- In Vitro-In Vivo Predictive Dissolution-Permeation-Absorption Dynamics of Highly Permeable Drug Extended-Release Tablets via Drug Dissolution/Absorption Simulating System and pH Alteration. [Journal Article]
- APAAPS PharmSciTech 2018; 19(4):1882-1893
- Each of dissolution and permeation may be a rate-limiting factor in the absorption of oral drug delivery. But the current dissolution test rarely took into consideration of the permeation property. D...
Each of dissolution and permeation may be a rate-limiting factor in the absorption of oral drug delivery. But the current dissolution test rarely took into consideration of the permeation property. Drug dissolution/absorption simulating system (DDASS) valuably gave an insight into the combination of drug dissolution and permeation processes happening in human gastrointestinal tract. The simulated gastric/intestinal fluid of DDASS was improved in this study to realize the influence of dynamic pH change on the complete oral dosage form. To assess the effectiveness of DDASS, six high-permeability drugs were chosen as model drugs, including theophylline (pKa1 = 3.50, pKa2 = 8.60), diclofenac (pKa = 4.15), isosorbide 5-mononitrate (pKa = 7.00), sinomenine (pKa = 7.98), alfuzosin (pKa = 8.13), and metoprolol (pKa = 9.70). A general elution and permeation relationship of their commercially available extended-release tablets was assessed as well as the relationship between the cumulative permeation and the apparent permeability. The correlations between DDASS elution and USP apparatus 2 (USP2) dissolution and also between DDASS permeation and beagle dog absorption were developed to estimate the predictability of DDASS. As a result, the common elution-dissolution relationship was established regardless of some variance in the characteristic behavior between DDASS and USP2 for drugs dependent on the pH for dissolution. Level A in vitro-in vivo correlation between DDASS permeation and dog absorption was developed for drugs with different pKa. The improved DDASS will be a promising tool to provide a screening method on the predictive dissolution-permeation-absorption dynamics of solid drug dosage forms in the early-phase formulation development.
- Comparison of three most frequently used alpha blocker agents in medical expulsive therapy for distal ureteral calculi, result of a retrospective observational study. [Journal Article]
- AIArch Ital Urol Androl 2018 Mar 31; 90(1):25-28
- CONCLUSIONS: The results of this study showed that medical expulsive therapy by using alpha blocker agents is safe and efficacious. This option must be kept in mind for patients who do not ask for surgery as the first-step treatment for eligible patients.
- Evaluation of apoptosis indexes in currently used oral alpha-blockers in prostate: a pilot study. [Journal Article]
- IBInt Braz J Urol 2018 Mar 18; 44
- CONCLUSIONS: Silodosin has higher apoptosis effect than other alpha-blockers in prostate. Thus, clinic improvement with silodosin was proved by histologic studies. Besides, static factor of BPH may be overcome with creating apoptosis.
- New alpha blockers to treat male lower urinary tract symptoms. [Journal Article]
- COCurr Opin Urol 2018; 28(3):273-276
- CONCLUSIONS: The two new selective alpha-blockers, silodosin, and naftopidil showed similar efficacy in IPSS and quality of life compared with other alpha-blockers. However, silodosin has more sexual adverse events.
- Efficacy of an Alpha-Blocker for the Treatment of Nonneurogenic Voiding Dysfunction in Women: An 8-Week, Randomized, Double-Blind, Placebo-Controlled Trial. [Journal Article]
- INInt Neurourol J 2018; 22(1):30-40
- CONCLUSIONS: Alfuzosin might not be more effective than placebo for treating FVD. The presence or the grade of BOO did not affect the results. A further study with sufficient power is needed to determine the efficacy of α1-AR blockers for the treatment of FVD.
- An efficient spectrofluorimetric method adopts doxazosin, terazosin and alfuzosin coupling with orthophthalaldehyde: Application in human plasma. [Journal Article]
- SASpectrochim Acta A Mol Biomol Spectrosc 2018 Apr 15; 195:215-222
- A new, selective and sensitive spectrofluorimetric method was designed for the quantitation of doxazosin (DOX), terazosin (TER) and alfuzosin (ALF) in their dosage forms and human plasma. The method ...
