ABSTRACT

The main aim of this review article is to introduce the basic concepts of drug targeting as they have evolved over previous decades. The most important chemical features and biological behavioral characteristics of the carrier molecules exploited for drug targeting purposes will be addressed. Targeted drug delivery is also known as smart drug delivery. This is self-contained, discrete dosage form which is applied to intact skin, at a controlled rate to the systemic circulation. In this system medicament given to a patient in a manner that increases the concentration of the medication in some parts of the body relative to others. System involves nanoparticles-mediated drug delivery in order to reduce drawback of conventional drug delivery. Active and passive targeting are two types of methods used for targeted drug delivery. Targeted drug delivery has some side advantages like reduces side effects, avoid hepatic first pass metabolism, enhance drug absorption, dose is less as compare to conventional drug delivery, reduced fluctuation in circulating drug levels etc. Brain targeted drug delivery system and tumor targeted drug delivery system are most widely used. Many drug carriers are used in this advanced drug delivery system are lipoprotein, liposome, micelles and immune micelles. The goal of targeted drug delivery system is to prolong, localize, target and have a protected drug interaction with disease tissues.

Keywords: - Nanoparticles, Brain targeted drug delivery system, Normal cell and cancerous cell.

ABSTRACT

Placental insufficiency or Uteroplacental vascular insufficiency is a complication of pregnancy when the placenta is unable to deliver an adequate supply of nutrients and oxygen to the foetus and thus cannot fully support the developing baby. It may be caused due to preeclampsia. Placental insufficiency can lead to Intra uterine growth retardation (IUGR) .IUGR is defined as estimated birth weight below 10^th percentile for gestational age which is quite common. This study aims to evaluate the effectiveness of L-arginine in placental insufficiency

Keywords:L Ardenin, uteroplacental

ABSTRACT

Cefixime, cefpodoxime and cefepime are cephalosphrin antibiotics used widely in the different infectious diseases. Newer HPTLC methods were developed for their estimation from individual dosage forms due to versatile applications and advantages. The HPTLC chromatogram of cefixime was developed by using a mobile phase ethylene acetate: methanol: water (4.5:5:0.5%v/v) and scanning wavelength was 292nm. The Rf value was 0.58±0.02. The mobile phase optimized for cepodoxime was methanol: ethyl acetate: toluene (1.5:3:5.5% v/v), with the Rf value 0.53±0.02. The cefixime was retained using methanol :water : chloroform (6:3:1%v/v), on a  silica gel G₆₀ F₂₅₄ aluminium sheet and  scanning wavelength kept at 285nm. The Rf value was 0.44. The methods were optimized validated as per guidelines and successfully applied for individual dosage form containing  of each of cephalosporin.

Keyword: HPTLC, Cefixime, Cepodoxime, Cefepime.

ABSTRACT:

The aim of the present study is to design and evaluate the controlled release Glyburide trilayer matrix tablets, to achieve zero-order drug release for sustained plasma concentration. Matrix tablets were prepared by direct compression whereas three-layer tablets were prepared by compressing polymer barrier layers on both sides of the core containing the drug. Formulations were prepared by using different grades of hydroxy propyl methyl cellulose and Ethyl cellulose. Based on the evaluation parameters, drug dissolution profile and release drug kinetics HF16 was found to be optimized formulation. These results also demonstrated the suitability of three-layered tablet formulation of Glyburide to provide controlled release for prolonged period and improved linearity for Glyburide in comparison to marketed product in the management of Diabetes.

Keywords: Glyburide, Type II Diabetes, HPMC Grades, EC, MCC, Release order kinetics.

ABSTRACT

Lehya is a polyherbal preparation which ensure its action from tongue itself. Our preparation acts by inducing anti inflammatory response on various cells, relaxing smooth muscles resulting in bronchodilation and it also has power to simultaneously enhance memory. Being prepared from plant materials it also has other beneficial effects on health and minimum side effects. The prepared lehya was evaluated for various physiochemical parameters. The preparation was evaluated by TLC and FTIR which have been discuss below. The further scope of the preparation can be studies using GC-MS

Keywords: Lehya, Standardization, TLC, FTIR.

