Pharmaceutics and Drug Design Commons^™

Lung Disposition Model-Based Analyses Of Clinical Pharmacokinetic Profiles For Inhaled Drugs, Anuja Raut

Theses and Dissertations

There has been a desire to accurately interpret the inhaled pharmacokinetic (PK) profiles of drugs in humans to aid successful inhaled drug and product developments. However, challenges are layered, as 1) the drug dose delivered to the lung (DTL) from inhalers is a portion of the formulated dose but rarely determined; 2) lung delivery and regional deposition differ, depending on drug, formulation and inhaler; 3) drugs are not only absorbed from the lung but may also be from the gastrointestinal (GI) tract; and 4) in addition to absorption into the systemic circulation, multiple non-absorptive processes also eliminate drugs from the …

Inhibition Of Oxidative And Conjugative Metabolism Of Buprenorphine Using Generally Recognized As Safe (Gras) Compounds Or Components Of Dietary Supplements, Neha V. Maharao

Theses and Dissertations

This dissertation aimed at developing an inhibitor strategy to improve the oral bioavailability (F_oral) and systemic exposure (AUC_∞) of buprenorphine (BUP) as well as reduce the variability associated with them. Twenty-seven generally recognized as safe (GRAS) compounds or dietary substances were evaluated for their potential to inhibit the oxidative and conjugative metabolism of BUP, using pooled human intestinal and liver microsomes. In both the organs, oxidation appeared to be the major metabolic pathway with a 6 fold (intestine) and 4 fold (liver) higher intrinsic clearance than glucuronidation. Buprenorphine was predicted to show low and variable F …

Pharmaceutical M&A Activity: Effects On Prices, Innovation, And Competition, Barak D. Richman, Will Mitchell, Elena Vidal, Kevin Schulman

Faculty Scholarship

The rise of blockbuster pharmaceutical acquisitions has prompted fears that unprecedented market concentration will weaken competition. Two of the most prominent concerns focus on the upstream and downstream ends of the pharmaceutical industry: (1) the concern that these mergers will concentrate the market for discovery and will therefore lead to fewer discoveries; and (2) the concern that merging large marketing, sales, and distribution forces will strengthen the hands of select pharmaceutical manufacturers and weaken downstream competition. Having considered potential dynamic effects in the industry and conducted a series of preliminary interviews with knowledgeable observers, though, this Article argues that neither …

Engineered Peptides For Applications In Cancer-Targeted Drug Delivery And Tumor Detection, R. Soudy, N. Byeon, Y. Raghuwanshi, S. Ahmed, A. Lavasanifar, Kamaljit Kaur

Pharmacy Faculty Articles and Research

Cancer-targeting peptides as ligands for targeted delivery of anticancer drugs or drug carriers have the potential to significantly enhance the selectivity and the therapeutic benefit of current chemotherapeutic agents. Identification of tumor-specific biomarkers like integrins, aminopeptidase N, and epidermal growth factor receptor as well as the popularity of phage display techniques along with synthetic combinatorial methods used for peptide design and structure optimization have fueled the advancement and application of peptide ligands for targeted drug delivery and tumor detection in cancer treatment, detection and guided therapy. Although considerable preclinical data have shown remarkable success in the use of tumor targeting …

Perbandingan Efek Larvasida Minyak Atsiri Daun Cengkeh (Syzygium Aromaticum L.) Varietas Zanzibar Dengan Temephos Terhadap Larva Nyamuk Aedes Aegypti, Ridzmullah Wishnu Pamungkas, Neneng Syarifah Syafei, Arto Yuwono Soeroto

Pharmaceutical Sciences and Research

The use of temephos as larvicides in disease prevention Dengue Hemorrhagic Fever (DHF) in Indonesia has been going on for 40 years. Larviciding very long led the resistance to temephos. Cloves, one of native Indonesia plant contains eugenol that are toxic to the insect’s body. This study aims to examine the effectiveness of Zanzibar clove leaf essential oil compared to temephos in killing the larvae of Aedes aegypti. This study uses experimental laboratory research design. The samples are larvae of Aedes aegypti stage III. The mosquito larvae were classified into six groups, each given a clove leaf essential oil with …

Assessment Of Achieved Systolic Blood Pressure In Newly Treated Hypertensive Patients Aged 60-79 Years Before And After Eighth Joint National Committee Recommendations, Michael S. Kelly, Joseph J. Saseen, Joel C. Marrs

Pharmacy Faculty Articles and Research

Objective:

To determine whether patients who were newly prescribed antihypertensive therapy after the Eighth Joint National Committee (JNC 8) update were treated to a relaxed systolic blood pressure (SBP) goal compared with patients treated before the update.

