Suppository base macrogol

Pharmaceutical grade poly(ethylene glycols) are poly(ethylene oxides) with terminal hydroxyl groups and have been approved by the E.D.A. and listed in both the United States Pharmacopoeia and Martindale under Macrogols for use as ointment and suppository bases (4J. Poly(ethylene glycol) can be chemically cross-linked retaining the hydrophilic nature of the PEO backbone in an infinite hydrogel network which will imbibe water and swell but not... 

A smdy of the effect of polyoxyethylene glycols on the rectal absorption of unionised sulfafurazole demonstrated the importance of the affinity of the dmg substance for base and for rectal mucosa. As the amount of Macrogol 4000 (polyoxyethylene glycol 4000) was increased, the partition coefficient (lipid/ vehicle) fell and absorption decreased correspondingly, because the affinity of the dmg for the suppository base increased and its tendency to partition to the rectal lipids decreased. In a similar way, incorporation of... 

Figure 5 shows the release profiles of FP and its complexes from Witepsol H-15 suppositories. It is evident that the release rate of FP was significantly improved by the inclusion complexations with g-and DM-3-CyDs, while that from TM 3 CyD complex was almost the same as FP alone. The different release behavior between the three complexes may be attributed to the difference in dissolution rate and binding affinity of the complexes to the hydrophobic suppository base. In fact, the release rate of FP from hydrophilic bases such as macrogol suppositories containing the DM-3-CyD and TM-3-CyD complexes, was greater than that from hydrophobic bases such as Witepsol H-15 (11). 

For the preparation of a solution suppository the macrogol base is melted, the active substance is dissolved in the melt and the mass is poured, without any additional step. Melting the base in a closed vessel on the water bath (see Sect. 11.7.1) fits better because the dispersion step is lacking. The closed vessel may be a medicine bottle or a squeeze bottle. The medicine bottle is to be preferred because no transfer of molten base is necessary (no loss), it is transparent for controlling the dissolution process and it is suitable for pouring as there is no suspension to be kept homogeneous. The squeeze bottle is less preferred because it is not transparent. 

The insolubility of acetylsalicylic acid is a contributing factor to its irritant action on the gastric mucosa it is hydrolysed in aqueous solution. It has, however, been incorporated in a suppository base with macrogols 1540 and 6000 which increase its solubility and appear to improve the absorption of the drug [198]. 

In the formulations presented here, mixtures of the polyethylene glycols, Lutrol E 400, Macrogol 1500, Macro-gol 4000, and Macrogol 6000, are intended as water-soluble base for suppositories and ovula. 

Chemical and physical processes may limit the stability of active substance, base and excipients in suppositories. Also the packaging and the conditions and times of storage need attention. Suppositories with a fatty or a macrogol base do not contain water. Therefore bacterial growth is unlikely and preservation is not needed. 

Indometacin is often formulated in a macrogol base to get a good biological availability [33]. In that base discoloration and esterification may easily occur. Furthermore, the indometacin slowly crystallises giving the suppository a spotted appearance. The antioxidants butyl hydroxytoluene (BHT), butyl hydroxyanisole (BHA) and disodium edetate are added to improve the stability as well as glycerol to limit crystallisation, for instance in Indocid suppositories (Aspen, UK) [34]. Nevertheless, a fatty base must be preferred. Indometacin is released almost equally from a fatty base as from a macrogol base [8a, 35, 36] and the... 

For the packaging of suppositories the chemical and physical properties of the active substance and the base have to be considered. This should be done with respect to sensitivity to oxygen and light, compatibility with the (plastic) package, material evaporation (chloral hydrate) and hygroscopicity (macrogol and different active substances). 

For the preparation of suspension suppositories with a macrogol base the preparation process steps are compared with Sect. 11.5 as follows ... 

Dispersing the active substance. It is performed similarly to fat-based suspension-suppositories, but when triturating the active substance with a little melted base it should be noted that the macrogol base solidifies sooner than a fatty base and thus it might be helpful to warm up the mortar a little. 

For an even better bioavailability and easier administration, a chloral hydrate suppository is often preferred. Chloral hydrate suppositories with a macrogol base (see Table 11.1) are chemically stable, this unlike the enema with macrogol... 

Uses Reagent in crystallization of proteins, peptides, and nucleic acids used in beeswax, carnauba wax and stearic acid based suppositories used in the mfg. of soap, detergents, in pharmacology, medicine, and cosmetics, in textiles, rubber Regulatory FDA approved for dentals, orals, topicals Manuf/Distrib. Mosselman NV Parchem Trading Trade Names Adeka PEG-1500 Ercawax C 60 Macrogol 1500... 

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