Pharmaceutical Technology II Supposetories PDF

‫لجنة عمداء كليات الصيدلة‬ ‫لجنة توحيد منهاج مادة )‪(Pharmaceutical Technology II‬‬ ‫‪Pharmaceutical Technology II‬‬ ‫المرحلة الثالثة‬ ‫‪2024‬‬ ‫‪1‬‬ ‫التقويم لكليات الصيدلة‬ ‫ي‬ ‫تم اعداد ومراجعة هذا المنهج الموحد لالمتحان‬ ‫كبب...

‫لجنة عمداء كليات الصيدلة‬ ‫لجنة توحيد منهاج مادة )‪(Pharmaceutical Technology II‬‬ ‫‪Pharmaceutical Technology II‬‬ ‫المرحلة الثالثة‬ ‫‪2024‬‬ ‫‪1‬‬ ‫التقويم لكليات الصيدلة‬ ‫ي‬ ‫تم اعداد ومراجعة هذا المنهج الموحد لالمتحان‬ ‫كببة‬ ‫خبة ر‬ ‫رن‬ ‫متخصصي لديهم ر‬ ‫اس ‪ 2024-2023‬من قبل اساتذة‬ ‫للعام الدر ي‬ ‫ن‬ ‫ن‬ ‫االكاديم ‪.‬لقد بذل االساتذة قصارى جهودهم يف جمع‬ ‫ي‬ ‫والعمل‬ ‫التدريس‬ ‫ف‬‫ي‬ ‫يسبة عىل‬‫المعلومات وحرصوا عىل ترتيبها وتنظيمها لتكون واضحة و ر‬ ‫الطلبة‪.‬نأمل من طلبتنا االعزاء االستفادة من هذا المنهج ن يف طريقهم اىل‬ ‫النجاح والتفوق ‪ ،‬وهللا الموفق‪.‬‬ ‫‪2‬‬ Suppositories and Inserts Chapter 12 Ansel's Pharmaceutical Dosage Forms and Drug Delivery Systems, Eleventh Edition Objectives After reading this topic, the student will be able to : Compare and contrast various suppository and insert, in terms of physical appearance, size and shape Describe the advantages of suppositories and inserts. Identify and explain physiologic factors that influence the drug absorption from rectal suppository administration Identify and explain the physicochemical factors of the drug and suppository/insert base as these influence absorption Compare and contrast the various classes of suppository bases Describe the three methods of suppository preparation 23  ‫ﻓﺘﺤﺎت اﻟﺠﺴﻢ ﺣﻴﺚ ﺗﺬوب أو ﺗﻠﻴﻦ‬ ‫اﻟﺘﺤﺎﻣﻴﻞ ﻫﻲ أﺷﻜﺎل ﺟﺮﻋﺎت ﺻﻠﺒﺔ ﻣﺨﺼﺼﺔ ﻟﻺدﺧﺎل‬ ‫اﻟﻤﺴﺘﻘﻴﻢ‬ ‫ ُﺗﺴﺘﺨﺪم اﻟﺘﺤﺎﻣﻴﻞ ﺑﺸﻜﻞ ﺷﺎﺋﻊ‬.‫أو ﺗﺬوب وﺗﻤﺎرس ﺗﺄﺛﻴﺮات ﻣﻮﺿﻌﻴﺔ أو ﺟﻬﺎ ﻳﺔ‬ ‫ﻣﺠﺮى اﻟﺒﻮل ُﺗﺴﺘﺨﺪم ﻟﺘﻮﺻﻴﻞ اﻷدوﻳﺔ ذات اﻟﻤﻔﻌﻮل اﻟﺠﻬﺎزي واﻟﻤﺤ‬ ‫واﻟﻤﻬﺒﻞ وأﺣﻴﺎﻧًﺎ‬ Suppositories Suppositories are solid dosage forms intended for insertion into body orifices where they melt, soften, or dissolve and exert local or systemic effects. Suppositories are commonly used rectally, vaginally, and occasionally urethrally They are used to deliver both systemically and locally acting medications 24  ‫أﺷﻜﺎل اﻟﺘﺤﺎﻣﻴﻞ‬ ‫اﻟﺘﺤﺎﻣﻴﻞ ﻟﻬﺎ أﺷﻜﺎل وأوزان ﻣﺨﺘﻠﻔﺔ‬. ‫اﻟﻔﺘﺤﺔ‬ ‫ﻳﺠﺐ أن ﻳﻜﻮن ﺷﻜﻞ وﺣﺠﻢ اﻟﺘﺤﻤﻴﻠﺔ ﺑﺤﻴﺚ ﻳﻤﻜﻦ إدﺧﺎﻟﻬﺎ ﺑﺴﻬﻮﻟﺔ‬ ‫ ﻳﺠﺐ اﻻﺣﺘﻔﺎظ ﺑﻬﺎ‬،‫ وﺑﻤﺠﺮد إدﺧﺎﻟﻬﺎ‬،‫اﻧﺘﻔﺎخ ﻻ ﻣﺒﺮر ﻟﻪ‬ ‫اﻟﻤﻘﺼﻮدة دون اﻟﺘﺴﺒﺐ‬ ‫ﻟﻔﺘﺮة ﻣﻨﺎﺳﺒﺔ‬. ‫ وﻟﻜﻦ ﻗﺪ ﻳﺘﻢ إدﺧﺎل ﺑﻌﺾ اﻟﺘﺤﺎﻣﻴﻞ‬،‫ﻳﺘﻢ إدﺧﺎل اﻟﺘﺤﺎﻣﻴﻞ اﻟﺸﺮﺟﻴﺔ ﺑﺎﻷﺻﺎﺑﻊ‬ Suppositories Shapes ‫ أﻋ اﻟﻘﻨﺎة‬،‫ أو اﻷﻗﺮاص اﻟﻤﺤﻀﺮة ﺑﺎﻟﻀﻐﻂ‬،‫ وﺧﺎﺻﺔ اﻟﺘﺤﺎﻣﻴﻞ‬،‫اﻟﻤﻬﺒﻠﻴﺔ‬ ‫ﺑﻤﺴﺎﻋﺪة أﺣﺪ اﻷﺟﻬﺰة‬. Suppositories have various shapes and weights. The shape and size of a suppository must be such that it can be easily inserted into the intended orifice without causing undue distension, and once inserted, it must be retained for the appropriate period. Rectal suppositories are inserted with the fingers, but certain vaginal suppositories, particularly the inserts, or tablets prepared by compression, may be inserted high in the tract with the aid of an appliance. ‫ ﻋﺎدة ﻣﺎ‬- ‫اﻟﺘﺤﺎﻣﻴﻞ اﻟﺸﺮﺟﻴﺔ‬ ‫ﻳﺒﻠﻎ ﻃﻮل اﻟﺘﺤﺎﻣﻴﻞ اﻟﺸﺮﺟﻴﺔ‬ Rectal suppositories (‫ ﺑﻮﺻﺔ‬1.5) ‫ ﻣﻠﻢ‬32 ‫ﺣﻮا‬، Rectal suppositories are usually about 32 mm (1.5 in.) long, are ‫ وﻟﻬﺎ ﻃﺮف‬،‫وﻫﻲ أﺳﻄﻮاﻧﻴﺔ‬ ‫ﻣﺴﺘﺪق واﺣﺪ أو ﻛﻼ اﻟﻄﺮﻓﻴﻦ‬. cylindrical, and have one or both ends tapered. Some rectal suppositories ‫ﺑﻌﺾ اﻟﺘﺤﺎﻣﻴﻞ اﻟﺸﺮﺟﻴﺔ‬ ‫ﺷﻜﻞ رﺻﺎﺻﺔ أو‬ ‫ﺗﻜﻮن ﻋ‬ are shaped like a bullet, a torpedo, or the little finger. ‫ﻃﻮ ﺑﻴﺪ أو اﻷﺻﺒﻊ اﻟﺼﻐﻴﺮ‬. ‫ﻛﺜﺎﻓﺔ اﻟﻘﺎﻋﺪة‬ ‫اﻋﺘﻤﺎدا ﻋ‬ Depending on the density of the base and the medicaments in the ‫واﻷدوﻳﺔ اﻟﻤﻮﺟﻮدة‬ suppository, the weight may vary. ‫ ﻗﺪ ﻳﺨﺘﻠﻒ اﻟﻮزن‬،‫اﻟﺘﺤﻤﻴﻠﺔ‬. ‫ﺗﺰن اﻟﺘﺤﺎﻣﻲل اﻟﺸﺮﺟﻴﺔ‬ Adult rectal suppositories weigh about 2 g when cocoa butter (theobroma ‫ ﺟﺮام ﻋﻨﺪ‬2 ‫ﻟﻠﺒﺎﻟﻐﻴﻦ ﺣﻮا‬ ‫اﺳﺘﺨﺪام ﺑﺪة اﻟﻜﺎﻛﺎو ) ﻳﺖ‬ oil) is employed as the base. ‫اﻟﺜﻴﻮﺑﺮوﻣﺎ( ﻛﻘﺎﻋﺪة‬. Rectal suppositories for use by infants and children are about half the ‫اﻟﺘﺤﺎﻣﻴﻞ اﻟﺸﺮﺟﻴﺔ‬ ‫اﻟﻤﺴﺘﺨﺪﻣﺔ ﻣﻦ ﻗﺒﻞ اﻟﺮﺿﻊ‬ weight and size of the adult suppositories and assume a more pencil-like ‫ﻧﺼﻒ‬ ‫واﻷﻃﻔﺎل ﻫﻲ ﺣﻮا‬ ‫وزن وﺣﺠﻢ اﻟﺘﺤﺎﻣﻴﻞ‬ ‫اﻟﺘﺤﺎﻣﻴﻞ اﻟﻤﻬﺒﻠﻴﺔ اﻟﺘﺤﺎﻣﻴﻞ‬ shape. ‫ﻟﻠﺒﺎﻟﻐﻴﻦ وﺗﺘﺨﺬ ﺷﻜﻼ ً ﻳﺸﺒﻪ‬ ً ‫ واﻟﺘﻲ ﺗﺴﻤﻰ‬،‫اﻟﻤﻬﺒﻠﻴﺔ‬ ‫أﻳﻀﺎ‬ ‫اﻟﻘﻠﻢ‬ (‫اﻟﻤﺎﺿﻲ‬ ) ‫ ﻋﺎدة ﻣﺎ‬،‫اﻟﺘﺤﺎﻣﻴﻞ‬ ‫ﺗﻜﻮن ﻛﺮوﻳﺔ أو ﺑﻴﻀﺎوﻳﺔ اﻟﺸﻜﻞ‬ ‫أو ﻣﺨﺮوﻃﻴﺔ اﻟﺸﻜﻞ وﺗﺰن ﺣﻮا‬ Vaginal suppositories 5 ‫ﺟﺮام ﻋﻨﺪﻣﺎ ﺗﻜﻮن ﺑﺪة اﻟﻜﺎﻛﺎو‬ Vaginal suppositories, also called (in past) pessaries, are usually globular, ‫ﻫﻲ اﻟﻘﺎﻋﺪة‬. ‫اﻟﻘﺎﻋﺪة‬ ‫ اﻋﺘﻤﺎدًا ﻋ‬،‫وﻣﻊ ذﻟﻚ‬ oviform, or cone- shaped and weigh about 5 g when cocoa butter is the ‫واﻟﻤﻨﺘﺞ اﻟﺨﺎص ﺑﺎﻟﺸﺮﻛﺔ‬ ‫ ﻗﺪ ﺗﺨﺘﻠﻒ أوزان‬،‫اﻟﻤﺼﻨﻌﺔ‬ base. ‫اﻟﺘﺤﺎﻣﻴﻞ اﻟﻤﻬﺒﻠﻴﺔ ﺑﺸﻜﻞ ﻛﺒﻴﺮ‬. However, depending on the base and the manufacturer's product, the weights of vaginal suppositories may vary widely. Urethral suppositories Urethral suppositories, also called bougies, are slender, pencil-shaped suppositories intended for insertion into the male or female urethra. Male urethral suppositories may be 3 to 6 mm in diameter and approximately 140 mm long. Female urethral suppositories are about half the length and weight of the male urethral suppository, being about 70 mm long and weighing about 2 g when made of cocoa butter. Urethral suppositories may be: antibacterial or a local anesthetic preparative for a urethral examination. ‫اﻟﺘﺤﺎﻣﻴﻞ اﻹﺣﻠﻴﻠﻴﺔ‬ ‫ﺷﻜﻞ ﻗﻠﻢ ﻣﺼﻤﻤﺔ ﻹدﺧﺎﻟﻬﺎ‬ ‫ ﻫﻲ ﺗﺤﺎﻣﻴﻞ رﻓﻴﻌﺔ ﻋ‬،‫ واﻟﺘﻲ ﺗﺴﻤﻰ أﻳﻀﺎ ً اﻟﺒﻮﺟﻴﺎت‬،‫اﻟﺘﺤﺎﻣﻴﻞ اﻹﺣﻠﻴﻠﻴﺔ‬ ‫ﻣﺠﺮى اﻟﺒﻮل ﻟﺪى اﻟﺬﻛﺮ أو اﻷﻧﺜﻰ‬. ‫ ﻣﻠﻢ‬140 ‫ ﻣﻠﻢ وﻃﻮﻟﻬﺎ ﺣﻮا‬6 ‫ إ‬3 ‫ﻳﻤﻜﻦ أن ﻳﺘﺮاوح ﻗﻄﺮ اﻟﺘﺤﺎﻣﻴﻞ اﻹﺣﻠﻴﻠﻴﺔ ﻋﻨﺪ اﻟﺬﻛﻮر ﻣﻦ‬. ‫ ﺣﻴﺚ ﻳﺒﻠﻎ ﻃﻮﻟﻬﺎ‬،‫ﻧﺼﻒ ﻃﻮل ووزن ﺗﺤﻤﻴﻠﺔ اﻹﺣﻠﻴﻞ اﻟﺬﻛ ﻳﺔ‬ ‫ﻳﺒﻠﻎ ﻃﻮل ﺗﺤﻤﻴﻠﺔ اﻹﺣﻠﻴﻞ اﻷﻧﺜﻮﻳﺔ ﺣﻮا‬ ‫ ﺟﺮام ﻋﻨﺪﻣﺎ ﺗﻜﻮن ﻣﺼﻨﻮﻋﺔ ﻣﻦ ﺑﺪة اﻟﻜﺎﻛﺎو‬2 ‫ ﻣﻠﻢ ووزﻧﻬﺎ ﺣﻮا‬70 ‫ﺣﻮا‬. 25 ‫ ﻣﻀﺎدة ﻟﻠﺠﺮاﺛﻴﻢ أو ﻣﺨﺪر ﻣﻮﺿﻌﻲ ﻣﺤﻀﺮ ﻟﻔﺤﺺ اﻹﺣﻠﻴﻞ‬:‫اﻟﺘﺤﺎﻣﻴﻞ اﻹﺣﻠﻴﻠﻴﺔ ﻳﻤﻜﻦ أن ﺗﻜﻮن‬.  ‫ﻣﺼﻴﺮ اﻟﺘﺤﻤﻴﻠﺔ‬ ‫ ﺗﺬوب ﻗﺎﻋﺪة‬،‫ﺑﻤﺠﺮد إدﺧﺎﻟﻬﺎ‬ ‫اﻟﺘﺤﻤﻴﻠﺔ أو ﺗﻠﻴﻴﻨﻬﺎ أو ﺗﺬوب‬، ‫أﻧﺴﺠﺔ‬ ‫وﺗﻮ ﻳﻊ أدوﻳﺘﻬﺎ ﻋ‬ ‫ اﻟﻤﻨﻄﻘﺔ‬. ‫ﻗﺪ ﺗﻜﻮن ﻫﺬه اﻷدوﻳﺔ‬ Fate of the suppository ‫ﻣﺨﺼﺼﺔ ﻟﻼﺣﺘﻔﺎظ ﺑﻬﺎ داﺧﻞ‬ ‫اﻟﺘﺠﻮﻳﻒ ﻣﻦ أﺟﻞ ﺗﺄﺛﻴﺮات‬ Once inserted, the suppository base melts, softens, or dissolves, ‫ أو ﻗﺪ ﺗﻜﻮن‬،‫ﻣﻮﺿﻌﻴﺔ‬ ‫ﻣﺨﺼﺼﺔ ﻟﻼﻣﺘﺼﺎص ﻣﻦ‬ distributing its medicaments to the tissues of the region. ‫أﺟﻞ ﺗﺄﺛﻴﺮات ﺟﻬﺎ ﻳﺔ‬. These medicaments may be intended for retention within the cavity for ‫ﻗﺪ ﻳﻈﻬﺮون اﻟﺘﺄﺛﻴﺮ ﻓﻮ ًرا أو‬ ‫إﻃﻼق اﻟﺪواء‬ ‫ﻳﺤﺎﻓﻈﻮن ﻋ‬ local effects, or they may be intended to be absorbed for systemic effects. ‫ﻣﺜﻞ اﻟﺘﺤﺎﻣﻴﻞ ﻃﻮﻳﻠﺔ‬ ‫اﻟﻤﻔﻌﻮل أو ﺑﻄﻴﺌﺔ اﻹﻃﻼق‬. They may exhibit the effect immediately or sustain the release of the drug ‫ﻳﺘﻢ ﺗﺤﻀﻴﺮ ﻛﺒ ﻳﺘﺎت‬ ‫اﻟﻤﻮرﻓﻴﻦ اﻟﻤﻮﺟﻮدة‬ such as Long-acting or slow-release suppositories are also prepared. ‫اﻟﺘﺤﺎﻣﻴﻞ ﺑﻄﻴﺌﺔ اﻟﺘﺤﺮر‬ Morphine sulfate in slow-release suppositories is prepared by ‫ﺑﻮاﺳﻄﺔ اﻟﺼﻴﺎدﻟﺔ اﻟﻤﺮﻛﺒﻴﻦ‬. ‫ﻣﺎدة‬ ‫ﺗﺸﺘﻤﻞ اﻟﻘﺎﻋﺪة ﻋ‬ compounding pharmacists. The base includes a material such as alginic ‫ واﻟﺘﻲ‬،‫ﻣﺜﻞ ﺣﻤﺾ اﻷﻟﺠﻨﻴﻚ‬ ‫إﻃﺎﻟﺔ ﻓﺘﺮة ﺗﺤﺮر‬ ‫ﺗﻌﻤﻞ ﻋ‬ acid, which will prolong the release of the drug over several hours. ‫اﻟﺪواء ﻟﻌﺪة ﺳﺎﻋﺎت‬. Local rectal suppositories Rectal suppositories intended for local action are most frequently used to relieve 1. Constipation A popular laxative, glycerin suppositories promote laxation by local irritation of the mucous membranes, probably by the dehydrating effect of the glycerin on those membranes. ‫اﻟﺘﺤﺎﻣﻴﻞ اﻟﻤﺴﺘﻘﻴﻤﻴﺔ اﻟﻤﻮﺿﻌﻴﺔ اﻟﺘﺤﺎﻣﻴﻞ اﻟﺸﺮﺟﻴﺔ اﻟﻤﺨﺼﺼﺔ ﻟﻠﻌﻤﻞ اﻟﻤﻮﺿﻌﻲ ﻫﻲ اﻷﻛﺜﺮ‬ ‫اﺳﺘﺨﺪاﻣﺎ ﻟﻠﺘﺨﻔﻴﻒ‬ ً 1. ‫اﻹﻣﺴﺎك‬ ‫ ﺗﻌﺰز ﻋﻤﻠﻴﺔ اﻻرﺗﺨﺎء ﻋﻦ ﻃ ﻳﻖ اﻟﺘﻬﻴﺞ اﻟﻤﻮﺿﻌﻲ ﻟﻸﻏﺸﻴﺔ‬،‫ وﻫﻲ ﻣﻠﻴﻦ ﺷﺎﺋﻊ‬،‫ﺗﺤﺎﻣﻴﻞ اﻟﺠﻠﺴ ﻳﻦ‬ ‫ﺗﻠﻚ اﻷﻏﺸﻴﺔ‬ ‫ ﺑﻤﺎ ﺑﺴﺒﺐ ﺗﺄﺛﻴﺮ اﻟﺠﻠﺴ ﻳﻦ اﻟﻤﺠﻔﻒ ﻋ‬،‫اﻟﻤﺨﺎﻃﻴﺔ‬. 