bluuebunny/crossref_metadata_2025 huggingface dataset:
"Preparation of Zidovudine Extended Release Matrix Tablets with Various Controlled Release Polymers: A Feasibility Study of Granulation and Compression"
Authors: Raju P Narayana , K Prakash , T Rama Rao , M Lakshmi Narasu
Published: August 2020

The matrix tablets were prepared by using Eudragit L 100, Poly ethylene oxide and Carbopol 971 P. The granules of Zidovudine using above polymers were prepared by direct mixing, wet granulation with water and wet granulation with IPA. The granules were characterized for the morphological study, bulk density, tapped density and particle size distribution. The granules were compressed in to tablets. The tablets were characterized for in vitro dissolution, DSC and FTIR. Different shapes of the granules were formed with the wet granulation process with different polymers. In vitro dissolution studies showed the prolonged release of the Zidovudine with these polymers. The drug release depended up on the type of polymer and granulation process. DSC and FTIR studies showed no drug polymer interaction. This study gives an idea about the feasibility of granulation process for the preparation of the Zidovudine matrix tablets with different polymers.
Development of Prolonged Delivery of Tramadol and Dissolution Translation by Statistical Data Treatment
Authors: Parejiya P B , Barot B S , Shelat P K
Published: August 2020

The present study was carried out to fabricate a prolonged design for tramadol using Kollidon SR (Polyvinyl acetate and povidone based matrix retarding polymer). Matrix tablet formulations were prepared by direct compression of Kollidon SR of a varying proportion with a fixed percentage of tramadol. Tablets containing a 1:0.5 (Drug: Kollidon SR) ratio exhibited a rapid rate of drug release with an initial burst effect. Incorporation of more Kollidon SR in the matrix tablet extended the release of drug with subsequent minimization of the burst effect as confirmed by the mean dissolution time, dissolution efficiency and f2 value. Among the formulation batches, a direct relationship was obtained between release rate and the percentage of Kollidon SR used. The formulation showed close resemblance to the commercial product Contramal and compliance with USP specification. The results were explored and explained by the difference of micromeritic characteristics of the polymers and blend of drug with excipients. Insignificant effects of various factors, e.g. pH of dissolution media, ionic strength, speed of paddle were found on the drug release from Kollidon-SR matrix. The formulation followed the Higuchi kinetic model of drug release. Stability study data indicated stable character of Batch T6 after short-term stability study.
Anti-aging: Review and Experimental Clinical Study of Bioavailable Calcium−Probiotics and their Effect on Reversing Osteopenia, Osteoporosis, and other Common and Chronic Health Conditions
Authors: Reddy Malireddy S , Reddy D.R.K.
Published: August 2020

This review highlights the innovative anti-aging strategies through effective use of calcium supplements. With the advent of pharmacology, modern medical technology and scientific advances in food and nutrition, the longevity of human being significantly improved. However, living long or anti-aging does not make any sense unless people maintain excellent health and quality of life. Thus, maintaining good health is the prime requirement for anti-aging. Two diseases that rob the physical fitness of the people are sarcopenia (muscle loss) and osteoporosis (loss of bone mineral density). Both of these wasting diseases can be effectively controlled with proper nutrition, life style changes, and medical supplementation. This article describes the calcium supplementation and its importance in reversing and preventing osteomalacia and osteoporosis. It particularly focuses on the bioavailable calcium and the mechanism of calcium absorption in the gastrointestinal tract (GIT). The calcium transport patterns (trans-cellular and para-cellular), sites of maximum absorption of calcium in the GIT, the role of probiotics, vitamin D and dairy peptides to improve absorption of calcium have been briefly discussed. It is clearly evident that not all the calcium supplements available in the market are bioavailable. The role of calcium in controlling hypertension, cholesterol, triglycerides, obesity and reduction of colon cancer has been described. The merits of administering combination regimens of bioavailable calcium and probiotics have also been elaborated. Specific but limited clinical data has been presented demonstrating the effect of bioavailable calcium, fortified with vitamin D and probiotics with or without isoflavones, on reversing the osteopenia and controlling the osteoporosis associated symptoms. In conclusion, bioavailable calcium formulations hold promise as effective calcium supplements for better health.
Formulation Development and Characterization of Itraconazole Granules
Authors: Subbarao G V , Kapoor B S
Published: August 2020

Itraconazole is practically insoluble in water; large inter-individual and intra-individual variations of its oral bioavailability are reported. The main purpose of this study was to prepare and evaluate itraconazole granules for immediate release as drug delivery formulations. As a part of formulation optimization, different concentrations of hydroxy-propyl-methyl cellulose (HPMC) E5 were taken for the preparation of itraconazole granules, and were optimized with different characteristic like size, shape, surface roughness, density, moisture content, assay and dissolution. Formulation optimization includes a detailed study of itraconazole granules with different concentrations of polymer. The results of the study showed that 6% of HPMC E5 is sufficient as a binding agent and gave good shape and surface, low moisture content, 100% assay and 98.24% drug release within one hour. Based on these results, it can be concluded that 6% HPMC E5 is suitable for formulation of itraconazole granules.
Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets
Authors: T Sakthikumar , N N Rajendran , R Natarajan
Published: August 2020

