Pharmaceutics and Drug Design Commons^™

Pengaruh Pemberian Kombinasi Ekstrak Air Akar Kucing (Acalypha Indica Linn.) Dengan Ekstrak Etanol 70% Rimpang Jahe Merah (Zingiber Officinale Rosc.) Terhadap Penurunan Kadar Asam Urat Tikus Putih, Anita Ayu Dwi Ajie Saputri, Juheini Amin, Azizahwati Azizahwati

Majalah Ilmu Kefarmasian

Hyperuricemia treatment can be given roots of Acalypha indica Linn. Combined with red ginger plant (Zingiber officinale Rosc.) as anti-inflammatory drug. This study aimed to examine the effect of aqueous extract the roots of Acalypha indica Linn. with 70%ethanol extract of rhizome of Red Ginger from the decrease in blood uric acid levels of male rats made hiperurisemia by potassium oxonate. There were 35 male white rats of Sprague Dawley strain weighing 180 g to 200 gs were divided into seven groups. Three groups were given a combination of extract, consist of a fixed dose 5.4 g/200 g bb of …

Optimasi Kecepatan Disintegrasi Tablet Terdisintegrasi Cepat (Fast Disintegrating Tablet) Domperidon Dengan Superdisintegran Sodium Starch Glycolate, Imam Prabowo, Iskandarsyah Iskandarsyah

Majalah Ilmu Kefarmasian

Fast disintegrating tablet is one of advanced pharmaceutical technologies. Fast disintegrating tablets is a tablet when placed on the tongue will be instantly disintegrated and releases the drug with the help of saliva. This technology can solve the problem of using oral drug in patients such as pediatrics, geriatrics or in circumstances where the patient can not swallow tablets conventionally with the help of water. The purpose of this study was to optimize the speed of disintegration in fast disintegrating tablet formulations both with varying concentrations of sodium starch glycolate. Optimization the speed of disintegration was done by using sodium …

Preclinical Pharmacology Of The Mdm2 Antagonist Nutlin-3a, Fan Zhang

Theses and Dissertations (ETD)

Nutlin-3a is an MDM2-p53 interaction antagonist that is under investigation in preclinical models for a variety of pediatric malignancies, including neuroblastoma, retinoblastoma, leukemia, and rhabdomyosarcoma. In the current research, we conducted preclinical pharmacology studies of nutlin-3a to evaluate the synergistic effect of the nutlin-3a and topotecan combination on neuroblastoma cell growth, to assess the effect of nutlin-3a on breast cancer resistance protein (BCRP), and to characterize the disposition of nutlin-3a in the mouse plasma and multiple tissues.

Activating the p53 pathway might offer a new therapy for neuroblastoma. In the first part of the study, we assessed the effect of …

Compound 49b: A Novel Beta-Adrenergic Receptor Agonist In The Treatment Of Diabetic Retinopathy, Kimberly Williams-Guy

Theses and Dissertations (ETD)

Diabetic retinopathy is the leading cause of blindness in working Americans. While there are therapeutic regimens for the disease, more effective methods are needed. We have previously shown that a non-specific beta-adrenergic receptor agonist, isoproterenol, was effective in preventing functional and morphological changes associated with diabetic retinopathy in the rat. Isoproterenol also produced left ventricle remodeling suggesting it entered the systemic circulation. We therefore synthesized various novel beta-adrenergic receptor compounds and screened these compounds in vitro for their ability to reduce markers of inflammation and apoptosis. Of the various compounds tested, Compound 49b was able to reduce both inflammation and …

Development And Evaluation Of Nano‑Scale Systems For Targeted Delivery To Treat Liver Fibrosis, Ningning Yang

Theses and Dissertations (ETD)

Excessive deposition of ECM is the common characteristic of liver fibrosis. During hepatic fibrosis, various inflammatory cytokines are released and trigger the activation of quiescent HSCs. The activated HSCs play the major role in producing extra amount collagen. It becomes very crucial to focus on HSCs to find out therapeutics, such as inhibiting collagen synthesis, inhibiting activation to myofibroblasts, or controlling inflammation.

