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Pharmaceutics and Drug Design

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Full-Text Articles in Pharmacy and Pharmaceutical Sciences

Ultra-Fine Particle Formation Using Principle Of Rapid Expansion Of Supercritical Solutions`, Miraj Minesh Sheth Jan 2008

Ultra-Fine Particle Formation Using Principle Of Rapid Expansion Of Supercritical Solutions`, Miraj Minesh Sheth

Theses

There are indications in the chemical and pharmaceutical industries that the reduction in size of a crystalline particle can lead to better performance of the drug compound, particularly for water insoluble drugs, in the final dosage form. Many particle formation techniques have been investigated in recent years by researchers to obtain desired particulate sizes and size distributions. Supercritical fluid technologies have been successfully investigated for particle formation due to its unique gas/liquid properties in the supereritical state. In this report, results of particle formation using the principles of Rapid Expansion of Supercritical Solutions (RESS) have been documented.

In the RESS …


Physical And Computational Models Of Human Lung For Optimizing Respiratory Drug Delivery, Mohammed Ali Jan 2008

Physical And Computational Models Of Human Lung For Optimizing Respiratory Drug Delivery, Mohammed Ali

Theses and Dissertations

Respiratory drug particles aerosolized from the commercially available drug delivery devices may charge electrostatically. Investigations of the relevance of this charge on deposition in the human lung are just quite a few and they started early eighties though the aerosol science study is a decade old discipline. Additionally, the localized deposition of drug particles at desired sites such as inflamed tissue and appropriate receptors has been recognized by clinical investigators as being critical factors for the effective administration of respiratory drugs. To accomplish these tasks, it is imperative to undertake in vitro and in silico studies of medicinal drug aerosol …


Synthesis Of Novel Sulfonamide-Based Calpain Inhibitors And Their Potential As Anti-Tumor Agents, Jin Xu Dec 2007

Synthesis Of Novel Sulfonamide-Based Calpain Inhibitors And Their Potential As Anti-Tumor Agents, Jin Xu

Theses and Dissertations (ETD)

Calpain is a class of intracellular cytoplasmic cysteine proteases.1 The enzyme participates in different intracellular signaling pathways that are mediated by Ca2+.2 The two major isoforms of calpain universally distributed in most mammalian tissues are calpain 1 (µ-calpain) and calpain 2 (m-calpain). The exact in vivo function of the enzyme is not clear, but calpain has been implicated in a variety of physiological and pathological conditions,3 such as cancer, stroke, cardiac ischaemia, muscular dystrophy, cataract and Alzheimer’s disease. Calpain inhibitors are therefore of interest as therapeutic agents and as biomedical tools.

Several potent calpain inhibitors isolated from natural sources as …


Development And Evaluation Of Brain Tumor Targeted Liposome Delivery System For Paclitaxel, Murali Krishna Divi Dec 2007

Development And Evaluation Of Brain Tumor Targeted Liposome Delivery System For Paclitaxel, Murali Krishna Divi

Theses and Dissertations (ETD)

Primary brain tumors are a relatively common cause of cancer-related deaths. High-grade gliomas are the most common type of primary brain cancer, and the affected patients have a median survival of less than 1 year. Almost all malignant gliomas are incurable with the present standards of healthcare. Currently accepted therapeutic adjuvants to surgery, such as radiotherapy and chemotherapy, provide only a minor improvement in the disease course and life expectancy for patients diagnosed with malignant gliomas. Often, chemotherapy has failed to make any significant impact on the prognosis of disease because of significant local and systemic toxicity, problems with transport …


The Role Of Multi-Drug Resistance Associated Protein 4 And P-Glycoprotein In Resistance Of Neuroblastoma To Topotecan And Irinotecan, Patricia Kellie Turner Dec 2007

The Role Of Multi-Drug Resistance Associated Protein 4 And P-Glycoprotein In Resistance Of Neuroblastoma To Topotecan And Irinotecan, Patricia Kellie Turner

Theses and Dissertations (ETD)