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.
Preparation and Evaluation of Sildenafil Rapidly Disintegrating Tablets
Authors: Aly Adel M , Mohammed A A
Published: August 2020

Sildenafil citrate is an oral therapy for erectile dysfunction (ED).  Sildenafil, a selective inhibitor of cyclic guanosine monophosphate-specific phosphodiesterase type 5 (PDE5), has been reported to be effective in men with ED associated with diabetes and prostate cancer, and in psychogenic ED.  The main objective of this study is to prepare more effective, rapidly disintegrating and rapid onset of action sildenafil oral tablets. Sildenafil tablets were prepared using the newly introduced Pharmaburst® as a direct compression vehicle in comparison with the well-known excipients, namely mannitol, anhydrous lactose and primojel. The formula containing Pharmaburst® showed the most rapidly-disintegrating effect (15 sec) compared to the other formulations. Thus, Pharmaburst® can be utilized as an effective direct compression vehicle as well as a superdisintegrant with very rapid disintegration time in vitro and in the oral cavity. The rapidly-disintegrating sildenafil tablets showed maximum serum concentration within only two minutes (Cmax of 0.76 µg) by applying the tablets to the oral cavity of rabbits, whereas, the conventional sildenafil tablets have a comparatively lower Cmax (0.56µg) through about 45 minutes.
Novel New Drug Approvals in 2011: A Succinct Analysis of Drug Discovery Trends in the United States
Authors: Reddy D Samba
Published: August 2020

Thirty (30) new drugs have been approved by the FDA in 2011 for marketing in the United States. This list includes novel new drugs, known as new molecular entities (NMEs), biologics and new indications for drugs already approved. Eleven of the 30 NMEs were new drugs approved for orphan diseases, while twelve are considered first-in-class drugs with a unique new mechanism of action. During 2011, the FDA approved many unique and new drugs for chronic obstructive pulmonary disease, deep vein thrombosis, systemic lupus erythematosus (SLE), and epilepsy. In addition,  several new biologicals were approved in the past year for the treatment of macular degeneration, acute lymphoblastic leukemia, Hodgkin lymphoma, melanoma, chronic hepatitis C, and SLE. The introduction of 30 NMEs in 2011 underscores a robust success rate. It confirms that innovation is once again beginning to pay off. Analysis of drug approvals reveals a unique new trend in drug discovery in the face of stiff competition from generic products and declining revenues. In the existing climate of reduced pipeline for NMEs, the future and survival of big companies rests heavily on their unique niche products and biologics with relatively less competition from generic manufacturers. However, the competition for biosimilars is growing by the hour and therefore, crafting innovative generic biologicals is vital for generic biotech companies. Although the number of NMEs approved in the past 10 years has been declining, there is a substantial increase in R&D expenditure for drug discovery. Overall, the new drug approval list unveils unique and emerging trends in drug discovery especially in the current generics era.
Star Polymers: An Overview
Authors: Patil Rohini Anandrao , Aloorkar N H , Kulkarni A S , Ingale D J
Published: August 2020

This review article describes the synthesis, properties and some applications of star-shaped polymers. The arms constituted of homo- or co-polymers of different polymers are also reviewed. Methods of synthesis of various types of star-shaped polymers, including “arm first” and “core first” procedures,  is given as an introduction along with some details. Then, the synthesis of star polymers (including miktoarm stars) with strictly defined as well as with varying number of arms and having cores formed from small and/or large molecules: branched, cross-linked, etc., is described. Interest in star-shaped and branched systems based on poly (ethylene oxide) (PEO) is mainly motivated by their potential applications in the biomedical and pharmaceutical areas. The properties and applications of PEO stars are also reported, such as drug carriers, surface modifiers, hydrogels, components of membranes, and also have some biomedical applications. Their potential applications as components of different types of complexes, hydrogels, networks, and ultrathin coatings are indicated.
Hydrogels: A Versatile Drug Delivery Carrier Systems
Authors: Baldaniya L H , N A Sarkhejiya
Published: August 2020

