earthworms, P. posthuma.

FORMULATION AND EVALUATION OF MUCOADHESIVE BUCCAL TABLETS OF CARVEDILOL

Objective: The aim of the study was to formulate and evaluate mucoadhesive buccal tablets of carvedilol to avoid the first-pass metabolism.
 Methods: Mucoadhesive Buccal tablets of carvedilol were prepared by direct compression techniques using a combination of bioadhesive polymers such as hydroxypropyl cellulose (HPC) and polyethlyelne oxide WSR-1105 (PEO WSR-1105). In order to improve solubility of carvedilol, solid dispersion was prepared using poloxamer 188. A 32 Full factorial design was applied to investigate the combined effect of the two independent variables i.e. concentration of HPC (X1) and concentration of PEO WSR-1105(X2) on the dependent variables, % in vitro drug release at 1 h (Y1), % in vitro drug release at 4 h (Y2), mucoadhesive strength (Y3) and mucoadhesion time (Y4).
 Results: Optimized mucoadhesive buccal tablets shows in vitro drug release of 96.23±2.45 in 8 h, mucoadhesive strength of 18.20±1.44 g, mucoadhesion time 420±2.6 min and surface pH 6.75±0.015. Drug excipients compatibility study by FTIR showed no interaction between drug and excipients.
 Conclusion: From all parameters and experimental design evaluation, it was concluded that the drug release rate decreased with an increase the concentration of HPC and PEO WSR-1105 and mucoadhesion property increased with increase the concentration of PEO WSR-1105. The in vitro release kinetics revealed the Korsmeyer-Peppas model is followed and drug release is by anomalous diffusion.

Development and Characterization of Sildenafil Citrate Oral Thin Films

The current work aimed to develop sildenafil citrate (SC) oral thin films. SC oral thin films (OTF) were prepared by solvent casting method. The ingredients include hydroxypropyl methylcellulose (HPMC), E4 (as film former), glycerol (as lubricating agent), polyethylene glycol 600 (as plasticizer), rose oil (as flavoring agent), and de-ionized water (as solvent). The SC-OTFs were successfully prepared by the solvent casting method. The drug excipient compatibility studies showed the absence of drug excipient interactions in fourier transform infrared spectroscopy (FTIR) spectra. All the prepared formulations (F1 to F6) were evaluated for several physicochemical parameters like morphology (i.e., size, shape, color), thickness, uniformity (i.e., content and weight), surface pH measurement, in vitro disintegration time, in vivo studies (i.e., taste), tensile strength, folding endurance and in vitro drug release and all were found within pharmacopoeial limits. In vitro, drug release studies (F1 to F6) in simulated salivary fluid (6.8 pH phosphate buffer) showed that 98 ± 1.26% drug was released from F4 in 60 sec. The OTF is a promising formulation for SC that results in high solubility, rapid onset of action, and enhanced systemic bioavailability (BA).

Solid-state compatibility studies of Ketoconazole-Fumaric acid co-crystal with tablet excipients

This work presents a detailed excipient compatibility study of the Ketoconazole-Fumaric acid (KET-FUM) co-crystal, which might be a good alternative to Ketoconazole in the oral treatment of antifungal infections, due to its substantially higher aqueous solubility. Physical mixtures of the co-crystal with hydroxypropyl-methyl cellulose K4M (HPMC), corn starch (CSt), silicon dioxide (SiO2), lactose monohydrate (Lact), talc, polyvinyl-pyrrolidone K90 (PVP) and magnesium stearate (MgSt) were prepared in a 1:1 (w:w) ratio and analyzed by thermal analysis (DSC/TG), powder X-ray diffraction, Fourier transform infrared spectroscopy (FT-IR) and Karl Fischer titration. Compatibility assessment was systematically evaluated using the above complementary techniques on the mixtures after preparation as well as after two storage conditions (12 months at ambient conditions and 3 months at elevated temperature and relative humidity (40 °C/75% RH). The solid-state compatibility of the co-crystal was confirmed with HPMC, Lact, CSt, SiO2, while in the case of MgSt and PVP possible interactions were identified. The co-crystal interaction with MgSt is heating induced, as evidenced by DSC alone. In the case of PVP, both DSC and FT-IR indicated possible hydrogen-bonding in the amorphous phase. The solid-state compatibility results evidence the potential of the KET-FUM co-crystal to be developed as an oral drug. Moreover, our study reinforces the applicability of the binary mixture approach designed for APIs and salt-based formulations to be used in the case of co-crystals, in order to assess their pharmaceutical developability.

