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In this study, we have developed two facile spectroscopic methods for quantifying oxybutynin (OBT) hydrochloride in its pure form and tablets using design of experiments (DOEs). The spectroscopic methods depended on the ion-pair complex formation between the tertiary amino group in the drug and eosin in 0.2 M acetate buffer of pH 4. Method I involves spectrophotometric measurement of the absorbance of the developed complex at 550 nm and showed linearity through 1.0–10.0 µg ml −1 . Method II involves spectrofluorometric measurement of the quenching influence of OBT on the native fluorescence of eosin (λ excitation/λ emission of 304/548 nm) and showed linearity through 1.0–6.0 µg ml −1 . Critical parameters were identified through preliminary trials and optimized using the DOE. Additionally, the quenching mechanism was investigated and the pathway of the reaction was postulated. The fluorescence quenching constant and thermodynamic parameters were explored using the Stern–Volmer plot and Van't Hoff graph, respectively. Assessments conducted via analytical ecoscale revealed the ‘excellent-greenness’ of the methodology. The two methods have the potentials of being green and fast compared with other reported methods.

According to class M2.1 of the World Anti-Doping Agency (WADA) Prohibited List, the manipulation of doping control urine samples to alter their integrity and validity is prohibited both in- and out-of-competition. However, some paraplegic athletes with an overactive bladder need to be regularly treated with anti-cholinergic and anti-spasmodic drugs such as oxybutynin, which are often administered intravesically to reduce the substantial side effects observed after oral application. So far, it remains unclear whether such bladder instillations have a negative impact on analytical procedures and thus represent an anti-doping rule violation. Within this pilot study, urine samples were collected from five paraplegic athletes before and after an intravesical oxybutynin hydrochloride instillation. The samples were routinely tested for the presence of performance-enhancing drugs and afterwards fortified with 25 model compounds representing different classes of doping agents (anabolic agents, cannabinoids, diuretics, glucocorticoids, hormone and metabolic modulators, and stimulants) at low and medium concentrations. Additionally, the pH value and specific gravity were measured and the presence of oxybutynin was qualitatively determined by gas chromatography-mass spectrometry (GC-MS). In initial testing procedures, all samples were tested negative. Oxybutynin was present in most of the samples but found to have no significant effect on the detectability of the 25 model compounds subsequently added to each urine specimen. Therefore, it can be concluded that intravesical instillations with oxybutynin hydrochloride do not alter the integrity and validity of doping control urine samples.

Pharmaceutical dosage forms contain both active ingredients and inactive materials called exipients, most of which cause high interference specially in direct UV-spectrophotometry. This problem is highly obvious in syrups which may contain preservatives, coloring agents, thickening agents and sweetening agents. Thus, there is an urgent need to develop and validate a simple, accurate and selective method named interference subtraction method for determination of drugs in syrups in presence of these excipients without pre-separation by solving this interference. This newly designed method was successfully applied to; Oxybutynin hydrochloride in Detronin® syrup, Ambroxol hydrochloride in Muco® syrup and Ibuprofen in both Brufen® syrup and Megafen N® oral suspension. These chosen syrups contain different excipients causing different types of interference. This innovative method was validated according to ICH guidelines. The results obtained by interference subtraction method were statistically compare...

Hyperhidrosis (HH) is characterized by sweating exceeding the amount necessary to meet the thermal regulation and physiological needs of the body. Approximately 9.41% of individuals with HH have craniofacial hyperhidrosis (FH). The present study aims to review the most current data in the literature regarding craniofacial hyperhidrosis, including pathophysiology, diagnosis and clinical presentation, treatment options (clinical and surgical), and outcomes. VATS (videothoracoscopy sympathectomy) is considered the gold standard for definitive treatment of axillary or palmar hyperhidrosis. Recently, several studies have shown the usefulness of clinical treatment with oxybutynin hydrochloride, leading to clinical improvement of HH in more than 70% of users. Both clinical and surgical treatment of craniofacial hyperhidrosis have good results. However, surgical treatment of FH is associated with more complications. Clinical treatment with oxybutynin hydrochloride yields good results and can be the first therapeutic option. When the patient is not satisfied with this treatment and has good clinical conditions, surgical treatment can be used safely. Resumo A hiperidrose (HH) é caracterizada por transpiração além da quantidade necessária para manter a regulação térmica e as necessidades fisiológicas do corpo. Aproximadamente 9,41% dos indivíduos com HH apresentam hiperidrose craniofacial (FH). Este estudo tem como objetivo revisar os dados mais atuais da literatura sobre FH, incluindo fisiopatologia, diagnóstico e apresentação clínica, opções de tratamento (clínico e cirúrgico) e desfechos. A simpatectomia por videotoracoscopia (VATS) é considerada o padrão-ouro para o tratamento definitivo da hiperidrose axilar ou palmar. Recentemente, vários estudos demonstraram a utilidade do tratamento clínico com cloridrato de oxibutinina, que leva à melhora clínica da HH em mais de 70% dos pacientes. O tratamento clínico e o cirúrgico apresentam bons resultados no tratamento da FH. No entanto, o tratamento cirúrgico da FH apresenta mais complicações. O tratamento clínico com cloridrato de oxibutinina fornece bons resultados e pode ser a primeira opção terapêutica. Quando o paciente não está satisfeito com esse tratamento e mostra boas condições clínicas, o tratamento cirúrgico pode ser usado com segurança.

