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Fulltext Protective Effect of Sundarban Honey against Acetaminophen-Induced Acute Hepatonephrotoxicity in Rats

Afroz R, Tanvir EM, Hossain MF, Gan SH, Parvez M, Aminul Islam M, et al.

Evid Based Complement Alternat Med, 2014;2014:143782.
PMID: 25530774 DOI: 10.1155/2014/143782

Honey, a supersaturated natural product of honey bees, contains complex compounds with antioxidant properties and therefore has a wide a range of applications in both traditional and modern medicine. In the present study, the protective effects of Sundarban honey from Bangladesh against acetaminophen- (APAP-) induced hepatotoxicity and nephrotoxicity in experimental rats were investigated. Adult male Wistar rats were pretreated with honey (5 g/kg) for 4 weeks, followed by the induction of hepatotoxicity and nephrotoxicity via the oral administration of a single dose of APAP (2 g/kg). Organ damage was confirmed by measuring the elevation of serum alkaline phosphatase (ALP), alanine transaminase (ALT), aspartate transaminase (AST), total protein (TP), total bilirubin (TB), urea, creatinine, and malondialdehyde (MDA). Histopathological alterations observed in the livers and the kidneys further confirmed oxidative damage to these tissues. Animals pretreated with Sundarban honey showed significantly markedly reduced levels of all of the investigated parameters. In addition, Sundarban honey ameliorated the altered hepatic and renal morphology in APAP-treated rats. Overall, our findings indicate that Sundarban honey protects against APAP-induced acute hepatic and renal damage, which could be attributed to the honey's antioxidant properties.

Matched MeSH terms: Administration, Oral
Fulltext Artesunate-mefloquine versus chloroquine for treatment of uncomplicated Plasmodium knowlesi malaria in Malaysia (ACT KNOW): an open-label, randomised controlled trial

Grigg MJ, William T, Menon J, Dhanaraj P, Barber BE, Wilkes CS, et al.

Lancet Infect Dis, 2016 Feb;16(2):180-188.
PMID: 26603174 DOI: 10.1016/S1473-3099(15)00415-6

BACKGROUND: The zoonotic parasite Plasmodium knowlesi has become the most common cause of human malaria in Malaysia and is present throughout much of southeast Asia. No randomised controlled trials have been done to identify the optimum treatment for this emerging infection. We aimed to compare artesunate-mefloquine with chloroquine to define the optimum treatment for uncomplicated P knowlesi malaria in adults and children.
METHODS: We did this open-label, randomised controlled trial at three district hospitals in Sabah, Malaysia. Patients aged 1 year or older with uncomplicated P knowlesi malaria were randomly assigned, via computer-generated block randomisation (block sizes of 20), to receive oral artesunate-mefloquine (target dose 12 mg/kg artesunate and 25 mg/kg mefloquine) or chloroquine (target dose 25 mg/kg). Research nursing staff were aware of group allocation, but allocation was concealed from the microscopists responsible for determination of the primary endpoint, and study participants were not aware of drug allocation. The primary endpoint was parasite clearance at 24 h. Analysis was by modified intention to treat. This study is registered with ClinicalTrials.gov, number NCT01708876.
FINDINGS: Between Oct 16, 2012, and Dec 13, 2014, we randomly assigned 252 patients to receive either artesunate-mefloquine (n=127) or chloroquine (n=125); 226 (90%) patients comprised the modified intention-to-treat population. 24 h after treatment, we recorded parasite clearance in 97 (84% [95% CI 76-91]) of 115 patients in the artesunate-mefloquine group versus 61 (55% [45-64]) of 111 patients in the chloroquine group (difference in proportion 29% [95% CI 18·0-40·8]; p<0·0001). Parasite clearance was faster in patients given artesunate-mefloquine than in those given chloroquine (18·0 h [range 6·0-48·0] vs 24·0 h [6·0-60·0]; p<0·0001), with faster clearance of ring stages in the artesunate-mefloquine group (mean time to 50% clearance of baseline parasites 8·6 h [95% CI 7·9-9·4] vs 13·8 h [12·1-15·4]; p<0·0001). Risk of anaemia within 28 days was lower in patients in the artesunate-mefloquine group (71 [62%; 95% CI 52·2-70·6]) than in those in the chloroquine group (83 [75%; 65·6-82·5]; p=0·035). Gametocytaemia as detected by PCR for pks25 was present in 44 (86%) of 51 patients in the artesunate-mefloquine group and 41 (84%) of 49 patients in the chloroquine group at baseline, and in three (6%) of 49 patients and two (4%) of 48 patients, respectively, at day 7. Fever clearance was faster in the artesunate-mefloquine group (mean 11·5 h [95% CI 8·3-14·6]) than in the chloroquine group (14·8 h [11·7-17·8]; p=0·034). Bed occupancy was 2426 days per 1000 patients in the artesunate-mefloquine group versus 2828 days per 1000 patients in the chloroquine group (incidence rate ratio 0·858 [95% CI 0·812-0·906]; p<0·0001). One (<1%) patient in the artesunate-mefloquine group had a serious neuropsychiatric event regarded as probably related to study drug.
INTERPRETATION: Artesunate-mefloquine is highly efficacious for treatment of uncomplicated P knowlesi malaria. The rapid therapeutic response of the drug offers significant advantages compared with chloroquine monotherapy and supports a unified treatment policy for artemisinin-based combination therapy for all Plasmodium species in co-endemic areas.
FUNDING: Malaysian Ministry of Health, Australian National Health and Medical Research Council, and Asia Pacific Malaria Elimination Network.

