Effect of penetration enhancers on the permeability of ketoconazole gels through rabbit skin

The influence of several penetration enhancers on the percutaneous penetration of ketoconazole [KC] from hydroxypropylmethyl cellulose [HPMC], sodium carboxymethyl cellulose [NaCMC] and carbopol 934 gel formulations was investigated. Skin permeation studies were performed using Franz-type diffusion cells and full-thickness abdominal rabbit skin. Various types of compounds such as oleic acid [OA], menthol [M] and isopropyl myristate [IPM] in various concentrations were employed as penetration enhancers. The steady-state flux, permeability coefficients, and enhancement ratios ER of [offlux] KC for each formulation were calculated. The results showed that the skin permeability of KC from gels tested was significantly increased [P< 0.05] by 10% w/w OA, 5% w/w M and 5% w/w IPM. ER [flux] of KC gels containing 10% OA were 19.5, 16.4 and 11.9 for NaCMC, HPMC and carbopol gel respectively. ER [flux] of 5% w/w M were 13.5, 13.3 and 10.9 for HPMC, NaCMC and carbopol gel respectively. About 11 fold increase in the ER [flux] at 5% w/w IPM for all gels. Kinetic analysis of the data indicated that the permeation of [KC] from different gel formulations obeyed Higuchi-diffusion model. In conclusion, OA, M and IPM could be considered as penetration enhancers for KC topical formulations

Phonophoresis of theophylline through cellophane membrane and rabbit skin

The influence of ultrasound waves upon the permeation of theophylline through cellophane membrane and rabbit skin was studied in vitro. Sonication was carried out with continuous mode at intensities [0.5, 1, 1.5, and 2 W/cm 2 at constant frequency 800 KHz for one sr. Different gel formulations with [hydroxypropylmethyl cellulose, sodium carboxymethylcellulose and carbopol 934P] in different concentrations [1-4% w/w] were utilized. Phonophoresis of theophylline through rabbit skin were significantly less than that obtained with the cellophane membrane. Ultrasound application has showed a significant increase in the amount of theophylline permeation with increasing intensity. For all the tested gelling agents, the amount of drug released was decreased by increasing polymer concentrations. The Flux values were 5.99, 3.69 and 2.4 [micro g/min cm 2] for 2% HPMC, 4% Na CMC and 2% carbopol 934P gels respectively. It was found that drug release from HPMC gels obeys Zero-Order model while its release from Na CMC and carbopol 934P were fitted with First-Order and Higuchi-diffusion model respectively

Role of Omega-3 essential fatty acids in pregnancy induced hypertension

Pre-eclampsia is a major health problem contributig largely to maternal and neonatal morbidity and mortality which is of obscure etiology. It is characterized by vasoconstriction and platelet aggregation which is attributed to imbalance of thromboxane A2 and prostacyclin A2. This imbalance could be corrected by polyunsaturated fatty acids of n-3 class by competing with arachidonic acid for cyclooxygenase enzyme producing inactive prostanoid. To study the relation of omega-3 fatty acids and the severity of pre-eclampsia. 10 mild pre-eclamptic, 10 severe pre-eclamptic and 10 eclamptic patients were compared to a control group of 20 normal pregnant patients for their plasma levels of omega-3 fatty acids using high performance liquid chromatography. pre-eclamptic patients were significantly lower in their plasma levels of fatty acids than in control group

Formulation and stability of atropine sulfate eye drops

Atropine sulfate was formulated in ophthalmic solutions using methylcellulose, sodium carboxymethylcellulose, polyvinyl alcohol, polyethylene glycol 6000, and polyvinyl-pyrrolidone K25. The formulations were subjected to stability studies. The obtained results revealed that, no degradation or complexion occur among the tested preparations with the exception of that contained methylcellulose. A significant decrease of drug content and viscosity of the solution was appeared after storage for the first month. Furthermore, the degradation in drug concentration was reached more than 60% after storage at 70C for two years. Also, TLC revealed a chemical decomposition of atropine sulfate in methylcellulose solution