26  2. ‫اﻷﻟﻢ واﻟﺘﻬﻴﺞ واﻟﺤﻜﺔ واﻻﻟﺘﻬﺎب اﻟﻤﺼﺎﺣﺐ ﻟﻠﺒﻮاﺳﻴﺮ أو ﻏﻴﺮﻫﺎ ﻣﻦ اﻟﺤﺎﻻت اﻟﺸﺮﺟﻴﺔ‬. ‫ وﻣﻘﺒﻀﺎت‬،‫ذﻟﻚ أدوﻳﺔ اﻟﺘﺨﺪﻳﺮ اﻟﻤﻮﺿﻌﻲ‬ ‫ ﺑﻤﺎ‬،‫ﻋﺪد ﻣﻦ اﻟﻤﻜﻮﻧﺎت‬ ‫ﻛﺜﻴﺮ ﻣﻦ اﻷﺣﻴﺎن ﻋ‬ ‫ﺗﺤﺘﻮي اﻟﺘﺤﺎﻣﻴﻞ اﻟﻤﻀﺎدة ﻟﻠﺒﻮاﺳﻴﺮ‬ ‫ وﻋﻮاﻣﻞ اﻟﺤﻤﺎﻳﺔ‬،‫ واﻟﻤﻄ ﻳﺎت اﻟﻤﻬﺪﺋﺔ‬،‫ واﻟﻤﺴﻜﻨﺎت‬،‫ واﻷدوﻳﺔ اﻟﻘﺎﺑﻀﺔ‬،‫اﻷوﻋﻴﺔ‬. 2. The pain, irritation, itching, and inflammation associated with hemorrhoids or other anoectal conditions. Anti-hemorrhoidal suppositories frequently contain a number of components, including local anesthetics, vasoconstrictors, astringents, ‫اﻟﺘﺤﺎﻣﻴﻞ اﻟﻤﻬﺒﻠﻴﺔ اﻟﻤﻮﺿﻌﻴﺔ‬ analgesics, soothing emollients, and protective agents. ‫اﻟﺘﺤﺎﻣﻴﻞ أو اﻟﺤﺸﻮات اﻟﻤﻬﺒﻠﻴﺔ‬ ‫اﻟﻤﺨﺼﺼﺔ ﻟﻠﺘﺄﺛﻴﺮات اﻟﻤﻮﺿﻌﻴﺔ‬ ‫ﺗﺴﺘﺨﺪم ﺑﺸﻜﻞ رﺋﻴﺴﻲ ﻛﻤﺎ ﻳ‬: 1. ‫ واﻷدوﻳﺔ‬،‫وﺳﺎﺋﻞ ﻣﻨﻊ اﻟﺤﻤﻞ‬ Local vaginal suppositories 9-‫اﻟﻤﺴﺘﺨﺪﻣﺔ ﻫﻲ اﻟﻨﻮﻧﻮﻛﺴﻴﻨﻮل‬ 2. ‫اﻟﻨﻈﺎﻓﺔ‬ ‫اﻟﻤﻄﻬﺮات‬ Vaginal suppositories or inserts intended for local effects are employed ‫ وﻣﺒﻴﺪات اﻟﻤﺸﻌﺮات‬،‫اﻟﻨﺴﺎﺋﻴﺔ‬ mainly as: ‫ﻟﻤﻜﺎﻓﺤﺔ اﻟﺘﻬﺎب اﻟﻤﻬﺒﻞ اﻟﻨﺎﺟﻢ‬ ‫ﻋﻦ اﻟﻤﺸﻌﺮة اﻟﻤﻬﺒﻠﻴﺔ‬ 1. Contraceptives, the drugs used are nonoxynol-9 3. ‫ﻋﻮاﻣﻞ ﻣﺤﺪدة ﻟﻤﻜﺎﻓﺤﺔ‬.‫ﻣﺴﺒﺒﺎت اﻷﻣﺮاض اﻟﻐﺎ ﻳﺔ‬ 2. Antiseptics in feminine hygiene, trichomonacides to combat vaginitis ‫ ﻣﻀﺎدات اﻟﻔﻄ ﻳﺎت‬،‫أﻏﻠﺐ اﻷﺣﻴﺎن‬ caused by Trichomonas vaginalis (‫ﻟﻌﻼج اﻟﻤﺒﻴﻀﺎت )اﻟﻤﻮﻧﻴﻠﻴﺎ‬ ‫ وﻣﻀﺎدات‬،‫اﻟﺒﻴﻀﺎء‬ 3. Specific agents to combat an invading pathogen. Most commonly, ‫اﻟﻤﻀﺎدات اﻟﺤﻴﻮﻳﺔ‬/‫اﻟﻌﺪوى‬ ‫اﻟﻤﻮﺟﻬﺔ ﺿﺪ اﻟﻜﺎﺋﻨﺎت اﻟﺤﻴﺔ‬ antifungals to treat Candida (Monilia) albicans, and anti- ‫اﻟﺪﻗﻴﻘﺔ اﻷﺧﺮى‬ infectives/antibiotics directed at other microorganism ‫اﻟﺘﺄﺛﻴﺮ اﻟﺠﻬﺎزي ﻟﻠﺘﺤﺎﻣﻴﻞ اﻟﺸﺮﺟﻴﺔ‬ ‫ ﻓﺈن اﻷﻏﺸﻴﺔ اﻟﻤﺨﺎﻃﻴﺔ ﻟﻠﻤﺴﺘﻘﻴﻢ واﻟﻤﻬﺒﻞ ﺗﺴﻤﺢ‬،‫ﺑﺎﻟﻨﺴﺒﺔ ﻟﻠﺘﺄﺛﻴﺮات اﻟﺠﻬﺎ ﻳﺔ‬ ‫ ﻻ ﻳﺘﻢ اﺳﺘﺨﺪام اﻟﻄ ﻳﻖ‬،‫ وﻣﻊ ذﻟﻚ‬.‫ﺑﺎﻣﺘﺼﺎص اﻟﻌﺪﻳﺪ ﻣﻦ اﻷدوﻳﺔ اﻟﻘﺎﺑﻠﺔ ﻟﻠﺬوﺑﺎن‬ ‫ﺑﺸﻜﻞ ﻣﺘﻜﺮر ﻷﻏﺮاض ﺟﻬﺎ ﻳﺔ‬ ‫اﻟﻤﻬﺒ‬. Systemic effect of rectal suppositories For systemic effects, the mucous membranes of the rectum and vagina permit the absorption of many soluble drugs. However, vaginal route is not frequently used for systemic purpose. ‫ﻣﺰاﻳﺎ اﻟﻄ ﻳﻖ اﻟﻤﺴﺘﻘﻴﻢ )ﻟﻠﺘﺄﺛﻴﺮات‬ ‫اﻟﻌﻼج ﻋﻦ ﻃ ﻳﻖ‬ ‫اﻟﺠﻬﺎ ﻳﺔ( ﻋ‬ ‫اﻟﻔﻢ ﻫﻲ‬: The advantages of the rectal route (for systemic effects) over oral (‫اﻷدوﻳﺔ اﻟﺘﻲ ﺗﻢ ﺗﺪﻣﻴﺮﻫﺎ أو )أ‬ ‫ﺗﻌﻄﻴﻠﻬﺎ ﺑﻮاﺳﻄﺔ اﻟﺮﻗﻢ‬ therapy are: ‫اﻟﻬﻴﺪروﺟﻴﻨﻲ أو اﻟﻨﺸﺎط اﻷﻧ ﻳﻤﻲ‬ ‫ﻟﻠﻤﻌﺪة أو اﻷﻣﻌﺎء ﻻ ﺗﺤﺘﺎج إ‬ (a) Drugs destroyed or inactivated by the pH or enzymatic activity of the ‫ﺗﻌ ﻳﻀﻬﺎ ﻟﻬﺬه اﻟﺒﻴﺌﺔ اﻟﻤﺪﻣﺮة‬ (‫ﻳﺠﻮز إﻋﻄﺎء أدوﻳﺔ ﻣﻬﻴﺠﺔ )ب‬ stomach or intestines need not be exposed to these destructive environment (‫اﻷدوﻳﺔ اﻟﺘﻲ ﻳﺘﻢ )ج‬ ‫ﻟﻠﻤﻌﺪة دون أن ﺗﺴﺒﺐ ذﻟﻚ‬ (b) Drugs irritating to the stomach may be given without causing such ‫ﺗﺪﻣﻴﺮﻫﺎ ﻋﻦ ﻃ ﻳﻖ‬ ‫اﻟﺘﻬﻴﺞ‬. ‫اﻟﺪوران اﻟﺒﺎ ﻗﺪ ﺗﺘﺠﺎوز‬ irritation. ‫اﻟﻜﺒﺪ )ﺟﺰﺋ ًﻴﺎ( ﺑﻌﺪ ﺗﻨﺎوﻟﻬﺎ‬ (c) Drugs destroyed by portal circulation may bypass the liver (partially) ‫ﻋﻦ ﻃ ﻳﻖ اﻟﻤﺴﺘﻘﻴﻢ‬. (‫اﻟﻄ ﻳﻖ ﻣﻨﺎﺳﺐ )د‬ after rectal administration. ‫ﻹﻋﻄﺎء اﻷدوﻳﺔ ﻟﻠﻤﺮﺿﻰ‬ ‫ﻏﻴﺮ اﻟﻘﺎد ﻳﻦ أو ﻏﻴﺮ‬ (d) The route is convenient for administration of drugs to patients who are ‫اﺑﺘﻼع اﻟﺪواء‬ ‫اﻟﺮاﻏﺒﻴﻦ‬. unable or unwilling to swallow medication. (‫)ﻫـ‬ ‫ﻳﻌﺪ وﺳﻴﻠﺔ ﻓﻌﺎﻟﺔ‬ ‫ﻋﻼج ﻣﺮﺿﻰ اﻟﻘﻲء‬. (e) It is an effective route in the treatment of patients with vomiting. Examples of drugs administered rectally for systemic effect Prochlorperazine for the relief of nausea and vomiting, indomethacin (NSAIDs) and ondansetron for the relief of nausea and vomiting Some factors affecting on drug absorption from rectal suppositories The dose of a drug administered rectally may be greater than or less than the dose of the same drug given orally, depending on such factors as: The physicochemical nature of the drug Its ability to traverse the physiologic barriers to absorption ‫اﻷدوﻳﺔ اﻟﺘﻲ ﺗﻌﻄﻰ ﻋﻦ ﻃ ﻳﻖ اﻟﻤﺴﺘﻘﻴﻢ ﻟﻠﺘﺄﺛﻴﺮ اﻟﺠﻬﺎزي‬ ‫أﻣﺜﻠﺔ ﻋ‬ ‫ إﻧﺪوﻣﻴﺘﺎﺳﻴﻦ )ﻣﻀﺎدات اﻻﻟﺘﻬﺎب ﻏﻴﺮ اﻟﺴﺘﻴﺮوﻳﺪﻳﺔ( وأوﻧﺪاﻧﺴﻴﺘﺮون ﻟﺘﺨﻔﻴﻒ‬،‫ﺑﺮوﻛﻠﻮ ﺑﻴﺮا ﻳﻦ ﻟﺘﺨﻔﻴﻒ اﻟﻐﺜﻴﺎن واﻟﻘﻲء‬ 27 ‫ ﻗﺪ ﺗﻜﻮن ﺟﺮﻋﺔ اﻟﺪواء اﻟﺘﻲ ﻳﺘﻢ‬.