ISRN Pharmaceutics最新文献

Tannic acid is a polyphenolic compound that could be labeled with technetium-99m. To produce about 90% yield of  (99m)Tc-tannic acid in acidic media (pH), the conditions required were 150 μg tin chloride, 30 min reaction time, and 200 μg of the substrate. (99m)Tc-tannic was stable for 6 h. Oral biodistribution of (99m)Tc-tannic showed that it concentrated in the stomach ulcer to reach about 50% of the total injected dose at 1 h after orall administration. This concentration of (99m)Tc-tannic in stomach ulcer may be sufficient to radio-image the presence of ulcer in the stomach.

The present investigation describes the influence of the concentration of PEG 6000 as a melt binder and ratio of HPMC K4M : PVP on Zolpidem tartrate controlled-release tablet formulations using 3(2) full factorial design. The ratio of HPMC K4M and PVP K30 (X(1)) and the concentration of melt binder (X(2)) were selected as independent variables, and drug release at 1 hr (Q(1)), 4 hr (Q(4)), 8 hr (Q(8)), diffusion coefficient (n), and release rate constant (K) were selected as a dependent variable. Tablets were prepared by melt granulation technique and evaluated for various evaluation parameters. It was observed that concentration of melt binder had significant effect on Q(1), Q(4), n, and K Binder concentration 25% w/w was found optimum. Optimized formulation (F(7)) showed good similarity with theoretical profile of drug. The X(2) variable had a significant effect on dependent variables, and the X(1) variable had no significant effect on dependent variables.

Objective. To investigate the mechanism of capsaicin in treating active psoriasis vulgaris. Methods. HIF-1α gene translation in active psoriatic lesions before and after 21-day treatment with capsaicin ointment was detected by in situ hybridization. Results. There was positive staining of HIF-1α gene in all the layers of psoriatic epidermis (100.0%) before the treatment with capsaicin ointment, but the dyeing in epidermis were reduced obviously (22.2%) after the treatment for 21 days. Conclusion. HIF-1α gene translation in psoriatic epidermis was downregulated after capsaicin treatment for 21 days.

Marine sponges have been recognized as potentially rich sources of various bioactive molecules. In our continuing search for new secondary metabolites from Indonesian marine invertebrates, we collected a sponge, whose extract showed cytotoxicity against cultured cells at 0.1 μg/mL. Purification of the extract yielded two new macrolides 2 and 3 along with known candidaspongiolide (1). The structures for compounds 2 and 3 were elucidated by spectral analysis ((1)H, (13)C, COSY, HMQC, HMBC) and by comparison of their NMR data with those of 1. Compounds 2 and 3 exhibited a little more potent cytotoxicity (IC(50) 4.7 and 19 ng/mL) than that (IC(50) 37 ng/mL) of candidaspongiolide (1) against NBT-T2 cells.

A high-performance liquid chromatographic (HPLC) and a ultraviolet (UV) methods were developed and validated for the quantitative determination of Dexibuprofen (DI) in pharmaceutical dosage form. HPLC was carried out by reversed phase technique on a RP-18 column with a mobile phase composed of acetonitrile and 0.5% triethylamine (pH 7.5 adjusted with orthophosphoric acid (30 : 70, v/v)). UV method was performed with the λ max at 222.0 nm. Both the methods showed good linearity, reproducibility and precision. No spectral or chromatographic interferences from the tablet excipients were found in UV and HPLC. The method was successfully applied to commercial DEXIFEN tablets. Validation parameters such as linearity, precision, accuracy, and specificity were determined. The proposed method could be applicable for routine analysis of DI and monitoring of the quality of marketed drugs.