Effect of atropine sulfate ointments and gels on the intraocular pressure of rabbit's eye

Atropine sulfate has been formulated in ointments and gels using absorption base, hydrocarbon base, water soluble base, polyvinylpyrrolidone gel and sodium carboxymethylcellulose gel. The release behaviour of the drug and the effect on intraocular pressure of rabbit's eye have been estimated. The results revealed that, the release of atropine sulfate was in the following order, polyvinylpyrrolidone gel > polyethylene glycol > sodium carboxymethylcellulose gel > lanolin-petrolatum > hydrocarbon base. However the maximum effect of drug on intraocular pressure was maintained within three hours in the following order, sodium carboxymethylcellulose gel < hydrocarbon base < polyethylene glycol base < polyvinylpyrrolidone gel < lanolin-petrolatum base

Effect of vehicle composition on bioavailability of atropine sulfate in rabbit's eyes

The effects of vehicle composition on ocular disposition of atropine sulfate was studied using different ophthalmic drops, ointments and gels on rabbit's eyes. The bioavailability of the drug in eye tissues showed that, their distribution were greatly affected by the type of the vehicle. In addition, the uptake by different eye tissues was variable. The peak time of atropine sulfate was found to be 2 hours for ophthalmic drops and 3 hours in case of ointments and gels. The total bioavailability of atropine sulfate in eye tissues of rabbit and aqueous humor after 2 hours were 4350,4010 and 3675 ugm/gm using NaCMC, PVP and PEG ophthalmic drops. While that from ointments and gels after 3 hours were 4355, 4320, 4255 and 4205 ugm/gm for PVP gel, PEG base, hydrocarbon base and NaCMC gel respectively

Cervical colonization with actinomyces in women using intrauterine contraceptive devices

Intrauterine contraceptive device [IUCD] was found to promote colonization by actinomyces species. The presence of cervical actinomyces colonization was verified by using direct endocervical smears stained by simple gram stain, it was found among 10% of long term IUCD users. By using culture on brain heart infusion blood agar containing 2.5 mg/L metronidazole, anaerobically incubated for a fortnight, the prevalence was 2% of long term IUCD users. The removed loops of these two cases were positive. Actinomyces was not detected among short term IUCD users. No statistical significant difference between negative, positive and control cases in age, parity and duration of marriage, however the frequency of sexual intercourse was an important which affected the colonization of the cervix with actinomyces species. Though most of the cases with positive actinomyces were asymptomatic, it seems wise enough to overcome this colonization by frequent change of IUCD and not allowing them to st and in utero for long periods

Formulation and release characteristics of phenylephrine hydrochloride suppositories

Phenylephrine hydrochloride suppositories were formulated using Witepsols H[15], W[35] and E[75] each alone or in combinations of two in different ratios of 1:1, 1:2 and 2:1. The prepared suppositories were evaluated for their mechanical properties, release characteristics and drug partitioning using different bases and water. The obtained results revealed that the prepared suppositories exhibited good mechanical properties and different release characteristics. The partition coefficient of the drug was found to be in a good correlation with its release profiles from the corresponding bases. Witepsol W[35] either alone or in combinations with E[75] or H[15] in a ratio of 2:1 [W[35]:E[75] or H[15]] were found to be the bases of choice for formulating phenylephrine hydrochloride suppositories referring to their good mechanical properties and high release characteristics. The bioavailability of the drug after rectal administration in rabbits was greater with Witepsol W[35] over Witepsols H[15] and H[15]+W[35] [1:2]. A highly significant in-vivo in-vitro correlation existed

Application of factorial design of experiments to predict the chemical stability of ferrous fumarate and thiamine hydrochloride tablets

