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    Compounding Suppositories - Part 2

    Copyright:

    © All Rights Reserved
    Download as PDF or read online from Scribd
    Flag for inappropriate content
    Download as pdf
    96 views6 pages

    Compounding Suppositories - Part 2

    Uploaded by

    patchris36
    Compounding Suppositories - Part 2

    Copyright:

    © All Rights Reserved
    Download as PDF or read online from Scribd
    Flag for inappropriate content
    Download as pdf
    of 6
    Secundum Artem Compounding Suppositories, Loyd V. Alen, I, PhD, RPh, This is the second in a two-part series on the cextemporaneous compounding of suppositories. Part Prclod pepaston sae ond house The part indudes physicochemical considerations, stability and calculations discussions. Supposilores have the potential for erhanced uilzation as a dasage form in today’s pharmaceutical armamertarium. For example, exterporaneously ‘compounded suppositories containing metodopre- ‘mide, haloperidol, dexamethasone, diphenhyeramine and bencropine can be administered prophylactically to flecively control severe nausea and vomiting salbuiamol can be administered recy for long term prophylactic treatment of ashma and a prolonged telease morphine allalod suppostory for chronic pain has ben introduced, These, ad other aspects of suppositories will be discussed here. PHYSICOCHEMICAL CONSIDERATIONS In general, when formulating suppositories, the pharmacist should consider the following questions: 1, Isthe desired efecto result rom systemic orlocal use! 2s the route of administration rectal, vaginal or urethral? 3. Isa rapid or a slow and prclonged release of the medication desired? Drugs for loca effect may include the treatment of By Loyd V. Alles, Jc, PuD. Universty of Oklahoma HSC (Colege of Parracy Oklahoma City. OK 73190. Part II hemorthoids, local anesthetics, anisepics,anibiotics and antifungals Orugs for systemic effec include analgesics aniasthmalcs,antinauseans and others. ‘A drug tha! doesnot release its medication within six hours may not be completely uized and may be expelled bythe patient. The cection ofa suppostory base's dependent upon a number of physicochemical variables including he solubility charactrstcs ofthe drug To obiain naximum release ofthe drugfrom the base, a princple of opposite characteris can be employed, For example, water soluble drugs can be placed in fat-soluble bases, ft soluble drugs can be placed in water-soluble bases Fatsoluble bases, eg. cocoa bute, melt quickly in the rectum io release the drug whereas polyethylene slycol bases must dssolvein mucosal fds. process ‘which may take longer. If higher molecular weight polyethylene cols are used. the time for dissolution 'sentended. Moistening wih warm walr immediately por 1o insertion faciales not only nsertion but aso dissolution. Drug release rate requirements are im poriatin the section ofthe suppository base. Factors such as the presence of water. hygrascopi city, viscosity, bitteness density, volume contraction, special problems incompaiiliies ai of drug release paar end bouvake wile dscsed re Presence of Water The presence of water, or using water fo asi in incorporairg an active drug, generally shoulé be avoided in the preparation of suppositories. Water may accelerate the oxidation of fa increase the degiadaion rate of many drugs, enhance reactions between the drug and other components in the Current & Practical Compounding Information for the Pharmacist. ‘suppository. support bacerl/fungal growth and recur the ation ‘ofbacteriosiatc agents Further, the water evaporaes he dissclved subsiances may crysalie roscopicity ‘Clycerin and polyethylene. glycol-contaning. suppositories are hygroscopic The rate of moisure change is dependent on the chain. length ofthe molecule. as wellas on the temperature and humidity of the environment. Poiyethylene gycols wth molecular weighs greater ‘han 4000 have esstendency tobe hygroscopic than the ower weight PFCs Viscosity ‘Viscosity consierations are important inthe preparation of the suppositories and in the release ofthe dug Ii the vscosty of a base i tow. itmay be necessary to adda suspending agentsuch assica get keep the drug uniformly dispersed unt sod fiaion. Dunn prepara tion of the suppository, the melt shoul be handled atthe lowest temperature posible to mainlan high viscosty and shouldbe sired «constant Ith viscosity ofthe base efter administration and when in tne body. is very high the release rte othe drug may be Sowedldueto 4 decrease in the difusion of the drug through the base to reach te mucosal memirane fr absorption. Approaches tha! have been ued to increase viscosty would beto increase the fatty aid chain lengh of compounds in the base. For ‘example, increased (-16 ard C-18 mono- and d-

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