Hydrogels are the material of choice for many applications in regenerative medicine due to their unique properties including biocompatibility, ﬂexible methods of synthesis, range of constituents, and desirable physical characteristics. Hydrogel (also called Aquagel) is a network of polymer chains that are hydrophilic, sometimes found as a colloidal gel in which water is the dispersion medium. Hydrogels are highly absorbent (contain ~99.9% water), natural or synthetic polymers. Hydrogel also possess a degree of flexibility very similar to natural tissue, due to its significant water content. It can serve as scaffolds that provide structural integrity to tissue constructs, control drug and protein delivery to tissues and cultures. Also serve as adhesives or barriers between tissue and material surfaces. The positive effect of hydrogels on wounds and enhanced wound healing process has been proven. Hydrogels provide a warm, moist environment for wound that makes it heal faster in addition to its useful mucoadhesive properties. Moreover, hydrogels can be used as carriers for liposomes containing variety of drugs, such as antimicrobial drugs. Hydrogels are water swollen polymer matrices, with a tendency to imbibe water when placed in aqueous environment. This ability to swell, under biological conditions, makes it an ideal material for use in drug delivery and immobilization of proteins, peptides, and other biological compounds. Hydrogels have been extensively investigated for use as constructs to engineer tissues in vitro. This review describes the properties, classification, preparation methods, applications, various monomer used in formulation and development of hydrogel products.
Antimicrobial Photodynamic Therapy with Single Application of Phthalocyanines in Staphylococcus aureus and Escherichia coli Wounds Infections
Authors: Ramadha Usama H , Hussein N S , Aboud H S
Published: August 2020

Phthalocyanines are considerable interest due to their general chemical and thermal stabilities. They are photochemical materials used in photodynamic therapy (PDT) and also as dyes due to their intense colors. In this study, we evaluated some phthalocyanines for their wound healing properties in mice models. Four groups of mice were tested for healing of wounds infected with Staphylococcus aureus and Escherichia coli. Animals were induced with a skin injury and infected 30 minutes later by applying Staphylococcus aureus into each right dorsal wound and Escherichia coli into each left dorsal wound. Three groups treated with phthalocyanine-containing ointments and the fourth group was used as control that was treated with ointment base only. The source of red light was applied for 5 minutes on these mice and observed them for one week. In treatment groups, the wounds had shown healing within the treated mice compared with the control group. The compound 1(PcZn) was more affective on E coli than S. aureus, compound 2(4-NH2)4PcZn.2H2O) more potency on S. aureus than E coli and the compound 3((4-NO2)4PcZn) has similar potency on both, S. aureus and E coli. In conclusion, these results show that the three phthalocyanine compounds were active as bactericidal on both S. aureus and E. coli in vivo, and helpful for rapid wound healing. These compounds might be suggested for treatment of infected burns.
In vitro and In vivo Characterization of Pectin Based In situ Gelling System of Famotidine
Authors: Modasiya Mohmadmoin K. , Patel A K , Patel V.M , Patel G.C
Published: August 2020

In this study famotidine was used as a model drug to formulate and evaluate pH-induced in situ gelling system for oral sustained release drug delivery in stomach which has shorter biological half-life. To study the effect of independent variables 32 full factorial design was employed, concentration of pectin as pH dependant polymer and concentration of calcium chloride on dependent variables like viscosity, drug content, 50% and 80% drug release and similarity factor. It was found that both the concentration of pectin and concentration of calcium chloride had significant effect on viscosity, drug content, 50% and 80% drug release and similarity factor of the system. In vitro drug release study showed that drug released from the in situ gel followed non-Fickian diffusion. Mathematical modeling was employed for quantitative evaluation of the effect of formulation variables. Rat pylorus legation model was used for in vivo study of the selected formulation. Results shows gel formation in gastric juice and reduction in ulcer index. There were few or no major changes in the formulation during three months stability testing. The in situ gelling systems are useful for delivery of famotidine.
Surface Solid Dispersion – A Review
Authors: Khatry Sadhna , Sood Neha , Arora Sandeep
Published: August 2020

Preparation of an effective formulation of poorly water-soluble drugs is a key challenge in pharmaceutical technology. Dissolution rate and solubility are the rate- limiting steps for increasing the bioavailability of poorly water‐soluble drugs. Solid dispersion is an efficient technique for improving dissolution rate and subsequently, the bioavailability of poorly water‐soluble drugs. Surface sSolid dDispersion is a novel technique of solid dispersion for dispersing one or more active ingredients on a water insoluble carrier of high surface area in order to achieve increased dissolution rates and bioavailability of insoluble drugs. The Vvarious polymers used in this technique are Avicel, Crosspovidone, sSodium starch glycolate, pPregelatinized starch, Cab-o-sil, Ac-di-sol, KyronT-314, Primojel and pPotato sStarch. This article reviews the various methods of preparation and characterization of surface solid dispersion and compiles some of the drugs formulated as surface solid dispersions. Some of the practical aspects to be considered for preparing surface solid dispersion are selection of a suitable carrier and method of preparation of surface solid dispersion.
Polymeric Drugs: A Novel Approach to Drug Delivery System
Authors: Chawla Pooja , Mis Monika
Published: August 2020

This review article describes the current status and recent advances of polymeric drugs with regard to their application in drug delivery system. Essentially polymer-drug conjugation aims to achieve improved drug targeting, decrease drug toxicity and overcome mechanisms of drug resistance. First generation conjugates used linear monomethoxy PEGs and other linear polymers. Modern polymeric chemistry is increasingly producing new polymeric architectures such as dendrimers, hyper branched polymers and hybrid macromolecular structures (such as star polymers, linear graft and dendronized linear polymers and novel therapeutic siRNA. This undoubtedly can be employed for designing of second generation polymer therapeutics. Clinical approval of products such as Copaxone®, Renagel®, Vivagel® and Welchol® have been successful in developing interest in polymer therapeutics as a growing field of research and development. In conclusion, there is emerging data that polymer drug conjugation has become useful in a wide range of treatments from infectious to chronic diseases such as cancer. Polymer therapeutics holds promising future applications in the field of nanotherapeutics. 