High-risk neuroblastoma presents a significant therapeutic challenge because the 5-year survival rate remains less than 30% despite the use of surgery, multi-agent chemotherapy, radiation, and autologous bone marrow transplant. Novel therapeutic modalities are under development. The camptothecin analogs topotecan and irinotecan have been identified as successful cytotoxic agents. For topotecan, pharmacokinetically guided dosing to achieve a systemic exposure associated with preclinical anti-tumor activity in neuroblastoma xenograft models is feasible and has elicited favorable responses in children with high-risk neuroblastoma. However, some children with high-risk disease did not respond to the putatively effective topotecan systemic exposure. These children represent a subset …


Characterization Of A 30s Ribsomal Subunit Intermediate Found In Escherichia Coli Cells Growing With Neomycin And Paromomycin., Cerrone Renee Foster Aug 2007

Characterization Of A 30s Ribsomal Subunit Intermediate Found In Escherichia Coli Cells Growing With Neomycin And Paromomycin., Cerrone Renee Foster

Electronic Theses and Dissertations

The bacterial ribosome is a target for inhibition by numerous antibiotics. Neomycin and paromomycin are aminoglycoside antibiotics that specifically stimulate the misreading of mRNA by binding to the decoding site of 16S rRNA in the 30S ribosomal subunit. Recent work has shown that both antibiotics also inhibit 30S subunit assembly in Escherichia coli and Staphylococcus aureus cells. This work describes the characteristics of an assembly intermediate produced in E.coli cells grown with neomycin or paromomycin. Antibiotic treatment stimulated the accumulation of a 30S assembly precursor with a sedimentation coefficient of 21S. The particle was able to bind radio labeled antibiotics …


Novel Carbopol-Wax Blends For Controlled Release Oral Dosage Forms, Natarajansoundarapandian Mariageraldrajan May 2007

Novel Carbopol-Wax Blends For Controlled Release Oral Dosage Forms, Natarajansoundarapandian Mariageraldrajan

Theses and Dissertations (ETD)

Carbopol is crosslinked acrylic acid. Carbopol can be used in developing formulations for transdermal, oral, rectal use. It is forms strong gel in low concentration. Therefore, it can be used in low concentration in developing controlled release formulations. This increases the cost effectiveness and number of formulation options. In spite of its effectiveness, carbopol is one of the most efficient however underutilized polymer in oral controlled drug delivery system development. This is attributed to the difficulty in processing the carbopol. Carbopol has poor flow characteristics and stickiness. Objective of our research is to eliminate processing difficulties of carbopol using hot …


Effect Of Standard Treatment Guidelines With Or Without Prescription Audit On Prescribing For Acute Respiratory Tract Infection (Ari) And Diarrhoea In Some Thana Health Complexes (Thcs) Of Bangladesh, M. O. Faruk Khan, A.K. Azad Chowdhury, M. A. Matin, K. Begum, M. A. Galib Apr 2007

Effect Of Standard Treatment Guidelines With Or Without Prescription Audit On Prescribing For Acute Respiratory Tract Infection (Ari) And Diarrhoea In Some Thana Health Complexes (Thcs) Of Bangladesh, M. O. Faruk Khan, A.K. Azad Chowdhury, M. A. Matin, K. Begum, M. A. Galib

Pharmaceutical Science and Research

Inappropriate prescribing for ARI and diarrhoea is a serious health problem in many developing countries including Bangladesh. A baseline retrospective prescribing survey for ARI and diarrhoea have been conducted in randomly selected 60 thana health complexes (THCs) of Dhaka division of Bangladesh. In the 38 of 60 THCs, the prescribers did not comply with the standard treatment guidelines (STG) for ARI. They are marked as 'unsatisfactory performers'. In these THCs unnecessary antibiotics were prescribed in more than 50% of the encounters. The study further revealed that in 26 THCs, comprising 41.6% of the 38 THCs, the situation was even worse …


Trypanothione Reductase: A Viable Chemotherapeutic Target For Antitrypanosomal And Antileishmanial Drug Design, M. O. Faruk Khan Jan 2007

Trypanothione Reductase: A Viable Chemotherapeutic Target For Antitrypanosomal And Antileishmanial Drug Design, M. O. Faruk Khan

Pharmaceutical Science and Research

Trypanosomiasis and leishmaniasis are two debilitating disease groups caused by parasites of Trypanosoma and Leishmania spp. and affecting millions of people worldwide. A brief outline of the potential targets for rational drug design against these diseases are presented, with an emphasis placed on the enzyme trypanothione reductase. Trypanothione reductase was identified as unique to parasites and proposed to be an effective target against trypanosomiasis and leishmaniasis. The biochemical basis of selecting this enzyme as a target, with reference to the simile and contrast to human analogous enzyme glutathione reductase, and the structural aspects of its active site are presented. The …


Amankah Pengawet Makanan Bagi Manusia ?, Harmita Harmita Apr 2006

Amankah Pengawet Makanan Bagi Manusia ?, Harmita Harmita

Majalah Ilmu Kefarmasian

No abstract provided.