To control excessive collagen synthesis, one triplex forming oligonucleotides (TFO), was systemically administrated to prevent type I collagen mRNA transcription. To enhance circulation time and targeted delivery efficiency, TFO was conjugated to M6P‑HPMA and showed efficient targeted delivery …

Reactive Oxygen Species Modulation Of Na/K-Atpase Regulates Fibrosis And Renal Proximal Tubular Sodium Handling, Jiang Liu, David J. Kennedy, Yanling Yan, Joseph I. Shapiro Md

Pharmaceutical Science and Research

The Na/K-ATPase is the primary force regulating renal sodium handling and plays a key role in both ion homeostasis and blood pressure regulation. Recently, cardiotonic steroids (CTS)-mediated Na/K-ATPase signaling has been shown to regulate fibrosis, renal proximal tubule (RPT) sodium reabsorption, and experimental Dahl salt-sensitive hypertension in response to a high-salt diet. Reactive oxygen species (ROS) are an important modulator of nephron ion transport. As there is limited knowledge regarding the role of ROS-mediated fibrosis and RPT sodium reabsorption through the Na/K-ATPase, the focus of this review is to examine the possible role of ROS in the regulation of Na/K-ATPase …

Acetaminophen: Beyond Pain And Fever-Relieving, Eric R. Blough, Miaozong Wu

MIIR Faculty Research

Acetaminophen, also known as APAP or paracetamol, is one of the most widely used analgesics (pain reliever) and antipyretics (fever reducer). According to the U.S. Food and Drug Administration, currently there are 235 approved prescription and over-the-counter drug products containing acetaminophen as an active ingredient. When used as directed, acetaminophen is very safe and effective; however when taken in excess or ingested with alcohol hepatotoxicity and irreversible liver damage can arise. In addition to well known use pain relief and fever reduction, recent laboratory and pre-clinical studies have demonstrated that acetaminophen may also have beneficial effects on blood glucose levels, …

Percobaan Sintesis 4-(4-Metoksibenzilidena) 2-Metiloksazol-5-On Dari Asetilglisin Dan 4-Metoksibenzaldehid, Arif Arrahman, Hayun Hayun, Arry Yanuar

Majalah Ilmu Kefarmasian

Compound 4-(4-methoxybenzylidene)-2-methyloxazole-5-one was one of oxazolone moety derivative. Oxazolones had several different pharmacological activity depend on substituent which was bonded to oxazolone ring. Oxazolones was an important precursor for synthesizing several compounds which had pharmacological activity. For that reason, experiment to synthesize 4-(4-methoxybenzylidene)-2-methyloxazole-5-one from acetyl- glicine and 4-methoxybenzaldehyde as an oxazolone derivative become necessary. Com- pound 4-(4-methoxybenzylidene)-2-methyloxazole-5-one was synthesized over two step of reaction. First step was reacted glycine with acetic anhydride in acidic environment yielded acetylglycine. Second step was reacted acetylglycine with 4-methoxybenzaldehyde yielded 4-(4-methoxybenzylidene)-2-methyloxazole-5-one. The product, which was collected in every step, was purified by washing and recrystalization …

Efek Nefroprotektif Infus Daun Sukun (Artocarpus Altilis (Park.) Fsb.) Pada Tikus Jantan Yang Diinduksi Karbon Tetraklorida, Rianti Adi Cahyaningsih, Azizahwati Azizahwati, Dadang Kusmana

Majalah Ilmu Kefarmasian

Renal dysfunction can be caused by several factors, including hypertension, urinary tract obstruction, autoimmune disorders, urinary tract infection, diabetes mellitus, consumption of drugs that affect nephrotoxic and antibiotic from aminoglycoside class. Breadfruit leaves (Artocarpus altilis (Park.) Fsb.) is a traditional plant that hasbeen used empirically to treat kidney diseases. The research has been done to figure out the nephroprotective effect of breadfruit leaves infusion on white male rats strain Sprague-Dawley previously induced by carbon tetrachloride. There were 25 rats which were divided randomly into five groups. Group I which was the normal control group received CMC 0,5%. Group II which …

Uji Penghambatan Tirosinase Dan Stabilitas Fisik Sediaan Krim Pemutih Yang Mengandung Ekstrak Kulit Batang Nangka (Artocarpus Heterophyllus), Ninin Kartika Juwita, Joshita Djajadisastra, Azizahwati Azizahwati