Polymeric Drugs: A Novel Approach to Drug Delivery System
Recent Advances in Nanosponges as Drug Delivery System
Authors: Bolmal Uday B , Manvi F V , Kotha Rajkumar , Palla Sai Sowjanya , Paladugu Anusha , Reddy Korivi Ramamohan
Published: August 2020

Major problem of many newly developed chemical entities is their poor solubility in water and pharmacokinetic issues. These poorly-water soluble drugs show many problems in formulating them in conventional dosage forms and the critical problem associated is its very low bio-availability. Nanotechnology has attracted increasing attention during recent years and it can resolve the problems associated with solubility and bio-availability. Nanosponges are a part of nanotechnology. Nanosponges delivery system, which was originally developed for topical delivery of drugs, can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Nanosponges are tiny sponges with a size of about a virus, which can be filled with wide variety of drugs. These tiny sponges can circulate around the body until they encounter the specific target site and stick on the surface and begin to release the drug in a controlled and predictable manner. Because the drug can be released at the specific target site instead of circulating throughout the body it will be more effective for specific disease targeted treatment. Another important character of these sponges is their aqueous solubility; this allows the use of these systems effectively for drugs with poor solubility.
Reverse Phase Ultrafast Liquid Chromatography Method for Simultaneous Estimation of Citicoline Sodium and Piracetam in Tablets
Authors: Panda Sagar Suman , B V V Ravi Kumar , Mohanta Ganeswar , Panda Jnyanaranjan
Published: August 2020

A simple, precise and accurate RP-UFLC method was developed for simultaneous determination of citicoline sodium and piracetam in tablets. Separation was carried on an Enable C18G column (250 mm × 4.6 mm i.d., 5 μm) using methanol: water (10 mM TEA) (75:25, v/v) as mobile phase at flow rate of 1 ml/min in isocratic mode. The PDA detection wavelength was 225 nm. The retention time of citicoline sodium and piracetam were 1.985 and 3.007 min, respectively. The method was validated for linearity, specificity, precision, accuracy and robustness as per ICH guidelines. The method was linear in the concentration range of 1.0 –250 µg/ml with correlation coefficients of 0.999 for both the drugs. The LOD and LOQ for citicoline sodium were 0.25 µg/ml and 0.81 µg/ml, respectively, and for piracetam 0.28 µg/ml and 0.93 µg/ml, respectively. The average recoveries for recovery study were found to be in the range of 100.24-101.09% and 100.08-101.05% for citicoline sodium and piracetam, respectively. The R.S.D. values for intraday, interday and system precision were found to be less than 2%. The method was applied successfully for simultaneous estimation of citicoline sodium and piracetam in combined tablet formulation.
Validation of RP-HPLC Method for Simultaneous Estimation of Cefixime Trihydrate and Clavulanate Potassium in Tablets
Authors: Zade S.S. , V.B Bhatpalliwar , Mendhule N S , Murkhekar M V , Alaspure R S , Durugkar N J
Published: August 2020

A simple, accurate, precise, rapid and economic HPLC method has been developed and validated for the simultaneous estimation of cefixime trihydrate and clavulanate potassium in tablet dosage forms. The chromatographic separation was achieved on a Hypersil C18 column (4.6 x 250 mm, 5 μm particle size). For HPLC method development, a mobile phase consisting of methanol: 30 mM potassium dihydrogen phosphate buffer pH 3.0 adjusted with orthophosphoric acid (30:70 v/v) was used at flow rate of 1.0 ml/min. The optimum wavelength selected was 278 nm. Under these chromatographic conditions, cefixime trihydrate and clavulanate potassium peaks were well resolved, with retention times of cefixime trihydrate and clavulanate potassium being 5.8266 and 3.2633 min, respectively. The proposed method was found to have excellent linearity in the concentration range 20-100 μg/ml with correlation coefficients r2 = 0.9946 and 0.9926, respectively. The method was validated for linearity, precision, LOD, LOQ and robustness. The proposed method was optimized and validated as per the ICH guidelines.
Formulation Development and Optimization of Nitrendipine Nanosuspension with Improved Pharmacokinetic Characteristics
Authors: Shah Anand , Patel Vipul , Shah Sunny
Published: August 2020