Preparation Of Silica-Coated Lanthanum-Strontium Manganite Particles With Designable Curie Point, For Application In Hyperthermia Treatments, Vuk Uskoković, Aljoša Košak, Miha Drofenik Mar 2006

Preparation Of Silica-Coated Lanthanum-Strontium Manganite Particles With Designable Curie Point, For Application In Hyperthermia Treatments, Vuk Uskoković, Aljoša Košak, Miha Drofenik

Pharmacy Faculty Articles and Research

Silica-coated lanthanum–strontium manganite particles with La0.76Sr0.24MnO3+δ stoichiometric formula, exhibiting Curie temperature at ∼40°C, were prepared by using a traditional solid-state method of synthesis of magnetic ceramic particles, followed by milling and a low-temperature coating procedure in an aqueous alcoholic alkali medium. The properties of the obtained material establish it as a potential candidate for self-regulated power-absorbing and temperature-controlling materials in hyperthermia treatments. Moreover, core-comprising LaSr–manganites with different stoichiometries, ranging from La0.5Sr0.5MnO3+δ to LaMnO3+δ, were synthesized, with magnetic and structural properties examined thereof. Herein reported findings can potentially be …


Cost Prevention Of Hiv, Jerika Lam Jan 2006

Cost Prevention Of Hiv, Jerika Lam

Pharmacy Faculty Articles and Research

"Since the introduction of highly active antiretroviral therapy (HAART) in the late 1990s, management of patients with human immunodeficiency virus (HIV) infection has improved where they are living longer and with fewer incidences of opportunistic illnesses. Furthermore, significant progress has been made in the understanding of the disease, the ability to quantify viral load and correlate with clinical outcomes, genotypic and phenotypic resistance assays designed to assess viral susceptibility, and a heightened awareness and appreciation of the importance of treatment adherence to ensure virologic suppression.' In spite of the benefits that HIV-infected patients may have acquired in terms of more …


Identifikasi Senyawa Antioksidan Dalam Spons Callyspongia Sp Dari Kepulauan Seribu, Endang Hanani Dec 2005

Identifikasi Senyawa Antioksidan Dalam Spons Callyspongia Sp Dari Kepulauan Seribu, Endang Hanani

Majalah Ilmu Kefarmasian

Antioxidant activity and identification of antioxidative compounds of Callyspongia sponge from Seribu Island (Kepulauan Seribu) were investigated. The sponge was extracted with acetone and the extract was concentrated using rotary vacuum evaporator. DPPH and tiocyanate methods were used to examine the antioxidant activity of the extract. The extract exhibited strong antioxidant activity in DPPH method with IC50 of 41.21 µg/ml. Chemical analysis indicated that the antioxidative compound in the sponge was alkaloid group.


Rna Therapeutic, Pendekatan Baru Dalam Terapi Gen, Amarila Malik Aug 2005

Rna Therapeutic, Pendekatan Baru Dalam Terapi Gen, Amarila Malik

Majalah Ilmu Kefarmasian

Some diseases, such as cancer, hereditary and genetic diseases, as well as viral infectious diseases, have been treated unsatisfied by the conventional therapy so far, and even more, by the gene therapy. Together with the pharmaceutical industries, researchers put their best effort to hunt some molecules that can be more favorable for such kind of therapy. After a pivotal study reported in May, 2001, it is certain that Ribonucleic acid (RNA) could effectively silence gene expression in mammalian cell line, so it was then proposed in 2004 the term RNA therapeutics. Antisense RNA therapy which came into the stage earlier …


