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Clinical Use of Eicosanoids for Cervical Ripening before Induction of Labor
Published in Murray D. Mitchell, Eicosanoids in Reproduction, 2020
Most of the investigations have been conducted with 0.5 mg PGE2 (Table 1), a dose that is much smaller than that used with either the oral or vaginal routes of administration. Most of the data relate to an Upjohn preparation of 0.5 mg PGE2 in a 2.5 ml triacetin gel; and these data include results from three multicenter studies conducted in Europe19,45 and Canada,33 which all used the same dose regimen and, together, involved more than 1400 women. Not surprisingly, therefore, the results of the endocervical trials closely resemble those presented in the section on controlled evaluations of any prostaglandin administered by any route. Moreover, the multicenter trials of endocervical prostaglandin administration have clearly demonstrated that such trials, provided they are adequately reported, have far more potential to answer questions that really matter to pregnant women and the clinicians who care for them than the many small single-center trials that have thus far constituted the large majority of the controlled clinical research effort to evaluate prostaglandin-induced cervical ripening.
Nanocarrier Technologies for Enhancing the Solubility and Dissolution Rate of Api
Published in Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Medicinal Chemistry with Pharmaceutical Product Development, 2019
Ashwini Deshpande, Tulshidas S. Patil
With the objective of enhanced dissolution rate and oral bioavailability SNEDDS of grapefruit flavonoid naringenin (NRG) SNEDDS were developed NRG is an aglycone flavonoid from grapefruits, possesses antiinflammatory, anti-carcinogenic, anti-lipid peroxidation and hepatoprotective activities. Its poor water solubility and the slow dissolution upon oral administration, restricts its use as therapeutic agent. The formulation was optimized based on the enhanced dissolution rate, optimal globule size and Polydispersity index (PDI). Improved solubility and bioavailability was noted when triacetin was used as oily phase, tween 80 as surfactant and transcutaol HP as co-surfactant [132].
Chemical Reactions of Glycerine
Published in Eric Jungermann, Norman O.V. Sonntag, Glycerine, 2018
Acetins are the mono-, di-, and triacetates of glycerine formed by the reaction of glycerine with acetic acid, acetic anhyride, or ketene [10]. The choice of catalyst plays a role in directing the reaction to form one isomer predominantly. Monoacetin is a thick hygroscopic liquid used in tanning and in the manufacture of explosives. Diacetin is a hygroscopic liquid and is used as a plasticizer and softening agent. The triacetin is a cellulose plasticizer used in cigarette filters and as a binder in solid rocket fuels. In the cosmetic area, it has found use as a fixative in perfumes.
Effect of vaginal pH on efficacy of dinoprostone gel for labour induction: a cross-sectional study
Published in Journal of Obstetrics and Gynaecology, 2022
G. K. Poomalar, N. Fathima Shantini, Rini Ezhil
Few in vivo and in vitro studies were done in the past to assess the release rate and absorption of prostaglandins. In vitro study done by Johnson et al. (1992), to assess the release of PGE2 from different commercial preparations (triacetin and starch-based gel, lactose-based tablets and hydrogel-based pessary) at different pH conditions. Triacetin based preparations are released at a very low rate at pH 3.4. Whereas at higher pH 5.4 and 7.4, they are released at a higher rate and found to be effective. Hydrogel based inserts also found to be released better at higher pH 7.4. Starch based preparations released better at pH 5.4. Lactose-based preparations work better at low pH 3.4. At higher pH 7.4, prostaglandins are released at a very low rate from lactose-based preparations (Johnson et al. 1992).
Experimental measurement – correlation of solubility and dissolution thermodynamics study of itraconazole in pure monosolvents at various temperatures
Published in Drug Development and Industrial Pharmacy, 2021
Sachin K. Jagdale, Rajesh B. Nawale
Glycerin, propylene glycol, polyethylene glycol-200, polyethylene glycol-400, and polyethylene glycol-600 are the polymerized derivatives of ethylene glycols and are physiologically acceptable. They have the adequate pharmaceutical properties like lower toxicity, low volatility, high stability, and complete miscibility with water almost at all the proportions. They are also preferred in the design and development of various pharmaceutical oral and parenteral formulations as well as used for the preclinical and clinical studies [21,22]. 1-Methyl-2-pyrrolidone (NMP) is biodegradable solvent with high solubilizing power and used in different fields of industrial applications including pharmaceutical, synthetic, and analytical industries [23]. N, N-dimethylacetamide (DMA) is an FDA approved solvent widely used in pharmaceutical industry to improve the solubility of lipophilic, high molecular weight drugs with poor water solubility [24]. Dimethyl formamide (DMF) is an extraordinary organic compound favored as solvent in pharmaceutical industry due to its favored dissolution provided by interactions with a substrate [25]. Triacetin is reported to be used as solvent in topical and cosmetic formulations and as a carrier for fragrances and flavors [26]. Diethylene glycol is used as strong solubilizer in many products including pharmaceutical, topical, transdermal, cosmetics, nutraceuticals, and is employed for various routes of administration [27]. Carbon tetrachloride, cyclohexane, and n-hexane are used in pharmaceutical industry as reaction media, in separation and purification of synthesis products [28].
Improvement of dissolution profile of eplerenone with solidified self-emulsifying drug delivery systems (S-SEDDS)
Published in Drug Development and Industrial Pharmacy, 2023
Rawan Ranna, Burcu Uner, Neslihan Ustundag Okur, Cetin Tas
The ingredients of lipid-based formulas can operate as permeability enhancers, increasing active pharmaceutical ingredient uptake in GIT [28]. Furthermore, following ingestion, chosen oil, surfactant, and co-solvent may simply generate an emulsion [11]. In general, the oil phase is normally selected upon the solubility of the active pharmaceutical ingredient [29]. Triacetin was selected as the oil phase. The choice of a surfactant in SEDDS formulation is primarily determined by its compatibility, safety, and capacity to reduce the surface free energy within the w/o interface, resulting in stable systems physically [30]. Nonionic surfactant has a lower physiological toxic effect than the ionic equivalent. Additionally, nonionic surfactants show emulsification features at lower doses, as shown by a reduced critical micelle concentration, which is ideal for oral delivery. Surfactants at elevated doses cause GIT irritation. Additionally, in o/w SEDDS, a water-sustainable nonionic surfactant (HLB value more than 10) exhibits an increased positive surface excess, leading to an accretion across the o/w interface efficient surface tension reduction and a better stable system [31]. The reduction in the free energy needed to produce the emulsion increases the formulation’s thermodynamic stability [13,14]. Pseudo-ternary phase diagram was developed to detect the self-emulsifying zones and calculate the optimal surfactant, oil, and co-surfactant quantities of three distinct SEDDS formulations. Any increases within the co-surfactant quantity resulted in an increase as well in the self-emulsifying zone as shown in the diagram of F3 (Figure 2) [32].