Poorly water-soluble drugs such as nitrendipine  (~2.0 µg/ml at  37◦C in water) offer challenging problems in drug formulation as poor solubility is generally associated to poor dissolution characteristics and thus to poor oral bioavailability. To enhance these characteristics, we prepared and evaluated nitrendipine nanosuspension using the nanoprecipitation technique. The important process parameters, the concentration of nitrendipine in the organic phase, concentration of surfactant in the anti-solvent, and starring speed were evaluated using 33 full factorial designs. It was observed that the concentration of nitrendipine in the organic phase, concentration of surfactant in the anti-solvent, and starring speed significantly affect the particle size as well as dissolution velocity. Differential scanning calorimetry studies confirmed that the crystallinity of the drug was maintained after the nanoprecipitation suggesting that improved dissolution of nitrendipine nanosuspensions could be attributed to reduction in particle size. This formulation may offer a superior pharmacokinetic profile due to nanotechnological design.
Formulation and Evaluation of Floating Microspheres of Ranolazine for the Treatment of Chronic Angina
Authors: Kotha Rajkumar , Bolmol U B , Reddy ER , P Sai Sowjanya , P Anusha , Reddy K.R
Published: August 2020

Ranolazine is indicated for the treatment of chronic angina alone or in combination with other cardiovascular agents. The objective of present investigation was to formulate floating microspheres of ranolazine to increase gastric residence time, increased bioavailability and reduce dose frequency of drug therapy. Novel o/w emulsion solvent diffusion technique was used for preparation of microspheres of ranolazine by using various polymers such as HPMC (hydroxyl propyl methyl cellulose), ethyl cellulose and Eudragit L 100. Entrapment efficiency of drug was up to 80.16%. Eudragit L100 based microspheres were found to be hollow cavity, spherical and porous nature from the results of scanning electron microscopy. Micromeritic profile of these microspheres was found satisfactory. From the results of FTIR spectroscopy it was revealed that there was no drug--polymer interaction. Eudragit L100 based microspheres shows good in vitro buoyancy and sustained release profile for longer period of time (> 14 hours), suggesting the viability of floating microspheres of ranolazine for improved pharmacokinetics for treatment of chronic angina.
Recent Advances in the Management of Viral Flu Infections
Authors: P Pitliya , Garg S K , Saini P , Pareek A K , Trivedi S K , Puri D , Bhambu S
Published: August 2020

Flu is an infectious respiratory disease which is caused by influenza viruses. The most common symptoms of flu are nausea, vomiting and diarrhoea. Different subtypes of influenza viruses are identified based on the combinations of these antigenic structures. Influenza viruses are negative-sense, single-strand RNA viruses that belong to the family Orthomyxoviridae. Antiviral medications are the current pharmacotherapy of flu because they are approximately 70% to 90% effective in preventing influenza. Influenza virus type A is readily prone to mutations, which can lead to minor antigenic changes (antigenic drift) or major antigenic changes (antigenic shift). These changes can result in viral strains capable of causing either an epidemic or a pandemic, because overall immunity in the population is lower.  Flublok is the first trivalent influenza vaccine made using an insect virus (baculovirus) expression system and recombinant DNA technology (i.e., without the use of actual influenza virus), so there is little risk of getting the flu from the vaccine.  Flublok is highly purified, has three times the amount of active ingredient in traditional influenza vaccines, and contains no preservatives, antibiotics or adjuvants. It provides protection against the latest strains of influenza by containing the corresponding hemagglutinin antigens for those strains. This review article provides brief information of influenza and its treatment by biotechnology-based vaccines introduced within the past few years.
Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery
Authors: Dhople Nagratna , Dandag P N , Gadad A P , Pandey C K , V S Masthiholimath
Published: August 2020

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.
Rifampicin and Ketoconazole Modulation of Intestinal Transport of Carbamazepine in Rats
Authors: Rao Y.M , Devandla Adukondalu , Yamsani Shravan Kumar
Published: August 2020

Many drug substances interact with each other and affect the CYP enzyme system and transport properties of other drugs.  The present study was aimed to investigate the effect of ketoconazole and rifampicin pre-treatment on the transport of carbamazepine across the intestine in rats. The transport of carbamazepine across different parts of intestine was studied by the everted and non-everted sac methods. The control and ketoconazole (80 mg/kg) and rifampicin (60 mg/kg) pre-treated rats were sacrificed and the intestine was harvested. The sacs of intestine were   prepared, treated with carbamazepine solution and then placed in Dulbecco’s buffer. Samples were collected periodically and the drug content was estimated using HPLC method. The results show that there was a significant (p<0.05) difference in the transport of carbamazepine from the intestinal sacs of pretreated with ketoconazole and rifampicin as compared to control. It appears that ketoconazole and rifampicin may affect the intestinal transport of carbamazepine and hence may result in pharmacokinetic interactions.
Effect of PHE against Trypsin and Egg-albumin Induced Experimental Model of Asthma in Mice
Authors: Mehta Anita A. , Gohil P V
Published: August 2020