In this-investigation factorial design of experiment of the type N = 2 [3]was applied to predict the chemical stability of ferrous fumarate and thiamine 'hydro chloride in tablets prepared by direct and wet granulation techniques, using Span 40, stearic acid and PEG 6000 as granulating agents. The quantitative factors were the temperature, humidity and time, corresponding to the accelerated storage conditions which are 52% and 95% relative humidity at two temperature levels [25 and 42 C]. The effect of the three operating factors and their interactions on the stability of both drugs as well as the derivation of impervical, regression equations were determined. The derived regression equations have the ability to predict the chemical stability of ferrous fumarate and thiamine hydrochloride tablets at any particular conditions within the limits specified. In addition, the coefficients of the factors and their interactions were found to have negative signs, which indicated that the effect of each factor was dependent on the level of the other two factors. The obtained results revealed that, there was very good agreement between the predicted and the experimental data obtained from the classical design of the experiments, carried out under the specified storage conditions. The reaction rate constants and [90%] of ferrous fumarate and thiamine hydrochloride tablets determined from the regression equations were found to be parallel with those determined from the first order plots. These findings indicated that, with the help of factorial design of experiments it could be possible to predict the expiry date of such tablets in a short time and less cost of experimentation

Release characteristics of saluzide from suppository bases

Saluzide suppositories were prepared using Witepsols and polyethylene glycols [PEG] bases. The physicochemical and the release behaviour of drug from the prepared suppositories were investigated. The data of release of drug were analyzed according to order of kinetics. It was found that the release of saluzide from Witepsols was lower than that from PEG. In addition the rate of release was found to be diffusion controlled from the fatty bases. However, the first order kinetic fitted the release of drug from suppositories prepared using PEG

Study on the effect of the combination of propranolol hydrochloride and pilocarpine hydrochloride on intraocular pressure of rabbit's eye

Pilocarpine hydrochloride and /or propranolol hydrochloride were formulated in aqueous solutions and gel form using methyl cellulose and sodium carboxymethylcellulose as thickening and gelling agents, respectively. Both formulations were instilled into normal rabbit's eyes and the changes in the intraocular pressure [IOP] were determined. It was found that the action of both drugs on the intraocular pressure was significantly increased in the presence of the added polymers. Moreover, the optimum decrease in IOP was reached in a shorter time with aqueous solution [2 h] and gel form [3 h] than with control drugs without polymer [4 h]. The peak heights of such decrease were in percentage for pilocarpine hydrochloride 7.2, 27.5 and 17.9, for propranolol hydrochloride 12.5, 18.4 and 17.3 and for their mixture 15.4, 15.4, 15.4 and 16 as aqueous solution, aqueous solution with methylcellulose and gel form, respectively. The study showed that the use of propranolol hydrochloride with pilocarpine hydrochloride with pilocarpine hydrochloride in a concentration of 1% each causes a maximal decrease in IOP in presence of methylcellulose as a thickening agent

Influence of microcapsule size on the bioavailability of acetylsalicylic acid

Preparation of ethylcellulose microcapsules containing ASA were achieved. Four microcapsule sizes were separated using standard sieves set. The percent release as well as the bioavailability of each size were studied to get a correlation between in-vitro and in-vivo drug availability. Larger size microcapsules were found to show a lower bio-availability when compared with smaller ones. The same was observed in-vitro. A good correlation between in-vitro and in-vivo data was noticed in testing the dissolution rate of microcapsules alter 15 and 30 min. with percent excretion of ASA after one hour

Salivary and serum immunoglobulin-A in pregnancy and its relation to the gingival condition

Thirty pregnant females in the three trimesters of pregnancy and ten controls were subjected to clinical dental examination together with estimation of salivary and serum immunoglobulin-A [Ig A] by the radio-immuno diffusion technique. The gingival index showed a significant increase in the third trimester while the plaque and retention indices did not show any statistical difference in the three trimesters of pregnancy. The serum and salivary IgA showed lowering in their values which may be due to an immune defect and/or the increased level of hydrocortisone or may be attributed to the depressed T-cell response associated with pregnancy