• Archives of Pharmacal Research
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• v.27 no.3
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• pp.351-356
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• 2004

A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol: ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.

• YAKHAK HOEJI
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• v.48 no.2
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• pp.111-116
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• 2004

The ethanol extracts of mixed vegetables (Bioactive Vegetables, BV), mixed fruits (Bioactive Fruits, BF) and their liquid formulation (Chungpae Plus , CP) were evaluated for their antioxidative and antigenotoxic activities. They were shown to possess the significant free radical scavenging effect against 1,1-diphenyl-2-picryl hydrazine (DPPH) radical generation and were revealed to show the inhibitory effect of lipid peroxidation as measured by malondialdehyde (MDA) formation although the potencies were not higher than those of vitamin C. They did not possess any pro-oxidant effect on bleomycin-Fe(III) dependent DNA degradation, whereas vitamin C showed strong pro-oxidant effect. Furthermore, oral administration of BV and BF inhibited micronucleated reticulocyte (MNRET) formation of mouse peripheral blood induced by KBrO3 treatment in vivo. CP also showed significant inhibition under same experimental condition. Therefore, the liquid formulation (CP) containing BV and BF may be a useful natural antioxidative and antigenotoxic agent by scavenging free radicals, inhibition of lipid peroxidation and protecting chromosomal damage.

• Archives of Pharmacal Research
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• v.27 no.1
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• pp.1-12
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• 2004

Initial burst is one of the major challenges in protein-encapsulated microparticle systems. Since protein release during the initial stage depends mostly on the diffusional escape of the protein, major approaches to prevent the initial burst have focused on efficient encapsulation of the protein within the microparticles. For this reason, control of encapsulation efficiency and the extent of initial burst are based on common formulation parameters. The present article provides a literature review of the formulation parameters that are known to influence the two properties in the emulsion-solvent evaporation/extraction method. Physical and chemical properties of encapsulating polymers, solvent systems, polymer-drug interactions, and properties of the continuous phase are some of the influential variables. Most parameters affect encapsulation efficiency and initial burst by modifying solidification rate of the dispersed phase. In order to prevent many unfavorable events such as pore formation, drug loss, and drug migration that occur while the dispersed phase is in the semi-solid state, it is important to understand and optimize these variables.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.413.2-413.2
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• 2002

Paclitaxel is an antitumor agent with poor water solubility and its pharmacokinetics are nonlinear. Cremophor EL. a surfactant used in the formulation of paclitaxel. may cause adverse effects. New solubilizer(Aceporol 460) was developed to reduce side effects of Cremophor EL and to increase the effect of drug as surfactant used in the intravenous micelle formulation of anticancer drug paclitaxel. We studied easy, rapid quantitative determination of Aceporol 460 in mouse plasma samples. which was achieved by complexation of the compound with the Coomassie brilliant blue G-250 dye in protein-free extracts. (omitted)

• CELLMED
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• v.12 no.3
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• pp.12.1-12.6
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• 2022

With a prevalence incidence of 8 % to 37%, unexplained infertility (Uqr) is by definition empiric because it does not address a particular defect or functional deficits. Couples with unexplained infertility have a higher than zero chance of becoming pregnant without treatment, but it is less likely than couples who are fertile. The ingredients in the Unani formulation, are baikh asgand (Withania somnifera Dunal), baikh piyabansa (Barleria prionitis Linn), gule dhawa (Anogeissus latifolia), and gule nilofar (Nymphaea alba Linn), were used to treat unexplained secondary infertility, possess the characteristics of muqawwi bah (Aphrodisiac), muqawwi Rahim (Uterotonic), muwallid-i-mani (ovulation-inducing), and mughalliz-i-mani (an agent which increases the viscosity of semen) beginning from the fifth day of the last menstrual cycle for five days with milk. The first cycle of treatment led to the conception of the women.

• CELLMED
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• v.14 no.2
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• pp.5.1-5.4
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• 2024

PCOS is the most common endocrine pathology in females of reproductive worldwide. The prevalence ranges between 5% and 15% depending on the diagnostic criteria applied.Its etiology involves both genetic and environmental factors. Typically, women with PCOS show clinical and biochemical hyperandrogenism, oligoanovulation, and micropolycystic morphology of the ovaries. Unani formulation containing Nankhwah, Badiyan and Wajturki possessing the properties of Mudirr-i-Bawl-o- Hayd, mujaff -iBalgham, Munaffis-i- balgham, Muhallil, Muqawwi-i-Jigar were used in the form of Joshanda 6gm BD Starting from 5 days prior to expected period date to 5 days during menses for 3 cycles, which led to regain regularity of menses, correcting the amount of flow and reducing the ovarian volume on US. Thus unani medications have the potential to treat ths symtoms of PCOS and improve the quality of life of women.