Methods:

A retrospective cohort study approved by the Colorado Multiple Institutional Review Board. Patients aged 60–79 years, without diabetes or chronic kidney disease (CKD), newly treated for hypertension at a University of Colorado primary care clinics were included. The mean first-achieved and last-stable SBPs of patients newly prescribed antihypertensive medications from 1 January 2012 to 31 December 31 2013 (before cohort) were compared …

Uji Aktivitas Anti-Inflamasi Minyak Atsiri Daun Kemangi (Ocimum Americanum L.) Pada Tikus Putih Jantan Yang Diinduksi Karagenan, Fadlina Chany Saputri, Rita Zahara

Pharmaceutical Sciences and Research

Kemangi (Ocimum americanum L.) is an aromatic plant that contains citral and known as anti-inflammatory agents. The aim of this study was to determine the anti-inflammatory activity of the essential oil kemangi leaves on carrageenan-induced rat. The male rats were divided into six groups, each consisting of four rats. Group I as negative control was given 0.5% CMC solution, group II as positive control was given diclofenac sodium, group III was given sitral, groups IV, V and VI were given 40 mg/200 g BW, 80 mg/200 g BW, and 160 mg/200 g BW essential oil of Ocimum americanum L., emulsified …

Pengaruh Cara Pengeringan Simplisia Daun Senggani (Melastoma Malabathricum L.) Terhadap Aktivitas Antioksidan Menggunakan Metode Dpph (2,2-Difenil-1-Pikrilhidrazil), Sri Luliana, Nera Umilia Purwanti, Kris Natalia Manihuruk

Pharmaceutical Sciences and Research

Drying is the most important step to keep the compound stability in simplicia. The objective of this research is to know the effect of drying methods on antioxidant activity in Melastoma malabathricum L. The drying methods tested were oven-drying at 40°C, direct sunlight, indirect sunlight, air-drying at ± 25°C and fresh samples as control. Result revealed that the drying methods of simplicia were significant differences for antioxidant activity in Melastoma malabathricum L. (p < 0,05). Drying method that has the highest antioxidant activity was by air-drying at ± 25°C is 54.60 %.

Efektivitas Snedds Ekstrak Kulit Manggis Terhadap Bakteri P. Mirabilis Dan S. Epidermidis Yang Terdapat Pada Ulkus Diabetik, Rafika Sari, Liza Pratiwi, Pratiwi Apridamayanti

Pharmaceutical Sciences and Research

Mangosteen rind possesses the ability to conduct antibacterial activity. Under the development relating to drug delivery system, SNEDDS were known to boost the penetration of active compound. The aim of this research is to compare the effectiveness of the antibacterial activity at both SNEDDS preparation and the ethanol extract of mangosteen rind as the antibacteria against the bacteria that cause diabetic ulcers with the most prevalence whether it was Gram positive or Gram negative bacteria like Proteus mirabilis and Staphylococcus epidermidis. The research started by maceration process with the crude extract as the result continued with the phytochemical screening which …

Comparison Of Outcomes Following A Switch From A Brand To An Authorized Vs. Independent Generic Drug, Richard Hansen, Jingjing Qian, Richard L. Berg, James G. Linneman, Enrique Seoane-Vazquez, Sarah Dutcher, Saeid Raofi, C. David Page, Peggy L. Peissig

Pharmacy Faculty Articles and Research

Authorized generics are identical in formulation to brand drugs, manufactured by the brand company but marketed as a generic. Generics, marketed by generic manufacturers, are required to demonstrate pharmaceutical and bioequivalence to the brand drug, but repetition of clinical trials is not required. This retrospective cohort study compared outcomes for generics and authorized generics, which serves as a generic vs. brand proxy that minimizes bias against generics. For the seven drugs studied between 1999-2014, 5,234 unique patients were on brand drug prior to generic entry and 4,900 (93.6%) switched to a generic. During the 12-months following the brand-to-generic switch, patients …

Polymeric Nanocarriers For Delivery Of Small Molecules And Mirnas For The Treatment Of Liver Fibrosis And Pancreatic Cancer, Virender Kumar

Theses & Dissertations

The aim of this thesis is to develop combination therapy of small molecules and miRNAs for treating liver fibrosis and pancreatic cancer. New amphiphilic biodegradable polymers capable of carrying small hydrophobic molecules and hydrophilic anionic nucleic acids were synthesized, characterized and evaluated in vitro and in vivo liver fibrosis and pancreatic cancer mouse models.