Formulation and Development of Enteric Coated Tablet for Parkinson's Disease

The current investigation is to formulate and develop enteric coated tablet of Ropinirole Hydrochloride. Enteric coated tablets were prepared by Wet Granulation method by using water as solvent. To protect drug from acid Eudragit L-100 was used as enteric coated polymer. Drug, Excipient and Polymer compatibility studies were performed by FTIR and DSC. The formulation was optimized with desirable Hardness, Friability and Disintegration time. Tablet exhibited Hardness between 5.1-5.8 Kg/Cm2, Friability 0.09-0.21 %, Disintegration time 40-60 minutes and drug release between 78-95.56 %. Optimized formula F4 showing the Friability 0.13 %, Hardness 5.5 Kg/Cm2 and drug release 95.56 %. Drug diffusion study was represented graphically.

OPTIMIZATION OF ROLL COMPACTOR VARIABLES AND FORMULATION OF ANTI-RETROVIRAL TABLET BY ROLL COMPACTION METHOD

Objective: This study emphasis on roll compaction variable and how the processing parameters influence the formation of granules in process of formulations of antiretroviral IR Tablet with help of optimization technique.
 Methods: In this present work we aimed to develop a stable pharmaceutical dosage form with anti-retroviral drug tenofovir disoproxil fumarate. % retention of granules over # 60 mesh in roll compaction method by sizing with 50G co-mill screen was assessed by optimization and results were evaluated by Design expert 12.0 software. Various parameters and optimization of the parameter for formulation for better product was done by using 23 factorial design and dry granulation technique for manufacturing tablets. Three operating parameters the roller speed, the hydraulic pressure and the gap width on the Chamunda CPMRC-200/150 Roll Compactor were varied. The planned response variable for study was % retention over #60 ASTM mesh. % retention of granules was calculated by weighing granules on digital electronic balance with respect to how much premix material was taken for compaction.
 Results: Excipients compatibility study gave positive way showing no change in physical appearance of drug-excipients mix. It reviled that drug was compatible with excipients used.
 By formation of granules with required ratio, the value of Compressibility index changed from 29 to 21.89, showed that flow properties were improved i.e. from poor to passable.
 Design expert 12.0 gave optimized solution for formation of required quantity of granules. Pareto chart showed envaulted positive and negative impact of factors on response as explained in results.
 The results clearly indicate that how granules manufacturing in roll compaction process are influenced by roller pressure, roller gap and speed. 70 % flakes formation and granules retention were observed with 4000 kg/cm2 pressure, 1 mm roller gap width and 6 rpm speed of roller.
 Pareto chart clearly indicate major impact is of roller pressure. Comparative dissolution profile graph showed that drug release pattern is similar with the innovator tablet.
 A stable, robust tablets were formed at the end of process.
 Conclusion: In this study, by optimizing processing variables stable antiretroviral immediate release oral solid dosage form was formed.

Ketoconazole: compatibility with pharmaceutical excipients using DSC and TG techniques

Ketoconazole (KTZ) is an antifungal agent responsible for the inhibition of 14-α-demethylase sterol. The drug–excipient compatibility studies play an important role in pharmaceutical formulations development. Interactions between drug and excipients may affect the chemical nature, stability, bioavailability and consequently the therapeutic efficacy and safety profile. The main goal of this work was to evaluate the compatibility of KTZ with some excipients: corn starch, microcrystalline cellulose, colloidal silicon dioxide, lactose monohydrate and povidone, using differential scanning calorimetry and thermogravimetry (TG). Binary mixtures in a mass ratio of 1:1 between drug and excipient were used to make the study feasible. The comparison was performed using Tonset of the melt from pure drug and its enthalpy value (ΔHf) with respective values obtained for each binary mixture. Experimental and simulated TG/DTG curves were compared using the Pearson’s correlation coefficients to assess possible incompatibilities due to thermal decomposition of organic matter and/or gaseous products released. Thus, the excipients corn starch and colloidal silicon dioxide have been shown to be incompatible with KTZ.

