RESUMEN
BACKGROUND: Camptothecin is known for its potent anticancer activity. However, its optimal activity is reduced due to its low solubility and stability in biological media. OBJECTIVE: The aim of the present study is to design and characterize a Camptothecin (CPT) suppository formulation. METHODS: Rectal suppositories of camptothecin alone, encapsulated with Cyclodextrin (CD) and in the ternary system (CPT encapsulated with cyclodextrin and dispersed in Polyethylene Glycol (PEG) 6000) were prepared using various hydrophobic and hydrophilic polymeric bases as semi-synthetic glyceride (Suppocire® AM Pellets) and Polyethylene Glycols (PEGs) mixtures. Formulations were evaluated by various parameters like weight variation, drug content, hardness and liquefaction time. In vitro release study was performed in USP type I apparatus using phosphate buffer pH 7.2 as dissolution media. RESULTS: Suppositories were within the permissible range of all physical parameters. In vitro drug released from water soluble base (PEG) was greater than that from oil soluble base with ninety percent (90%) of drug dissolution. It was also established that drug release from various formulations was by diffusion mechanism, according to the Higuchi's equation. CONCLUSION: This new formulation offers a new approach to colorectal cancer treatment by offering an alternative and simple drug administration route.
Asunto(s)
Antineoplásicos/química , Camptotecina/química , Supositorios/química , Antineoplásicos/síntesis química , Camptotecina/síntesis química , Cápsulas/síntesis química , Cápsulas/química , Composición de Medicamentos , Liberación de Fármacos , Humanos , Estructura Molecular , Polietilenglicoles/química , Supositorios/síntesis químicaRESUMEN
The objective of present study was to develop and evaluate polyethylene glycol (PEG) based diclofenac sodium suppositories. This study used water soluble PEG bases (1000, 4000 and 6000) in different combinations to formulate suppositories, which were further subjected for their physicochemical properties evaluation such as weight variation, average melting point, content uniformity and disintegration. Dissolution test was used to perform the in vitro release rate studies of the suppositories. The suppository (P3) containing PEG-6000 (50%) and PEG-4000 (50%) exhibited rapid in vitro release rate of diclofenac sodium. Moreover, homogeneous distribution of diclofenac sodium is found in all six formulations. The in vitro release patterns of diclofenac sodium from the marketed Voltral suppository (100mg) and formulated suppositories were also compared and found in standard limits.
Asunto(s)
Diclofenaco/farmacocinética , Desarrollo de Medicamentos/métodos , Polietilenglicoles/farmacocinética , Supositorios/farmacocinética , Diclofenaco/síntesis química , Evaluación Preclínica de Medicamentos/métodos , Polietilenglicoles/síntesis química , Supositorios/síntesis químicaRESUMEN
A vaginal suppository containing ulinastatin (UTI) was developed as a hospital pharmacy product from UTI injection solution and Witepsol® S-55. After mixing at 50°C for 0-8 h, UTI suppositories were prepared, which had good UTI content uniformity. Because 2% surfactant was contained in S-55, the UTI injection solution formed a water-in-oil type emulsion as a suppository base. The measured residual moisture content (loss on drying (LOD)) in the prepared vaginal suppositories decreased as the mixing time increased, but their hardness (hardness test (HT)) increased. Near (N) IR spectra of UTI suppositories were measured after mixing for 0-8 h. The best calibration models to predict the HT and LOD of the suppositories were determined based on the NIR spectra by the leave-one-out method in a partial least-squares regression analysis (PLS). The validation result indicated that PLS models for HT and LOD were obtained based on the spectra treated by a combination of smoothing and normalized, respectively, and the model consisted of three latent variables. The plots between the predicted and measured pharmaceutical properties (HT and LOD) based on the calibration data were superimposed with those of the external validation data. The developed NIR spectroscopy method was applied to the preparation process monitoring for UTI vaginal suppositories. In the prepared vaginal suppositories, the predicted LOD decreased as the mixing time increased, and the measured LOD values superimposed well with the predicted values. In contrast, the predicted HT increased as the mixing time increased, and the measured values superimposed with the predicted values.