ABSTRACT

The present study was to formulate and characterize oral floating microspheres of Pramipexole to sustain the gastric residence time and to target gastritis. The floating microspheres were prepared by ionotropic gelation technique. Sodium alginate was used as polymer, sodium bicarbonate as gas generating agent, calcium chloride as cross-linking agent, HPMC K4, as rate retarding agent. Microspheres were characterized for the Micromeretic properties, incorporation efficiency, buoyancy test, SEM analysis, FTIR, and in vitro diffusion studies. The diffusion studies were carried out in 0.1N HCl and the results were applied to various kinetic models.  Among the total 14 formulations F12 was found to be optimized on the basis of different evaluation parameters. The % yield of F12 formulation was found to be 98.58%. On the basis of optical microscopy, the particle size was 65.12±0.04µm. The % buoyancy, % entrapment efficiency and swelling index of F12 formulation was 98.12%, 96.56% and 97.10, respectively. The Cumulative % drug release of F12 formulation was 98.3±5.10% in 12h.  SEM studies showed the particles were in spherical shape. On the basis of obtained results, Floating microspheres were of good candidate for targeting to GIT.

Keywords: Pramipexole, floating microspheres, SEM, Ionotropic gelation technique, Parkinson's disease.

ABSTRACT

Free Radicals are molecules with an unpaired electron. They are generated in our body by various endogenous systems, exposure to different physicochemical conditions or pathophysiological states. At low levels, free radicals exert beneficial effects while at high concentrations, they generate oxidative stress and damage all cell structures. This review deals with the sources of the free radicals, their beneficial and deleterious effects on cellular activities; it highlights the role of free radicals and oxidative stress in various physiological states like cancer, cardiovascular diseases, Alzheimer’s disease, kidney disease, etc. The harmful effect of free radicals is neutralized by antioxidants, which prevents oxidative damage by reacting with free radicals. Therefore, the best remedy is to increase the intake of natural antioxidant.

Keywords: Free radicals, Oxidative stress, Disease, Reactive Oxygen Species.

ABSTRACT

Ranitidine hydrochloride tablet is used as a drug of choice for peptic ulcer therapy. It is   available in several brands in the Sudanese pharmaceutical market. The aim of this study was to evaluate the quality, safety and efficacy of the different brands and to assure the interchangeability among different brands and the originator (Zantac®).Four brands available in the market were assessed “evaluated” using pharmacopoeial parameters for quality such as weight variation test, hardness test, friability test, dissolution test and assay along with the similaritydissimilarity factors were evaluated. The results obtained in this study showed that the different brands satisfied pharmacopoeial parameters, although not all of them were pharmaceutically equivalent or interchangeable with the originator.

Key words: Ranitidine, Sudanese drug market, quality control, interchangeable.

ABSTRACT

As per the current expectation USFDA, MHRA and other major Regulatory Authorities, especially with respect to the Data Integrity policies, the Sponsor has decided to implement e-BMR project by end of 2020. However considering the current state of our different Electronic Records, and the complexity of the e-BMR project, this project cannot be achieved directly. A multitude of different systems has to be converted to ‘Electronic Records’. A number of other Systems and Equipments, which has Electronic Records, works in isolation and don’t interact with others. The systems which are to be converted to ‘Electronic Records’ includes different logs, like ‘Area and Equipment Usage Logs’, ‘Calibration Logs’, ‘Weighing Balance Verification Logs’, ‘Temperature and Relative Humidity Logs’. All these logs are to be converted to electronic records, before the next stage i.e. Integrating all Equipments and Instruments to the Central Server. Only after these two major system, along with other standalone systems like Bar Code Enabled Dispensing and Intermediate Storage Records are Online, that the main project e-BMR can be implemented, as it will require data from all other systems. This project is aimed for the 'Development and Validation of Electronic Data Recording System, Integra table with all Other Systems to create Complete Electronic Documentation’. There are no computerized systems available in Market which can meets this requirement. So a new computerized systems was configured and validated, which will later be integrated with other systems so smooth flow of data between all systems.