The present investigation was carried out to study the effect of PHE in experimental induced bronchial asthma in mice. Trypsin and egg-albumin induced chronic model of asthma was used and various parameters were measured on 35th day. The asthmatic control group showed lower level of pO2, tidal volume, airflow rate and higher respiratory rate, serum bicarbonate level, eosinophil count in bronchoalveolar lavage (BAL) fluid compared to normal control group. Dexamethasone and PHE treated groups showed higher pO2 level, tidal volume, airflow rate whereas lower respiratory rate, serum bicarbonate level, eosinophil count in bronchoalveolar lavage fluid compared to asthmatic control group. Histopathological examination of lungs showed more prominent alveolar and muscular layer destruction in asthmatic control group than dexamethasone and PHE treated groups. PHE has beneficial effect in asthma and might be used for the treatment of bronchial asthma.
Modifications of Chitosan for Use in Nanoparticulate Drug Delivery Systems
Authors: Kumar D. Gowtham , R Naresh , Varma K. Rakesh , D Nagasen , B Sudheer , V Sai Kishore
Published: August 2020

Nanoparticles with naturally occurring biodegradable polymers have emerged as potential carriers of various therapeutic agents. Chitosan, a cationic polysaccharide, is one of such biodegradable polymers, which has been extensively exploited for the preparation of nanoparticles with several therapeutic agents. In recent years, the area of focus has shifted from chitosan to chitosan derivatized polymers due to its vastly improved properties such as better drug retention capability, improved permeation, enhanced mucoadhesion, and sustained release of therapeutic agents. Chitosan derivatized polymers are primarily the quaternized chitosan derivatives, chitosan cyclodextrin complexes, thiolated chitosan, pegylated chitosan, chitosan combined with sugar ligands, chitosan with cholanic acid, chitosan-linolenic acid and chitosan-DTPA. This review article covers the various modifications of chitosan, their preparation procedures and various works done with them.
Formulation and Evaluation of Oral Controlled Release Clarithromycin Matrix Tablets using Hydrophilic Polymer
Authors: T N K Suriyaprakash , Prabu S. Lakshmana , A Arumugarajan , A Sumathi
Published: August 2020

The objective of the present study was to develop clarithromycin tablets from polymeric hydrophilic matrices using methocel and characterization for its physic-chemical properties and in vitro release studies to optimize its release profile with the standard marketed product. Matrix tablets were prepared by wet granulation method using PVP and ethyl cellulose as binding agents. The matrix tablets were evaluated for its thickness, hardness, friability, weight variation, drug content and in vitro release studies. The drug delivery was analyzed using the paddle method in phosphate buffer pH 6.0 (dissolution medium I) and phosphate buffer pH 6.8 containing 0.5% sodium lauryl sulfate (dissolution medium II) and compared with USP dissolution limits. The dissolution release profile of formulation F9 was comparable with the market formulation and the difference factor and similarity factor f1 and f2 was found to be 2.44 and 83.18 in dissolution medium I; 1.44 and 89.71 in dissolution medium II. Stability studies were carried out as per ICH guidelines and tested for its physicochemical properties and in vitro studies. The study shows that the matrix method can be employed for preparing clarithromycin sustained release formulation using combination of hydrophilic polymers like Methocels and sodium carboxy methyl cellulose.
Formulation and Ex-vivo Evaluation of Glipizide Buccal Tablets
Authors: Singh Sudarshan , Maru Sandip G , Bothara B Sunil
Published: August 2020

Bioadhesive materials are agents which adhere to the mucous membrane due to specific properties and release the drug at the site of action in controlled manner. Since the biodegradability of the synthetic polymer is at some instance hesitant. In this exploration, a bioadhesive polymer has been developed which was isolated from leaves of Aloe vera (L.) Burm. f. The mucilage isolated from A. vera were used as a bioadhesive polymer in tablet formulation and evaluated for the parameters such as swelling, pH, and bioadhesive property like bioadhesive strength, record of adherence and ex-vivo residence time. The buccal bioadhesive tablet was prepared using glipizide as model drug. The prepared tablet was evaluated against existing bioadhesive polymer such as guar gum and hydroxyl propyl cellulose. Swelling index and surface pH was found to be 13.12-18.06% and 6.5-6.9 respectively. The drug permeation through goat buccal mucosa was found to be 60.21 ± 0.06 % in the end of 7 h with a Jss of 0.24 mg h-1 cm-2. The stability studies were performed on optimized formulation as per ICH guideline, result showed that there was no significant change in physical characteristic, adhesive strength and in vitro release. It was observed that as the concentration of mucilage increases swelling index also increases. Results of pH showed that mucilage is slightly near to neutral in nature. Formulations were evaluated for preformulation parameters, in vitro drug release profile and release kinetics. The formulations were found to have good preformulation characteristics. FTIR spectroscopy showed no significant chemical interaction within drug and excipients. The release mechanism of glipizide from buccal tablets indicated anomalous (non-fickian) transport mechanism and followed zero order kinetics. It was concluded that the mucilage of A. vera can be used as a pharmaceutical excipient in buccal bioadhesive drug delivery systems.
Formulation of Oral Mucoadhesive Tablets using Mucilage Isolated from Buchanania lanzan spreng Seeds
Authors: Singh Sudarshan , Ahmad Ayaz , Bothara B Sunil
Published: August 2020