Gastric Ulcer Prevention by Lansoprazole

The objective of the current investigation is to formulate ethyl cellulose and hydroxypropyle methyle cellulose based sustained release microspheres, containing lansoprazole as model drugs. lansoprazole is type II anti-ulcer agent when administered shows synergetic effect in their action. Microspheres were prepared by W/O/O double emulsion solvent evaporation method with different stabilizer concentration and at different speeds of emulsification while maintaining constant amount of lansoprazole. Drug excipient compatibility study was performed prior to formulation development and only compatible excipients were used in the fabrication of microspheres. Prepared microsphere formulations were characterized by percentage yield, particle size analysis, entrapment efficiency, invitro release behavior, differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). SEM studies showed that the microspheres were spherical with rough surface morphology. The drug loaded microspheres showed 10.4-57.9% entrapment capacity for lansoprazole and The invitro release profile showed a slow and steady release pattern for lansoprazole. A 95-98% was releases within a period of 12 hrs . The drug release was found to be diffusion controlled mechanism. The n value of Korsmeyer Peppas equation indicated non Fickian type of diffusion.

DESIGN, OPTIMIZATION AND EVALUATION OF CETRIZINE DIHYDROCHLORIDE FAST DISSOLVING FILMS EMPLOYING STARCH TARTRATE–A NOVEL SUPERDISINTEGRANT

Objective: The aim of the current research is optimization, preparation and evaluation of starch tartrate (novel super disintegrant) and preparation of fast dissolving oral films of cetirizine dihydrochloride by employing starch tartrate.
 Methods: To check the drug excipient compatibility studies of the selected drug (Cetrizine dihydrochloride) and the prepared excipient i. e starch tartrate, different studies like FTIR (Fourier-transform infrared spectroscopy), DSC (Differential scanning calorimetry) and thin-layer chromatography (TLC) were carried out to find out whether there is any interaction between cetirizine dihydrochloride and starch tartrate. The solvent casting method was used for the preparation of fast dissolving films. The prepared films were then evaluated for thickness, folding endurance, content uniformity, tensile strength, percent elongation, in vitro disintegration time and in-vitro dissolution studies. Response surface plots and contour plots were also plotted to know the individual and combined effect of starch tartrate (A), croscarmellose sodium (B) and crospovidone (C) on disintegration time and drug dissolution efficiency in 10 min (dependent variables).
 Results: Films of all the formulations are of good quality, smooth and elegant by appearance. Drug content (100±5%), thickness (0.059 mm to 0.061 mm), the weight of films varies from 51.33 to 58.06 mg, folding endurance (52 to 67 times), tensile strength (10.25 to 12.08 N/mm2). Fast dissolving films were found to disintegrate between 34 to 69 sec. Percent dissolved in 5 min were found to be more in F1 formulation which confirms that starch tartrate was effective at 1%.
 Conclusion: From the research conducted, it was proved that starch tartrate can be used in the formulation of fast dissolving films of cetirizine dihydrochloride. The disintegration time of the films was increased with increase in concentration of super disintegrant.

FORMULATION AND EVALUATION OF IN SITU MUCOADHESIVE THERMOREVERSIBLE NASAL GEL OF SERTRALINE HYDROCHLORIDE

Objective: The objective of the study was to aiming to formulate and evaluate temperature based in situ nasal gel of sertraline HCL.
 Materials and Methods: Preformulation studies of sertraline hydrochloride including tests for identification, solubility studies, Fourier-transformer infrared (FTIR) spectroscopy, melting point determination, and other studies were carried out and compared with the specification as per literature. The solubility of sertraline hydrochloride was determined in different solvents such as in distilled water, ethanol, acetone, isopropyl alcohol, and 2-propanol. Each value for solubility was determined in triplicate and average values were reported. The drug excipient compatibility study was determined by FTIR. Thermal analysis was performed using a differential scanning calorimetric equipped with a computerized data station. The UV spectrum of sertraline hydrochloride was obtained using UV JascV630. The in situ gel formulation was prepared by changing the concentration and using only one polymer (Carbopol 934) has been used at the same concentration. Mucoadhesive strength and in vitro permeation study were determined using gout nasal mucosal membrane, whereas in vitro drug release study was carried out using diffusion cell through egg membrane as a biological membrane. The stability studies were conducted according to ICH guidelines.
 Results: The FTIR studies of formulation show no interaction between drug and excipient. In situ gel was prepared using Carbopol 934 and Poloxamer 407 to improve its adhesion property. The optimized formulation (F6) was transparent and clear in appearance with 101.15% drug content. The sol-gel transformation of in situ gel was found at temperature 34.92°C with immediate gelation property. The in vitro drug release of optimized formulation was found 95.80% drug release in 8 h. Formulations F4 and F6 showed immediate gelation within 60 s and remained stable for an extended period. All the formulations were liquid at room temperature and underwent rapid gelation on contact with simulated nasal fluid.
 Conclusion: The results concluded that the formulations of in situ nasal gel showing to improve the bioavailability through its longer residence time and ability to sustain drug release.