Keywords: Data Integrity, Electronic Records, e-BMR

ABSTRACT

Gestational Diabetes Mellitus [GDM] is defined as the carbohydrate intolerance during pregnancy. In GDM glucose intolerance can be notified due to fetal development and other contributing factors, this may response to severe condition of hyperglycemia in pregnancy. Various maternal and prenatal adverse outcomes may resulted by GDM. The prevalence of GDM have a steep increase by  year to year by the influence of contributing factors such as advancing age,  life style modifications,  changed diet pattern etc. The overall prevalence of GDM noted as 1-14% among population, also the epidemiological studies states that the occurrence of GDM varies on the basis of ethnic and racial composition. The pathophysiology of gestational diabetes is assumed by various factors but exact cause of is unknown. Gestational diabetes is influenced by hormones produced by placenta, progesterone, estrogen, human placental lactogen [HPL], human chronic somatotropin [HCS] etc. Women with Polycystic Ovarian Syndrome [PCOS] and family history of Type 2 diabetes mellitus are at high risk of having GDM. GDM on pregnancy period causes some important complications such as high cesarean sections, preeclampsia, post partum type 2 diabetes mellitus, urinary tract infection in both neonate and the mother, cardiovascular disease,  hypertension and stroke in mother, also neonatal consequences such as congenital malformations, macrosomia, adiposity, hypoglycaemia, birth injuries and prenatal death. This overview describes all the complications of pregnant women and newborns due to GDM with the conclusion of treatment profile.

Keywords:Gestational Diabetes Mellitus, Oral Glucose Tolerance Test.

ABSTRACT

Diabetic foot complications are contributing to both mortality and morbidity among the diabetic population leading to physical, physiological and financial burden for the patients and community. The risk of ulceration and amputation among diabetic patient’s increases by two to four folds with the progression of age and duration of diabetes regardless of the type of diabetes Foot ulceration is a preventable condition, where simple interventions can reduce amputations by up to 70% through programs that could reduce its risk factors. The outcomes of education on foot self-care practices among patients with diabetes depend on the type of education provided. The management of diabetic foot ulcers remains a major therapeutic challenge which implies an urgent need to review strategies and treatments in order to achieve the goals and reduce the burden of care. Prevention of diabetic foot ulceration is critical in order to reduce the associated high morbidity and mortality rates, and the danger of amputation. It is essential to identify the “foot at risk,” through careful inspection and physical examination of the foot followed by neuropathy and vascular tests. Regular foot examination, patient education, simple hygienic practices, provision of appropriate footwear, and prompt treatment of minor injuries can decrease ulcer occurrence by 50% and eliminate the need for major amputation.These key educational elements for diabetes patients at low risk of complications are captured with CARE.

Keywords: Diabetic foot complications, foot self-care practices, amputation, risk of ulceration.

ABSTRACT

Microbially induced carbonate precipitation (MICP) is a biologically induced mineralization process and has found its application in various engineering realms. The process of MICP is often mediated by the enzymes urease and carbonic anhydrase. The bacterial cell wall acts as the nucleation site for the formation of CaCO₃. This review summarizes the mechanism associated with the microbial CaCO₃ precipitation process and the function of urease. The role of extracellular polymeric substances (EPS) and their ability to influence MICP are also discussed. The various polymorphs of CaCO₃ that are formed in the due course of MICP and the conditions that determine the polymorph selection are discussed as well. Biocalcification by different classes of bacteria isolated from various sources are summarized. This review describes in detail the various applications of MICP including its role in biocementation, removal of heavy metals, CO₂ sequestration, fracture sealing in underground geology, remediation of limestone structures and as a counter measure for erosion. Over the last few years, various process improvements have emerged for improving the quality of MICP and thereby enhancing their potential, viz. optimization of bacterial growth medium, using industrial by-products as growth media components, etc. Some of these process improvements are also discussed in this review. The shortfalls of MICP, particularly those while implementing it at the field level, issues associated with commercialization of the process are also described along with its future perspectives.

Keywords: MICP, urease, CaCO₃, polymorphs, engineering applications

ABSTRACT

The aim of this study was to assess the drug utilization pattern of parenteral antibiotics in medicine units. A prospective and observational study was done on patients admitted in medicine indoor. Information regarding patient demographic details, patient medication history, and reason for admission, medication details and lab investigations. Patient drug therapy details such as diagnosis, clinical condition, therapy details such as name of the antibiotics, dose, route, frequency, duration of treatment were collected and recorded in performa. Rationality was assessed by using standard guidelines, micromedex, and NFI. Drug interactions and ADR were assessed  by using standard text books like stockley drug interactions text book 8^th edition. And Micromedex. A 310 patients received parenteral antibiotics in the medicine units was found to be 12.54%. amongst incidence of use of parenteral antibiotics was highest in medicine unit B (42.12%). Cephalosporins (64.54%) were the most frequently prescribed class of  parenteral antibiotics. ceftriaxone (53.63%) was the frequently used antibiotic. Cefriaxone is commonly prescribed for viral fever. 43% of major drug interactions were identified. It is essential that appropriate guidelines on the use of parenteral antibiotics are implemented to prevent irrational use of antibiotics.