Asunto(s)
Composición de Medicamentos , Glicoproteínas/química , Preparaciones Farmacéuticas/química , Calibración , Química Farmacéutica , Hospitales , Preparaciones Farmacéuticas/síntesis química , Espectroscopía Infrarroja Corta , Supositorios/síntesis química , Supositorios/químicaRESUMEN
We designed a new complex drug with antiallergic effect containing, in addition to the main component loratadine, a phytocomplex for an extra therapeutic effect. A collection of plants with sedative activity is chosen and the optimal agent for extraction of bioactive compounds (40% ethanol) and optimal degree of plant fragmentation are determined. Chemical composition of the sedative tea is evaluated by reverse phase HPLC. The marker components of the species are detected: xanthohumol and isoxanthohumol - Humulus lupulus cone components, Mentha piperita rosmarinic acid, and scutellareine, Menyanthes trifolia element - quercetin-3-rutinoside, and caffeic acid. Standardization of the species by the absolute graduation method in conversion to quercetin-3-rutinoside is suggested.
Asunto(s)
Antagonistas de los Receptores Histamínicos H1/aislamiento & purificación , Humulus/química , Mentha piperita/química , Fitoquímicos/aislamiento & purificación , Supositorios/síntesis química , Apigenina/química , Apigenina/aislamiento & purificación , Ácidos Cafeicos/química , Ácidos Cafeicos/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Cinamatos/química , Cinamatos/aislamiento & purificación , Depsidos/química , Depsidos/aislamiento & purificación , Etanol/química , Flavonoides/química , Flavonoides/aislamiento & purificación , Antagonistas de los Receptores Histamínicos H1/química , Antagonistas de los Receptores Histamínicos H1/normas , Humanos , Fitoquímicos/química , Fitoquímicos/normas , Extractos Vegetales/química , Propiofenonas/química , Propiofenonas/aislamiento & purificación , Rutina/química , Rutina/aislamiento & purificación , Solventes/química , Xantonas/química , Xantonas/aislamiento & purificación , Ácido RosmarínicoRESUMEN
Parasitic diseases are of immense global significance as around 30% of world's population experiences parasitic infections. Among these, malaria is the most life-threatening disease. Various routes of administration have been explored for delivering antimalarial actives. The present investigation aims at formulating self-microemulsifying suppositories of ß-artemether with faster onset of action and prolonged effect to be administered by rectal route. These were compared with conventional polyethylene glycol suppositories with respect to melting range, rheology, texture analysis, disintegration time, self microemulsification time, particle size, and drug content. In vitro drug release was studied by using USP apparatus II. Further, the suppositories were evaluated in murine model against virulent rodent malaria parasite Plasmodium berghei wherein the developed self-microemulsifying suppositories could sustain the activity (94%) for 20 days post infection. The survival of animals was also better as compared to the conventional formulation.
Asunto(s)
Artemisininas/administración & dosificación , Artemisininas/química , Modelos Animales de Enfermedad , Emulsiones/síntesis química , Malaria/tratamiento farmacológico , Supositorios/administración & dosificación , Supositorios/síntesis química , Animales , Antimaláricos/administración & dosificación , Antimaláricos/química , Composición de Medicamentos/métodos , Humanos , Malaria/diagnóstico , Masculino , Ratones , Ratones EndogámicosRESUMEN
PURPOSE: To prepare and evaluate a suppository dosage form of salbutamol sulfate. The prepared formulae with and without different concentrations of gels were tested for hardness, melting time, content uniformity, and drug release. The stability of some of the selected formulae was assessed. METHODS: Salbutamol sulfate was formulated as a rectal suppository with emulsifying fatty bases (suppocire and witepsol) and water-soluble bases (PEG) adopting the molding from a melt technique. Physical characteristics and dissolution profiles of the prepared formulations were determined as the responses. The effects of adding gels, methyl cellulose (MC), and Eudispert (Eud) and their concentrations (1, 3, and 6%) on these responses were also investigated. Formulations showing high rank order were scaled up for shelf-life stability study for one year. RESULTS: The results showed that all the investigated formulae have acceptable physical characteristics with respect to hardness, melting time (except F7), and uniformity of drug content. The amount of drug dissolved in 100 min of dissolution time was inversely affected by the melting point of the fatty base. The release from PEG bases was found to be molecular weight dependent. Addition of 1% MC or Eud gel increased the release from all the investigated formulae. Increasing gel concentration to 3% then to 6% showed different effects on the release. The degradation of salbutamol sulfate in the investigated formulae was found to be a first-order reaction. CONCLUSIONS: Rectal suppository of salbutamol sulfate could be prepared as an alternative to the oral dosage form to circumvent the first-pass metabolism.