A new, selective and sensitive spectrofluorimetric method was designed for the quantitation of doxazosin (DOX), terazosin (TER) and alfuzosin (ALF) in their dosage forms and human plasma. The method adopts efficient derivatization of the studied drugs with ortho-phthalaldehyde (OPA), in the presence of 2-mercaptoethanol in borate buffer (pH9.7) to generate a highly fluorescent isoindole derivatives, which can strongly enhance the fluorescence intensities of the studied drugs, allowing their sensitive determination at 430nm after excitation at 337nm. The fluorescence-concentration plots were rectilinear over the ranges (10.0-400.0) ng/mL. Detection and quantification limits were found to be (0.52-3.88) and (1.59-11.76) ng/mL, respectively. The proposed method was validated according to ICH guidelines, and successfully applied for the determination of pharmaceutical preparations of the studied drugs. Moreover, the high sensitivity of the proposed method permits its successful application to the analysis of the studied drugs in spiked human plasma with % recovery (96.12±1.34-100.66±0.57, n=3). A proposal for the reaction mechanism was presented.
- Efficacy and safety of alpha blockers in medical expulsive therapy for ureteral stones: a mixed treatment network meta-analysis and trial sequential analysis of randomized controlled clinical trials. [Review]
- ERExpert Rev Clin Pharmacol 2018; 11(3):291-307
- Alpha blockers (AB) are the main group of drugs used for medical expulsive therapy (MET) in patients with ureteral stones. However, there is no consensus on the relative efficacy and safety of indivi...
Alpha blockers (AB) are the main group of drugs used for medical expulsive therapy (MET) in patients with ureteral stones. However, there is no consensus on the relative efficacy and safety of individual AB in MET. Areas covered: The present work is a network meta-analysis of randomized controlled trials comparing AB with either placebo or standard of care in patients with ureteral stones. Electronic databases of Medline, Cochrane CENTRAL and Google Scholar were searched for eligible clinical studies. Inverse variance heterogeneity model was used for mixed treatment comparisons. Stone expulsion rate (SER) and stone expulsion time (SET) were the primary outcomes. Sub-group analyses for the following sub-groups were carried out: children; after shockwave lithotripsy; stone size of ≤5 mm; >5 mm; proximal and distal ureteral stones. Expert review: AB, phosphodiesterase inhibitors and combined AB with corticosteroids were observed with significant stone expulsion rate compared to control group in a recent network meta-analysis. Due to lack of head-to-head clinical trials within AB, only tamsulosin has been widely recommended by various urological guidelines. The results of this network meta-analysis will guide the future researchers in evaluating other promising ABs as agents for MET.
- Tamsulosin and the risk of dementia in older men with benign prostatic hyperplasia. [Journal Article]
- PDPharmacoepidemiol Drug Saf 2018; 27(3):340-348
- CONCLUSIONS: Tamsulosin may increase the risk of dementia in older men with BPH.
- Silodosin for the treatment of lower urinary tract symptoms in men with benign prostatic hyperplasia. [Review]
- CDCochrane Database Syst Rev 2017 11 22; 11:CD012615
- CONCLUSIONS: Silodosin may reduce urologic symptom scores in an appreciable number of men compared to placebo. Quality of life and treatment withdrawals for any reason appears similar. Its efficacy appears similar to that of other alpha blockers (tamsulosin, naftopidil and alfuzosin) but the rate of sexual side effects is likely higher. Our certainty in the estimates of effect was lowered due to study limitations, inconsistency and imprecision.
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- The Effects of Systemic Alfuzosin and Tamsulosin Hydrochloride on Choroidal Thickness and Pupil Diameter Sizes in Cases with Benign Prostatic Hyperplasia. [Randomized Controlled Trial]
- CECurr Eye Res 2017; 42(12):1638-1643
- CONCLUSIONS: The repeated measure of ANOVA for the mean CT values within AH group showed statistically significant increases in baseline CTs, although these differences did not reach statistical significance between 2 groups at follow-ups. We found significant different outcomes for PD sizes during study in the groups. The mean outcome in this study is that using αAR antagonists have potential effects on CT and PD sizes. Abbreviations and Acronyms: AH: alfuzosin hyrdrochloride; ANOVA: analyses of variance; AR: adrenergic receptor; BCVA: best-corrected visual acuity; BPH: benign prostatic hyperplasia; CT: choroidal thickness; EDI-OCT: enhanced depth imaging spectral-domain optical coherence tomography; IFIS: intraoperative floppy iris syndrome; MPD: mesopic pupil diameter; NCT: nasal choroidal thickness; PD: pupil diameter; PPD: photopic pupil diameter; SCT: subfoveal choroidal thickness; SPD: scotopic pupil diameter; TCT: temporal choroidal thickness; TH: tamsulosin hydrochloride.