Matched MeSH terms: Administration, Oral
Population pharmacokinetics of orally administered mefloquine in healthy volunteers and patients with uncomplicated Plasmodium falciparum malaria

Reuter SE, Upton RN, Evans AM, Navaratnam V, Olliaro PL

J Antimicrob Chemother, 2015 Mar;70(3):868-76.
PMID: 25377567 DOI: 10.1093/jac/dku430

BACKGROUND: The determination of dosing regimens for the treatment of malaria is largely empirical and thus a better understanding of the pharmacokinetic/pharmacodynamic properties of antimalarial agents is required to assess the adequacy of current treatment regimens and identify sources of suboptimal dosing that could select for drug-resistant parasites. Mefloquine is a widely used antimalarial, commonly given in combination with artesunate.
PATIENTS AND METHODS: Mefloquine pharmacokinetics was assessed in 24 healthy adults and 43 patients with Plasmodium falciparum malaria administered mefloquine in combination with artesunate. Population pharmacokinetic modelling was conducted using NONMEM.
RESULTS: A two-compartment model with a single transit compartment and first-order elimination from the central compartment most adequately described mefloquine concentration-time data. The model incorporated population parameter variability for clearance (CL/F), central volume of distribution (VC/F) and absorption rate constant (KA) and identified, in addition to body weight, malaria infection as a covariate for VC/F (but not CL/F). Monte Carlo simulations predict that falciparum malaria infection is associated with a shorter elimination half-life (407 versus 566 h) and T>MIC (766 versus 893 h).
CONCLUSIONS: This is the first known population pharmacokinetic study to show falciparum malaria to influence mefloquine disposition. Protein binding, anaemia and other factors may contribute to differences between healthy individuals and patients. As VC/F is related to the earlier portion of the concentration-time profiles, which occurs during acute malaria, and CL/F is more related to the terminal phase during convalescence after treatment, this may explain why malaria was found to be a covariate for VC/F but not CL/F.

