Preparation and in vitro release study of ligustrazine pamoate sustained-release nanosuspension / 中草药

Objective: To prepare ligustrazine pamoate (Lig-PAM) sustained-release nanosuspension (Lig-PAM-NSps) and determine its in vitro release characteristics. Methods: Lig-PAM was prepared by hydrophobic salt formation method and its physicochemical properties were characterized. Then, Lig-PAM-NSps was prepared by miniaturized medium grinding method. The prescription and preparation process of Lig-PAM-NSps were optimized by the single factor and orthogonal experiment with average particle size, polydispersity index (PDI) and stability coefficient (SI) as indicators. Lig-PAM-NSps was characterized, and its stability and in vitro release was also investigated. Results: The compound ratio of Lig-PAM prepared by Lig and PAM in the amount of 1:1 was (97.48 ± 0.04)%. Compared with Lig, the solubilities of Lig-PAM in water and simulated body fluids were decreased by 95.50% and 77.39%, respectively. Fourier transform infrared spectroscopy (FT-IR) and X-ray powder diffraction (XRD) showed that the Lig and PAM formed Lig-PAM. The optimum prescription size of Lig-PAM-NSps was (585 ± 5) nm, PDI was (0.328 ± 0.015) and SI was (0.928 ± 0.012). The scanning electron microscopy (SEM) showed that Lig-PAM-NSps was spherical with uniform size distribution, and the particle size was about 600 nm and its physical stability was good within 60 d. The results of in vitro release showed that Lig-PAM-NSps had obvious sustained-release effect compared with Lig solution within 48 h, and showed the first-order release characteristics [ln(1-Q) = 0.153 67 t + 80.458 14, r = 0.998 26]. Conclusion: The preparation progress of Lig-PAM-NSps is stable and can release Lig slowly in vitro.

A Validated Rp-Hplc Method For Simultaneous Estimation Of Pyrantel Pamoate And Praziquantel In Bulk And Pharmaceutical Dosage Form

Objective: To develop a simple, accurate and precise reverse-phase high-performance liquid chromatography (RP-HPLC) method and subsequently validate for the simultaneous estimation of praziquantel (PZQ) and pyrantel pamoate (PP) in the pharmaceutical dosage form. Methods: The chromatographic separation was achieved on Phenomenex Luna C18 column (250 mm × 4.6 mm, 5 μm) as stationary phase maintained at an ambient temperature with a mobile phase comprising of water: acetonitrile (20: 80) at a flow rate of 1.0 ml/min and UV detection at 220 nm. Results: The retention time of PZQ and PP was found to be 3.897 min and 1.697 min respectively. The method was validated in terms of specificity, accuracy, precision, linearity and robustness as per ICH guidelines. Linearity was obtained in the concentration range of 20–60 μg/ml for both PZQ and PP with correlation coefficients of 0.987 and 0.998 respectively. The accuracy of the method was determined using a recovery test and found as 98.44 % to 100.35 %. All parameters are found to be within the acceptable limit. Conclusion: The developed RP-HPLC method was simple, rapid, accurate, precise for the simultaneous estimation of PZQ and PP in bulk and tablet dosage form.

EFECTO DEL ALBENDAZOL Y LA VITAMINA A PERIÓDICOS SOBRE HELMINTOS INTESTINALES Y ANEMIA EN NIÑOS DEL URABÁ ANTIOQUEÑO (COLOMBIA) / EFFECT OF PERIODIC ALBENDAZOLE AND VITAMIN A TREATMENT ON INTESTINAL HELMINTHS AND ANEMIA IN CHILDREN FROM URABÁ (ANTIOQUIA, COLOMBIA)

Problema: En Colombia no hay informes sobre efectos en humanos del tratamiento periódico antihelmíntico-vitamina A. Objetivo: Evaluar efectos de albendazol/pamoato de pirantel-vitamina A trimestrales sobre Ascaris lumbricoides, Trichuris trichiura, Necator americanus y sobre niveles séricos de retinol y hemoglobina, en niños del Urabá antioqueño. Metodología: Estudio clínico, aleatorio, con grupos paralelos, cerrado, intervenidos y evaluados cada 3-4 meses por 4 veces, seguidos 12 meses. Intervención: suministro de pamoato de pirantel (pamoato) (< 2 años) o albendazol (≥ 2 años), con o sin vitamina A oral. Resultados: Ingreso: 25% presentó desnutrición crónica y hemoglobina (g/L), 106 g/L en < 2 años y 115 g/L en ≥ 2 años. A) Prevalencias: estrongiloides 7%, uncinarias 29%, áscaris 45%, tricocéfalos 45%. Cambios postratamiento: pamoato únicamente causó reducción de áscaris y, en general, aumentó tricocéfalos y uncinarias. Albendazol: redujo cada helminto, como lo hicieron tratamientos sin este medicamento, pero fue mayor con albendazol. B) Cambio en carga parasitaria: únicas diferencias significativas fueron para tricocéfalos con pamoato-vitamina y albendazol-vitamina, por aumento, y áscaris con albendazol-vitamina, por reducción. No hubo diferencia significativa entre ingreso y egreso en niveles de hemoglobina ni retinol en ninguno de los cuatro tratamientos. Conclusiones: En general, no hubo efecto del albendazol sobre la carga helmintiana, pero sí efecto moderado sobre la prevalencia de uncinarias, áscaris y tricocéfalos. Quizás la desparasitación de solo parte de la población < 15 años, sin tratar el resto de convivientes, y el mantenimiento de muy deficientes condiciones de vida expliquen estos resultados.

