Bollettino chimico farmaceutico最新文献

A critical quality control of seven brands of ciprofloxacin hydrochloride tablets marketed in Nigeria [Cifran (Ranbaxy, Nigeria), Ciproxin (Bayer, Nigeria), Cenox (Micro labs, India), Ciprotab (Fidson Drugs, India), Ciprofloxacin MS1 and MS2 (Sintacrus Medical stores] were carried out with the aim of selecting brands that are interchangeable. The weight uniformity, disintegration time, absolute drug content and in vitro dissolution profile of the various brands of the tablets were evaluated in simulated intestinal fluid (SIF) and simulated gastric fluid (SGF) without enzymes. The concept of dissolution efficiency (DE) was used to predict the likely in vivo availability. The weight uniformity and the disintegration time of most of the tablets were within the acceptable official ranges. The DE varies widely in the two media. Based on the DE in SGF, Cifran, Ciproxin, Cenox and Ciproflox are bioequivalent and therefore interchangeable. In SIF, however only Ciproflox and Ciprofloxacin MS1 (blue label) were bioequivalent with the innovator brand (Ciproxin, Bayer). In vitro dissolution studies using the concept of dissolution efficiency could serve as a rapid means of selecting probable therapeutically effective brands of ciprofloxacin HCl marketed in Nigeria. Using this concept, four brands (Cifran, Ciproflox, Cenox and Ciproxin) have been shown to be bioequivalent.

In the present study formulation of sustained release capsule of acetazolamide 250 mg was tried using nonpareil seeds. Nonpareil seeds were coated with drug, polyvinylpyrrolidone, glyceryl monostearate, microcrystalline wax, and glyceryl distearate either individually or in combination to achieve sustained release capsule 250 mg. In successful formulation 20% drug coated pellets and 80% wax coated pellets were taken. Wax coated pellets for successful formulation contained coating of microcrystalline wax and glyceryl distearate on drug coated pellets of the same concentration of 1.6% w/w. Successful formulated sustained release capsule 250 mg of acetazolamide was compared in in vitro study with theoretical sustained release formulation suggested by wagner and one marketed sustained release capsule 250 mg. Formulated capsule showed result superior to or on par with marketed capsule. For successful formulation pellets were filled in '1' size hard gelatin capsule and stability study was carried out in hot air over at room temperature and 45 degrees C for 5 weeks. The formulation was found stable in respect of drug content and release rate.

The dynamics of peptide release from suspensions in the form of solid, sparingly soluble Zn(II)-Peptide complexes in molar ratio 50:1 was observed in vitro conditions. Thyroliberine and dalareline release from suspensions is statistically significant in comparison with gonadrenaline release. Pulsatile character of peptide release in 6 significant peaks of released dalareline, 5--of gonadoreline release and 4--thyroliberine were observed. Thyroliberine was released fastest from the obtained suspensions--63 h +/- 3.1, and dalareline was released slowest--26.5 h +/- 2.3. The release time for gonadoreline from suspensions was 12.0 h +/- 1.0. Molecular weight of the peptide and properties of the Zn(II)-Peptide complexes have major influence upon the character and time of peptide release from suspensions. The greater is the molecular weight and durability of Zn(II)-Peptide complex, the bigger is the number of peaks of the peptide released from suspensions. The release time of the peptides is longer when the molecular weight of the released peptide is bigger.

The present study describes the analgesic effects of the crude extracts (hexane, methylene chloride and ethanol) obtained from the aerial parts of Miconia albicans (Melastomataceae) using the writhing test and the hot plate models for pain in mice. The extracts in hexane and methylene chloride, given orally, produced significant antinociception in the writhing test. On the other hand, none of the extracts had a significant effect on the hot plate test, a fact suggesting that the substances present in the extracts may rather have peripheral analgesic activity.

