Development of time and pH dependent controlled release colon specific delivery of tinidazole

Tinidazole is used in treatment of amoebiasis and other protozoal infections in doses of 2.0 g/ day [60 mg/kg] for three days. In the present paper, controlled release formulation of tinidazole was developed with an objective to achieve colon specific drug delivery with reduced frequency of dosing, to minimize gastric side effects and thus to increase patient compliance. Matrix systems of tinidazole [500 mg] were prepared by using swellable and pH dependent polymers like hydroxypropyl methylcellulose [HPMC K4M and K15M] and eudragit [eudragit L-100 and S-100]. Prepared tablets were enteric coated in order to overcome variability in gastric emptying time and delay in the release, to reduce gastric side effects and to provide prolonged localized action in colon. Process of manufacture was optimized during the scale up studies. Bioavailability study [using parallel group design] was carried of on conventional marketed, developed uncoated and enteric coated tablets in healthy human volunteers. Bioavailability study showed that greater portion of tinidazole was released in the large intestine and drug level in plasma was above 4 micro g/mL in blood for 24 hours. From the results of this study it appears that, the proposed single enteric coated tinidazole [500 mg] tablet per day could be used in place of 3-4 doses of 500 mg tinidazole conventional tablet with better control of drug release for targeted drug delivery. In addition developed colon-specific drug delivery system [CDDS] was relatively inexpensive and easy to manufacture using conventional pharmaceutical coating technique

Eficácia e tolerabilidade do secnidazol suspensão versus tinidazol suspensão no tratamento da giardíase em crianças / Efficacy and tolerability of secnizadol and tinizadol both in the suspension form in the treatment of giardiasis in children

Objetivo: Comparar a eficácia e tolerabilidade do secnidazol(SEC) e tinidazol(TIN) no tratamento da giardíase em crianças. Métodos: Em estudo multicêntrico, aberto, randomizado, 321 crianças de 2 a 14 anos de idade, dos sexos feminino e masculino e portadores de giardíase, receberam secnidazol suspensäo, 30mg/kg(N=160) ou tinidazol suspensäo, 50mg/kg(N=161), ambos em dose única. Todas as crianças apresentavam exame protoparasitológico positivo par Giardia lambia antes do tratamento e foram reavaliadas laboratorialmente (métodos Faust e Kato-Katz) 7, 14 e 21 dias após a administraçäo das drogas. Resultados: Cura parasitológica foi obtida em 95 porcento dos pacientes do grupo SEC e 97 porcento dos pacientes do grupo TIN, näo apresentando diferença estatística significativa (p=0,430). Eventos adversos, possível ou provavelmente relacionados ao medicamento em estudo, ocorreram em 7 porcento dos pacientes do grupo SEC versus 16 porcento do grupo TIN, uma diferença estatisticamente significativa (p=0,009). Os eventos individuais "gosto amargo" (1,9 porcento SEC vs 7,5 porcento TIN, p=0,018) e "vômito" (0,6 porcento SEC versus 4,3 porcento TIN, p=0,032) também tiveram uma incidência significativamente diferente nos dois grupos. Conclusöes: Secnidazol e tinidazol foram igualmente eficazes no tratamento da giardíase, mas o secnidazol apresentou melhor perfil de tolerabilidade nesta faixa etária

Comparative study of the efficacy and tolerability of Secnidazole suspension (single dose) and Tinidazole suspension (two days dosage) in the treatment of amebiasis in children

Amebiasis caused by Entamoeba histolytica may be considered the most aggressive parasitic disease affecting human intestine, causing acute amoebic colitis and extra-intestinal diseases of high morbidity and mortality. 5-nitroimidazoles are the drugs of choice. In this multicenter, open and randon clinical trial, the efficacy and tolerability of secnidazole suspension in a single oral dose of 1ml/kg was compared with 0.5ml/kg doses of tinidazole suspension given for 2 consecutive days to 303 Entamoeba histolytica-positive children aged 2 to 13. Patients with extra-intestinal complications were excluded from the study. Clinical and parasitological follow-up using the Faus and Kato-Katz method were carried out 7, 14, and 21 days after treatment. Clinical improvement/cure was observed in 93 percent of the patients in the secnidazole group and 91 percent in the tinidaloze group. Parasitological sucess was reported for 77 percent and 63 percent of the secnidazole and tinidazole patients, respectively, showing a significant statistical difference between the two groups (p=0.007). Both drugs were well tolerated, and the adverse effects reported were mild, consisting mainly of digestive disturbances. This comparative study showed that a single oral dose of 1ml/kg of secnidazole produced a significantly higher parasitological cure rate than 2 doses of tinidazole. Secnidazole is a safe and effective drug for the treatment of uncomplicated intestinal amebiasis.

Post marketing surveillance of ciprofloxacin-tinidazole combination

The post marketing surveillance of ciprofloxacin and tinidazole combination was designed to monitor clinical experience and adverse reactions of this combination in actual clinical settings. Though adequate efficacy and safety information is available on ciprofloxacin and tinidazole as individual drugs, there is no study on post marketing surveillance or adverse drug reaction monitoring of ciprofloxacin and tinidazole combination, so we decided to conduct this study in India. This study was conducted on 729 patients, with the help of 152 practising doctors all over India. This was an open, non-comparative post marketing surveillance study to monitor the clinical experience with ciprofloxacin 500mg and tinidazole 600mg combinations in adult patients in actual clinical settings. From the results of the study, it was observed that this combination is used in a variety of indications like surgical, gynaecological, gastrointestinal, bone and respiratory tract infections. A good response was observed in surgical, gynaecological and gastrointestinal infections while a satisfactory response was observed in bone infection. No adverse drug reaction was observed in 55% of the cases. In conclusion, our study confirms the efficacy of ciprofloxacin and tinidazole combination in various surgical, gynaecological and gastrointestinal infections. It also showed good results in dental, ENT, and respiratory tract infections and chronic osteomyelitis. This combination has also been used in paediatric patients with good results and no arthropathies. This study also showed that this ciprofloxacin and tinidazole combination is well tolerated in the Indian population

Evaluation of secnidazole gel and tinidazole suspension in the treatment of giardiasis in children

Giardiasis is a cosmopolitan parasitosis. Diarrhea, abdominal colic, and flatulence are the main clinical symptoms, however, malabsorption, and impairment of growth of children may occur. The 5-nitroimidazoles are drugs of choice in the treatment of giardiasis. Methods: The efficacy and tolerability of secnidazole and tinidazole were evaluated in a randomized, open-label clinical trial performed with 267 Giardia lamblia-positive children. Secnidazole , in a new gel formulation, and tinidazole suspension were prescribed as single oral doses of 30mg/kg and 50mg/kg, respectively. Clinical and parasitological follow-up was carried out before, and at 7, 14, and 21 days after treatment. Results: Clinical cure was observed in 77,3 percent and 75,7 percent of the patients in the secnidazole and tinidazole groups, respectively. Parasitological cure was obtained in the 91,3 percent and 89,6 percent in the secnidazole and tinidazole groups, respectively. A metallic taste after drug ingestion was more commonly reported in the tinidazole group than in the secnidazole group (p<0.05). Conclusions: The authors conclude that both secnidazole gel and tinidazole administered as a single oral dose are effective treatments for children with giardiasis since both high cure rates and good tolerability were observed