Aims To verify the efficacy, safety and tolerability of intravesical administration of 0.1% oxybutynin hydrochloride compared to its oral administration for treatment of neurogenic detrusor overactivity (NDO) in a randomized, prospective, controlled, open-label, multi-center trial in 35 adult patients. Methods NDO was confirmed within the previous 24 months by urodynamic studies (UDS). Group 1 (n = 18) received 10 ml 0.1% oxybutynin hydrochloride intravesically three times per day and group 2 (n = 17) 5 mg oxybutynin hydrochloride orally three times per day for a period of 28 days. Primary efficacy criterion was the change in the maximum bladder capacity between the beginning of the study and after 4 weeks as assessed by UDS. Adverse drug reactions (ADR) were collected and an evaluation of anticholinergic effects was conducted. Results The increase in maximum bladder capacity was 117 ml with intravesical application (P = 0.0002) versus 18 ml with the oral application (P = 0.51). The difference was statistically significant (P = 0.0086). ADR were reported by 10 (55.6%) of patients with intravesical administration, and by 14 (82.4%) of patients with oral administration. Significant differences in favor of the intravesical application were observed in ADR affecting vision (1/10 vs. 9/14), gastrointestinal tract (8/10 vs. 14/14), nervous system (2/10 vs. 8/14), and skin and subcutis (1/10 vs. 6/14). No serious adverse drug reactions were reported. Conclusions This study demonstrates the efficacy and safety of intravesical 0.1% oxybutynin hydrochloride in the treatment of NDO with respect to the increase in maximum bladder capacity. Neurourol. Urodynam. © 2015 Wiley Periodicals, Inc.

Oxybutynin hydrochloride (OB) is often used in intravesical instillation therapy for spastic neurogenetic bladder.The purposeof this study was to determine the expiration date and administration device for intravesically administered OB solutionscontaining sodium hyaluronate (HYA) as a pharmaceutical additive to enhance the muco-adhesiveness of the solution.The stability of OB in containers made of glass,polystyrene (PS),polypropylene (PP) and polyethylene (PE) was investigatedunder various temperature and light exposure conditions.Sorption of OB was observed in PP and PE containers andfor the latter,it was enhanced at higher temperatures and pHs.Based on these results,the optimal expiration date and storageconditions of OB solution were determined to be 84 days in a cool place (4°C),in a PP container.

Isothermal microcalorimetry was used to evaluate excipient compatibility of solid dosage form. Oxybutynin hydrochloride and cefaclor were used as model drugs for compatibility test with excipients. The calorimetric data for compatibility test were compared with those of HPLC data. Evaluation of compatibility between drug and excipient of solid dosage form might be possible to use isothermal microcalorimetry instead of conventional method. By using microcalorimetric method, the evaluation of the compatibility between drug and excipient could be successfully performed with a simple operation in a short time. The application of the isothermal microcalorimetry would be useful for the screening test of the drug compatibility with excipients.

Purpose. To investigate the potential use of a monoolein/water lyotropic liquid crystalline gel for the vaginal delivery of the antimuscarinic drugs, propantheline bromide and oxybutynin hydrochloride to treat urinary incontinence, using Myverol 18-99 as a commercially available grade of monoolein.