Keywords: parenteral antibiotics, drug utilization study, and irrational drug use.

ABSTRACT

Atorvastatin calcium is a HMG-CoA reductase inhibitor used in the treatment of hyperlipidaemia. It has oral bioavailability of less than 12%. It also undergoes high first pass metabolism. The objective of the present work was to formulate, optimize and in vivo evaluation of the potential novel proniosomal gel containing atorvastatin for transdermal delivery. On the basis of the preliminary trials a 3-factor, 3-level Box–Behnken design was employed to study the effect of Cholesterol, soya lecithin and Span 60 independent variable on dependent variables (particle size and % entrapment efficiency). Atorvastatin optimized proniosomal formulation F2 shown better particle size and % entrapment efficiency and also the drug release was 99.72% within 24h in slow and controlled manner when compared with control. The particle size and Zeta potential of the optimized atorvastatin proniosomal gel was found to be 65.72 and -10.5 respectively. Optimized batch of Proniosomes was used for the preparation of Atorvastatin - based proniosomal hydrogel by incorporating hydrated Proniosomes to Carbopol matrix to enhance the stability and viscosity of the system. The enhanced skin permeation for prolonged period of time, may lead to improved efficacy and better patient compliance. From in vivo studies the maximal concentrations (C_max) of drug was significantly reduced while the areas under the plasma concentration–time curve (AUC) and t_1/2 were evidently increased and extended. This study suggests that proniosomal gel of atorvastatin would be a promising alternative to improve the bioavailability problems of atorvastatin.

Keywords: Atorvastatin, Proniosomes, Box Behnken Design, Span 60, zeta potential

ABSTRACT

Lovastatin belongs to the class of cholesterol lowering drugs and is the first clinically used statin. It is available as conventional and extended release tablets, but its low aqueous solubility finally escorts it to low oral bioavailability (less than 5 %). Therefore, improvement in aqueous solubility of Lovastatin is the foremost aim. In the present work Self-nanoemulsifying drug delivery systems (SNEDDS) of Lovastatin is being formulated to increase the water solubility. Lovastatin SNEDDS was formulated with various oils, surfactants and co-surfactants and tested for its maximum solubility and drug release. The optimized Lovastatin SNEDDS formulation (F8) has a composition of Acrysol EL 135 as oil phase, Lauro glycol 90 and Capmul MCM as surfactant and co-surfactant respectively. Formulation F8 was found to be best formulation based on evaluation parameters. No drug precipitation or phase separation was observed in the optimized formulation. The particle size of the optimized formulation was found to be 4.9 nm & Z-Average of 71.5 nm indicating all the particles were in the nanometer range. The zeta potential of the optimized SNEDDS formulation was found to be -13.7 mV which comply with the requirement of the zeta potential for stability. The current investigation of nano emulsion may serve as a promising approach for the formulation development of poorly soluble drug Lovastatin, which has undoubtedly proved the potential effectiveness of SNEDDS for formulating Lovastatin with improved solubility and dissolution.

Key words: Lovastatin, SNEDDS, Statin, Lauro Glycol 90, Solubility

ABSTRACT

Present generation is a fast moving generation and no doubt about the potency of allopathic medicine, they provide fast result, but the darkest side of this medicine is their several side effects and contraindications. On the other hand the Ayurvedic medicines are good substitution for those medicines because of their less or no side effect and their ability to cure the problem from their root. The present study is based on the pharmacological activity of Dhanwantari’s Ditoxifie capsule. This drug is having great potential to deal with ache of muscles or joints, frequent headaches, low energy or frequent being tired, frequent cold or sickness, coughs or a sore throat, runny nose or sinus congestion, dense or yellow urine, painful bowel movements, acne or oily skin, lack of taste and many more. In the present work, experiments were conducted to evaluate the possible anthelmintic effects of Ditoxifie capsule on Indian earthworm (Pheretima posthuma) at 400mg/ml, 600mg/ml, and 800mg/ml concentration. Results were expressed in terms of time for paralysis and time for death of worms.

Keywords: Anthelmintic, Ditoxifie capsule.