In Chapter 1, an overview of liver fibrosis, current treatments and the role of miRNAs in liver fibrosis as well as the design of their delivery systems is given. Further, a general introduction to pancreatic cancer and role of miRNAs in pancreatic cancer is given. In …

Development Of Cxcr4-Inhibiting Nanoparticles For The Treatment Of Metastatic Cancer, Yan Wang

Theses & Dissertations

Metastasis is the main cause of cancer mortality and morbidity, leading to several million deaths every year. Less than 20% of pancreatic cancer (PC) patients are candidates for surgery due to spread beyond the pancreas. Desmoplasia presents substantial barriers to perfusion, diffusion, and convection of antitumor therapeutics into the PC tissues. We focus on developing novel therapies that regulates tumor microenvironment, chemosensitizing tumor to therapeutics and preventing metastasis.

Gene therapy is emerging as a promising new therapeutic agents for cancer treatment. A targeted, systemic, effective and safe gene delivery system should be developed. CXCR4/SDF-1 axis plays a crucial role in …

Mechanism Of Interaction Of Peptide Modified Nanoparticles With Porphyromonas Gingivalis., Ankita Jain

Electronic Theses and Dissertations

Studies suggest that P. gingivalis functions as a keystone pathogen and interacts with primary colonizers in the supragingival biofilm such as S. gordonii. This interaction contributes to the initial colonization of the oral cavity by P. gingivalis and thus represents a potential target for therapeutic intervention. We have identified a peptide (BAR) derived from the streptococcal SspB protein that functions to inhibit P. gingivalis adherence to S. gordonii. In addition, we showed that nanoparticles (NPs) functionalized with BAR inhibit this interaction more potently than free soluble peptide, possibly by promoting interaction with P. gingivalis at higher valency than …

Carriers For The Tunable Release Of Therapeutics: Etymological Classification And Examples, Vuk Uskoković, Shreya Ghosh

Pharmacy Faculty Articles and Research

Introduction—Physiological processes at the molecular level take place at precise spatiotemporal scales, which vary from tissue to tissue and from one patient to another, implying the need for the carriers that enable tunable release of therapeutics.

Areas Covered—Classification of all drug release to intrinsic and extrinsic is proposed, followed by the etymological clarification of the term “tunable” and its distinction from the term “tailorable”. Tunability is defined as analogous to tuning a guitar string or a radio receiver to the right frequency using a single knob. It implies changing a structural parameter along a continuous quantitative scale and …

Validasi Metode Analisis Ofloksasin Dalam Plasma In Vitro Secara Kromatografi Cair Kinerja Tinggi-Fluoresensi Mengacu Pada European Medicines Agency Guideline, Letitia Tania, Eme Stepani Sitepu, Yahdiana Harahap

Pharmaceutical Sciences and Research

Ofloxacin is an antibiotic from second generation of fluoroquinolones group. Concentration of ofloxacin in human plasma is in low level, and due to that fact, it requires a selective, accurate, sensitive method of analysis. In this study, the optimization and validation of ofloxacin analysis in human plasma using high performance liquid chromatography-fluorescence with ciprofloxacin-HCl as an internal standard were carried out. Separation of ofloxacin was performed using C18 (Waters, SunfireTM 5 µm; 250 x 4.6 mm) column with an isocratic mobile phase consisted of triethylamine 1% in water pH 3.0–acetonitrile (84:16) in the flow rate of 1.0 mL/min, 40oC column …

Skrining Aktivitas Antibakteri Bakteriosin Dari Minumance Hun Tiau, Rafika Sari, Lia Deslianri, Pratiwi Apridamayanti