Two formulations of insulin suppositories were prepared to contain different amounts of sodium salicylate and sodium cholate as absorption promoters and also of insulin with the purpose of obtaining the most effective formulation in reducing plasma glucose levels after rectal administration to diabetic patients. The results show that insulin suppositories containing 100 mg sodium salicylate and 100 or 200 U of crystalline insulin showed no significant difference in AUC, Cmax and Tmax and both formulations showed significant reduction in plasma glucose level compared to initial values within 1.5-2 h. The results from experiments carried out in health volunteers showed that 100 mg sodium salicylate is the optimum amount to be included in insulin suppositories producing significantly higher Cmax and AUC compared to those produced after rectal administration of insulin suppositories containing 50 or 200 mg sodium salicylate. The results also show that using sodium cholate in 50 mg amount did not produce any significant reduction in plasma glucose levels of insulin dependent diabetic patients given suppositories containing 100 U of insulin, but this amount in suppositories containing 200 U of insulin was able to produce significant (p < 0.05) reduction in plasma glucose level within 1 h which lasted till end of experiment producing Cmax of 29.7 +/- 6.61% at Tmax of 1.5 +/- 0.61 h. On increasing the amount of sodium cholate to 100 mg in the suppositories, a marked (p < 0.01) reduction in plasma glucose level took place and the Cmax increased to 47.7 +/- 12.24% at Tmax of 1.5 +/- 0.63 h. This resulted in AUC of 86.7 +/- 22.4 mg%h which was non significantly higher from that produced after administration of suppositories containing 50 mg sodium cholate and 200 U insulin (62.5 +/- 17.6 mg%h). The results also show that insulin suppositories containing 100 mg sodium cholate and 200 U insulin resulted in a non significant differences in Cmax and AUC from those produced by S.C. injection of insulin (20 U) but significantly (p < 0.001) shorter Tmax. This formulation also shows non significant differences in Tmax and AUC and significantly (p < 0.05) higher Cmax than from those produced after rectal administration of suppositories containing 100 mg of sodium salicylate and same amount of insulin. Further more this formulation produced severe hypoglycemia in control healthy volunteers within 1 h of administration producing Cmax of 57.0 +/- 18.8% at Tmax of 0.75 +/- 0.35 h. The results of this study showed that the formulation containing 100 mg of sodium cholate and 200 U of insulin tested in fasted insulin dependent diabetic patients produced a maximum % reduction in plasma glucose levels (Cmax) of 47.7 +/- 12.24% at tmax of 1.5 +/- 0.63 h compared to Cmax of 50.56 +/- 6.8% at tmax of 2.93 +/- 0.19 h resulted after subcutaneous injection of 20 U insulin. These suppositories produced an area under the curve (AUC) of 87 +/- 22.4 mg%h compared to an AUC of 81

The objective of this investigation was an attempt to conclusively prove the accidental observation that the AUC of apomorphine in rabbits was repeatedly lower after intravenous injection compared to subcutaneous injection. Apomorphine was administered to rabbits by intravenous and subcutaneous routes at 2 different doses (0.31 mg/kg, n=10; and 0.25 mg/kg, n=6). Plasma drug concentrations were measured by HPLC-ECD and pharmacokinetic parameters were estimated by compartmental and non-compartmental approaches. The AUC of apomorphine in rabbits were: for subcutaneous injection, 14138 +/- 502 ng/ml/min and 12680 +/- 855 ng/ml/min, n=10 and 6, respectively; for intravenous injection, 11850 +/- 718 ng/ml/min and 9147 +/- 671 ng/ml/min, n=10 and 6, respectively. These AUC values were statistically significantly lower when given as intravenous injection compared to subcutaneous injection (p=0.0011 and 0.0117, n=10 and 6, respectively). The T1/2,elim values were: for subcutaneous injection, 17.1 +/- 1.70 min and 18.7 +/- 1.68 min, n=10 and 6, respectively; for intravenous injection, 15.3 +/- 1.20 min and 15.0 +/- 2.24 min, n=10 and 6, respectively. There were no significant differences between the T1/2,elim from both administration routes (p=0.3984 and 0.2158, n=10 and 6, respectively). Given the reproducibility of the results, it was concluded that the AUC of apomorphine after intravenous injection in rabbits is anomalously lower than that of subcutaneous injection.