ABSTRACT

The major problem in formulation of oral films of cilnidipine is that it belongs to BCS Class II moiety. Pharmacologically Cilnidipine is a dihydropyridine (DHP) type of calcium channel antagonist. Unlike other calcium channel antagonists, Cilnidipine blocks the influx of Ca²⁺ ions into both vascular smooth muscle at the level of L-type Ca²⁺ channels and neuronal cells at the level of N-type Ca²⁺ channels. Cilnidipine was absorbed over 2 hours and its bioavailability is 64-90%. Hence there is a need to increase the solubility and oral bioavailability of cilnidipine by formulating it in to solid dispersions and incorporating the same in to the formulation of fast dissolving films which gives fast onset of action. Nine formulations (FC 1 - FC 9) of cilnidipine films were prepared and evaluated for their physical characteristics such as thickness, weight variation, folding endurance, drug content uniformity and gave satisfactory results. The compatibility of the drug in the formulation was confirmed by FTIR and DSC studies. The formulations were subjected to disintegration, in vitro drug release studies and formulation FC 6 was found to be best formulation which contain HPMC, PVP as film forming polymers along with cilnidipine solid dispersion with poly ethylene glycol at weight ratio of 1:4 showed excellent film forming characteristics such as disintegration time of 49.3 sec and percentage drug release 97.92 within 8 minutes.

Keywords: Cilnidipine, Solid dispersions, Fast dissolving film, Solvent casting method, HPMC and PVP.

ABSTRACT

This presented work is based on application of two multivariate calibration methods for simultaneous UV-Visible spectrophotometric determination of active substances in combined pharmaceutical formulation contained of Tinidazole (TINI) and Norfloxacin (NFX). The methods used were Partial Least Square (PLS) and Principal Component Regression (PCR). The spectra of both NFX and TINI were recorded at concentrations within their linear range 2.0-12.0 μg/mL for NFX and 5.0-30.0 μg/mL for TINI. The 29 set of mixtures were used for calibration and 07 set of mixtures were used for validation in the wavelength range of 260 to 320 nm with the wavelength interval λ= 0.2 nm in methanol. The methods were validated as per International Conference on Harmonization Q2 (R1) (ICH) guidelines. These methods were successfully applied for determination of drugs in pharmaceutical formulation (tablet) with no interference of the excipients as indicated by the recovery study results. The proposed methods are simple, rapid and can be easily used as an alternative analysis tool in the quality control as well as in process control of drugs and formulation.

Keywords: Norfloxacin, Tinidazole, PLS, PCR, Validation.

ABSTRACT

The present study was aimed to develop and optimize extended release (ER) matrix tablets of Lamivudine trilayer tablets to achieve zero-order drug release for prolonged period of time. Lamivudine tablets were prepared by direct compression and consist of middle active layer with different grades of HPMC, MCC and PVP K30, upper and lower layers were prepared with Carnauba wax, Xanthan gum, EC and MCC. The tablets were also evaluated for physicochemical characteristics and release kinetics. The physicochemical characteristics of the prepared tablets were satisfactory. The developed drug delivery systems showed prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF23) was described by the Zero-order and Higuchi model. The results indicate that the approach used could lead to a successful development of extended release formulation of short biological half-life drug. These results also demonstrated the suitability of three-layered tablet formulation of Lamivudine to provide controlled release for prolonged period of time and improved linearity for Lamivudine in comparison to marketed product in the effective management of AIDS with patient compliance.

Keywords: Lamivudine, Trilayer matrix tablet, HPMC, Xanthan gum, Geomatrix

ABSTRACT

Natural remedies are more acceptable in the belief that they are safer with fewer side effects than the synthetic ones. Herbal formulations have growing demand in the world market. The present work deals with the development & evaluation of the herbal anti-acne face wash containing aqueous extract of Luffa cylindrica seed oil, neem leaves (Azadirachta indica), Pumpkin. Although various topical herbal formulations for acne are available in the market, we propose to make pure herbal formulation without using any synthetic soap . The plants have been reported in literature having good anti-microbial, anti-oxidant & anti-inflammatory activity also and saponins present in the Luffa cylindrica seeds used as a base to form the soap. Prepared formulations were evaluated for various parameters like colour, appearance, consistency, washability, pH & spreadability. The formulation was compared with the marketed preparation.