Problem: There are no reports about the effect of periodic anthelminthic-vitamin A treatment in humans In Colombia. Objective: To evaluate effects of albendazole/ pamoate pyrantel-vitamin A administered quarterly on Ascaris lumbricoides, Trichuris trichiura, Necator americanus, and on serum retinol and hemoglobin levels in children from Urabá (Antioquia, Colombia). Methodology: Clinical, randomized, controlled trial with parallel groups intervened and evaluated each 3-4 months for 4 times, followed 12 months. Intervention: administration of pyrantel pamoate (pamoate) (< 2 years) or albendazole (≥ 2 years), with or without oral vitamin A. Results: Entry: 25% presented chronic malnutrition and hemoglobin, 10.6 g/L (< 2 years) and 11.5 g/L (≥ 2 years). A) Prevalence: strongyloides 7%, uncinaria 29%, ascaris 45%, whipworms 45%. Post-treatment changes: pamoate only caused reduction of ascaris and, in general, increased whipworms and uncinarias. Albendazole: reduced the prevalence of each helminth, as treatments without this medication did, but it was higher in treatments with albendazole. B) Change in parasite load: only significant differences were for whipworms with pamoate-vitamin and albendazole-vitamin, because of increase, and ascaris with albendazole-vitamin, because of reduction. No significant difference between entry and leave in hemoglobin or retinol levels in any of the four treatment groups. Conclusions: Overall, there was no effect of albendazole on helminth communities, but there was moderate effect on prevalence of uncinaria, ascaris and whipworms. Possibly deworming only part of the population < 15 years without treating the rest of cohabitants, and the maintenance of very poor living conditions can explain these results.

Development and Validation of UV Spectrophotometric Area Under Curve (AUC) method for estimation of Pyrantel Pamoate in Bulk and Tablet Dosage Form.

The aim of present work was to develop an accurate, precise, reproducible and economical UV spectrophotometric method for estimation of Pyrantel Pamoate. This method was based on Area Under Curve (AUC) of UV spectrum between 231 to 241 nm and validated as per ICH guideline Q2 (R1). The method is linear in the range of 1.5-3.5 μg/ml. The value of correlation coefficient is 0.999. Values of % relative standard deviation (%RSD) for the intra-day and inter-day precision indicated that method is precise. Results of the recovery studies (99.94 %) showed accuracy of the method. LOD and LOQ were calculated as 0.017μg/ml and 0.0541μg/ml respectively. The developed method can be used for routine estimation of Pyrantel Pamoate in bulk and tablet dosage forms.

In vitro Dissolution of Olanzapine Pamoate Long-acting Injections / 中国药师

Objective:To develop a dissolution method for olanzapine pamoate long-acting injections. Methods:The in vitro dis-solution profile of olanzapine pamoate was detected by an oar method and an HPLC method. The stirring speed respectively was 25, 50 and 75 r·min-1, and 500 ml of sodium lauryl sulfate simulated muscle fluid [0.5% , with pH of (7.0 ±0.05)] at (37 ±0.5)℃was used as the bio-relevant dissolution media. Results: The linearity between the peak areas and the concentrations was observed within the range of 2. 15-107. 40 mg·L-1(r=0. 999 9) for pamoate and 1. 75-87. 40 mg·L-1(r=0. 999 9) for olanzapine, respec-tively, and the average recovery of olanzapine pamoate was 99. 80%(RSD=0. 55%, n=9). The f2 for the dissolution in the dissolu-tion medium of shelf-prepared products and the innovation preparations was 70. 80. Conclusion:The dissolution method can be utilized to control the quality of olanzapine pamoate long-acting injections.

Studies on the anti-parasitic efficacy and safety of ivermectin and pyrantel pamoate compound against Dirofilaria immitis in dogs / 대한수의학회지

Dirofilaria (D.) immitis is an important canine parasitic nematode in dogs. D. immitis parasitizes the right ventricle and pulmonary artery of dogs. An ivermectin and pyrantel pamoate compound (IPPC) was administered to dogs naturally infected with this parasite. IPPC is composed of 68.0, 136.0 and 272.0 microg of ivermectin and 57.0, 114.0 and 227.0 mg pyrantel pamoate for small, middle, and large animals. Ivermectin has activity against nematodes and ectoparasites in dogs. Pyrantel pamoate is also effective against nematodes in dogs. Our results showed that this drug combination has good efficacy in D. immitis infected dogs.