Pharmaceutical Sciences and Research

Lactic acid bacteria is one of the beneficial bacteria because it can produce an antimicrobial peptide called bacteriocin. Bacteriocin has been applied as a natural food preservative because it effectively prevents the growth of pathogenic bacteria in food or drink. This study aims to identify the lactic acid bacteria as producers of bacteriocin from Ce hun tiau which have inhibitory activity againts pathogenic bacteria such as Escherichia coli, Staphylococus aureus and Salmonella typhi. In this study, Lactic acid bacteria were isolated from Ce Hun Tiau using streak plate method on media deMan Rogose Sharpe. Screening bacteriocin using disc diffusion method …

Optimasi Kombinasi Karbopol 940 Dan Hpmc Terhadap Sifat Fisik Gel Ekstrak Dan Fraksi Metanol Daun Kesum (Polygonum Minus Huds.) Dengan Metode Simplex Lattice Design, Rafika Sari, Siti Nani Nurbaeti, Liza Pratiwi

Pharmaceutical Sciences and Research

Indonesia especially Kalimantan Barat well known by its biodiversity, one of the potential resource is Kesum leaves. Kesum leaves are potential by its antibacterial effect, so that it can be formulated into pharmaceutical dosage form, especially gel. This research aims to know the best comparison between Carbopol 940 and Hydroxypropyl methylcellulose (HPMC) gel base affecting the physical stability of methanol extract and fraction of kesum leaves gel by Simplex Lattice Design (SLD) method. Gels were prepared into three variation base such as gel A (100% Carbopol - 0% HPMC); gel B (0% Carbopol - 100% HPMC); and gel C (50% …

Potensi Ekstrak Etanol Daun Petai (Parkia Speciosa Hassk.) Terhadap Kadar Superoksida Dismutase (Sod) Pada Plasma Tikus Yang Mengalami Stres Oksidatif, Ruth Haryati Butarbutar, Robiyanto Robiyanto, Eka Kartika Untari

Pharmaceutical Sciences and Research

Cigarette smoke is free radicals superoxide resources that contains, hydrogen peroxide, hidrosil and peroksil. Superoxide dismutase (SOD) is an enzymatic antioxidants that protect cells from oxidative stress by catalyzing superoxide dismutase (O2 *) into O2 and H2O2 . This study aims to determine the potential of ethanolic extract petai leaves against plasma SOD enzyme activity in animals exposed by cigarette smoke. The simplicia extracted by maseration using ethanol 96%. Thirty-six rats Sprague Dawley strain were divided into six groups: normal group was not given treatment, negative group received 10% CMC-Na, positive control group received vitamin E, and treatment group received …

Antibiotic Sensitivity In Pseudomonas Aeruginosa Of Diabeticpatient’S Foot Ulcer, Pratiwi Apridamayanti, Khairunnisa Azani Meilinasary, Rafika Sari

Pharmaceutical Sciences and Research

Diabetes Mellitus (DM) patients are at risk to have the diabetic ulcer. The main reason for DM’s patient with ulcer complication to be treated and healed in hospital is bacterial infection. One of many bacteria that infects diabetic ulcer is Pseudomonas aeruginosa. The effort to treat this infection is by using antibiotic. The use of antibiotic unfortunately, is often found inaccurate causing the microbe resistance to occur. To choose the right antibiotic, it needs to test the antibiotic’s sensitivity towards Pseudomonas aeruginosa. The aim of this study is to determine the sensitivity of antibiotics against Pseudomonas aeruginosa. Sample used was …

Long-Acting Antiretroviral Nanoformulation Development And Subcellular Trafficking, Dongwei Guo

Theses & Dissertations

The introduction of nanoformulated antiretroviral therapeutic regimens is a promising alternative to standard once a day oral treatment of HIV infection. Our lab has pioneered this effort and was successful in harnessing mononuclear phagocytes (monocytes, dendritic cells and macrophages) as nanoformulated drug carriers. The approach was developed as Trojan horses for drug transport, delivery and distribution to sites of viral replication in order to facilitate microbial elimination in HIV sanctuaries. However, the remaining challenges for current antiretroviral nanoformulations include to formulate a broad range of hydrophilic short-acting drugs, and to elucidate the mechanism of sequestered nanoparticles in macrophages at the …