Matched MeSH terms: Administration, Oral
Internal radiation dosimetry of orally administered radiotracers for the assessment of gastrointestinal motility

Yeong CH, Ng KH, Abdullah BJJ, Chung LY, Goh KL, Perkins AC

Appl Radiat Isot, 2014 Dec;94:216-220.
PMID: 25222875 DOI: 10.1016/j.apradiso.2014.08.009

Radionuclide imaging using (111)In, (99m)Tc and (153)Sm is commonly undertaken for the clinical investigation of gastric emptying, intestinal motility and whole gut transit. However the documented evidence concerning internal radiation dosimetry for such studies is not readily available. This communication documents the internal radiation dosimetry for whole gastrointestinal transit studies using (111)In, (99m)Tc and (153)Sm labeled formulations. The findings were compared to the diagnostic reference levels recommended by the United Kingdom Administration of Radioactive Substances Advisory Committee, for gastrointestinal transit studies.

Matched MeSH terms: Administration, Oral
Fulltext Efficacy of azithromycin in the treatment of bronchiectasis

Lourdesamy Anthony AI, Muthukumaru U

Respirology, 2014 Nov;19(8):1178-82.
PMID: 25183304 DOI: 10.1111/resp.12375

We evaluated the efficacy of a 12-week oral treatment with azithromycin in adult patients with bronchiectasis. The objectives were to demonstrate that this treatment reduces sputum volume, improves quality of life and to assess the lengths of effects after cessation of therapy.

Matched MeSH terms: Administration, Oral
Fulltext Acute toxicity study of zerumbone-loaded nanostructured lipid carrier on BALB/c mice model

Rahman HS, Rasedee A, Othman HH, Chartrand MS, Namvar F, Yeap SK, et al.

Biomed Res Int, 2014;2014:563930.
PMID: 25276798 DOI: 10.1155/2014/563930

Zerumbone- (ZER-) loaded nanostructure lipid carrier (NLC) (ZER-NLC) prepared for its antileukemia effect in vitro was evaluated for its toxicological effects by observing changes in the liver, kidney, spleen, lung, heart, and brain tissues, serum biochemical parameters, total haemogram, and bone marrow stem cells. The acute toxicity study for ZER-NLC was conducted by orally treating BALB/c mice with a single dose with either water, olive oil, ZER, NLC, or ZER-NLC for 14 days. The animals were observed for clinical and behavioral abnormalities, toxicological symptoms, feed consumption, and gross appearance. The liver, kidney, heart, lung, spleen, and brain tissues were assessed histologically. Total haemogram was counted by hemocytometry and microhematocrit reader. Bone marrow examination in terms of cellular morphology was done by Wright staining with bone marrow smear. Furthermore, serum biochemical parameters were determined spectrophotometrically. Grossly all treated mice, their investigated tissues, serum biochemical parameters, total haemogram, and bone marrow were normal. At oral doses of 100 and 200 mg/kg ZER-NLC there was no sign of toxicity or mortality in BALB/c mice. This study suggests that the 50% lethal dose (LD50) of ZER-NLC is higher than 200 mg/kg, thus, safe by oral administration.

Matched MeSH terms: Administration, Oral
Fulltext The use of Hibiscus esculentus (Okra) gum in sustaining the release of propranolol hydrochloride in a solid oral dosage form

Zaharuddin ND, Noordin MI, Kadivar A

Biomed Res Int, 2014;2014:735891.
PMID: 24678512 DOI: 10.1155/2014/735891

The effectiveness of Okra gum in sustaining the release of propranolol hydrochloride in a tablet was studied. Okra gum was extracted from the pods of Hibiscus esculentus using acetone as a drying agent. Dried Okra gum was made into powder form and its physical and chemical characteristics such as solubility, pH, moisture content, viscosity, morphology study using SEM, infrared study using FTIR, crystallinity study using XRD, and thermal study using DSC and TGA were carried out. The powder was used in the preparation of tablet using granulation and compression methods. Propranolol hydrochloride was used as a model drug and the activity of Okra gum as a binder was compared by preparing tablets using a synthetic and a semisynthetic binder which are hydroxylmethylpropyl cellulose (HPMC) and sodium alginate, respectively. Evaluation of drug release kinetics that was attained from dissolution studies showed that Okra gum retarded the release up to 24 hours and exhibited the longest release as compared to HPMC and sodium alginate. The tensile and crushing strength of tablets was also evaluated by conducting hardness and friability tests. Okra gum was observed to produce tablets with the highest hardness value and lowest friability. Hence, Okra gum was testified as an effective adjuvant to produce favourable sustained release tablets with strong tensile and crushing strength.