Gelatin magnetic microspheres loaded with diclofenac sodium were prepared by emulsification and crosslinking by glutaraldehyde. The microspheres were formulated with 23-30% theoretical diclofenac sodium and magnetite content. The formulated microspheres were characterized by drug loading, entrapment efficiency, encapsulation efficiency, magnetite content, FT-IR spectroscopy, particle size analysis, optical microscopy, scanning electron microscopy, and in vitro release studies. The data obtained from the in vitro release studies were applied to various kinetic models. The FT-IR revealed no drug/polymer interaction. The average particle size was between 36 to 61 microm depending on quantity of magnetite and gelatin used. Optical microscopy and SEM showed spherical and compact nature of microspheres. The formulated microspheres released the drug for a period of 42 to 78 hours depending on drug loading. The release was diffusion controlled at lower drug loading and dissolution/diffusion controlled at higher drug loading.

Carbopol 941 (C-941) and Abelmuschus esculentus gum (Okra gum, AEG) were used as bioadhesive polymers in the formulation of mucoadhesive indomethacin tablets. Different batches of the tablet compacts were formulated based on different combination ratios of the polymers. The bioadhesive properties of the tablets were studied using a tensiometer: Tablets coated with 50% w/v solution of Eudragit I. 100 in ethanol, were also prepared and evaluated. The following tablet physical properties were evaluated: hardness, uniformity of weight, disintegration time, friability, and absolute drug content. Release studies were determined in simulated intestinal fluid (SIF pH 7.2) without pancreatin, and in 0.1 N solution of HCl. Result obtained indicated that tablets with equal ratio of C-941 and AEG (1:1) gave the highest bioadhesive strength for both the coated and uncoated tablets. The percentage of drug released ranged from 53-90% for uncoated tablets in 0.1 N HCl and SIF, and 9-16% for coated tablets in 0.1 N HCl, and 63-100% for coated tablets in SIF after 8 hrs.

By means of bioluminiscence ATP present in a sample can be quantified. Thus, it would be a method able to evaluate microbiological or organic matter (from vegetal or animal origin) contamination. The present work analyzes the possibility to assess--from the microbiological point of view--the air of pharmaceutical clean rooms by means of bioluminiscence, using the luminomiter HY-LITE 2 [Merck]. It is thought that the use of this methodology versus microbiological classical methods, will allow to obtain results in the working day. Classical methods demand a minimum of 72 hs incubation to read results. But the real conclusion is that with the used technology, it is not possible to evaluate microbiologically the air of pharmaceutical clean rooms.

The stability studies of tablets containing 5 mg of policosanol, a new cholesterol lowering drug, were conducted to predict an expiration date and to search the appearance of putative degradation products. All quality parameters such as colour, moisture content, hardness, disintegration, policosanol content and microbiological limits of the tablets were assessed. The effect of extreme treatments such as acid and basic hydrolysis, oxidative and photolytic degradation as well as thermal degradation, on the policosanol content was studied. In addition, studies under extreme conditions of storage [(40 +/- 2) degree C and (75 +/- 5)% R.H.] as well as 37, 45, 55 and 60 degrees C combined with 50, 75 and 92% R.H.) and under ambient conditions of storage for climatic zones II and IV were performed. These studies demonstrate that these tablets are a stable pharmaceutical formulation, without significant changes in their quality criteria at the stressed conditions used, so that policosanol content remains unchanged during the entire studies. The chromatographic profile of the samples after 9 months of thermal degradation shows chromatographic peaks that corresponds to the palmitate and stearate esters of octacosanoyl, triacontanoyl and hexacosanoyl, being the only degradation products observed on these studies.