Majalah Ilmu Kefarmasian

The cortex of jackfruit (Artocarpus heterophyllus) contains some flavonoids which have activity as tyrosinase inhibitors. This compound can inhibit the oxidation of l-tyrosine and levodopa in the mechanism of melanogenesis. The extract of jackfruit cortex formulated into creams differentiated by the extract concentration of 1,5% and 2,0%. Physical stability test was conducted with storing the creams at three different temperatures, 7 ± 2°, 27 ± 2°, and 40±2°C respectively. Centrifugal tests and cycling test was also performed on both cream. Tyrosinase inhibitory activity measurement was done by in vitro studies with measuring dopachrome. The result showed that both of formulations …

Formulasi Sediaan Granul Mukoadhesif Kombinasi Ekstrak Kulit Batang Mimba (Azadirachta Indica A. Juss) Dan Kunyit (Curcuma Domestica Val.), Sutriyo Sutriyo, Khairunnisya Khairunnisya, Abdul Mun’Im

Majalah Ilmu Kefarmasian

Neem bark (Azadirachta indica A.Juss) and turmeric (Curcuma domestica Val.) extracts have been found posses gastroprotective effect so that they are used in the treatment of gastric ulcer. Administration of combination of both extracts can give synergistic effect so that the administration dose can be reduced. In this research, combination of neem bark and turmeric extracts were formulated as mucoadhesive granules to improve their effectivenesses by increasing the residence time of dosage form in the stomach. Mucoadhesive granules were prepared by wet granulation method in six formulas using HPMC, Carbopol, and combination of HPMC and Carbopol as mucoadhesive polymers. Granules …

Analisis Kandungan Ion Fluorida Pada Sampel Air Tanah Dan Air Pam Secara Spektrofotometri, Yodifta Astriningrum, Herman Suryadi

Majalah Ilmu Kefarmasian

Fluoride ion is one of the compounds that are known to have benefits in the prevention of dental caries when used in certain concentrations, but also hasnegative effects that may cause the occurrence of dental and bone fluorosis when the intake was in excessive concentration. One of the fluoride intakes comes fromwater that is consumed. The aim of this research was to identify and measurefluoride ion levels in groundwater and piped water that used as drinking water consumption in the community. Measurement of fluoride ion concentration isdone by using visible spectrophotometry at the maximum wavelength of 586 nm using the …

A System Dynamics Model Of Pharmaceutical Opioids: Medical Use, Diversion, And Nonmedical Use, Teresa Schmidt, Wayne Wakeland, J. David Haddox

Complex Systems Faculty Publications and Presentations

A dramatic rise in the nonmedical of pharmaceutical opioids has presented the United States with a substantial public health problem. Nonmedical use of prescription pain relievers has become increasingly prevalent in the US over the last two decades, and diversion of medicines obtained by prescription is assumed to be a major source of supply for nonmedical opioid use. Policymakers striving to protect population health by ameliorating the adverse outcomes of nonmedical use of opioid analgesics could benefit from a systems-level model which reflects the complexity of the system and incorporates the full range of available data. To address this need, …

Transdermal And Transbuccal Delivery Of Lidocaine And Nicotine : Combined Effects Of Iontophoresis And Chemical Enhancers, Ran Wei

Theses

This study focused on the effects of iontophoresis and chemical enhancers on drug release. The transport of Lidocaine HCl (LHCl) and Nicotine Hydrogen Tartrate (NHT) through the skin and mucosa was evaluated for potential clinical applications. These two potential delivery routes have the advantage of avoiding first-pass effect. Samples were pretreated with enhancer solutions for one hour before the experiments. Passive or 0.3 mA iontophoresis-assisted drug diffusion was conducted for 8 hours to monitor the cumulative amount of drug released. Graphical methods and mathematical optimization techniques were implemented to analyze the data. The effects of chemical enhancers on the delivery …

Dissolution Of Disintegrating Solid Dosage Forms In A Modified Dissolution Testing Apparatus 2, Shrutiben Rameshbhai Parekh

Theses

Dissolution tests are routinely carried out in the pharmaceutical industry to determine the dissolution rate of solid dosage forms. Dissolution testing serves as a surrogate for drug bioavailability through in vitro–in vivo correlation (IVIVR), and it additionally helps in guiding the development of new formulations and in assessing lot-to-lot consistency, thus ensuring product quality. The United States Pharmacopoeia (USP) Dissolution Testing Apparatus 2 is the device most commonly used for this purpose. Despite its widespread use, dissolution testing using this apparatus remains susceptible to significant error and test failures. There is documented evidence that this apparatus is sensitive to several …