FORMULATION AND OPTIMIZATION OF LEVAMISOLE CHEWABLE TABLETS

Objective: The aim of the present study was to prepare and optimize levamisole chewable tablets by using various super disintegrants, namely; sodium starch glycolate, DRC Indion 204, and DRC Indion 234.
 Methods: Drug excipient compatibility study was carried out by FTIR spectroscopy to verify the compatibility of levamisole with the excipients. Nine batches of levamisole chewable tablets were prepared according to 32 factorial designs using a direct compression method by optimizing the super disintegrant concentration. The powder blend was exposed to pre-compression studies of the powder blend followed by post-compression studies of the formulated tablets.
 Results: FTIR study revealed that the excipients used in the formulations were compatible with the drug. The pre-compression and post-compression parameters were found within the IP limits. Form the dissolution studies, it was evident that the formulation prepared with DRC Indion 234 (50 mg) showed maximum percentage drug release in 45 min (97.13%) hence it is considered as optimized formulation. When compared to all other formulation, the batches with DRC Indion 234 (F7-F9) showed a better release of the drug (90 % drug release within 45 min).
 Conclusion: Nine batches of levamisole chewable tablets were successfully formulated by optimizing the concentration of super disintegrants such as sodium starch glycolate, DRC Indion 204, and DRC Indion 234. It was concluded from the dissolution studies that the DRC Indion 234 is the best super disintegrant irrespective of their concentration for the formulation of levamisole chewable tablets when compared to sodium starch Glycolate and DRC Indion 204.

DESIGN, OPTIMIZATION, AND EVALUATION OF ACYCLOVIR FAST DISSOLVING TABLETS EMPLOYING STACH PHTHALATE – A NOVEL SUPERDISINTEGRANT

Objective: The objective of the present research was to prepare starch phthalate (a novel superdisintegrant) and to optimize and formulate acyclovir fast dissolving tablets employing 23 factorial design using starch phthalate as superdisintegrant.
 Materials and Methods: Drug excipient compatibility studies such as Fourier-transform infrared spectroscopy, differential scanning calorimetry, and thin-layer chromatography were carried out to check the drug interaction between acyclovir and starch phthalate. The direct compression method was used for tablet preparation. Prepared tablets were then evaluated for hardness, friability, drug content, disintegration time, water absorption, and wetting time, in vitro dissolution studies. Response surface plots and contour plots were also plotted to know the main effects and interaction effects of independent variables (starch phthalate [A], croscarmellose sodium [B], and crospovidone [C] on dependent variables [disintegration time and drug dissolution efficiency in 1 min]) and stability studies were also done.
 Results: Tablets of all formulations were of good quality concerning drug content (100±5%), hardness (3.6–4.0 kg/cm2), and friability (<0.16%). In all formulations, formulation F8 found to be optimized formulation with least disintegration time 9±3 s, less wetting time 10±0.17 s, and enhanced dissolution rate in 1 min, i.e., 99.92±0.11 as compared to other formulation.
 Conclusion: From the research, it was concluded that on combination with crospovidone (5%) and croscarmellose sodium (5%), starch phthalate (10%) enhanced the dissolution efficiency of the drug. Hence, starch phthalate can be used as a novel disintegrant in the manufacturing of fast dissolving tablets.