The present study was taken to formulate and evaluate mucilage obtained from Buchanania lanzan spreng seeds (BL) belonging to family anacardiacea for oral mucoadhesive drug delivery system containing losartan potassium. Physiochemical characteristics of mucilage, such as swelling index, microbial count, viscosity, hydration capacity, flow property, and pH were studied. The mucilage was evaluated for its mucoadhesive properties in compressed tablet, containing losartan potassium. Granules were prepared by wet granulation process using polyvinylpyrrolidone as binding agent. Mucilage was used in four different concentrations i.e., 21, 42 and 55% w/w. The tablet were prepared and evaluated for its physical property. Further, in vitro dissolution and swelling index was determined. The property of bioadhesive strength of isolated mucilage was compared with Guar gum and HPMC E5LV, which was used as standard mucoadhesive agent concentration. Bioadhesive strength of the tablet was measured on the modified physical balance. Result revealed that tablets had good physiochemical properties, and drug release was retarded as concentration of mucilage was increased. The force of adhesion was obtained 0.1238N, 0.2822N, 0.5175N, 0.8679N and 0.3983N respectively for F1, F2, F3, F4 and F5. Formulations were subjected for study the effect of agitation at different rpm. Formulation showed relative effect on release of drug from formulation. All the formulations were subjected to stability studies for three months, all formulations showed stability with respect to release pattern. In conclusions, these results indicate that the seed mucilage of BL can be a suitable excipient for oral mucoadhesive drug delivery systems.
Formulation and Evaluation of Atenolol and Indapamide SR Matrix Tablets for Treatment of Hypertension
Authors: Pundir Sarika , Badola Ashutosh
Published: August 2020

In the present study we have formulated (F1 to F6) matrix tablets of atenolol and indapamide for the management of hypertension. As in simultaneous estimation of these drugs it was found that a confined release can be formulated. In the formulation of SR matrix tablet by using different concentration of delayed release agent DCP and pregelatinized starch as disintegrant we prepared tablets by wet granulation method. For sustained release action HPMC polymers were used for film coating. Preformulation studies were performed prior to compression. The compressed SR matrix tablets were evaluated for weight variation, hardness, friability, drug content, disintegration time and in vitro drug release using USP dissolution apparatus type 2 (paddle). It was found that the optimized formulation showed 49.33%, 48.90%, 48.52%, 47.65%, 46.84% and 46.51% release for atenolol in 12 hours respectively. However, indapamide released 49.62%, 49.39%, 48.72%, 48.27%, 47.59% and 47.36% at the end of 12 hr. The IR spectrum study revealed that there is no disturbance in the principal peaks of pure drugs atenolol and indapamide. This confirms the integrity of pure drugs and no incompatibility of them with excipients. The stability studies were carried out for the optimized batch for one months and it showed satisfactory results. The kinetic studies of the formulations revealed that diffusion is the predominant mechanism of drug and release follows Zero-order, Super case II transport.
Development and In vivo Evaluation of Cefdinir Nanosus-pension for Improved Oral Bioavailability
Authors: V. Kishan , Thota Suman , Syed Muzammil Afzal , Bomma Ramesh
Published: August 2020

Cefdinir belongs to III generation cephalosporins and is an oral extended spectrum antibiotic. It is a BCS class IV drug, with low solubility resulting in a low oral bioavailability of about 21% for capsules and 25% for suspension. The aim of this work was to develop cefdinir nanosuspension to improve the oral bioavailability. Nanosuspensions were prepared by using single stabilizer and combination of two stabilizers by employing high speed homogenization followed by sonication method and the prepared nanosuspensions were characterized. Initially, the drug excipient compatibility was checked by Differential Scanning Calorimeter (DSC). In trial experiments, tween80 concentration was varied from 0.25 to 0.75% and homogenization time was varied from 2.5 min to 10 min, and 0.5% surfactant concentration was found optimal. Further, trials were conducted with SLS and poloxamer 188 at the same concentration to know the role of stabilizers. Trials were also done by preparing cefdinir nano-suspensions with different techniques for comparative studies and their size and poly dispersity indices (PDI) were found. The mean size and zetapotential (ZP) of nanosuspensions, prepared by high speed homogenization followed by sonication varied from 541.7 to 947.2 and-13.7mV to -22.4mV respectively. Results of saturation solubility and dissolution studies were used to optimize the nanosuspension. Optimized nanosuspension showed improved saturation solubility, dissolution rate and oral bioavailability by 1.752 fold when compared to marketed suspension and found to be stable at RT for 2 months.The bioavailability improvement was significant at a level of         P value < 0.05 when student unpaired t-test was used. Hence, cefdinir nanosuspension formulation holds a great promise in improving dissolution rate and oral bioavailability.
Formulation and Characterization of Solid Self- Microemulsifying Cefuroxime Axetil Products
Authors: Puttachari Satish , Kalyane Navanath V. , Duttagupta Sarbani , Yetukuri Koushik
Published: August 2020