Antitrypanosomal, Antileishmanial, And Antimalarial Activities Of Quaternary Arylalkylammonium 2-Amino-4-Chlorophenyl Phenyl Sulfides, A New Class Of Trypanothione Reductase Inhibitor, And Of N-Acyl Derivatives Of 2-Amino-4-Chlorophenyl Phenyl Sulfide, Seheli Parveen, M. O. Faruk Khan, Susan E. Austin, Simon L. Croft, Vanessa Yardley, Peter Rock, Kenneth T. Douglas Aug 2005

Antitrypanosomal, Antileishmanial, And Antimalarial Activities Of Quaternary Arylalkylammonium 2-Amino-4-Chlorophenyl Phenyl Sulfides, A New Class Of Trypanothione Reductase Inhibitor, And Of N-Acyl Derivatives Of 2-Amino-4-Chlorophenyl Phenyl Sulfide, Seheli Parveen, M. O. Faruk Khan, Susan E. Austin, Simon L. Croft, Vanessa Yardley, Peter Rock, Kenneth T. Douglas

Pharmaceutical Science and Research

Quaternization of the nitrogen atom of 2-amino-4-chlorophenyl phenyl sulfide analogues of chlorpromazine improved inhibition ∼40-fold (3′,4′-dichlorobenzyl-[5-chloro-2-phenylsulfan- ylphenylamino)-propyl]-dimethylammonium chloride inhibited trypanothione reductase from Trypanosoma cruzi with a linear competitive Ki value of 1.7 ( 0.2 µM). Molecular modelling explained docking orientations and energies by: (i) involvement of the Z-site hydrophobic pocket (roughly bounded by F396′, P398′, and L399′), (ii) ionic interactions for the cationic nitrogen with Glu-466′ or -467′. A series of N-acyl-2-amino-4-chlorophenyl sulfides showed mixed inhibition (Ki, Ki′ ) 11.3-42.8 µM). The quaternized analogues of the 2-chlorophenyl phenylsulfides had strong antitrypanosomal and antileishmanial activity in vitro against T. bruceirhodesiense STIB900, …


Mathematical Modeling Of Transient State Transdermal Drug Delivery, Alison Nickol Weltner May 2004

Mathematical Modeling Of Transient State Transdermal Drug Delivery, Alison Nickol Weltner

Theses

In this work, a two-pathway mathematical model for transdermal drug delivery with iontophoresis is presented. The partial differential equations are described and then solved. An alternative, two-pathway, three-layer model is also presented, and the implications of the coefficients within the equation are discussed. Using Franz cell iontophoretic delivery data from three drug substances (amitriptyline HCl, clomipramine HCl, and nortriptyline HCl), the two-pathway model is regressed to determine the diffusion coefficient and the concentration within the skin at the drug reservoir interface. ANOVA analysis indicates a correlation between iontophoretic current and concentration of drug within the stratum corneum.


Pembuatan Niosom Berbasis Maltodekstrin De 5-10 Dari Pati Singkong (Manihot Utilissima), Mahdi Jufri, Effionora Anwar, Joshita Djajadisastra Apr 2004

Pembuatan Niosom Berbasis Maltodekstrin De 5-10 Dari Pati Singkong (Manihot Utilissima), Mahdi Jufri, Effionora Anwar, Joshita Djajadisastra

Majalah Ilmu Kefarmasian

Niosomes are non ionic surfactant vesicles that have potential application in the delivery of hydrophobic or amphilic drugs. We developed proniosomes, a dry formulation using a maltodextrin as a carrier coated with non ionic surfactant, which can be used to produce niosomes within a minutes by addition of hot water followed by agitation. A novel method is reported here for rapid preparation of proniosomes with wide range of surfactant loading. Maltodextrin DE 5-10 was hidrolyzed from tapioca starch using Thermamyl L 120 da Novo at 85ºC. The result from SEM analyses shown that proniosomes appear very similar to the maltodextrin, …


Penyuluhan Penggunaan Oralit Untuk Menanggulangi Diare Di Masyarakat, Harianto Harianto Apr 2004

Penyuluhan Penggunaan Oralit Untuk Menanggulangi Diare Di Masyarakat, Harianto Harianto

Majalah Ilmu Kefarmasian

Diarrhea is one of the common deseases and a attack any level of ages. Diarrhea can be tuated effectively by using oralit to replace the lost of body water. To increase the use of oralit against diarrhea, this trestment should be socialized to public with undergo a general lecture to enhanced the public knowledges cncerning diarrhea and causing factors, to make a group discussion of senior citizen and public figures to build positive attitude in using oralit, and to demonstrate the processing of oralit/LGG and how to use it to people.


Pemberian Vaksin Melalui Tanaman Transgenik, Maksum Radji Apr 2004

Pemberian Vaksin Melalui Tanaman Transgenik, Maksum Radji

Majalah Ilmu Kefarmasian

Vaccines have played an important role in preventive medicine since Edward Jenner discovered that cowpox induced protection against human smallpox. Until recently, a vaccination has meant a needle in the arm. However, with the increasing need for inexpensive, easily administered vaccines, along with the improvements in genetic engineering, the concept of edible vaccines is fast becoming reality. This is especially important in developing countries, where it is estimated that three to five million children die each year from common diseases, which could have easily been prevented with the proper vaccination. Compared to traditional lab-synthesized vaccines, plants are capable of producing …


Pengaruh Kandungan Pati Singkong Terpregelatinasi Terhadap Karakteristik Fisik Tablet Lepas Terkontrol Teofilin, Juheini Juheini, Iskandarsyah Iskandarsyah, Animar J.A, Jenny Jenny Apr 2004

Pengaruh Kandungan Pati Singkong Terpregelatinasi Terhadap Karakteristik Fisik Tablet Lepas Terkontrol Teofilin, Juheini Juheini, Iskandarsyah Iskandarsyah, Animar J.A, Jenny Jenny

Majalah Ilmu Kefarmasian

In order to make use of pregelatinized Manihot starch in controlled release tablet, the research was done by heating the starch suspension up to its gelatinized temperatur, then dried. The particle size of pregelatinized Manihot starch used were (100-150 mesh) : (150-250 mesh) : smaller than 200 mesh = 3,5 : 1 : 1. The effect of pregelatinized Manihot starch on physical characteristic of Theophyllin controlled relase tablet was known by using 4 formulas containing variety of pregelatinized starch as follows: 30%, 40%, 50%, and 60%. Evaluation on the tablet results including tablet mass and size uniformity, hardness and friability. …


Pemanfaatan Maltodekstrin Pati Terigu Sebagai Eksipien Dalam Formula Sediaan Tablet Dan Niosom, Effionora Anwar, Joshita Djajadisastra, Arry Yanuar, Anton Bahtiar Apr 2004

Pemanfaatan Maltodekstrin Pati Terigu Sebagai Eksipien Dalam Formula Sediaan Tablet Dan Niosom, Effionora Anwar, Joshita Djajadisastra, Arry Yanuar, Anton Bahtiar

Majalah Ilmu Kefarmasian

The Use of Maltodextrin from Wheat Starch as an Exipient in Formula Tablet and Niosom dosage form. Wheat starch normally can be used as a tablet filler only, because the flow rate and binding capacity are not good enough. The wheat starch should be treated as follows : protein and amine free Bogasari wheat flour starch were hydrolyzed by α-amylase enzyme (Liquezym EX®) at variable temperature and time incubation to produce maltodextrin with different Dextrose Equivalent (DE) value. The maltodextrin could be used as tablet binder on wet granulation, tablet filler and binder on direct compress, a proniosom carrier to …


Optimasi Biotransformasi Total Sterol Limbah Tahu Menggunakan Mycobacterium Phlei Dsm 43286 Menjadi 1,4-Androstadien-3,17-Dion, Dengan Pengaruh Variasi Konsentrasi Inhibitor A, A’- Dipiridil, Maryati Kurniadi, Usman Sumo Friend Tambunan, Harmita Harmita Apr 2004

Optimasi Biotransformasi Total Sterol Limbah Tahu Menggunakan Mycobacterium Phlei Dsm 43286 Menjadi 1,4-Androstadien-3,17-Dion, Dengan Pengaruh Variasi Konsentrasi Inhibitor A, A’- Dipiridil, Maryati Kurniadi, Usman Sumo Friend Tambunan, Harmita Harmita