Keywords: Face wash, Luffa cylindrica seed oil, saponins , soap,  neem leaves, antimicrobial activity

ABSTRACT

Nateglinide is an anti-diabetic drug that lowers the blood glucose levels by stimulating insulin secretion from pancreas. Because of low solubility and bioavailability, its usage is limited. In the present study solid dispersions of Nateglinide were prepared by solvent evaporation method and evaluated through various steps for biological correlation. Nateglinide solid dispersions were prepared using PEG 6000, Pluronic F 127 and Labrafil M 1944. A 3-factor, 3-level Central composite design employed to study the effect of each independent variable on dependent variables. X-ray diffraction was used to analyze the crystallinity and FTIR was used to analyze the drug and excipient compatibility. Scanning electron microscopy was performed to analyze the surface of solid dispersion samples. The correlation coefficient showed that the release profile followed Higuchi model (R2= 0.95836). From Korsmeyer peppas model, the release exponent, n was found to be 0.80635 (0.43 < n < 0.85) and followed anomalous behaviour and hence release mechanism was indicative of diffusion. From in vitro dissolution studies it was proved that a Nateglinide solid dispersion may achieve good formulation capability for pharmaceutical manufacturer by increasing solubility and dissolution rate.

Key words: Nateglinide, Diabetes mellitus, solid dispersions, solubility, Central composite

ABSTRACT

Gutika Anjana is an important Ayurvedic formulation containing Gairika (Ochre), Saindhava (Sodii chloridum), Pippali (Piper longum Linn.) and Shunthi (Zingiber officinale  Roxb.) as main ingredient. All the constituents are available and prepared according to the reference present in Sushruta Samhita Uttaratantra Vataabhishyanda Pratishedha. Till date no work has been carried out to standardize the formulation. Hence the present study was undertaken to standardize the compound Ayurvedic formulation through Pharmacognostical and pharmaceutical evaluation. The sample was subjected for various Phytochemical parameters like water soluble extractive (32.8%w/w), alcohol soluble extractive (32.3% w/w), ash value (8.4% w/w), loss on drying (14.25% w/w), the pH (6), HPTLC. The HPTLC, solvent system was Toluene:ethyl acetate (9:1), showed the presence of 11 spots at 254nm and 13 spots at 366nm. Thus the physiochemical and microscopic characters achieved may provide guidelines for standardization of formulation, Gutika Anjana.

 Keywords: Gutika Anjana, HPTLC, Pharmacognostical, Physiochemical Evaluation

ABSTRACT

A new Reverse Phase High Performance Liquid Chromatographic (RP-HPLC) method has been developed for estimation of Paracetamol and Alprazolam in bulk and tablet dosage forms using UV-detector. A RP Cell Pack C18 column (250 mm × 4.6 mm, 5 µ particle size) using acetonitrile and water (80:20 % V/V) as mobile phase by maintaining flow rate of 1 mL/min at 236 nm as detection wavelength. The peaks were eluted at 4.8 and 6.2 mins for Paracetamol and Alprazolam, respectively. The method was validated in accordance with ICH guidelines, the linearity curve for Paracetamol was obtained over the range of 50-175 µg/mL, and it was found to be linear with y = 1961x + 9226 (r² = 0.999). The linearity curve for Alprazolam was obtained over the range of 0.25-1.5 µg/mL and was found to be linear with y =23328x + 939.3 (r² = 0.998). The percentage recoveries were found to be 99-101% and 99-102%, respectively. The system suitability parameters such as number of theoretical plates and tailing factor were found to be 7242, 1.56 for PAR and 6755, 1.15 for ALP. Hence the developed RP-HPLC method was found to be simple, accurate, economical, rapid and can be applied for routine analysis of these drugs in their combined formulations.

Keywords: Paracetamol, Alprazolam, Acetonitrile, RP-HPLC, Method development, Method Validation.

ABSTRACT

A series of novel N-(substituted)-2-[4-oxo-2-phenylquinazolin-3(4H)-yl] acetohydrazide derivatives were designed and synthesized, and their structures were characterized by ¹H, ¹³C NMR, IR and Mass Spectral analysis. Their antimicrobial activity against bacterial strains and unicellular and multicellular pathogenic fungal strains were evaluated, and the results of in vitro antimicrobial evaluations of all newly synthesized compounds revealed that compounds 4(a-g) found to possess varied degree of antibacterial and antifungal activities Therefore, it can be inferred that presence of Schiff base nucleus in newly synthesized compounds can act as better system for antimicrobial activity. Lipinski rule were evident that all synthesized compounds have a good potential for development as an oral agent and can be potentially active drug candidate.