Intravesical oxybutynin hydrochloride was administered to 17 patients with a neuropathic bladder (myelomeningocele in 15 and spinal cord tumour in two) and urinary incontinence refractory to intermittent catheterisation. Therapy consisted of instillation of a 10 ml solution containing 5 mg oxybutynin hydrochloride twice daily. The cystometric bladder capacity before and after 1 hour of intravesical oxybutynin hydrochloride was 132 +/- 45 ml and 193 +/- 71 ml (mean +/- 1 standard deviation, p0.01) in all 17 patients. In 13 patients with low compliant bladders, the mean bladder compliance before and after 1 hour of instillation was 4.2 +/- 2.4 ml/cmH2O and 8.5 +/- 6.4 ml/cmH2O respectively (p0.01). The period of the intravesical oxybutynin hydrochloride treatment ranged from 2 to 16 months (mean 11.1 months). The improvement rate of 'moderately improved' and better response was 76.5% in all 17 patients. One patient complained of slight lower abdominal pain, which receded as treatment continued. Since the pH value of the solution appeared to be so low as to irritate the vesical mucosa, the value was adjusted to 5.85. No local or systemic side effects were observed thereafter. These encouraging results suggest that intravesical instillation of oxybutynin hydrochloride is an attractive alternative in patients with a neuropathic bladder, who are either unresponsive to or have intolerable side effects from oral medications.

The effect of intravesical oxybutynin hydrochloride on detrusor behaviour was studied in 15 patients with urinary incontinence due to detrusor hyper-reflexia by ambulatory bladder monitoring. Twelve patients had a reduction in the frequency and amplitude of hyper-reflexic contractions and incontinence episodes following oxybutynin administration. Intravesical oxybutynin may have a role in the management of patients on intermittent self-catheterisation with detrusor hyper-reflexia who cannot tolerate the side effects of anticholinergic agents, including oxybutynin.

The purpose of this article is to investigate the efficacy of intravesical oxybutynin hydrochloride (OH) to treat patients with overactive detrusors who are unresponsive to oral anticholinergic therapy alone. Twenty-five patients who were treated with oral OH for overactive detrusor (but who did not respond to treatment and were using indwelling urethral catheters) were given intravesical OH without changing oral treatment. Pre- and posttreatment bladder capacities were compared in urodynamic studies. The study showed that positive clinical results can be achieved with combined oral and intravesical OH treatments in patients with overactive detrusors who had indwelling urethral catheters because of severely reduced bladder capacity. However, a significant number of patients discontinued this treatment because of infection and difficulty in performing the procedure. Clinicians and rehabilitation nurses should provide education and support to eliminate these problems. In addition, the development of single-use standard sterile OH preparations for intravesical applications may increase the efficacy of the method.

The results of an investigation dealing with the therapy of instability of the detrusor using oxybutynin hydrochloride are presented. Out of an unselected group of patients 21 were enrolled in the trial. After therapy 19 patients showed significant improvement of subjective symptoms and objective urodynamic parameters. Twenty patients reported on tolerable side effects.

Objective: To find the efficacy and optimal dosage of oxybutynin HCl in a group of enuretic children, who were non-responsive to imipramine. Material and Methods: Thirty-six patients with enuresis who were non-responsive to imipramine were urodynamically assessed and subsequently treated with oxybutynin hydrochloride (HCl). Patients with inadequate bladder storage function (IBSF) were started on 10-mg daily oxybutynin HCl for one month. If the initial treatment was found to be inadequate, the dose was increased to 15 mg daily. The dose in patients who were non-responsive to 15-mg daily dose was increased to 20-mg daily dose. Patients who were normal urodynamically were treated with a dose of 15 mg daily for one month. Results: Before the treatment, 17 patients had IBSF (47.2%). The majority of the patients (88.2%) with IBSF were responsive to the 15-mg daily oxybutynin HCl. The treatment in patients with normal bladder function was generally unsuccessful. Conclusions: Oxybutynin HCl in sufficient dosages seems to be effective in the treatment of enuretic patients with IBSF.