Majalah Ilmu Kefarmasian

Isolation of total sterol from waste product of soy bean cake has been conducted, followed by biotransformation to 1,4-androstadien-3,17-dione (ADD). The waste product consist of; β-sitosterol, stigmasterol, kaemfesterol, which are isolated by column chromatography technique using silica gel as stationary phase and chloroform as mobile phase. Biotransformation was conducted by using Mycobacterium phlei DSM 43286 in the present of α, α’- dipiridil as an inhibitor with concentration of 0,5; 1; 1,5; 2,0 mM. The main product of biotransformation were ADD and pregnenolon. The optimum yield of ADD 0,48% is achieved by adding 1,5 mM α, α’- dipiridil are two hours …


Probing Proteinase Active Sites Using Oriented Peptide Mixture Libraries – Adam-10, John L. Krstenansky, Jihong Wang, Gregg R. Chenail, Matthew R. Tiffany, Geoffrey M. Kuesters, Barbara C. Natke, John L. Nestor Jr. Jan 2004

Probing Proteinase Active Sites Using Oriented Peptide Mixture Libraries – Adam-10, John L. Krstenansky, Jihong Wang, Gregg R. Chenail, Matthew R. Tiffany, Geoffrey M. Kuesters, Barbara C. Natke, John L. Nestor Jr.

Pharmaceutical Science and Research

Oriented Peptide Mixture Libraries can provide a full matrix of preferred and disfavored amino acids at each subsite of an optimal substrate for a new proteinase. This approach is rapid and convenient, requiring only two mixture libraries to complete the analysis. In this paper we demonstrate an extension of this type of analysis, using a focused library employing unnatural amino acids to probe the depth of the S1 position in the catalytic site of the alpha secretase ADAM-10. This analysis indicates that ADAM- 10 will accept amino acids with substantial length and hydrophobicity (e.g. 2- naphthylalanine), but suggests that the …


Legal Movements In Intellectual Property: Trips, Unilateral Action, Bilateral Agreements, And Hiv/Aids, Margo A. Bagley Jan 2003

Legal Movements In Intellectual Property: Trips, Unilateral Action, Bilateral Agreements, And Hiv/Aids, Margo A. Bagley

Faculty Articles

This Article begins with an overview of the relationship between the Agreement on Trade-Related Aspects of Intellectual Property Rights (the "TRIPS Agreement") and the HIV/AIDS pandemic which created the need for the Doha Declaration. It then discusses two trade-related movements, unilateral action and TRIPS-plus bilateral agreements, that call into question the long-term effectiveness of the TRIPS Agreement process, generally, and the benefits of the Doha Declaration, in particular, in addressing multiple facets of the access to essential medicines problem. This Article concludes that a consideration of these issues should be included in the development of any further TRIPS-related solutions to …


Dextran-Methylprednisolone Succinate As A Prodrug Of Methylprednisolone: Plasma And Tissue Disposition, Xiaoping Zhang, Reza Mehvar Dec 2001

Dextran-Methylprednisolone Succinate As A Prodrug Of Methylprednisolone: Plasma And Tissue Disposition, Xiaoping Zhang, Reza Mehvar

Pharmacy Faculty Articles and Research

Plasma and tissue disposition of a macromolecular prodrug of methylprednisolone (MP), dextran (70 kDa)–methylprednisolone succinate (DMP), was studied in rats. Single 5‐mg/kg doses of DMP or unconjugated MP were administered into the tail veins of different groups of rats (n  = 4/group/time point). Blood (cardiac puncture) and tissues (liver, spleen, kidney, heart, lung, thymus, and brain) were collected at various times after DMP (0–96 h) or MP (0–2 h) injections. Concentrations of DMP and MP in samples were analyzed by size‐exclusion chromatography (SEC) and reversed‐phase high‐performance liquid chromatography (HPLC), respectively. Conjugation of MP with 70‐kDa dextran resulted in 22‐, …


Analysis Of Loratadine By Potentiometry And Reverse-Phase High Performance Liquid Chromatography, Kian Yong Puen Jan 2001

Analysis Of Loratadine By Potentiometry And Reverse-Phase High Performance Liquid Chromatography, Kian Yong Puen

Student Works (2000-2009)

A non-aqueous titration method was developed to assay Loratadine bulk active and a High Performance Liquid Chromatography (HPLC) method was developed to determine Loratadine's manufacturing impurity. The HPLC method was also suitable for simultaneously assay and related substance determination of Loratadine pharmaceutical preparations. In the tritation method, glacial acetic acid was chosen as an amphiprotic solvent. Loratadine ionised in glacial acetic acid; the conjugated base of acetic acid (Ac·), was then titrated with standardised perchloric acid. The method was validated found to be precise, linear and robust. Reverse-phase HPLC method using a Novapak Cl8 column with a CH3CN: I0mM K2HPO4 …