Dissolution Testing Of Prednisone And Salicylic Acid Calibrator Tablets At Different Tablet Locations, Anandhavalavan Arulmozhi

Theses

Dissolution testing is routinely carried out in the pharmaceutical industry to determine the rate of dissolution of solid dosage forms. This test is one of the several tests that pharmaceutical companies typically conduct on oral dosage formulations (e.g., tablets) to determine compliance. The USP Dissolution Testing Apparatus 2 is the most common of the apparatuses listed in the USP. However, it has been shown previously that the dissolution profile of a tablet undergoing dissolution in the USP Dissolution Apparatus 2 can be affected by the tablet location in the apparatus.

In this work, the dissolution rates of both non-disintegrating tablets …

The Design And Synthesis Of Autotaxin Inhibitors And Analogs Of Lysophosphatidic Acid, Renuka Niranjan Gupte

Theses and Dissertations (ETD)

Lysophosphatidic acid (LPA) is a naturally occurring bioactive phospholipid. It has a wide array of biological effects like cell proliferation, survival, migration, apoptosis invasion, wound healing and angiogenesis. Autotaxin (ATX) was identified as an autocrine tumor cell motility factor from A2058 melanoma conditioned medium. ATX has lysophospholipase D enzyme activity and is responsible for the cleavage of lysophophatidylcholine (LPC) leading to the generation of LPA. Antagonists of Autotaxin would have a potential therapeutic application in cancer research. Chapter 1 is an introduction of LPA and autotaxin. It provides the background and significance of the research. Chapter 2 explores the synthesis …

Rna Interference For Improving The Outcome Of Islet Transplantation And Polymeric Micelle‑Based Nanomedicine For Cancer Therapy, Feng Li

Theses and Dissertations (ETD)

Ex vivo gene transfer has been used to improve the outcome of islet transplantation for treating type I diabetes. RNA interference is an effective approach for reducing gene expressions at the mRNA level. The application of RNA interference to improve the outcome of islet transplantation was reviewed in Chapter 2, where I summarized biological obstacles to islet transplantation, various types of RNAi techniques, combinatorial RNAi in islet transplantation, and different delivery strategies.

Upregulation of inducible nitric oxide synthase (iNOS) and subsequent product of radical nitric oxide (NO) impair islet β cell function. Therefore, we hypothesized that iNOS gene silencing could …

Pharmacokinetic And Pharmacodynamic Studies Of A Novel Spectinamide Series Of Antituberculosis Agents, V. N. R. Pavan Kumar Vaddady

Theses and Dissertations (ETD)

Spectinamides are novel amide derivatives of the antibiotic spectinomycin that have emerged as a new class of agents to treat tuberculosis. These agents showed potent in vitro activity against Mycobacterium tuberculosis (MTB) compared to spectinomycin and in a preliminary in vivo study in interferon gamma (IFN‑γ) knockout mice, spectinamide Lee1329 reduced the lung bacillary load of TB comparable to streptomycin. We hypothesized that the application of an iterative pharmacokinetics and pharmacodynamics (PK/PD) guided approach would facilitate the optimization of these lead compounds suitable for further development.

A series of in vitro experiments including parallel artificial membrane permeability assay (PAMPA), microsomal …

Pembuatan Sediaan Tablet Mengapung Famotidin Menggunakan Kompleks Polielektrolit Kitosan-Pektin Sebagai Bahan Matriks, Erny Sagita, Effionora Anwar, Silvia Surini

Majalah Ilmu Kefarmasian

Floating tablet is one of the drug delivery system retained in the stomach which aims to prolong the lag time of the drug in the stomach. This principle can be used to improve the efficacy of famotidine in treating diseases in the stomach The purpose of this research is to develop dosage form afloat by using Chitosan Pectin Electrolytes (PEC) as matrix then used as the matrix in tablet dosage form with famotidine as a drug model. PEC also combined with hydroxypropylmethylcellulose (HPMC) with different. PEC was also combined with hydroxypropilmethylcellulose (HPMC) in different concentrations. The results of the dissolution …