Matched MeSH terms: Administration, Oral
Fulltext Effect of dietary intake of avocado oil and olive oil on biochemical markers of liver function in sucrose-fed rats

Carvajal-Zarrabal O, Nolasco-Hipolito C, Aguilar-Uscanga MG, Melo Santiesteban G, Hayward-Jones PM, Barradas-Dermitz DM

Biomed Res Int, 2014;2014:595479.
PMID: 24860825 DOI: 10.1155/2014/595479

Metabolic changes, along with cardiovascular and hepatic factors, are associated with the development of diseases such as diabetes, dyslipidemia, and obesity. We evaluated the effect of avocado oil supplementation (centrifuged and solvent extracted), compared with olive oil, upon the hepatic function in sucrose-fed rats. Twenty-five rats were divided into five groups: control (basal diet), a sucrose-fed group (basal diet plus 30% sucrose solution), and three other groups (S-OO, S-AOC, and S-AOS, indicating basal diet plus 30% sucrose solution plus olive oil OO, avocado oil extracted by centrifugation AOC or using solvent AOS, resp.). Glucose, total cholesterol, triglycerides, total protein, albumin, globulin, direct bilirubin, glutamic pyruvic transaminase, glutamic oxaloacetic transaminase, alkaline phosphatase, cholinesterase, and α -amylase concentrations were determined and avocado oil effect on them was studied. In some cases the induced metabolic alteration significantly affected total protein and bilirubin levels and also had a highly significant effect on α -amylase levels. AOC and AOS exhibited effects similar to those of olive oil, according to the nonsignificant difference in fatty acid profile observed by other authors. Avocado oil consumption could be beneficial in the control of altered metabolic profile illnesses as it presents effects on hepatic function biochemical markers similar to olive oil.

Matched MeSH terms: Administration, Oral
Nanoparticulate assembly of mannuronic acid- and guluronic acid-rich alginate: oral insulin carrier and glucose binder

Kadir A, Mokhtar MT, Wong TW

J Pharm Sci, 2013 Dec;102(12):4353-63.
PMID: 24258282 DOI: 10.1002/jps.23742

The relationship of high and low molecular weight mannuronic acid (M)- and guluronic acid (G)-rich alginate nanoparticles as oral insulin carrier was elucidated. Nanoparticles were prepared through ionotropic gelation using Ca(2+) , and then in vitro physicochemical attributes and in vivo antidiabetic characteristics were examined. The alginate nanoparticles had insulin release retarded when the matrices had high alginate-to-insulin ratio or strong alginate-insulin interaction via OH moiety. High molecular weight M-rich alginate nanoparticles were characterized by assemblies of long polymer chains that enabled insulin encapsulation with weaker polymer-drug interaction than nanoparticles prepared from other alginate grades. They were able to encapsulate and yet release and have insulin absorbed into systemic circulation, thereby lowering rat blood glucose. High molecular weight G- and low molecular weight M-rich alginate nanoparticles showed remarkable polymer-insulin interaction. This retarded the drug release and negated its absorption. Blood glucose lowering was, however, demonstrated in vivo with insulin-free matrices of these nanoparticles because of the strong alginate-glucose binding that led to intestinal glucose retention. Alginate nanoparticles can be used as oral insulin carrier or glucose binder in the treatment of diabetes as a function of its chemical composition. High molecular weight M-rich alginate nanoparticles are a suitable vehicle for future development into oral insulin carrier.