‫اﻣﺘﺼﺎص اﻟﺪواء ﻣﻦ اﻟﺘﺤﺎﻣﻴﻞ اﻟﺸﺮﺟﻴﺔ‬ ‫ ﺑﻌﺾ اﻟﻌﻮاﻣﻞ اﻟﺘﻲ ﺗﺆﺛﺮ ﻋ‬.‫اﻟﻐﺜﻴﺎن واﻟﻘﻲء‬ ‫ﻋﻮاﻣﻞ ﻣﺜﻞ‬ ‫ اﻋﺘﻤﺎدًا ﻋ‬،‫ﺗﻨﺎوﻟﻬﺎ ﻋﻦ ﻃ ﻳﻖ اﻟﻤﺴﺘﻘﻴﻢ أﻛﺒﺮ أو أﻗﻞ ﻣﻦ ﺟﺮﻋﺔ ﻣﻦ ﻧﻔﺲ اﻟﺪواء ُﺗﻌﻄﻰ ﻋﻦ ﻃ ﻳﻖ اﻟﻔﻢ‬: ‫اﻟﻄﺒﻴﻌﺔ اﻟﻔﻴ ﻳﺎﺋﻴﺔ واﻟﻜﻴﻤﻴﺎﺋﻴﺔ ﻟﻠﺪواء‬. ‫اﺟﺘﻴﺎز اﻟﺤﻮاﺟﺰ اﻟﻔﺴﻴﻮﻟﻮﺟﻴﺔ ﻟﻼﻣﺘﺼﺎص‬ ‫ﻗﺪرﺗﻪ ﻋ‬.  ‫ﺗﺤﺮر اﻟﺪواء وإﺗﺎﺣﺘﻪ ﻟﻼﻣﺘﺼﺎص‬ ‫ﻃﺒﻴﻌﺔ اﻟﺘﺤﻤﻴﻠﺔ ك وﺳﻴﻠﺔ وﻗﺪرﺗﻬﺎ ﻋ‬. The nature of the suppository vehicle and its capacity to release the drug and make it available for absorption. Rectal absorption The factors that affect rectal absorption of a drug may be divided into two main groups: ‫اﻻﻣﺘﺼﺎص ﻋﻦ ﻃ ﻳﻖ اﻟﻤﺴﺘﻘﻴﻢ‬ ‫ﻳﻤﻜﻦ ﺗﻘﺴﻴﻢ اﻟﻌﻮاﻣﻞ اﻟﺘﻲ ﺗﺆﺛﺮ ﻋ اﻣﺘﺼﺎص اﻟﺪواء ﻋﺒﺮ اﻟﻤﺴﺘﻘﻴﻢ‬ (a) Physiological factors ‫إ ﻣﺠﻤﻮﻋﺘﻴﻦ رﺋﻴﺴﻴﺘﻴﻦ‬: (b) Physicochemical factors of the drug and the base (‫اﻟﻌﻮاﻣﻞ اﻟﻔﺴﻴﻮﻟﻮﺟﻴﺔ )أ‬ (‫اﻟﻌﻮاﻣﻞ اﻟﻔﻴ ﻳﺎﺋﻴﺔ واﻟﻜﻴﻤﻴﺎﺋﻴﺔ ﻟﻠﺪواء واﻟﻘﺎﻋﺪة )ب‬ ‫اﻟﻌﻮاﻣﻞ اﻟﻔﺴﻴﻮﻟﻮﺟﻴﺔ ﻳﺒﻠﻎ ﻃﻮل‬ ‫ إ‬15 ‫اﻟﻤﺴﺘﻘﻴﻢ ﻋﻨﺪ اﻹﻧﺴﺎن ﺣﻮا‬ 20 ‫ﺳﻢ‬. Physiological factors ‫ﻋﻨﺪﻣﺎ ﻳﻜﻮن اﻟﻤﺴﺘﻘﻴﻢ ﻓﺎرﻏﺎ ﻣﻦ‬ ‫ ﻓﺈﻧﻪ ﻳﺤﺘﻮي ﻓﻘﻂ ﻋ‬،‫ اﻟﻤﻮاد اﻟﺒﺮا ﻳﺔ‬The human rectum is approximately 15 to 20 cm long. 2 ‫ ﻣﻞ ﻣﻦ اﻟﺴﺎﺋﻞ اﻟﻤﺨﺎﻃﻲ‬3 ‫إ‬ ‫ )ﺣﺠﻢ ﻣﻨﺨﻔﺾ ﻣﻦ‬.‫اﻟﺨﺎﻣﻞ‬ When empty of fecal material, the rectum contains only 2 to 3 mL ‫)اﻟﺴﻮاﺋﻞ اﻟﻤﺘﺎﺣﺔ‬ ‫ ﻻ ﻳﻜﻮن‬،‫ﺣﺎﻟﺔ اﻟﺮاﺣﺔ‬ of inert mucous fluid. (Low volume of fluid available) ً ‫اﻟﻤﺴﺘﻘﻴﻢ ﻣﺘﺤﺮﻛﺎ؛ ﻻ ﺗﻮﺟﺪ زﻏﺎﺑﺎت‬ In the resting state, the rectum is not motile; there are no villi or ‫أو زﻏﻴﺒﺎت ﺻﻐﻴﺮة ﻋ اﻟﻐﺸﺎء‬ ‫اﻟﻤﺨﺎﻃﻲ ﻟﻠﻤﺴﺘﻘﻴﻢ‬. microvilli on the rectal mucosa. ‫ ﻫﻨﺎك وﻓﺮة ﻣﻦ اﻷوﻋﻴﺔ‬،‫وﻣﻊ ذﻟﻚ‬ ‫اﻟﺪﻣﻮﻳﺔ اﻟﻤﻨﻄﻘﺔ ﺗﺤﺖ اﻟﻤﺨﺎﻃﻴﺔ‬ However, there is abundant vascularization of the submucosal region ‫ﻟﺠﺪار اﻟﻤﺴﺘﻘﻴﻢ ﺑﺎﻟﺪم واﻷوﻋﻴﺔ‬ of the rectum wall with blood and lymphatic vessels. ‫اﻟﻠﻴﻤﻔﺎوﻳﺔ‬. ‫ﻣﻦ ﺑﻴﻦ اﻟﻌﻮاﻣﻞ اﻟﻔﺴﻴﻮﻟﻮﺟﻴﺔ‬ Among the physiologic factors that affect drug absorption from the ‫اﻟﺘﻲ ﺗﺆﺛﺮ ﻋ اﻣﺘﺼﺎص اﻟﺪواء ﻣﻦ‬ ‫اﻟﻤﺴﺘﻘﻴﻢ ﻫﻲ ﻣﺤﺘﻮﻳﺎت اﻟﻘﻮﻟﻮن‬، rectum are the colonic contents, and the pH and lack of buffering ‫ودرﺟﺔ اﻟﺤﻤﻮﺿﺔ وﻧﻘﺺ اﻟﻘﺪرة‬ ‫اﻟﺘﺨ ﻳﻨﻴﺔ ﻟﺴﻮاﺋﻞ اﻟﻤﺴﺘﻘﻴﻢ‬. capacity of the rectal fluids. Colonic Content ‫ﻣﺤﺘﻮى اﻟﻘﻮﻟﻮن‬ When systemic effects are desired, greater absorption may be expected ‫ﻋﻨﺪﻣﺎ ﺗﻜﻮن اﻟﺘﺄﺛﻴﺮات اﻟﺠﻬﺎ ﻳﺔ‬ ‫ ﻳﻤﻜﻦ ﺗﻮﻗﻊ اﻣﺘﺼﺎص‬،‫ﻣﺮﻏﻮﺑﺔ‬ from a rectum that is void than from one that is distended with fecal matter. ‫أﻛﺒﺮ ﻣﻦ اﻟﻤﺴﺘﻘﻴﻢ اﻟﻔﺎرغ‬ ‫ﻣﻘﺎرﻧﺔ ﺑﺎﻟﻤﺴﺘﻘﻴﻢ اﻟﻤﻨﺘﻔﺦ‬ A drug will obviously have greater opportunity to make contact with the ‫ﺑﺎﻟﻤﺎدة اﻟﺒﺮا ﻳﺔ‬. ‫ﻣﻦ اﻟﻮاﺿﺢ أن اﻟﺪواء ﺳﻴﻜﻮن‬ absorbing surface of the rectum and colon in an empty rectum. ‫ﻟﺪﻳﻪ ﻓﺮﺻﺔ أﻛﺒﺮ ﻟﻼﺗﺼﺎل‬ Therefore, when deemed desirable, an evacuation enema may be ‫ﺑﺴﻄﺢ اﻻﻣﺘﺼﺎص ﻟﻠﻤﺴﺘﻘﻴﻢ‬ ‫اﻟﻤﺴﺘﻘﻴﻢ اﻟﻔﺎرغ‬ ‫واﻟﻘﻮﻟﻮن‬. administered and allowed to act before the administration of a suppository ‫ ﻋﻨﺪﻣﺎ ﻳﻜﻮن ذﻟﻚ‬،‫ﻟﺬﻟﻚ‬ ‫ ﻳﻤﻜﻦ إﻋﻄﺎء ﺣﻘﻨﺔ‬،‫ﻣﺮﻏﻮﺑًﺎ‬ of a drug to be absorbed. ‫ﺷﺮﺟﻴﺔ إﺧﻼء واﻟﺴﻤﺎح ﻟﻬﺎ‬ Other conditions, such as diarrhea, colonic obstruction due to tumorous ‫ﺑﺎﻟﻌﻤﻞ ﻗﺒﻞ إﻋﻄﺎء ﺗﺤﻤﻴﻠﺔ‬ ‫ﻟﻠﺪواء اﻟﻤﺮاد اﻣﺘﺼﺎﺻﻪ‬. growths, and tissue dehydration can all influence the rate and degree of ‫ ﻣﺜﻞ اﻹﺳﻬﺎل‬،‫ﺣﺎﻻت أﺧﺮى‬، ‫واﻧﺴﺪاد اﻟﻘﻮﻟﻮن ﺑﺴﺒﺐ اﻟﻨﻤﻮ‬ drug absorption from the rectum. ‫ وﺟﻔﺎف اﻷﻧﺴﺠﺔ ﻳﻤﻜﻦ‬،‫اﻟﻮرﻣﻲ‬ ‫ﻣﻌﺪل‬ ‫أن ﺗﺆﺛﺮ ﺟﻤﻴﻌﻬﺎ ﻋ‬ ‫ودرﺟﺔ اﻣﺘﺼﺎص اﻟﺪواء ﻣﻦ‬ Circulation Route ‫اﻟﻤﺴﺘﻘﻴﻢ‬. Drugs absorbed rectally, unlike those absorbed after oral administration, bypass the portal circulation during their first pass into the general circulation, thereby enabling drugs otherwise destroyed in the liver to exert systemic effects. The lower hemorrhoidal veins surrounding the colon receive the absorbed drug and initiate its circulation throughout the body, bypassing the liver. Lymphatic circulation also assists in the absorption of rectally administered drugs ‫ﻃ ﻳﻖ اﻟﺪورة اﻟﺪﻣﻮﻳﺔ‬ ‫ ﺗﺘﺠﺎوز اﻟﺪورة‬،‫ ﻋ ﻋﻜﺲ ﺗﻠﻚ اﻟﻤﻤﺘﺼﺔ ﺑﻌﺪ ﺗﻨﺎوﻟﻬﺎ ﻋﻦ ﻃ ﻳﻖ اﻟﻔﻢ‬،‫اﻷدوﻳﺔ اﻟﻤﻤﺘﺼﺔ ﻋﻦ ﻃ ﻳﻖ اﻟﻤﺴﺘﻘﻴﻢ‬ ‫اﻟﻜﺒﺪ‬ ‫ﺗﻤﻜﻦ اﻷدوﻳﺔ اﻟﺘﻲ ﺗﻢ ﺗﺪﻣﻴﺮﻫﺎ‬ ‫ وﺑﺎﻟﺘﺎ‬،‫اﻟﺪورة اﻟﺪﻣﻮﻳﺔ اﻟﻌﺎﻣﺔ‬ ‫اﻟﺪﻣﻮﻳﺔ اﻟﺒﺎﺑﻴﺔ أﺛﻨﺎء ﻣﺮورﻫﺎ اﻷول إ‬ 28 ‫ﻣﻦ ﻣﻤﺎرﺳﺔ ﺗﺄﺛﻴﺮات ﺟﻬﺎ ﻳﺔ‬. ‫ﺟﻤﻴﻊ أﻧﺤﺎء‬ ‫ﺗﺘﻠﻘﻰ اﻷوردة اﻟﺒﻮاﺳﻴﺮ اﻟﺴﻔﻠﻴﺔ اﻟﻤﺤﻴﻄﺔ ﺑﺎﻟﻘﻮﻟﻮن اﻟﺪواء اﻟﻤﻤﺘﺺ وﺗﺒﺪأ اﻟﺪورة اﻟﺪﻣﻮﻳﺔ‬ ‫ اﻟﺠﺴﻢ ﻣﺘﺠﺎوزة اﻟﻜﺒﺪ‬. ‫اﻣﺘﺼﺎص اﻷدوﻳﺔ اﻟﺘﻲ ﻳﺘﻢ ﺗﻨﺎوﻟﻬﺎ ﻋﻦ ﻃ ﻳﻖ اﻟﻤﺴﺘﻘﻴﻢ‬ ً ‫ﺗﺴﺎﻋﺪ اﻟﺪورة اﻟﻠﻤﻔﺎوﻳﺔ‬ ‫أﻳﻀﺎ‬  ‫اﻟﺮﻗﻢ اﻟﻬﻴﺪروﺟﻴﻨﻲ وﻧﻘﺺ اﻟﻘﺪرة اﻟﺘﺨ ﻳﻨﻴﺔ ﻟﺴﻮاﺋﻞ اﻟﻤﺴﺘﻘﻴﻢ‬ ‫ ﻓﺈن اﻟﺸﻜﻞ اﻟﺬي ﻳﺘﻢ ﻓﻴﻪ إﻋﻄﺎء اﻟﺪواء‬،‫( وﻟﻴﺲ ﻟﻬﺎ ﻗﺪرة ﻋﺎزﻟﺔ ﻓﻌﺎﻟﺔ‬7) ‫اﻟﺮﻗﻢ اﻟﻬﻴﺪروﺟﻴﻨﻲ‬ ‫ﻧﻈ ًﺮا ﻷن ﺳﻮاﺋﻞ اﻟﻤﺴﺘﻘﻴﻢ ﻣﺤﺎﻳﺪة ﺑﺸﻜﻞ أﺳﺎﺳﻲ‬ ‫ﻟﻦ ﻳﺘﻐﻴﺮ ﻛﻴﻤﻴﺎﺋ ًﻴﺎ ﺑﺸﻜﻞ ﻋﺎم ﺑﻮاﺳﻄﺔ اﻟﺒﻴﺌﺔ‬. ‫ ﺑﺴﺒﺐ ﻋﺪم اﻣﺘﺰاﺟﻬﺎ‬،‫ ﺑﻴﻨﻤﺎ ﺗﺬوب ﺑﺪة اﻟﻜﺎﻛﺎو ﺑﺴﺮﻋﺔ ﻋﻨﺪ درﺟﺔ ﺣﺮارة اﻟﺠﺴﻢ‬.‫ﺗﺤﺮر اﻟﻤﻜﻮﻧﺎت اﻟﻨﺸﻄﺔ‬ ‫ﻟﻘﺎﻋﺪة اﻟﺘﺤﻤﻴﻠﺔ ﺗﺄﺛﻴﺮ ﻣﻠﺤﻮظ ﻋ‬ ‫اﻟﺪﻫﻮن ﺑﺴﻬﻮﻟﺔ‬ ‫إﻃﻼق اﻷدوﻳﺔ اﻟﻘﺎﺑﻠﺔ ﻟﻠﺬوﺑﺎن‬ ‫ ﻓﺈﻧﻬﺎ ﺗﻔﺸﻞ‬،‫ﺑﺎﻟﺴﻮاﺋﻞ‬. pH and Lack of Buffering Capacity of the Rectal Fluids Because rectal fluids are essentially neutral in pH (pH 7) and have no effective buffer capacity, the form in which the drug is administered will not generally be chemically changed by the environment. The suppository base has a marked influence on the release of active constituents. While cocoa butter melts rapidly at body temperature, because of its immiscibility with fluids, it fails to release fat-soluble drugs readily. Physicochemical factors of the drug and suppository base Physicochemical factors of the drug include such properties as: 1. The relative solubility of the drug in lipid and in water and ‫اﻟﻌﻮاﻣﻞ اﻟﻔﻴ ﻳﺎﺋﻴﺔ واﻟﻜﻴﻤﻴﺎﺋﻴﺔ ﻟﻠﺪواء وﻗﺎﻋﺪة اﻟﺘﺤﻤﻴﻠﺔ‬ 2. The particle size of a dispersed drug, and surface properties ‫ﺗﺸﻤﻞ اﻟﻌﻮاﻣﻞ اﻟﻔﻴ ﻳﺎﺋﻴﺔ واﻟﻜﻴﻤﻴﺎﺋﻴﺔ ﻟﻠﺪواء ﺧﺼﺎﺋﺺ ﻣﺜﻞ‬: 1. ‫اﻟﺬوﺑﺎن اﻟﻨﺴﺒﻲ ﻟﻠﺪواء اﻟﺪﻫﻮن و اﻟﻤﺎء و‬ 3. Amount of drug 2. ‫ﺳﻄﺤﻪ‬ ‫ وﺧﺼﺎﺋﺺ‬،‫ﺣﺠﻢ ﺟﺴﻴﻤﺎت اﻟﺪواء اﻟﻤﺸﺘﺖ‬ 3. ‫ﻛﻤﻴﺔ اﻟﺪواء‬ 4. pKa of the drug 4. ‫ﺛﺎﺑﺖ ﺣﻤﺾ اﻟﺪواء‬ Physicochemical factors of the base include: 1. Its ability to melt, soften, or dissolve at body temperature 2. Its ability to release the drug substance 3. Its hydrophilic or hydrophobic character (composition of the base) ‫اﻟﻌﻮاﻣﻞ اﻟﻔﻴ ﻳﺎﺋﻴﺔ واﻟﻜﻴﻤﻴﺎﺋﻴﺔ ﻟﻠﻘﺎﻋﺪة ﺗﺸﻤﻞ‬: 4. Rheological properties. 1. ‫ﻗﺪرﺗﻪ ﻋ اﻟﺬوﺑﺎن أو اﻟﺘﻠﻴﻴﻦ أو اﻟﺬوﺑﺎن ﻋﻨﺪ درﺟﺔ ﺣﺮارة اﻟﺠﺴﻢ‬ 2. ‫إﻃﻼق اﻟﻤﺎدة اﻟﺪواﺋﻴﺔ‬ ‫ﻗﺪرﺗﻪ ﻋ‬ 3. (‫ﻃﺎﺑﻌﻬﺎ اﻟﻤﺤﺐ ﻟﻠﻤﺎء أو اﻟﻜﺎره ﻟﻠﻤﺎء )ﺗﻜﻮﻳﻦ اﻟﻘﺎﻋﺪة‬ Lipid-Water Solubility of drug 4. ‫اﻟﺨﺼﺎﺋﺺ اﻟ ﻳﻮﻟﻮﺟﻴﺔ‬. The lipid-water partition coefficient of a drug is an important consideration in the selection of the suppository base and in anticipating drug release from that base. A lipophilic drug that is distributed in a fatty suppository base in low concentration has less tendency to escape to the surrounding aqueous fluids than a hydrophilic substance in a fatty base. Water soluble bases—for example, polyethylene glycols—that dissolve in the anorectal fluids release for absorption water-soluble and oil-soluble drugs. ‫ﻗﺎﺑﻠﻴﺔ ذوﺑﺎن اﻟﺪواء اﻟﻤﺎء واﻟﺪﻫﻮن ﻳﻌﺪ ﻣﻌﺎﻣﻞ ﺗﻘﺴﻴﻢ اﻟﺪواء اﻟﻤﺎء ﻣﻦ اﻻﻋﺘﺒﺎرات اﻟﻤﻬﻤﺔ اﺧﺘﻴﺎر ﻗﺎﻋﺪة‬ ‫ﺗﻮﻗﻊ إﻃﻼق اﻟﺪواء ﻣﻦ ﺗﻠﻚ اﻟﻘﺎﻋﺪة‬ ‫اﻟﺘﺤﻤﻴﻠﺔ و‬. ‫اﻟﺴﻮاﺋﻞ‬ ‫ﻗﺎﻋﺪة ﺗﺤﻤﻴﻠﺔ دﻫﻨﻴﺔ ﺑﺘﺮﻛﻴﺰ ﻣﻨﺨﻔﺾ ﻟﺪﻳﻪ ﻣﻴﻞ أﻗﻞ ﻟﻠﻬﺮوب إ‬ ‫اﻟﺪواء اﻟﻤﺤﺐ ﻟﻠﺪﻫﻮن اﻟﺬي ﻳﺘﻢ ﺗﻮ ﻳﻌﻪ‬ ‫اﻟﻘﺎﻋﺪة اﻟﺪﻫﻨﻴﺔ‬ ‫اﻟﻤﺎﺋﻴﺔ اﻟﻤﺤﻴﻄﺔ ﻣﻦ اﻟﻤﺎدة اﻟﻤﺤﺒﺔ ﻟﻠﻤﺎء‬. ‫ ﺗﻄﻠﻖ‬،‫اﻟﺴﻮاﺋﻞ اﻟﺸﺮﺟﻴﺔ‬ ‫ اﻟﺘﻲ ﺗﺬوب‬- ‫إﻳﺜﻴﻠﻴﻦ ﺟﻼﻳﻜﻮل‬ ‫ اﻟﺒﻮ‬،‫ﺳﺒﻴﻞ اﻟﻤﺜﺎل‬ ‫ ﻋ‬- ‫اﻟﻤﺎء‬ ‫ﻗﻮاﻋﺪ ﻗﺎﺑﻠﺔ ﻟﻠﺬوﺑﺎن‬ ‫اﻟ ﻳﺖ‬ ‫اﻟﻤﺎء واﻟﻘﺎﺑﻠﺔ ﻟﻠﺬوﺑﺎن‬ ‫ﻻﻣﺘﺼﺎص اﻷدوﻳﺔ اﻟﻘﺎﺑﻠﺔ ﻟﻠﺬوﺑﺎن‬. 