DESIGN, OPTIMIZATION AND EVALUATION OF IBUPROFEN FAST DISSOLVING TABLETS EMPLOYING STARCH PHTHALATE-A NOVEL SUPERDISINTEGRANT

Objective: The objective of the present research was to prepare starch phthalate (a novel super disintegrant) and to optimize and formulate ibuprofen fast dissolving tablets employing 23factorial design using starch phthalate as super disintegrant.
 Methods: Drug excipient compatibility studies like Fourier-transform infrared spectroscopy (FTIR) and thin-layer chromatography (TLC) studies were carried out to check the drug interaction between ibuprofen and starch phthalate. Direct compression method was used for tablet preparation. Prepared tablets were then evaluated for hardness, friability, drug content, disintegration time, water absorption and wetting time, in vitro dissolution studies. Response surface plots and contour plots were also plotted to know the main effects and interaction effects of independent variables (starch phthalate (A), croscarmellose sodium (B) and crospovidone (C)) on dependent variables (disintegration time and drug dissolution efficiency in 1 minute) and stability studies were also done.
 Results: Tablets of all formulations were of good quality concerning drug content (100±5%), hardness (3-6 kg/cm2), and friability (less than 0.16%). In all formulations, formulation F5 found to be optimized formulation with least disintegration time 20±0.28 seconds, less wetting time 09±0.12 seconds and enhanced dissolution rate in one minute, i.e., 91.95±0.22 as compared to other formulation.
 Conclusion: From the research, it was concluded that on combination with crospovidone, starch phthalate enhanced the dissolution efficiency of the drug. Hence, starch phthalate can be used as a novel disintegrant in the manufacturing of fast dissolving tablets.

APPLICATION OF SYNTHETIC AND NATURAL POLYMERS IN PREPARATION AND CHARACTERIZATION OF DOMPERIDONE FAST-DISSOLVING FILMS

Objective: The present research work is mainly focused on solubility enhancement of domperidone which is a biopharmaceutical classification system Class II drug using natural and synthetic polymers.
 Methods: The solubility was enhanced by the kneading method with the drug: polymer (1:0.5, 1:0.75, and 1:1) using β-cyclodextrin. The fast dissolving films (FDFs) of domperidone were prepared by incorporating the solid dispersion (SD) SDK3 by solvent casting method using hydroxypropyl methylcellulose K15 M (HPMC) and gellan gum in various concentrations for preparing FDFs. Various pre- and post-compression parameters, drug and excipients compatibility studies were evaluated by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction analysis (XRD).
 Results: The maximum drug release of 98.86 % was achieved within 30 min for 1:1 ratio of solid dispersion using β-cyclodextrin, was optimized and taken for further development of FDFs. From the in vitro drug release studies films prepared with 10% w/w of HPMC K 15 (FH5) and 10% w/w of gellan gum (FG5) showed enhanced dissolution rate compared to other formulations. The formulation FHG with combination of polymers, namely, HPMC K 15 and gellan gum in 1:1 ratio showed drug release of 97.22% within 15 min only when compared with the optimized formulations. FTIR and DSC studies revealed that there were no interactions between drug and excipients. XRD studies revealed slight conversion of crystalline form to amorphous. The optimized formulation FHG found to be stable under accelerated stability studies.
 Conclusions: The polymers in combination are a potential candidate for use in the formulation of FDF.

FORMULATION AND COMPARATIVE EVALUATION OF ONDANSETRON HYDROCHLORIDE MOUTH DISSOLVING TABLETS IN INDIA

Objective: The aim of the present study was to prepare the ondansetron hydrochloride Mouth Dissolving Tablets (MDTs) followed by its comparison with ethical and non-ethical (generic) marketed tablets.
 Methods: Prior to the formulation, drug excipient compatibility study was carried out by FTIR spectroscopy. The λmax was determined by UV spectroscopy. The ondansetron hydrochloride MDTs were prepared by direct compression method using Sodium Starch Glycolate (SSG) as super disintegrant and camphor as a sublimating agent. Then the prepared MDTs were subjected to evaluation of post compression parameters such as thickness and diameter, weight variation, wetting time, hardness, friability, disintegration and dissolution. The results obtained were compared with that of ethical and non-ethical marketed ondansetron hydrochloride 4 mg tablets.
 Results: The λmax was found at 310 nm. FTIR study revealed that excipients used in the prepared formulations are compatible with the drug. The thickness and diameter was in the range of 2.646 to 3.27 mm and 6.0 to 8.12 mm, respectively. Friability was in the range of 0.43 to 0.88 % and had a slightly higher friability (1.27%) for sublimated tablets. Wetting time and disintegration time were in the range of 15 to 40 sec and 23 to 50 sec, respectively. The 100 % drug release was found within 180 sec for all the codes. These results were then compared with non-ethical film coated ondansetron marketed tablets.
 Conclusion: Ondansetron hydrochloride MDT 4 mg tablets prepared in the laboratory were under specified IP limits. The experimental findings demonstrated that any of these ethical and non-ethical tablets of ondansetron hydrochloride can be selected, advised by the physician or pharmacist, as per the patient’s need and economical status.