• Journal of Pharmaceutical Investigation
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• v.38 no.4
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• pp.241-247
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• 2008

Paclitaxel is a taxane diterpene amide, which was first extracted from the stem bark of the western yew, Taxus brevifolia. This natural product has proven to be useful in the treatment of a variety of human neoplastic disorders, including ovarian cancer, breast and lung cancer. Paclitaxel is a highly hydrophobic drug that is poorly soluble in water. It is mainly given by intravenous administration. Therefore, The pharmaceutical formulation of paclitaxel ($Taxol^{(R)}$; Bristol-Myers Squibb) contains 50% $Cremophor^{(R)}$ EL and 50% dehydrated ethanol. However the ethanol/Cremophor EL vehicle required to solubilize paclitaxel in $Taxol^{(R)}$ has a pharmacological and pharmaceutical problems. To overcome these problems, new formulations for paclitaxel that do not require solubilization by $Cremophor^{(R)}$ EL are currently being developed. Therefore this study utilized a supercritical fluid antisolvent (SAS) process for cremophor-free formulation. To select hydrophilic polymers that require solubilization for paclitaxel, we evaluated polymers and the ratio of paclitaxel/polymers. HP-${\beta}$-CD was used as a hydrophilic polymer in the preparation of the paclitaxel solid dispersion. Although solubility of paclitaxel by polymers was increased, physical stability of solution after paclitaxel/polymer powder soluble in saline was unstable. To overcome this problem, we investigated the use of surfactants. At 1/20/40 of paclitaxel/hydrophilic polymer/ surfactant weight ratio, about 10 mg/mL of paclitaxel can be solubilized in this system. Compared with the solubility of paclitaxel in water ($1\;{\mu}g/mL$), the paclitaxel solid dispersion prepared by SAS process increased the solubility of paclitaxel by near 10,000 folds. The physicochemical properties was also evaluated. The particle size distribution, melting point and amophorization and shape of the powder particles were fully characterized by particle size distribution analyzer, DSC, SEM and XRD. In summary, through the SAS process, uniform nano-scale paclitaxel solid dispersion powders were obtained with excellent results compared with $Taxol^{(R)}$ for the physicochemical properties, solubility and pharmacokinetic behavior.

• Journal of Pharmaceutical Investigation
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• v.32 no.3
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• pp.161-164
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• 2002

Gentisic acid is a skin-whitening agent which inhibits the tyrosinase activity, an essential enzyme in the process of biological synthesis of melanin. Since melanin is synthesized in melanocytes located between the viable epidermis and dermis layer, drug amount delivered into the epidermis/dermis layer can provide valuable information for the biological effect of skin-whitening agents. The purpose of this study was to prepare the gentisic acid patches with 2% dodecylamine as enhancer, and to observe the in vitro skin permeation and in vivo skin deposition of gentisic acid. Gentisic acid in DuroTak 87-2510 patch formulation permeated across hairless mouse skin at the rate of $40.79\;{\mu}g/cm^2/hr$. In vivo study showed that the gentisic acid amount in both the stratum corneum and the viable epidermis/dermis increased with the increase of application time. The amount of gentisic acid in the stratum corneum was higher than that in the epidermis/dermis layer, and was expected to provide a reservoir effect even after removing the patches. Thus, the patch formulation seems to be useful for the topical delivery of skin-whitening agent into the epidermis/dermis layer, the target site.

• YAKHAK HOEJI
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• v.42 no.2
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• pp.187-195
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• 1998

In order to ameliorate disadvantages of buccal ointments and mucoadhesive tablets used for the treatment of aphthosis, a thin mucoadhesive patch containing triamcinolone acetoni de was designed and evaluated for the pharmaceutical properties. The adhesive gel layer consisting of Noveon AA-1, hydroxypropylcellulose-M and ethylcellulose N 100, and the protective gel layer of ethylcellulose N 100, Eudragit RSPO and castor oil have been formulated and various properties such as viscosity of drug gel layer, thickness, in vitro adhesion time, adhesive strength, surface pH, content uniformity and drug release are tested. The mean viscosity of drug-containing gel layer was found to increase with increasing amount of Noveon OAA-1 or hydroxypropylcellulose-M. The optimum formulation showed the thickness of 171 ${\mu}$m, surface pH of 4.6, in vitro adhesion time of 8 hours and adhesive strength of 272.7g/sheet. The drug content of each patch was relatively homogeneous with the value of 273${\pm}$6.77g. Drug release study showed that compared to mucoadhesive tablet, the patch showed a faster drug release. Drug release was delayed by hydroxypropylcellulose-M, but not by ethylcellulose N 100. The patches prepared were nonirritant and the muco adhesion was better than the commercial product (AftachR) on the market. Based on these results, this mucoadhesive patch is expected to be an effective dosage form for the treatment of aphthosis.

• Proceedings of the PSK Conference
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• 2002.04a
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• pp.211.2-212
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• 2002