Novel Approaches For Designing 5'-O-Ester Prodrugs Of 3'-Azido-2'3'-Dideoxythymidine (Azt), Keykavous Parang, Leonard I. Wiebe, Edward E. Knaus Jan 2000

Novel Approaches For Designing 5'-O-Ester Prodrugs Of 3'-Azido-2'3'-Dideoxythymidine (Azt), Keykavous Parang, Leonard I. Wiebe, Edward E. Knaus

Pharmacy Faculty Articles and Research

3'-Azido-2'3'-dideoxythymidine (AZT, 1, zidovudine, RetrovirTM) is used to treat patients with human immunodeficiency virus (HIV) infection. AZT, after conversion to AZT-5'-triphosphate (AZT-TP) by cellular enzymes, inhibits HIV-reverse transcriptase (HIV-RT). The major clinical limitations of AZT are due to clinical toxicities that include bone marrow suppression, hepatic abnormalities and myopathy, absolute dependence on host cell kinase-mediated activation which leads to low activity, limited brain uptake, a sort half-life of about one hour in plasma that dictates frequent administration to maintain therapeutic drug levels, low potential for metabolic activation and/or high susceptibility to catabolism, and the rapid development of resistance by HIV-1. …


What Is The Risk Of Teratogenicity With The Use Of Selective Serotonin Reuptake Inhibitors During Pregnancy?, Michael Z. Wincor, Mary Gutierrez, Ann Nguyen Jan 1996

What Is The Risk Of Teratogenicity With The Use Of Selective Serotonin Reuptake Inhibitors During Pregnancy?, Michael Z. Wincor, Mary Gutierrez, Ann Nguyen

Pharmacy Faculty Articles and Research

"The lifetime prevalence of major depressive disorder in women is 10 to 25%, with an average age of onset in the mid-20s.1 Over the nine years that the selective serotonin reuptake inhibitors (SSRis) have been available, for many prescribers, they have become first-line agents in the treatment of depression. In addition, sorne of them are also being used in the treatment of obsessive- compulsive disorder and panic disorder. In light of these facts, itis not unlikely that women of childbearing age would be treated with one of the SSRis. In considering the risks of exposing a fetus to an SSRI, …


Effect Of Ibogaine On Morphine: Induced Modifications Of Palatability, Hardy Joseph Rideout Jan 1995

Effect Of Ibogaine On Morphine: Induced Modifications Of Palatability, Hardy Joseph Rideout

Theses and Dissertations (Comprehensive)

The ability of the potential anti-addictive agent ibogaine to module the morphine-induced modification of quinine and sucrose palatability was assessed utilizing the taste reactivity test. Ibogaine (40mg/kg) was administered 24 hr prior to an injection of morphine (2 mg/kg), followed 30 min later by a 5 min intraoral infusion of 0.05% quinine solution (Experiment 1) or 10% sucrose solution (Experiment 2). Treatment with morphine enhanced the palatability of both quinine and sucrose solution. Morphine reduced the aversiveness of quinine solution during the 5 min of testing and enhanced ingestive responding to sucrose solution, however, only during min 1 of the …


Transdermal Drug Permeation Enhancement Using Low Molecular Weight Primary Aliphatic Thiols, Robert M. Bennett Jan 1991

Transdermal Drug Permeation Enhancement Using Low Molecular Weight Primary Aliphatic Thiols, Robert M. Bennett

MUSC Theses and Dissertations

Current transdermal drug delivery systems are limited to delivery, via passive diffusion, of a few substances exhibiting natural skin penetrability. These substances are low molecular weight, highly potent agents possessing a certain degree of hydrophilicity as well as lipophilicity. These limitations are dictated by the outermost layer of the skin, the stratum corneum, which acts as a barrier. The stratum corneum consists mostly of the protein keratin. The barrier strength of keratin is attributed to its extensive disulfide bond cross-linking. In order to expand the spectrum of transdermal drug candidates this keratin barrier must be overcome. Low molecular weight primary …