29  Drug solubility and suppository formulation Solubility of drug in Fat Water Choice of base Low High Fatty base High Low Aqueous base Low Low Intermediate Amount of drug Naturally, the more drug a base contains, the more drug will be available for absorption. However, if the concentration of a drug in the intestinal lumen is above a particular amount, which varies with the drug, the rate of. absorption is not changed by a further increase in the concentration of the ‫ﺣﺠﻢ اﻟﺠﺴﻴﻤﺎت ﺑﺎﻟﻨﺴﺒﺔ‬ ‫ﻛﻤﻴﺔ اﻟﺪواء‬ ‫ﻟﻸدوﻳﺔ ﻏﻴﺮ اﻟﻤﺬاﺑﺔ‬ drug. ‫ ﻛﻠﻤﺎ زاد اﻟﺪواء اﻟﻤﺘﺎح ﻟﻼﻣﺘﺼﺎص‬،‫ ﻛﻠﻤﺎ زادت ﻛﻤﻴﺔ اﻟﺪواء اﻟﺬي ﺗﺤﺘﻮﻳﻪ اﻟﻘﺎﻋﺪة‬،‫وﺑﻄﺒﻴﻌﺔ اﻟﺤﺎل‬. ‫ ﻓﺈن‬،(‫اﻟﺘﺤﻤﻴﻠﺔ )اﻟﻤﻌﻠﻖ‬ ‫ﺣﺠﻢ ﺟﺴﻴﻤﺎت اﻟﺪواء ﺳﻮف‬ Particle Size ‫ ﻓﺈن ﻣﻌﺪل اﻻﻣﺘﺼﺎص ﻻ ﻳﺘﻐﻴﺮ ﺑ ﻳﺎدة أﺧﺮى ﺗﺮﻛﻴﺰ اﻟﺪواء‬،‫ واﻟﺘﻲ ﺗﺨﺘﻠﻒ ﺑﺎﺧﺘﻼف اﻟﺪواء‬،‫ إذا ﻛﺎن ﺗﺮﻛﻴﺰ اﻟﺪواء اﻟﺘﺠﻮﻳﻒ اﻟﻤﻌﻮي أﻋ ﻣﻦ ﻛﻤﻴﺔ ﻣﻌﻴﻨﺔ‬،‫وﻣﻊ ذﻟﻚ‬ ‫ﻣﻌﺪل ذوﺑﺎﻧﻬﺎ‬ ‫ﻳﺆﺛﺮ ﻋ‬ ‫وﺗﻮاﻓﺮﻫﺎ ﻟﻼﻣﺘﺼﺎص‬. For un-dissolved drugs in a suppository (suspension), the size of the drug ‫ﻛﻠﻤﺎ ﻛﺎن اﻟﺠﺴﻴﻢ أﺻﻐﺮ‬، particle will influence its rate of dissolution and its availability for ‫زادت ﻣﺴﺎﺣﺔ اﻟﺴﻄﺢ‬، ‫وأﺻﺒﺢ ذوﺑﺎن اﻟﺠﺴﻴﻢ أﻛﺜﺮ‬ absorption. ‫ﺳﻬﻮﻟﺔ وزادت ﻓﺮﺻﺔ‬ ‫اﻻﻣﺘﺼﺎص اﻟﺴ ﻳﻊ‬. The smaller the particle, the greater the surface area, the more readily the dissolution of the particle and the greater the chance for rapid absorption. ‫ﻃﺒﻴﻌﺔ اﻟﻘﺎﻋﺪة ﻳﺠﺐ أن ﺗﻜﻮن‬ ‫اﻟﺬوﺑﺎن أو‬ ‫اﻟﻘﺎﻋﺪة ﻗﺎدرة ﻋ‬ Nature of the Base ‫اﻟﺘﻠﻴﻴﻦ أو اﻟﺬوﺑﺎن ﻟﺘﺤ ﻳﺮ اﻟﺪواء‬ ‫ إذا‬.‫اﻟﺨﺎص ﺑﻬﺎ ﻟﻼﻣﺘﺼﺎص‬ The base must be capable of melting, softening, or dissolving to release its ‫ﺗﻔﺎﻋﻠﺖ اﻟﻘﺎﻋﺪة ﻣﻊ اﻟﺪواء ﻟﻤﻨﻊ‬ drug for absorption. If the base interacts with the drug to inhibit its release, ‫ ﻓﺴﻴﺘﻢ ﺿﻌﻒ اﻣﺘﺼﺎص‬،‫إﻃﻼﻗﻪ‬ ‫اﻟﺪواء أو ﺣﺘﻰ ﻣﻨﻌﻪ‬. drug absorption will be impaired or even prevented. ً ‫ إذا ﻛﺎﻧﺖ اﻟﻘﺎﻋﺪة ﺗﻬﻴﺞ‬،‫أﻳﻀﺎ‬ ‫اﻷﻏﺸﻴﺔ اﻟﻤﺨﺎﻃﻴﺔ ﻟﻠﻤﺴﺘﻘﻴﻢ‬، Also, if the base irritates the mucous membranes of the rectum, it may ‫ﺣﺪوث اﺳﺘﺠﺎﺑﺔ‬ ‫ﻓﻘﺪ ﺗﺆدي إ‬ ‫ ﻣﻤﺎ‬،‫ﻗﻮﻟﻮﻧﻴﺔ وﺗﺤﻔﺰ ﺣﺮﻛﺔ اﻷﻣﻌﺎء‬ initiate a colonic response and prompt a bowel movement, eliminating the ‫ﻳﻠﻐﻲ اﺣﺘﻤﺎﻟﻴﺔ إﻃﻼق اﻟﺪواء‬ prospect of complete drug release and absorption. ‫واﻣﺘﺼﺎﺻﻪ ﺑﺸﻜﻞ ﻛﺎﻣﻞ‬. ‫ﺑﺴﺒﺐ اﺣﺘﻤﺎل ﺣﺪوث‬ Because of the possibility of chemical and/or physical interactions ‫أو ﻓﻴ ﻳﺎﺋﻴﺔ‬/‫ﺗﻔﺎﻋﻼت ﻛﻴﻤﻴﺎﺋﻴﺔ و‬ between the medicinal agent and the suppository base, which may affect the stability and/or bioavailability of the drug, the absence of any drug interaction between the two agents should be ascertained before or during formulation. Properties of the ideal suppository base 1. Non-toxic, non- irritating to sensitive and inflamed tissues. 2. Inert and compatible with medicaments.. ‫ﺧﺼﺎﺋﺺ ﻗﺎﻋﺪة اﻟﺘﺤﻤﻴﻠﺔ اﻟﻤﺜﺎﻟﻴﺔ‬ 1. ‫ﻏﻴﺮ ﺳﺎﻣﺔ وﻏﻴﺮ ﻣﻬﻴﺠﺔ ﻟﻸﻧﺴﺠﺔ اﻟﺤﺴﺎﺳﺔ واﻟﻤﻠﺘﻬﺒﺔ‬. 30 2. ‫ ﺧﺎﻣﻞ وﻣﺘﻮاﻓﻖ ﻣﻊ اﻷدوﻳﺔ‬.  3. ‫ﻋﺪم ﻓﺴﺎد اﻟﺪواء أو ﺗﻠﻮﻳﺜﻪ أﺛﻨﺎء اﻟﺘﺨ ﻳﻦ‬. 4. ‫ﻳﺘﻢ ﺗﺼﻨﻴﻌﻬﺎ ﺑﺴﻬﻮﻟﺔ ﻋﻦ ﻃ ﻳﻖ اﻟﻀﻐﻂ أو اﻟﻘﻮﻟﺒﺔ‬. 5. ‫اﻹﻓﺮازات اﻟﻤﺨﺎﻃﻴﺔ أو ﻳﺬوب ﺑﺴﺮﻋﺔ ﻋﻨﺪ درﺟﺔ ﺣﺮارة اﻟﺠﺴﻢ ﻟﻴﺴﻤﺢ ﺑﺘﺤﺮر اﻟﺪواء‬ ‫ﻳﺬوب أو ﻳﺘﻔﻜﻚ‬. 6. ‫اﻟﻘﻮاﻟﺐ‬ ‫ﻳﺒﻘﻰ ﻣﻨﺼﻬﺮا ً ﻟﻤﺪة ﻛﺎﻓﻴﺔ ﻟﻠﺴﻤﺎح ﺑﺼﺒﻪ‬. 7. ‫ﺗﺼﻠﺐ ﺑﺴﺮﻋﺔ ﻟﺘﻘﻠﻴﻞ‬ 3. Not deteriorated or contaminating the drug during storage. ‫ﺗﺮﺳﻴﺐ اﻟﻤﻮاد اﻟﺼﻠﺒﺔ‬ 4. Easily manufactured by compression or molding. ‫اﻟﻤﺸﺘﺘﺔ‬. 8. ‫ﻳﺘﻢ اﻻﺣﺘﻔﺎظ ﺑﺎﻟﺘﺒ ﻳﺪ‬ 5. Dissolve or disintegrate in mucous secretions or melt quickly at body ‫ﻟﺴﻬﻮﻟﺔ ﺳﺤﺐ اﻟﺘﺤﻤﻴﻠﺔ ﻣﻦ‬ ‫اﻟﻘﺎﻟﺐ‬. temperature to allow the release of medicament. 9. ‫ﻟﻪ ﺧﺼﺎﺋﺺ ﺗﺮﻃﻴﺐ‬ 6. Remain molten for a sufficient period of time to allow pouring into ‫واﺳﺘﺤﻼب‬. 10. ‫ﻣﺴﺘﻘﺮ ﻋﻨﺪ اﻟﺘﺨ ﻳﻦ‬، molds. ‫ﺷﻜﻠﻪ أﺛﻨﺎء‬ ‫وﻳﺤﺎﻓﻆ ﻋ‬ ‫اﻟﺘﺨ ﻳﻦ أو اﻟﻤﻘﺒﺾ )ﻻ ﻳﺘﻐﻴﺮ‬ 7. Solidify rapidly to minimize sedimentation of dispersed solids. ‫اﻟﻠﻮن واﻟﺮاﺋﺤﺔ وﻧﻤﻂ إﻃﻼق‬ ‫)اﻟﺪواء‬ 8. Contract on cooling to allow easy withdrawal of the suppository from the mold. 9. Has wetting and emulsifying properties. 