Patent GB-887872-A (GB)
Title: Improvements in or relating to pharmaceutical preparations
Filed: 1959-05-07
Abstract: A pharmaceutical base suitable for shaping by extrusion comprises a solid polyethylene glycol of molecular weight from about 4,000 to about 6,000; a liquid polyethylene glycol soluble in the solid polyethylene glycol; a non-toxic, non-ionic solid oil-soluble surface-active agent; spermaceti; a non-toxic, non-ionic solid water-soluble surface-active agent; and a non-toxic, solid carrier mixture of which between about 80% and 90% by weight is water-soluble.  Preferred oil-soluble surface-active agents are polyoxyethylene sorbitan mono- and tri-stearates.  Water-soluble surface-active agents preferred have the formula HO(C2H4O) (C3H6O) (C2H4O)H with a polypropyleneoxy base molecular weight of about 1,750 and a total molecular weight of about 8,750.  Also suitable are polyoxyethylene stearate and palmitate.  In the carrier beta lactose, sucrose, dextrose, sodium chloride or sodium sulphate may form the water-soluble part and the balance may be starch with which methylcellulose, guar gum or purified wood cellulose may be mixed.  A number of medicinal ingredients for mixing with the base are listed (see Group VI).ALSO:A pharmaceutical preparation contains a medicament and a base suitable for shaping by extrusion-moulding comprising a polyethylene glycol having a molecular weight between about 4000 and about 6000; a liquid polyethylene glycol soluble in the solid polyethylene glycol; a non-toxic non-ionic solid oil-soluble surface-active agent; spermaceti; a non-toxic non-ionic solid water-soluble surface-active agent; and a non-toxic solid carrier mixture of which between about 80% and about 90% is water-soluble. Preferred oil-soluble surface-active agents are polyoxyethylene mono- and di-stearates.  Water-soluble surface-active agents preferred have the formula HO(C2H4O)(C3H6O)(C2H4O)H with a polypropylene oxy base molecular weight of about 1750 and a total molecular weight of about 8750.  Also suitable are polyoxyethylene stearate and palmitate.  In the carrier beta lactose, sucrose, dextrose, sodium chloride, or sodium sulphate may form the water-soluble part and the balance may be starch with which methylcellulose, guar gum or purified wood cellulose may be mixed. Shaped preparations for nasal, urethral, vaginal and rectal application are prepared.  As medicinal ingredients there can be incorporated: steroids, for example, estrone, testosterone, progesterone, hydrocortisone, prednisolone, 6-methyl prednisolone, and their therapeutically active derivatives; hypnotics and sedatives, for example phenobarbital, pentobarbital and amobarbital; antibiotics, for example, neomycin, bacitrocin, polymyxin, erythromycin, tyrothricin, gramicidin; diuretics, for example, aminophylline and theophylline; trichomonicides, for example, phenylmercuric acetate, sodium lauryl sulphate, oxyquinoline benzoate; antiseptics and bactericidal agents, for example, hexachlorophene, hexylresorcinol, nitrofurazone, myristyl g -picolinium chloride, sulfadiazine, phenol, secondary amyl tricresols; anaesthetics, for example, benzocaine, procaine, tetracaine; vasoconstrictors, for example, epinephrine, phenylephrine; analgesics, for example, caffeine and ergotamine tartrate, acetylsilicylic acid, acetophenetidin, N-acetyl-p-amino-phenol; narcotitizing medicaments, for example, morphine, dihydromorphinone, scopolamine and codeine.