We explored the potential for EXPAREL to interact with lidocaine. Sixty (60) male Yucatan Swine were randomized into 20 groups (N = 3/group). EXPAREL (2 or 4 mg/kg) and/or lidocaine HCl solution 1% or 2% (with epinephrine 1 : 200,000) were injected subcutaneously along a 5 cm virtual incision line. The effects on the pharmacokinetics of bupivacaine and lidocaine were examined when 5, 10, 20, and 40 minutes had passed between administration of lidocaine and EXPAREL. Systemic exposure to lidocaine was increased (AUC(0-24 hr) by 48%; C(max) by 1,640%) when lidocaine (4 mg/kg) was followed 5 minutes later by EXPAREL (4 mg/kg) compared to lidocaine administered alone. Plasma bupivacaine was increased (AUC(0-24 hr) by 50-95%; C(max) by 67-1,000%) when lidocaine (4 mg/kg) was followed 5 or 10 minutes later by EXPAREL (4 mg/kg) compared to EXPAREL alone. While EXPAREL should not be admixed with lidocaine, this study shows that local administration of EXPAREL after at least 20 minutes following local administration of lidocaine did not increase the release of either drug.

This study was done to investigate the effects of water-soluble fraction (WSF) of the fruits of Abelmoschus esculentus L (okra/lady's fingers) on absorption of oral glucose as well as metformin from the gastrointestinal tract in the Long Evans rats. WSF of A. esculentus significantly (P < 0.05) reduced the absorption of glucose as studied in the 24 hrs fasting rats. The effect of WSF of A. esculentus on metformin absorption was studied in alloxan-induced diabetic rats. Significant differences (P < 0.05) were observed in the average blood glucose level from 2 to 24 hours after metformin therapy in presence (33.6 to 34.2 mmol/L) or absence (15.2 to 20.2 mmol/L) of oral WSF of A. esculentus. In both of the experiments, Na-carboxymethylcellulose (CMC) was used as positive control. The results of this study indicate that A. esculentus may improve glycemic control but should not be taken concurrently with metformin hydrochloride in controlling diabetes mellitus.

The aim of the current study was to formulate and optimize the formulation on the basis of in vitro performance of microsphere. A 3(2) full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio (X(1)) and stirring speed (X(2)), on dependent variables, encapsulation efficiency, particle size, and time to 80% drug release. The best batch exhibited a high entrapment efficiency of 70% and mean particle size 290 μm. The drug release was also sustained for more than 12 hours. The study helped in finding the optimum formulation with excellent sustained drug release.

Chitosan (CS) nanoparticles have been developed as a versatile drug delivery system to transport drugs, genes, proteins, and peptides into target sites. Demands on fluorescent nanoparticles have increased recently due to various applications in medical and stem-cell-based researches. In this study, fluorescent CS nanoparticles were prepared by a mild method, namely, complex coacervation. Entrapment efficiency of sulforhodamine (SR101) loaded into CS nanoparticles was investigated to evaluate their capacity in incorporating fluorescent molecule. Particle size of produced fluorescent nanoparticles was in the range of 600-700 nm, and their particle size was highly dependent on the CS molecular weight as well as concentration. A high entrapment efficiency of SR101 into CS nanoparticles could also be obtained when it was dissolved in methanol. In conclusion, highly loaded fluorescent CS nanoparticles could be easily prepared using complex coacervation method and therefore can be applied in various medical researches.

Objectives. β(2)-adrenergic agonists, such as clenbuterol, have been shown to promote the hypertrophy of healthy skeletal muscles and to ameliorate muscle wasting in a few pathological conditions in both animals and humans. We intended to investigate the clinical efficacy of clenbuterol on attenuating denervation-induced muscle atrophy. Methods. A double-blind, placebo-controlled, parallel, and randomized trial was employed. 71 patients, suffering from brachial plexus injuries, were given either clenbuterol (60 μg, bid) or placebo for 3 months. Before and at the end of the study, patients were given physical examinations, biopsies of biceps brachii, electromyograms (EMGs), and other laboratory tests. Results. Compared with placebo treatment, clenbuterol significantly mitigated the decreases in cross-sectional areas of type I and II muscle fibers and alleviated the reduction in fibrillation potential amplitudes, without any adverse effects. Conclusions. Clenbuterol safely ameliorated denervated muscle atrophy in this cohort; thus larger clinical studies are encouraged for this or other β(2) agonists on denervation-induced muscle atrophy.