Synthesis and Characterization of Valacyclovir HCl Hybrid Solid Lipid Nanoparticles by Using Natural Oils.

The Jojoba Simmondsia Chinensis oil is used as one of the main ingredients which has an antioxidant, moisturizing and stabilizing activity. Likewise, grape seed (Vitis vinifera) oil is also used in this preparation which also has some remarkable medicinal properties such as antioxidant, astringent and is also used as a moisturizer. The Valacyclovir Solid Lipid Nanoparticles (SLN) are prepared in combination. The prime objective of the study was to prepare a nanodispersion with good stability indicating zeta potential. The formulations were prepared by varying concentrations of jojoba oil and grape seed oil which form the hybrid nanoparticles with the drug. The high-pressure hot-homogenization technique was used to prepare the nanoparticles. The prepared nanoparticles were subjected to characterization analysis such as Mean particle size, Zaverage, and Zeta potential by using Dynamic Light Scattering (DLS) and Photon Correlation Spectroscopy (PCS). The best formulation was subjected to Transmission Electron Microscopy (TEM) technique for surface morphology and other characterizations. The crystalline pattern of the drug alone, drug-loaded nanoparticles and nanoparticles without the drug was studied by XRD. The drug excipients compatibility studies were performed by using Fourier-Transform Infrared Spectroscopy (FTIR) Differential Scanning Calorimetry and (DSC). The other factors such as in vitro drug release, and % drug entrapment efficiency were studied by using suitable methods. The results demonstrated that the particles are in nano range with good stability with appreciable Zeta potential (-48.2±mV). The selected formulations were analyzed for MPS which demonstrated the value of 306.7±183.4 and 416.5±289.3. The best formulation VNP5 demonstrated the Bellshaped curve and confirmed the uniform distribution. Based on the patents, it was demonstrated that valacyclovir is widely used in the treatment and prophylaxis of viral infections in human, particularly infections caused by the herpes group of viruses. Valacyclovir is an effective drug for the treatment of cold sores.

TASTE MASKING BY HOT MELT EXTRUSION WITHOUT LOSS OF BIOAVAILABILITY FOR PEDIATRICS

Objective: The aim of present work was to develop a platform technology for the pediatric dosage form to mask the bitter taste of Furosemide (FUR) and prepare a flexible solid oral dosage form.
 Methods: Excipient compatibility study was carried out by using Fourier-transform infrared spectroscopy (FTIR). Taste masking was done by hot melt extrusion (HME) technology. Eudragit EPO and Soluplus were used as a taste masking and solubilizing polymers respectively. The prepared solid dispersion and tablets were evaluated for their physicochemical parameters such as hardness, friability, disintegration, in vitro drug release.
 Results: Experimental data revealed that physical integrity, brittleness of granules, conversion of a drug in amorphous form was improved by combining Eudragit EPO with Soluplus. Plasticizer helped to complete HME at 80 °C. Less than 10% drug release in pH 6.8 medium revealed that release would be extremely limited in the saliva and thus avoiding bitterness. Animal study data revealed that bioavailability has been increased by 30%. Differential scanning calorimetry (DSC) and x-ray diffraction (XRD) tests confirmed the existence of molecularly dispersed drug. Fourier-transform infrared spectroscopy (FTIR) confirmed the unchanged functional groups of FUR after HME processing.
 Conclusion: Proposed platform technology masked the bitter taste and enhanced the bioavailability of FUR in D: P ratio of 1:2.