Keyword: Quinazolinone, Schiff base, NMR, IR, Mass spectra, antimicrobial evaluation and Lipinski rule

ABSTRACT

Nimodipine, a poorly soluble drug, was considered to be fit for solid dispersions to improve its solubility and bioavailability. Our study intended to prepare Nimodipine solid dispersions by solvent evaporation method using various novel polymers. Solubility and dissolution studies indicate that Kolliwax RH 40 and SLS is the most suitable polymer. The solubility studies were corresponded with dissolution data and the formulation SD15 was found to be having highest drug release of about 98.96±5.15% in about 90 minutes. In-vitro release data from several formulations containing XRD and SEM studies indicate no crystallinity in the optimized formulation SD15. FTIR studies suggested good drug excipient compatibility between all components of prepared formulation. From in vivo bioavailability studies, C_max of the optimized formulation SD15 was 4.34±0.08ng /ml, was significantly higher as compared to pure drug suspension, i.e., 2.78±0.35ng/ml. T_max of optimized formulation was decreased significantly when compared with pure drug (1.00±0.05hr, 2.00±0.01hr), AUC_0-? and AUC_0-t for optimized solid dispersion formulation was significantly higher (p<0.05) as compared to pure drug suspension. The present study demonstrated that formulation of Nimodipine solid dispersion by solvent evaporation technique is a highly effective strategy for enhancing the bioavailability of poorly water soluble Nimodipine.

Keywords: Nimodipine, Solid dispersions, Hypertension, Kolliwax, Solvent evaporation, Bioavailability studies.

ABSTRACT

A fluconazole o/w microemulsion was developed for topical application using isopropyl myristate as the oil phase. Pseudo-ternary phase diagrams were constructed for the determination of existence region of micro emulsion region using the surfactant (tween 80 & Cremophor RH-40) and co-surfactant (ethanol). Different formulations were prepared for the evaluation of oil content, surfactant/co-surfactant concentration on in-vitro permeation rates. In-vitro transdermal permeability of flucanazole from the micro emulsions was evaluated using Keshary Chien diffusion cells mounted with 0.45µ with cellulose acetate membrane. The amount of drug (Fluconazole) permeated was analyzed by HPLC.

Keywords: Fluconazole, Micro emulsion, In-vitro studies.

ABSTRACT

The aim of present work was to design and evaluate sustained release matrix tablets of antihyperlipidemic drug. In the present investigation, polymers used in different combinations such as Eudragit RL100 and HPMC E5 in the ratio of 1:1, 1:2, 1:3 and vice versa with PVP K25 using direct compression technique were prepared. The tablets were evaluated for physical parameters like thickness, hardness, friability, weight variation, and in vitro release studies. The FTIR study indicated that the drug is stable in formulation. The maximum drug release was found to be 94.41% over a period for 12 hours for F4 batch, thus concluded that as the concentration of Eudragit RL100 is increased the drug release decreased. The drug release mechanism followed non-fickian transport from both polymer matrices. All the formulations were stored at 25⁰C/60% RH and 45⁰C/75% RH for 3 months. It showed that all the formulations were physically and chemically stable.

Keywords: Sustained release, direct compression, Matrix tablets, Simvastatin, EudragitRL100, HPMC E5.

Controlled topical release drug delivery system for Fluconazole  is potentially useful in improving drug deposition in the skin and reducing the incidence of adverse side effects. The purpose of the present experiment was to produce a topical gel system for the delivery of . Drug loaded microsponges (1–10) were formulated by an emulsion solvent diffusion method. Optimization of the microsponges was selected by drug loading efficiency. The optimized microsponges was formulated as topical gel and evaluated. The in vitro drug release, ex vivo drug deposition, primary skin irritancy study and in vivo antibacterial activity of  loaded formulations were studied. The spherical and porous microparticles were obtained. Moreover, the optimized microsponge possess particle size, entrapment efficiency and production yield and of 84.49 µm, 72.21% and 39.40% respectively. Microsponge loaded gels indicated controlled release, no irritancy to rat skin and antifungal activity. An in vivo skin deposition study proved three fold higher retention in the stratum corneum layer as compared with plain  gel. Microsponges-based gel formulations showed prolonged efficacy in a rat surgical wound model infected with Candida albicans. These results suggest that was stable in topical formulations and amplifying retention in the skin, indicating better potential of the delivery system for treatment of primary and secondary skin infections.

Keywords: Microsponges, Particle size, Entrapment efficiency, Primary skin irritancy, in vivo skin deposition Candida albicans.