The Cefuroxime axetil has been used in treatment of wide range of infections but exhibits poor and variable bioavailability thus it is difficult to establish optimal oral dosage schedule. The purpose of this work was to prepare stable solid self-microemusifying drug delivery system (S-SMEDDS) of cefuroxime to improve the solubility and dissolution. The saturation solubility of drug in oils, solvents, surfactants and co-surfactants were determined and ternary phase diagram was drawn. Based on the results SMEDDS were prepared and characterized for self-emulsification properties and in-vitro dissolution. One of the best SMEDDS formulations was converted to S-SMEDDS by adsorption technique using maltodextrin as adsorbent. SEM of the S-SMEDDS revealed that particles were well separated and were free flowing, characterization by DSC, XRD revealed no interaction between drug and excipients. In-vitro dissolution was rapid and complete and no marked changes in physical and emulsification property were observed on stability.
Overview of Current Challenges of Nanoparticle Toxicity
Authors: Kushwaha Poonam
Published: August 2020

Nanomaterials improve everyday products but their safety for human health is poorly known. Due to the complex nature of nanomaterials, conflicting studies have led to different views of their safety. Many nanoparticles used by industry contain heavy metals, thus toxicity and bioaccumulation of heavy metals contained in nanoparticles may become important environmental issues. Due to the fast spreading of nanoproducts in the market, there is an urgent need for new research programs related to the broad area of nanotoxicology. This paper considers the properties of dispersed metallic nanoparticles and highlights the relationship between these nanoparticles and their toxicity.
Antioxidant Activity of Selected Chemical Constituents of Quinchamaliumchilensis
Authors: Muñoz Orlando , Aquino Rita , Mencherin Teresa , Picern Patrizia , Christen Philippe , Castro Consuelo , Villarroel Pamela , Delporte Carla
Published: August 2020

Antioxidant compounds from plant sources have been used worldwide for a variety of indications.  In this study, phytochemical investigation of the aerial parts of QuinchamaliumchilensisMol. (Santalaceae) resulted in the isolation and identification of fourflavonol glycolsides, quercetin-3-O-β-D-glucopyranosyl-(1→2)-[α-L-rhamnopyra-nosyl-(1→6)]-β-D glucopyranoside(1), kaempferol-3-O-β-D-glucopyranosyl-(1→2)-[α-L-rhamn opyranosyl-(1→6)]-β-D-glucopyranoside(2),quercetin-3-O-xylosyl-(1→2)-[α-L-rha-mnopyranosyl-(1→6)]-β-D-glucopyranoside(3) and rutin(4), as well as one flavanone glycoside, pinocembroside(5). The compounds were identified by 1D- and 2D-NMR experiments, mass spectrometry and UV spectra by comparison with those reported in literature. These compounds were isolated for the first time from the leaves of Q. chilensis. The antioxidant properties of the extract were investigated using DPPH and ferric reducing antioxidant potential (FRAP) assays. Total phenolic content was determined by the Folin-Ciocalteau method. Significant relationship between antioxidant capacity and total phenolic content was found, indicating that phenolic compounds are the major contributors to the antioxidant properties of this plant. These active molecules have therapeutic potential in treating conditions associated with oxygen free radicals.
Preparation, Characterization and In vivo Evaluation of Rosuvastatin Calcium Loaded Solid Lipid Nanoparticles
Authors: V Kishan , G Suvarna , D Narender
Published: August 2020

Rosuvastatin calcium (RC), is a hypolipidemic drug, and has poor oral bioavailability of about 20% due to first-pass effect. For improving the oral bioavailability of RC, solid lipid nanoparticles (SLNs) were developed using triglycerides (tristearin, tripalmitin, and trimyristin). Hot homogenization followed by ultrasonication method was used to prepare RC-SLNs. The prepared SLNs were characterized for particle size, PDI, zeta potential (ZP), entrapment efficiency (EE) and drug content. In vitro release studies were performed in 0.1N HCl and pH 6.8 phosphate buffer of by open tube method. Physical stability the SLNs was observed at refrigerated temperature and room temperature for 60 days. Pharmacokinetics of RC- SLNs after oral administration, in male Wistar rats was studied. SLNs prepared with tristearin (Dyanasan-118) having size of 207.3 ± 8.52 nm, PDI of 0.344 ± 0.084, ZP of – 20.9 ± 4.88 mV with 97.06 ± 0.210 % EE were optimized. Differential scanning calorimetric (DSC) study revealed that no interaction between drug and lipid. In vitro release studies showed that more cumulative release of RC in     pH 6.8 phosphate buffer than in 0.1NHCl during 24 hours. The lyophilized SLN formulation was used in knowing morphology of SLNs and was found to have spherical shape with increased polydispersity by Scanning electron microscopy. Pharmacokinetic studies showed the relative oral bioavailability of SLNs was 2.2 fold when compared to that of a suspension (p<0.001). Taken together, the results are indicative of SLNs as lipid based carriers for improving the oral bioavailability of this drug by minimizing first pass metabolism.