Development of Extended Release Formulations of Ilaprazole Tablets

Extended release products are designed to release their medication in a controlled manner at a predetermined rate, duration, and location to achieve and maintain optimum therapeutic blood levels of a drug. The objective of the study is to formulate and evaluate Ilaprazole Controlled release tablets comparable to the innovator product. F1-F9 formulations were prepared using varying concentrations of super disintegrates like Crospovidone, Croscarmellose sodium and Sodium starch glycolate in different concentrations. Based on the hardness, friability, weight variation, drug content, F6 formulation was found to be optimised. The selected F6 formulation was sub coated with HPMC P 50 and followed by enteric coating with Acryl-EZE-80 (Eudragit L100-55). 3 formulations (F10-F12) were prepared by using coating. Among the three formulations, F11 formulation was found to be best. FTIR studies were carried out to find out drug and excipient compatibility studies, the studies revealed that there were no interactions. DSC studies also carried out to demonstrate any changes in physical forms of the drug molecule.
 Keywords: Ilaprazole, Extended release tablets, Crospovidone, Croscarmellose sodium, Sodium starch glycolate, HPMC P 50, Acryl-EZE-80.

BIOAVAILABILITY AND DISSOLUTION ENHANCEMENT OF GLYBURIDE NANOSUSPENSION

Objective: The main objective was to develop nanosuspension of glyburide (GLY) by quasi emulsification solvent diffusion method and to enhance dissolution and bioavailability characteristics of the drug GLY, an antidiabetic drug which belongs to Biopharmaceutical Classification System-II category.
 Materials and Methods: In this work, nanoparticles were prepared using polyvinyl alcohol, hydroxypropyl methyl cellulose, and Eudragit RL100. Twelve formulations of GLY (GLY-1–GLY-12) were formulated using the excipients at various compositions. Drug and excipient compatibility studies were conducted using Fourier transform infrared and differential scanning calorimeter. The prepared nanosuspension was analyzed using scanning electron microscopy for surface of the particle analysis, melting point, solubility, particle charge zeta (mv), percentage drug entrapment efficiency (%), and in vitro drug release. The optimized formulations of nanosuspension were further studied for in vivo pharmacokinetic evaluation. Reverse-phase high-performance liquid chromatography method was developed, validated, and used for the study of these formulations in rat plasma.
 Results: From these studies, it was confirmed that drugs and excipients chosen were compatible with each other. GLY-8 was the best formulation with a particle size of 85–96 nm with 168.7°C melting point, freely soluble in phosphate buffer pH 7.4, 93.53% drug entrapment, and 90.26±1 mV of zeta potential. This formulation shows percentage drug release of 99.85% in 24 h. In vivo pharmacokinetic study for optimized formulation (GLY -8) suggested that there was no reaction with the rat plasma. From the results, it was shown that Cmax and Tmax were found to be 0.604±0.03 μg/ml and 2±1.01 h, respectively. The values of t1/2 (h), area under the curve (AUC) (0-t), and AUC (0-∞) were found to be 10.04 h, 2.562±0.41 μg.h/ml, and 2.147±0.45 μg.h/ml, respectively.
 Conclusion: Based on the results obtained, oral administration of nanosuspension could not only provide the better absorption of poorly water soluble drugs but may also reduce toxicity and provide a new tool in drug delivery system.

FORMULATION IN VITRO AND IN VIVO EVALUATION OF CEFUROXIME AXETIL FLOATING TABLETS USING NATURAL GUMS

Floating tablets of Cefuroxime Axetil were prepared using Albizia gum, Dammar gum and Moi gum as polymers for controlling the drug release. Cefuroxime Axetil is a poorly water-soluble drug (second-generation cephalosporin) and its bioavailability is very low. The rate of absorption and the extent of bioavailability for such insoluble drug are controlled by the rate of dissolution in the gastrointestinal fluids. Two types of diluents were used and the drug release was compared. Pure drug and optimized formulation were subjected to the drug excipient compatibility studies using FTIR and DSC. The studies revealed that there was no interaction between the drug and excipients. In order to increase the drug release, channeling agents were introduced namely Lactose and DCP. Lactose is water soluble diluent and DCP is water insoluble diluent. All the formulations were taken and studied for the precompression parameters and found that they were within the limits. Precompression parameters were performed to all the formulations and were found to be in the acceptable limit which ensures the good flow properties. Formulation F4CADL containing gum dammar and lactose as channeling agent showed good results when compared with other formulations. The floating lag time of the optimized formulation was very short and the percentage of drug release at the end of 12 hours was found to be high. The drug release kinetics revealed that F4CADL follows KorsmeyerPeppas and the mechanism was non-fickian diffusion. Optimized formulation was selected for in vivo studies by using albino rabbits. It was found that the tmax was extended for prolonged period of time