Objective: To clarify the effects of systematic treatment based on overnight simultaneous monitoring by electroencephalography (EEG) and cystometry (CM) on each type of enuresis. Methods: For enuresis type I, the change in the awakening response during the conditioning treatment with a therapeutic machine was observed. For enuresis type IIa, the effect of imipramine on the EEG was observed. For enuresis type IIb, the effect of oxybutynin hydrochloride on the cystometrogram (CMG) was observed. Results: Values, in which the awakening score on the second night was subtracted from the score on the last night, were significantly higher in the effective cases than in the unchanged cases. Out of the 3 patients in whom imipramine was effective, an awakening response on the EEG was observed in 2. Neither of the 2 unchanged cases showed an awakening response. Out of 4 patients in whom oxybutynin hydrochloride was effective, uninhibited contractions (UIC) on the CMG disappeared in 3. UIC stopped in neither of the 2 unchanged cases. Conclusions: Improvement of the awakening response plays an important role in the effectiveness of conditioning treatment with our therapeutic machine. The generation of awakening response is thought to be the most important result of imipramine directly concerned with its clinical effect on enuresis type IIa. The main result with oxybutynin hydrochloride in enuresis type IIb is thought to be related to its antispasmodic effect.

Background: Oral pharmacotherapy has been commonly used as an adjunct to clean intermittent catheterization (CIC) in the treatment of neurogenic bladder in order to achieve continence, but may be associated with unacceptable side effects. The authors' experience with sterile intravesical preparations of oxybutynin hydrochloride and ephedrine in children is reported here. Methods: Patients requiring CIC for neurogenic bladder but with incontinence that was unresponsive to standard oral therapy or that was associated with severe systemic side effects were studied over a 1-year period. Clinical, radiological and urodynamic assessments were made prior to commencing treatment with intravesical oxybutynin hydrochloride. Patients who remained incontinent with poor internal sphincter muscle tone had intravesical ephedrine added. Results: Seven patients were involved in the study over a 1-year period. Two patients became continent and one patient had an improvement in upper tract dilatation. One patient had a limited improvement with oxybutynin alone but became continent with the addition of ephedrine. Three patients had no response to treatment. There were few side effects. Conclusion: Intravesical agents have a role in the management of paediatric neurogenic bladder for those children with significant adverse sequelae from oral pharmacotherapy who would otherwise require surgical intervention. Intravesical therapy is a safe technique in children with sterile preparations. Further investigation of this modality should be pursued.

PURPOSE This study was carried out to determine the effectiveness of intravesical oxybutynin hydrochloride on urinary urge incontinence in elderly people. METHODS The subjects consisted of 13 patients with an average age of 75 years who demonstrated uninhibited detrusor contraction on cystometrogram. The trial protocol consisted of a pretreatment cystometrogram followed by the intravesical administration of 10 ml solution containing 5 mg oxybutynin hydrochloride (pH 5.85). The urodynamic studies were repeated one hour later. RESULTS The mean bladder capacity before and after one hour of intravesical oxybutynin hydrochloride was 161 +/- 62 ml and 196 +/- 71 ml (mean +/- 1 S.D., n.s.). The rate of improvement was 15.4% (2 cases) in all 13 patients. Four patients out of 13 patients continued intravesical administration of the solution twice daily. Urinary incontinence disappeared in two patients and incontinence was markedly decreased in one. In the remaining patient, urinary incontinence did not change because of increased residual urine. Three patients have continued this therapy over one years and no side effects were observed. In these patients, residual urine volume did not increase. CONCLUSION It is suggested that intravesical oxybutynin hydrochloride is an effective option of therapy for intractable urge incontinence in elderly people, however, the immediate posttreatment cystometrogram was not predictive of the response to intravesical therapy on overactive bladder in the elderly.

In 36 women with cystometric evidence of bladder instability we investigated the efficacy of intravesical instillation of oxybutynin. The intravesical application of oxybutynin had a significant effect regarding the reduction of pollakiuria and nocturia and an improvement of bladder capacity. No local or systemic side effects were noted.

The metabolites, metabolizing organs of oxybutynin and its effect on the induction of drug metabolizing enzymes were investigated in rat, dog and human after oral administrations of oxybutynin and following the results were obtained.1. Eight metabolites of oxybutynin and their glucuronide were identified in the dog and human urine after oral administration.2. About 18 %, and 8.7 to 27.5 % of the administrated dose were excreted as a metabolites to urine in dogs and humans, respectively.3. It was presumed that oxybutynin was metabolized by the following four pathways; a) de-ethylation b) hydrolysis of ester c) hydroxylation at 3' and 4' positions on cyclohexyl ring and d) conjugation of each metabolites.4. The highest metabolic activity for oxybutynin was shown in the rat liver.5. The induction of drug metabolizing enzymes by oxybutynin, administered orally every day for 8 days, was not found.