Matched MeSH terms: Administration, Oral
Fulltext Mucosal genetic immunization through microsphere-based oral carriers

Rosli R, Nograles N, Hanafi A, Nor Shamsudin M, Abdullah S

Hum Vaccin Immunother, 2013 Oct;9(10):2222-7.
PMID: 24051430 DOI: 10.4161/hv.25325

Polymeric carriers in the form of cellulose acetate phthalate (CAP) and alginate (ALG) microspheres were used for encapsulation of plasmid DNA for oral mucosal immunization. Access into the intestinal mucosa by pVAX1 eukaryotic expression plasmid vectors carrying gene-coding sequences, either for the cholera enterotoxin B subunit (ctxB) immunostimulatory antigen or the green fluorescent protein (GFP), delivered from both types of microsphere carriers were examined in orally immunized BALB/c mice. Demonstration of transgene protein expression and IgA antibody responses at local mucosal sites suggest immunological response to a potential oral DNA vaccine formulated within the microsphere carriers.

Matched MeSH terms: Administration, Oral
The effectiveness of transmeatal low-power laser stimulation in treating tinnitus

Ngao CF, Tan TS, Narayanan P, Raman R

Eur Arch Otorhinolaryngol, 2014 May;271(5):975-80.
PMID: 23605244 DOI: 10.1007/s00405-013-2491-3

The aim of this study is to examine the effectiveness of transmeatal low-power laser stimulation (TLLS) in treating tinnitus. This is a prospective, double-blinded, randomized, placebo-controlled trial. Patients with persistent subjective tinnitus as their main symptom were recruited into the study from the outpatient clinics. The recruited patients were randomized into the experimental group or TLLS+ group (patients in this group were prescribed to use TLLS at 5 mW at 650 nM wavelength for 20 min daily and oral betahistine 24 mg twice per day for a total of 10 weeks) and the control group or TLLS- group (patients in this group were prescribed with a placebo device to use and oral betahistine 24 mg twice per day for 10 weeks). All patients were required to answer two sets of questionnaires: the Tinnitus handicap inventory (THI) and visual analogue scales (VAS) symptoms rating scales, before starting the treatment and at the end of the 10-week treatment period. The total score of the THI questionnaire was further graded into five grades, grade 1 being mild and grade 5 being catastrophic. Wilcoxon-signed ranks test and Mann-Whitney test were used to compare and analyze the THI and VAS scores before and after treatment for each group. Changes with p value of <0.05 were considered as statistically significant. Chi square test was used to analyze the change of parameters in categorical forms (to compare between TLLS+ and TLLS-). Changes with p value of <0.05 were considered as statistically significant. Forty-three patients successfully and diligently completed their treatment. It was noted that using any condition of the device, TLLS+ or TLLS-, patient's tinnitus symptoms improved in terms of THI scores (TLLS+, p value = 0.038; TLLS-, p value = 0.001) or VAS scores with a change of at least one grade (TLLS+, p value = 0.007; TLLS-, p value = 0.002) at p value <0.05 significant level. In contrast when TLLS+ group was compared with TLLS- group, no statistically significant result was obtained. In term of VAS scores, there seems to be no statistically significant improvement in patients' annoyance, sleep disruption, depression, concentration and tinnitus loudness and pitch heard between the two groups. Transmeatal low-power laser stimulation did not demonstrate significant efficacy as a therapeutic measure in treating tinnitus.
Study site: Otorhinolaryngology clinic, University Malaya Medical Centre (UMMC), Kuala Lumpur, Malaysia

Matched MeSH terms: Administration, Oral
Fulltext Clinicians' knowledge, beliefs and acceptance of intravenous-to-oral antibiotic switching, Hospital Pulau Pinang

Lee SL, Azmi S, Wong PS

Med J Malaysia, 2012 Apr;67(2):190-8.
PMID: 22822642 MyJurnal

A cross-sectional study was conducted to explore clincians' baseline knowledge, practice beliefs and acceptance of intravenous (IV)-to-oral antibiotic switching practice in Hospital Pulau Pinang. The factors most highly rated for antibiotic conversion were the ability to maintain oral intake (85.6%) and microbiology etiology (85.0%). Majority of the clinicians (76%) agreed with the traditional clinical rule that "patient should be afebrile for 24 hours before IV-to-oral switch". Specialists and consultants had the highest knowledge score among the clinicians. However, they were generally less positive about a guideline being integrated into practice.