Sterile Abscess Formation Associated with Two Different Forms of Gonadotropin-Releasing Hormone Agonist in Central Precocious Puberty

Long-acting formulations of gonadotropin-releasing hormone (GnRH) agonists are indicated for treating central precocious puberty. Leuprolide acetate and triptorelin acetate are widely used in Korea. Local reactions related to GnRH agonists, including erythematous macules, granulomas, subcutaneous nodules, and sterile abscesses, are the most side effects and sterile abscesses occur in less than 2-3% of treated patients. We report on two patients who had been injected with leuprolide acetate for the treatment of central precocious puberty and who subsequently presented with a sterile abscess at the injection sites. After the patients were switched to triptorelin acetate, one patient had another subcutaneous abscess at the injection site, and the other patient had no further problems. There are many theories as to the cause of these local reactions, but the mechanism has still not been elucidated. Further studies are required to identify the mechanism and the relationship between treatment effect and local reaction.

Sterile Abscess Formation Associated with Two Different Forms of Gonadotropin-Releasing Hormone Agonist in Central Precocious Puberty

Long-acting formulations of gonadotropin-releasing hormone (GnRH) agonists are indicated for treating central precocious puberty. Leuprolide acetate and triptorelin acetate are widely used in Korea. Local reactions related to GnRH agonists, including erythematous macules, granulomas, subcutaneous nodules, and sterile abscesses, are the most side effects and sterile abscesses occur in less than 2-3% of treated patients. We report on two patients who had been injected with leuprolide acetate for the treatment of central precocious puberty and who subsequently presented with a sterile abscess at the injection sites. After the patients were switched to triptorelin acetate, one patient had another subcutaneous abscess at the injection site, and the other patient had no further problems. There are many theories as to the cause of these local reactions, but the mechanism has still not been elucidated. Further studies are required to identify the mechanism and the relationship between treatment effect and local reaction.

The anti-parasitic efficacy of ivermectin and pyrantel pamoate compound against canine Toxocara canis and Trichuris vulpis / 대한수의학회지

Toxocara (T.) canis and Trichuris (T.) vulpis are very important canine parasitic nematodes. T. canis parasitize in small intestine and T. vulpis parasitize in large intestine. In order to control of these nematodes, ivermectin and pyrantel pamoate compound was applied to the dogs infected with these parasites naturally and artificially. This drug was composed of 68.0 microg of ivermectin and 57.0 mg of pyrantel pamoate for small animal, 136.0 microg of ivermectin and 114.0 mg of pyrantel pamoate for middle animal, and 272.0 microg of ivermectin and 227.0 mg of pyrantel pamoate for large animal. Ivermectin in this drug is activity to nematodes and ectoparisites. Pyrantel pamoate in this drug is also activity to nematodes. In this experiment, this drug had a good efficacy against T. canis and T. vulpis in the infected dogs.

Pyrvinium pamoate with piperazine in the treatment of enterobiasis and ascariasis

The efficacy and tolerance of CI-578 suspension (combination of pyrvinium pamoate and piperazine) against ascariasis and enterobiasis was determined. Patients were 103 children with enterobiasis including 98 with concurrent ascariasis. CI-0578 suspension was given as a single dose on 2 consecutive days. The daily dose provided 2.5 mg. of pyrvinium per kg. and 75 mg. of piperazine per kg. Two weeks after treatment, 84% of all patients were negative for Enterobius eggs. Overall reduction of Ascaris eggs was 95% with 74% of the 98 patients negative after treatment. CI-578 was well tolerated and well accepted. Mild and transient nausea occured in 9 children. (Summary)

The dangers of enterobiasis: treatment with thiabendazole chewable tablets

The incidence of Enterobiasis particularly in the Philippines has been reviewed. The hazards of Enterobiasis particularly in females has been emphasized. The different drugs used for the treatment of Enterobiasis have also been reviewed. Twenty nine out of 33 cases of Enterobiasis were found to be negative by Scotch Tape Swab technic for pinworm eggs on or about the 12th day after treatment with Thiabendazole Chewable tablets at a dose of 25 mg./kg. body weight. On or about the 21th day and the 36th day after treatment, all the 33 cases treated were all negative for pinworm eggs by the same technic of diagnosis. It appears that Thiabendazole Chewable tablets is as efficient and convenient to use as Pyrivinium pamoate with the added advantage that it can be used in the presence of Ascaris lumbricoides because of its broad spectrum anthelmintic properties. Pyrivinium pamoate is indicated only against Enterobius. The broad specturm anthelmintic property of Thiabendazole makes it the ideal anthelmintic to use in the tropics where multiple infection with intestinal parasites is the rule.(Summary and Conclusions)