Matched MeSH terms: Administration, Oral
The influence of consumers' preferences and perceptions of oral solid dosage forms on their treatment

Ibrahim IR, Ibrahim MI, Al-Haddad MS

Int J Clin Pharm, 2012 Oct;34(5):728-32.
PMID: 22744843 DOI: 10.1007/s11096-012-9667-6

BACKGROUND: Beyond the direct pharmacological effect of medicines, preferences and perceptions toward a particular oral solid dosage form (OSDF) play a crucial role in recovery and may reduce adherence to the prescribed treatment.
OBJECTIVES: This study conducted to investigate the most preferred OSDF and the degree to which swallowing solid medication is an issue, to assess perceptions of the therapeutic benefits of the OSDF, and to find predictors of the most preferred OSDF.
METHOD: A cross-sectional study, through convenience sample method, was conducted to survey consumers visiting community pharmacies in Baghdad, Iraq. Data was collected by self-administered and pre-piloted questionnaires, and analyzed using Statistical Package for Social Science. Multiple logistic regression analysis and Chi-square tests were used at alpha level = 0.05.
RESULTS: A total of 1,000 questionnaire were included in the analysis. Of all respondents, 52.9 % preferred capsule among other OSDF and this preference varied significantly with a number of socio-demographic factors. Ease of swallowing solid medication was the main issue which resulted in preferences for a particular form. A negative perception of the therapeutic benefits of the OSDF was found among 89.1 % of the consumers. Multiple logistic regression analysis indicated that gender, ease of swallowing, and perceptions of the therapeutic benefits of the OSDF were significant predictors of capsule preferences.
CONCLUSIONS: Given the fact that consumers are the end users of medicines and their preferences may influence response to the treatment, efforts are worthwhile by the prescribers and medicines' manufactures to understand consumers' preferences of a particular dosage form in order to achieve successful therapy outcomes.

Matched MeSH terms: Administration, Oral
Fulltext Acute oral toxicity of methanolic seed extract of Cassia fistula in mice

Jothy SL, Zakaria Z, Chen Y, Lau YL, Latha LY, Sasidharan S

Molecules, 2011 Jun 23;16(6):5268-82.
PMID: 21701437 DOI: 10.3390/molecules16065268

BACKGROUND AND OBJECTIVE: Cassia fistula is widely used in traditional medicine to treat various types of ailments. The evaluation of toxic properties of C. fistula is crucial when considering public health protection because exposure to plant extracts can result in undesirable effects on consumers. Hence, in this study the acute oral toxicity of C. fistula seeds extract was investigated in mice.
RESULTS: Oral administration of crude extract at the highest dose of 5000 mg/kg resulted in no mortalities or evidence of adverse effects, implying that C. fistula in nontoxic. Throughout 14 days of the treatment no changes in behavioural pattern, clinical sign and body weight of mice in both control and treatment groups. Also there were no any significant elevations observed in the biochemical analysis of the blood serum. Further, histopathological examination revealed normal architecture and no significant adverse effects observed on the kidney, heart, liver, lung and spleen.
CONCLUSIONS: Overall, the results suggest that, the oral administration of C. fistula methanolic seeds extract did not produce any significant toxic effect in mice. Hence, the extract can be utilized for pharmaceutical formulations.

Matched MeSH terms: Administration, Oral
Oral fast-release solid dispersion-paradigm shift to nanoparticles

Wong TW

Recent Pat Drug Deliv Formul, 2011 Sep;5(3):227-43.
PMID: 21834774

Design of oral fast-release solid dispersion of poorly water-soluble drugs has been a great challenge over past decades on issues of drug recrystallization, drug polymorphism, formulation limited to low drug-to-carrier ratio and drug particle aggregation in matrix. The complexity in solid dispersion design is envisaged to be resolvable by the use of nanoparticulate system as solid dosage form. This manuscript reviews several patented processing approaches of nanoparticulate solid dispersion that have been reported recently. Through drug nanoencapsulation, a higher content of drug may be delivered with less aggregation via placing the same drug mass in a greater number of tinier carriers. Nanoencapsulation, by its own process of formation, brings about submicron particles. Keeping drug in these nanoparticles, a remarkable rise in specific surface area of drug is realized for dissolution. The augmentation of drug dissolution can be sufficiently high to the extent that the influences of polymorphism and crystallization phenomenon on drug dissolution in a solid dispersion may be negligible.

Matched MeSH terms: Administration, Oral
Fulltext Characterization of oral disintegrating film containing donepezil for Alzheimer disease

Liew KB, Tan YT, Peh KK

AAPS PharmSciTech, 2012 Mar;13(1):134-42.
PMID: 22167416 DOI: 10.1208/s12249-011-9729-4

The aim of this study was to develop a taste-masked oral disintegrating film (ODF) containing donepezil, with fast disintegration time and suitable mechanical strength, for the treatment of Alzheimer's disease. Hydroxypropyl methylcellulose, corn starch, polyethylene glycol, lactose monohydrate and crosspovidone served as the hydrophilic polymeric bases of the ODF. The uniformity, in vitro disintegration time, drug release and the folding endurance of the ODF were examined. The in vitro results showed that 80% of donepezil hydrochloride was released within 5 minutes with mean disintegration time of 44 seconds. The result of the film flexibility test showed that the number of folding time to crack the film was 40 times, an indication of sufficient mechanical property for patient use. A single-dose, fasting, four-period, eight-treatment, double-blind study involving 16 healthy adult volunteers was performed to evaluate the in situ disintegration time and palatability of ODF. Five parameters, namely taste, aftertaste, mouthfeel, ease of handling and acceptance were evaluated. The mean in situ disintegration time of ODF was 49 seconds. ODF containing 7 mg of sucralose were more superior than saccharin and aspartame in terms of taste, aftertaste, mouthfeel and acceptance. Furthermore, the ODF was stable for at least 6 months when stored at 40°C and 75% relative humidity.

Matched MeSH terms: Administration, Oral
Formation and characterization of pDNA-loaded alginate microspheres for oral administration in mice

Nograles N, Abdullah S, Shamsudin MN, Billa N, Rosli R

J Biosci Bioeng, 2012 Feb;113(2):133-40.
PMID: 22093752 DOI: 10.1016/j.jbiosc.2011.10.003

Alginate, a natural polysaccharide, was explored in this study as an oral delivery vehicle of a mammalian expression vector into the murine intestinal mucosa. Alginate microspheres were produced through water-in-oil (W/O) emulsification method. Average diameter sizes of microspheres were 46.88 μm±3.07 μm with significant size reduction upon utilization of 1.0% Span80. Plasmid DNA (pDNA) carrying green fluorescent protein reporter gene (GFP), pVAX-GFP, was encapsulated within microspheres at efficiencies of 72.9 to 74.4%, carrying maximum load of 6 μg pDNA. Alginate microspheres demonstrated shrinkage in pH 1.2 and swelling in pH 9.0 with pDNA release about twice the amount released in acidic environment. Oral delivery of pVAX-GFP loaded-microspheres, at 50 μg, 100 μg and 150 μg dose, was performed on BALB/c mice. Tissue biodistribution, investigated through flow cytometric analysis, demonstrated GFP positive intestinal cells (<1.0%) with 1.3-fold higher levels for the 100 μg dose; therefore suggesting feasibility of the approach for oral gene delivery and vaccination.

Matched MeSH terms: Administration, Oral
Fulltext Pectin matrix as oral drug delivery vehicle for colon cancer treatment

Wong TW, Colombo G, Sonvico F

AAPS PharmSciTech, 2011 Mar;12(1):201-14.
PMID: 21194013 DOI: 10.1208/s12249-010-9564-z

Colon cancer is the fourth most common cancer globally with 639,000 deaths reported annually. Typical chemotherapy is provided by injection route to reduce tumor growth and metastasis. Recent research investigates the oral delivery profiles of chemotherapeutic agents. In comparison to injection, oral administration of drugs in the form of a colon-specific delivery system is expected to increase drug bioavailability at target site, reduce drug dose and systemic adverse effects. Pectin is suitable for use as colon-specific drug delivery vehicle as it is selectively digested by colonic microflora to release drug with minimal degradation in upper gastrointestinal tract. The present review examines the physicochemical attributes of formulation needed to retard drug release of pectin matrix prior to its arrival at colon, and evaluate the therapeutic value of pectin matrix in association with colon cancer. The review suggests that multi-particulate calcium pectinate matrix is an ideal carrier to orally deliver drugs for site-specific treatment of colon cancer as (1) crosslinking of pectin by calcium ions in a matrix negates drug release in upper gastrointestinal tract, (2) multi-particulate carrier has a slower transit and a higher contact time for drug action in colon than single-unit dosage form, and (3) both pectin and calcium have an indication to reduce the severity of colon cancer from the implication of diet and molecular biology studies. Pectin matrix demonstrates dual advantages as drug carrier and therapeutic for use in treatment of colon cancer.

Matched MeSH terms: Administration, Oral
A bioequivalence comparison of two formulations of rifampicin (300- vs 150-mg capsules): An open-label, randomized, two-treatment, two-way crossover study in healthy volunteers

Chik Z, Basu RC, Pendek R, Lee TC, Mohamed Z

Clin Ther, 2010 Sep;32(10):1822-31.
PMID: 21194606 DOI: 10.1016/j.clinthera.2010.09.006

Rifampicin is a semisynthetic antibiotic derivative of rifamycin used worldwide for the treatment of various forms of tuberculosis.

Matched MeSH terms: Administration, Oral
Fulltext Evaluation of the antinociceptive activity and acute oral toxicity of standardized ethanolic extract of the rhizome of Curcuma xanthorrhiza Roxb

Devaraj S, Esfahani AS, Ismail S, Ramanathan S, Yam MF

Molecules, 2010 Apr;15(4):2925-34.
PMID: 20428088 DOI: 10.3390/molecules15042925

Ethanolic extract of Curcuma xanthorrhiza was used to evaluate the analgesic and toxicity effects in vivo. The extract was standardized using GC-MS, which showed that 1 mg of Curcuma xanthorrhiza ethanolic extract contains 0.1238 mg of xanthorrhizol. The analgesic activity was studied in rats using three different models, namely the hot plate test, tail flick test and formalin-induced pain test. The acute oral toxicity was examined by the oral administration of standardized Curcuma xanthorrhiza ethanolic extract in mice at doses ranging from 300-5,000 mg/kg and observation for 14 days. Standardized Curcuma xanthorrhiza ethanolic extract did not show significant analgesic effect in the hot plate and tail flick tests. However, in the formalin-induced pain test, Curcuma xanthorrhiza ethanolic extract significantly (P < 0.05) suppressed the paw licking time of rats in both early and late phases at doses 200 and 400 mg/kg of the extract, respectively. In the acute oral toxicity study, Curcuma xanthorrhiza ethanolic extract did not show any toxic effects in mice at 5 g/kg. These experimental results suggest that the standardized Curcuma xanthorrhiza ethanolic extract showed peripheral and central antinociceptive activity associated with neurogenic pain as well as a relative absence of toxic effects which could compromise the medicinal use of this plant in folk medicine.

Matched MeSH terms: Administration, Oral

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