10. Stable on storage, keeps its shape during storage or handle (does not. change color, odor and drug release pattern). ‫ﻗﻮاﻋﺪ ﺗﺤﻤﻴﻠﺔ‬ ‫درﺟﺔ ﺣﺮارة اﻟﻐﺮﻓﺔ وﻟﻜﻨﻬﺎ ﺗﻠﻴﻦ أو‬ ‫ﻣﺘﻄﻠﺒﺎت ﻗﺎﻋﺪة اﻟﺘﺤﻤﻴﻠﺔ ﻫﻲ أن ﺗﻈﻞ ﺻﻠﺒﺔ‬ ‫درﺟﺔ ﺣﺮارة اﻟﺠﺴﻢ ﺑﺤﻴﺚ ﻳﻜﻮن اﻟﺪواء ﻣﺘﺎﺣًﺎ ﺑﺎﻟﻜﺎﻣﻞ ﺑﻌﺪ‬ ‫ﺗﺬوب أو ﺗﺬوب ﺑﺴﻬﻮﻟﺔ‬ Suppository bases ‫وﻗﺖ ﻗﺼﻴﺮ ﻣﻦ إدﺧﺎﻟﻪ‬. ‫اﻷﻧﻮاع اﻟﺮﺋﻴﺴﻴﺔ ﻟﻘﻮاﻋﺪ‬ Requisites for a suppository base is that it should remain solid at room ‫ اﻟﺘﺤﻤﻴﻠﺔ‬: 1. ‫اﻟﻘﻮاﻋﺪ اﻟﺪﻫﻨﻴﺔ أو‬ temperature but soften, melt, or dissolve readily at body temperature so ‫ ﺑﺪة اﻟﻜﺎﻛﺎو‬:‫اﻟﻘﻮاﻋﺪ اﻟ ﻳﺘﻴﺔ‬ (‫ﺗﺬوب ) ﻳﺖ اﻟﺜﻴﻮﺑﺮوﻣﺎ‬ that the drug is fully available soon after insertion. ‫ﺑﺴﺮﻋﺔ ﻋﻨﺪ درﺟﺔ ﺣﺮارة‬ Main types of suppository bases: ‫ وﻟﻜﻨﻬﺎ ﻏﻴﺮ ﻗﺎﺑﻠﺔ‬،‫اﻟﺠﺴﻢ‬ ‫ﻟﻼﻣﺘﺰاج ﻣﻊ ﺳﻮاﺋﻞ اﻟﺠﺴﻢ‬ 1. Fatty bases or oleaginous bases, Cocoa butter (theobroma oil) melts ‫أﻣﺎ اﻷدوﻳﺔ اﻟﺘﻲ ﺗﺬوب‬ ‫اﻟﺪﻫﻮن ﻓﺈﻧﻬﺎ ﺗﻤﻴﻞ إ‬ quickly at body temperature, but is immiscible with body fluids as for ‫اﻟ ﻳﺖ وﻟﻬﺎ ﻣﻴﻞ‬ ‫اﻟﺴﻮاﺋﻞ‬ ‫اﻟﺒﻘﺎء‬ ‫ﻗﻠﻴﻞ ﻟﻠﺪﺧﻮل إ‬ fat-soluble drugs tend to remain in the oil and have little tendency to ‫اﻟﻔﺴﻴﻮﻟﻮﺟﻴﺔ اﻟﻤﺎﺋﻴﺔ‬. enter the aqueous physiologic fluids. ‫ﺑﺎﻟﻨﺴﺒﺔ ﻟﻸدوﻳﺔ اﻟﻘﺎﺑﻠﺔ‬ ‫ﺑﺪة‬ ‫اﻟﻤﺎء‬ ‫ﻟﻠﺬوﺑﺎن‬ For water- soluble drugs in cocoa butter, the reverse is usually true and ‫ ﻋﺎدة ﻣﺎ ﻳﻜﻮن‬،‫اﻟﻜﺎﻛﺎو‬ ‫اﻟﻌﻜﺲ ﺻﺤﻴﺤًﺎ وﻧﺘﺎﺋﺞ‬ good release results. Also, when irritation or inflammation is to be relieved, ً.‫إﻃﻼق ﺟﻴﺪة‬ ‫ ﻋﻨﺪﻣﺎ‬،‫أﻳﻀﺎ‬ as in the treatment of anorectal disorders, cocoa butter appears to be the ‫ﻧ ﻳﺪ ﺗﺨﻔﻴﻒ اﻟﺘﻬﻴﺞ أو‬ ‫ ﻛﻤﺎ ﻫﻮ اﻟﺤﺎل‬،‫اﻻﻟﺘﻬﺎب‬ superior base because of its emollient or soothing, spreading action ‫ﻋﻼج اﻻﺿﻄﺮاﺑﺎت اﻟﺸﺮﺟﻴﺔ‬، ‫ﻳﺒﺪو أن ﺑﺪة اﻟﻜﺎﻛﺎو ﻫﻲ‬ 2. Water soluble or water miscible bases, glycerinated gelatin or ‫اﻟﻘﺎﻋﺪة اﻟﻤﺘﻔﻮﻗﺔ ﺑﺴﺒﺐ‬ ‫ﺗﺄﺛﻴﺮﻫﺎ اﻟﻤﻄﺮي أو اﻟﻤﻬﺪئ‬. polyethylene glycol, Fat-soluble drugs seem to be released more readily from these bases, but both of which dissolve slowly in body fluids. 3. Miscellaneous bases, generally combinations of lipophilic and hydrophilic substances. 2. ‫ ﻳﺒﺪو أن اﻷدوﻳﺔ اﻟﻘﺎﺑﻠﺔ‬،‫ اﻟﺠﻴﻼﺗﻴﻦ اﻟﻐﻠﻴﺴﻴ ﻳﻦ أو اﻟﺒﻮ إﻳﺜﻴﻠﻴﻦ ﺟﻼﻳﻜﻮل‬،‫اﻟﻘﻮاﻋﺪ اﻟﻘﺎﺑﻠﺔ ﻟﻠﺬوﺑﺎن اﻟﻤﺎء أو اﻟﻘﻮاﻋﺪ اﻟﻘﺎﺑﻠﺔ ﻟﻼﻣﺘﺰاج ﺑﺎﻟﻤﺎء‬ ‫ﺳﻮاﺋﻞ اﻟﺠﺴﻢ‬ ‫ ﻟﻜﻦ ﻛﻼﻫﻤﺎ ﻳﺬوب ﺑﺒﻂء‬،‫اﻟﺪﻫﻮن ﺗﺘﺤﺮر ﺑﺴﻬﻮﻟﺔ أﻛﺒﺮ ﻣﻦ ﻫﺬه اﻟﻘﻮاﻋﺪ‬ ‫ﻟﻠﺬوﺑﺎن‬. 3. ‫ ﺑﺸﻜﻞ ﻋﺎم ﻣﺠﻤﻮﻋﺎت ﻣﻦ اﻟﻤﻮاد اﻟﻤﺤﺒﺔ ﻟﻠﺪﻫﻮن واﻟﻤﺎء‬،‫ﻗﻮاﻋﺪ ﻣﺘﻨﻮﻋﺔ‬. Fatty or Oleaginous Bases 1. Cocoa butter 2. Hydrogenated fatty acids of vegetable oils, such as palm kernel oil and cotton seed oil. 3. Fat-based compounds, esters of glycerin with the higher-molecular- weight fatty acids, such as palmitic and stearic acids, such as glyceryl monostearate and glyceryl monopalmitate. ‫اﻟﻘﻮاﻋﺪ اﻟﺪﻫﻨﻴﺔ أو اﻟ ﻳﺘﻴﺔ‬ 1. ‫ﺑﺪة اﻟﻜﺎﻛﺎو‬ 2. ‫ و ﻳﺖ ﺑﺬرة اﻟﻘﻄﻦ‬،‫ ﻣﺜﻞ ﻳﺖ ﻧﻮاة اﻟﻨﺨﻴﻞ‬،‫اﻷﺣﻤﺎض اﻟﺪﻫﻨﻴﺔ اﻟﻤﻬﺪرﺟﺔ ﻣﻦ اﻟ ﻳﻮت اﻟﻨﺒﺎﺗﻴﺔ‬. 3. ‫ ﻣﺜﻞ‬، ‫ اﺳﺘﺮات اﻟﺠﻠﺴ ﻳﻦ ﻣﻊ اﻷﺣﻤﺎض اﻟﺪﻫﻨﻴﺔ ذات اﻟﻮزن اﻟﺠ ﻳﺌﻲ اﻷﻋ‬،‫اﻟﻤﺮﻛﺒﺎت اﻟﺪﻫﻨﻴﺔ‬ 31 ‫ ﻣﺜﻞ أﺣﺎدي ﺳﺘﻴﺎرات اﻟﺠﻠﻴﺴ ﻳﻞ وأﺣﺎدي ﺑﺎﻟﻤﻴﺘﺎت‬،‫اﻷﺣﻤﺎض اﻟﺒﺎﻟﻤﺘﻴﻜﻴﺔ واﻷﺣﻤﺎض اﻟﺪﻫﻨﻴﺔ‬ ‫اﻟﺠﻠﻴﺴ ﻳﻞ‬.  ‫اﻟﻌﺪﻳﺪ ﻣﻦ اﻟﻤﻨﺘﺠﺎت اﻟﺘﺠﺎ ﻳﺔ ﺗﺮﻛﻴﺒﺎت ﻣﺘﻨﻮﻋﺔ ﻣﻦ ﻫﺬه اﻷﻧﻮاع ﻣﻦ اﻟﻤﻮاد ﻟﺘﺤﻘﻴﻖ اﻟﺼﻼﺑﺔ‬ ‫ﺗﺴﺘﺨﺪم اﻟﻘﻮاﻋﺪ اﻟﻤﻮﺟﻮدة‬ ‫ﻇﻞ ﻇﺮوف اﻟﺸﺤﻦ واﻟﺘﺨ ﻳﻦ واﻟﺠﻮدة اﻟﻤﻄﻠﻮﺑﺔ ﻟﻠﺨﻀﻮع ﻟﺪرﺟﺔ ﺣﺮارة اﻟﺠﺴﻢ ﻟﺘﺤ ﻳﺮ اﻷدوﻳﺔ اﻟﺨﺎﺻﺔ ﺑﻬﺎ‬ ‫اﻟﻤﻄﻠﻮﺑﺔ‬. The bases in many commercial products employ varied combinations of ‫ ﺑﺪة اﻟﻜﺎﻛﺎو‬، these types of materials to achieve the desired hardness under conditions ‫اﻟﺪﻫﻮن ﻣﻦ‬ ‫ﻳﺘﻢ اﻟﺤﺼﻮل ﻋ‬ ‫ﺑﺬور اﻟﻜﺎﻛﺎو اﻟﻤﺤﻤﺼﺔ‬. of shipment and storage and the desired quality of submitting to the ‫ ﻫﻮ‬،‫درﺟﺔ ﺣﺮارة اﻟﻐﺮﻓﺔ‬ ‫ﻋﺒﺎرة ﻋﻦ ﻣﺎدة ﺻﻠﺒﺔ ﺑﻴﻀﺎء‬ temperature of the body to release their medicaments. ‫ﻣﺼﻔﺮة ذات راﺋﺤﺔ ﺑﺎﻫﺘﺔ ﺗﺸﺒﻪ‬ ‫راﺋﺤﺔ اﻟﺸﻮﻛﻮﻻﺗﺔ )ﻣﺮﻛﺐ‬ ‫)ﻃﺒﻴﻌﻲ‬. Cocoa Butter, NF ‫ اﻟﻤﻜﻮن اﻟﺮﺋﻴﺴﻲ‬،ً‫ﻛﻴﻤﻴﺎﺋﻴﺎ‬ ‫ﻟ ﺑﺪة اﻟﻜﺎﻛﺎو ﻫﻮ اﻟﺪﻫﻮن اﻟﺜﻼﺛﻴﺔ‬ Are fat obtained from the roasted seed of Theobroma cacao. ‫ﻣﺸﺘﻖ ﻣﻦ ﺣﻤﺾ اﻟﺒﺎﻟﻤﺘﻴﻚ‬، At room temperature, it is a yellowish-white solid having a faint, ‫ وﺣﻤﺾ اﻷوﻟﻴﻚ‬،‫وﺣﻤﺾ دﻫﻨﻲ‬، ‫اﻟﻤﻘﺎم اﻷول ﻣﻦ أوﻟﻴﻮﺑﺎﻟﻤﻴﺘﻮ‬ - agreeable chocolate-like odor (naturally occurring comp.) ‫دﻳﺴﺘﻴ ﻳﻦ‬-‫ﺳﺘﻴ ﻳﻦ وأوﻟﻴﻮ‬ ‫ﺗﺬوب ﺑﺪة اﻟﻜﺎﻛﺎو ﻋﻨﺪ درﺟﺔ‬ Chemically, the main constituent of cocoa butter is the triglyceride ‫ درﺟﺔ ﻣﺌﻮﻳﺔ‬36 ‫ إ‬30 ‫ﺣﺮارة‬، ‫وﻫﻲ ﻗﺎﻋﺪة ﺗﺤﻤﻴﻠﻴﺔ ﻣﺜﺎﻟﻴﺔ‬، derived from palmitic acid, stearic acid, and oleic acid, primarily of oleo- ‫ﺗﺬوب ﺗﺤﺖ درﺟﺔ ﺣﺮارة اﻟﺠﺴﻢ‬ palmito-stearin and oleo-distearin ‫ﺻﻼﺑﺘﻬﺎ‬ ‫ﺑﻘﻠﻴﻞ وﺗﺤﺎﻓﻆ ﻋ‬ ‫درﺟﺔ ﺣﺮارة اﻟﻐﺮﻓﺔ اﻟﻤﻌﺘﺎدة‬. ‫ ﺑﺴﺒﺐ ﻣﺤﺘﻮاﻫﺎ ﻣﻦ‬،‫وﻣﻊ ذﻟﻚ‬ ‫ ﺗﻈﻬﺮ ﺑﺪة‬،‫اﻟﺪﻫﻮن اﻟﺜﻼﺛﻴﺔ‬ Cocoa butter melts at 30°C to 36°C, it is an ideal suppository base, ‫اﻟﻜﺎﻛﺎو ﺗﻌﺪد اﻷﺷﻜﺎل ﺑﺸﻜﻞ‬ ‫ﻋﺪة‬ ‫ أو وﺟﻮدﻫﺎ‬،‫ﻣﻠﺤﻮظ‬ melting just below body temperature and yet maintain in its solidity at ‫ﺗﻌﺪد أﺷﻜﺎل ﺑﺪة اﻟﻜﺎﻛﺎو‬ ‫أﺷﻜﺎل ﺑﻠﻮ ﻳﺔ‬ usual room temperature. ‫ﻋﻨﺪﻣﺎ ﻳﺘﻢ إذاﺑﺔ ﺑﺪة‬ However, because of its triglyceride content, cocoa butter exhibits ‫اﻟﻜﺎﻛﺎو ﺑﺈﻫﻤﺎل ﻋﻨﺪ درﺟﺔ‬ ‫ﺣﺮارة ﺗﺘﺠﺎوز ﺑﻜﺜﻴﺮ اﻟﺤﺪ‬ marked polymorphism, or existence in several crystalline forms ‫ﻟﺪرﺟﺔ اﻟﺤﺮارة‬ ‫اﻷد‬ ‫ درﺟﺔ‬35 ‫اﻟﻤﻄﻠﻮﺑﺔ )ﺣﻮا‬ ‫ﻣﺌﻮﻳﺔ( ﺛﻢ ﻳﺘﻢ ﺗﺒ ﻳﺪﻫﺎ‬ Cocoa Butter polymorphism ‫ ﻓﺈن اﻟﻨﺘﻴﺠﺔ ﻫﻲ‬،‫ﺑﺴﺮﻋﺔ‬ ‫ﺷﻜﻞ ﺑﻠﻮري ﺷﺒﻪ ﻣﺴﺘﻘﺮ‬ When cocoa butter is carelessly melted at a temperature greatly exceeding (‫ﻣﻊ ﻧﻘﻄﺔ )ﺑﻠﻮرات أﻟﻔﺎ‬ ‫اﻧﺼﻬﺎر أﻗﻞ ﺑﻜﺜﻴﺮ ﻣﻦ ﺗﻠﻚ‬ the minimum required temperature (about 35°C) and is then quickly ‫اﻷﺻﻠﻴﺔ ﺑﺪة اﻟﻜﺎﻛﺎو )ﺗﺬوب‬ ‫ درﺟﺔ‬22 ‫ﻋﻨﺪ درﺟﺔ ﺣﺮارة‬ chilled, the result is a metastable crystalline form (alpha crystals) with a ‫)ﻣﺌﻮﻳﺔ‬. melting point much lower than that of the original cocoa butter (melts at ‫ ﻷن اﻟﺸﻜﻞ‬،‫وﻣﻊ ذﻟﻚ‬ ‫اﻟﺒﻠﻮري ﻫﻮ ﺣﺎﻟﺔ ﺷﺒﻪ‬ 22°C). ‫ ﻫﻨﺎك‬،‫ﻣﺴﺘﻘﺮة‬ ‫ﺷﻜﻞ ﺑﻴﺘﺎ‬ ‫اﻧﺘﻘﺎل ﺑﻄﻲء إ‬ However, because the crystalline form is a metastable condition, there is ‫اﻷﻛﺜﺮ اﺳﺘﻘﺮا ًرا ﻣﻦ اﻟﺒﻠﻮرات‬ a slow transition to the more stable beta form of crystals having the greater ‫اﻟﺘﻲ ﺗﺘﻤﺘﻊ ﺑﺜﺒﺎت أﻛﺒﺮ‬ ‫ وﻗﺪ‬. ‫وﻧﻘﻄﺔ اﻧﺼﻬﺎر أﻋ‬ stability and a higher melting point. This transition may require several ‫ﻳﺘﻄﻠﺐ ﻫﺬا اﻟﺘﺤﻮل ﻋﺪة أﻳﺎم‬. ‫ﻳﺠﺐ ﺗﺬوﻳﺐ ﺑﺪة اﻟﻜﺎﻛﺎو‬ days. ‫ﺑﺒﻂء وﺑﺸﻜﻞ ﻣﺘﺴﺎ ٍو‬، ‫وﻳﻔﻀﻞ أن ﻳﺘﻢ ذﻟﻚ ﻓﻮق‬ Cocoa butter must be slowly and evenly melted, preferably over a bath of ‫ﺣﻤﺎم ﻣﻦ اﻟﻤﺎء اﻟﺪا‬، warm water, to avoid formation of the unstable crystalline form and ensure ‫ﻟﺘﺠﻨﺐ ﺗﻜﻮﻳﻦ اﻟﺸﻜﻞ‬ ‫اﻟﺒﻠﻮري ﻏﻴﺮ اﻟﻤﺴﺘﻘﺮ‬ retention in the liquid of the more stable beta crystals that will constitute ‫اﻟﺴﺎﺋﻞ‬ ‫وﺿﻤﺎن اﻻﺣﺘﻔﺎظ‬ ‫ﺑﺒﻠﻮرات ﺑﻴﺘﺎ اﻷﻛﺜﺮ ﺛﺒﺎﺗًﺎ‬ nuclei upon which the congealing may occur during chilling of the liquid. ‫واﻟﺘﻲ ﺳﺘﺸﻜﻞ اﻟﻨﻮى اﻟﺘﻲ‬ Disadvantages of theobroma oil: ‫ﻗﺪ ﻳﺤﺪث ﻋﻠﻴﻬﺎ اﻟﺘﺠﻤﺪ أﺛﻨﺎء‬ ‫ ﻣﻦ اﻟﺴﺎﺋﻞ‬.‫ اﻟﺘﺒ ﻳﺪ‬. 1. Polymorphism: when melt &solidify it form different crystal form depending on the temperature. if its melt at low temp, not exceed 36 °C it will form β-polymorph form which is stable form, if melted suddenly and quickly at high temperature then freezing or cooling it will form unstable γ form that melt at 15 °C. ‫ ﻋﻴﻮب ﻳﺖ اﻟﺜﻴﻮﺑﺮوﻣﺎ‬: 1. ‫ إذا اﻧﺼﻬﺮ ﻋﻨﺪ درﺟﺔ‬.‫ ﻋﻨﺪ ذوﺑﺎﻧﻬﺎ وﺗﺼﻠﺒﻬﺎ ﺗﺸﻜﻞ أﺷﻜﺎﻻ ً ﺑﻠﻮ ﻳﺔ ﻣﺨﺘﻠﻔﺔ ﺣﺴﺐ درﺟﺔ اﻟﺤﺮارة‬:‫ﺗﻌﺪد اﻷﺷﻜﺎل‬ ‫ إذا ذاب‬،‫ درﺟﺔ ﻣﺌﻮﻳﺔ ﻓﺈﻧﻪ ﺳﻴﺸﻜﻞ ﺷﻜﻞ ﺑﻴﺘﺎ ﻣﺘﻌﺪد اﻷﺷﻜﺎل وﻫﻮ ﺷﻜﻞ ﻣﺴﺘﻘﺮ‬36 ‫ﺣﺮارة ﻣﻨﺨﻔﻀﺔ ﻻ ﺗﺘﺠﺎوز‬ 15 ‫ﻓﺠﺄة وﺑﺴﺮﻋﺔ ﻋﻨﺪ درﺟﺔ ﺣﺮارة ﻋﺎﻟﻴﺔ ﻓﺈن ﺗﺠﻤﻴﺪه أو ﺗﺒ ﻳﺪه ﺳﻴﺸﻜﻞ ﺷﻜﻞ ﺟﺎﻣﺎ ﻏﻴﺮ ﻣﺴﺘﻘﺮ ﻳﺬوب ﻋﻨﺪ‬ 32 ‫درﺟﺔ ﻣﺌﻮﻳﺔ‬.  2. ‫ ﻳﻤﻜﻦ ﺣﻞ‬،‫اﻻﻟﺘﺰام ﺑﺎﻟﻘﺎﻟﺐ‬ ‫ذﻟﻚ ﺑﺎﺳﺘﺨﺪام ﻣﺎدة اﻟﺘﺸﺤﻴﻢ‬ ‫ ﻏﻴﺮ ﻗﺎﺑﻞ ﻟﻼﻣﺘﺰاج ﻣﻊ اﻟﻘﺎﻋﺪة‬. 3. ‫ﻧﻘﻄﺔ اﻧﺼﻬﺎر ﻣﻨﺨﻔﻀﺔ وﻳﻤﻜﻦ‬ 2. Adherence to the mold, this can be solved by using lubricant agent that ‫ﺣﻞ ذﻟﻚ ﻋﻦ ﻃ ﻳﻖ إﺿﺎﻓﺔ اﻷدوﻳﺔ‬ ‫وإﺿﺎﻓﺔ اﻟﻨﺤﻞ اﻷﺑﻴﺾ‬ is immiscible with the base. ‫اﻟﺸﻤﻊ‬. 4. ‫اﻧﺨﻔﺎض اﻣﺘﺼﺎص اﻟﻤﺎء‬ 3. Low m.p, this can be solved by added medication, adding white bees (‫ ﺿﻌﻒ اﻟﻘﺪرة ﻋ اﻣﺘﺼﺎص‬wax. ‫ وﻫﺬا ﻳﻤﻜﻦ أن ﻳﻜﻮن‬،(‫اﻟﻤﺎء‬ ‫ ﻳﺘﻢ ﺣﻠﻬﺎ ﻋﻦ ﻃ ﻳﻖ إﺿﺎﻓﺔ ﻋﺎﻣﻞ‬4. Low water absorbance (poor water-absorbing capacity), this can be ‫ﻧﺸﻂ اﻟﺴﻄﺢ‬. 5. ‫ﻣﺸﻜﻠﺔ اﻟﺜﺒﺎت )اﻟﺘﺪﻫﻮر‬ solved by adding surface-active agent. ‫ اﻟﻜﻴﻤﻴﺎ‬،‫ اﻟﺒﻄﻲء أﺛﻨﺎء اﻟﺘﺨ ﻳﻦ‬5. Stability problem (slow deterioration during storage, chemical ‫ )ﻋﺪم اﻻﺳﺘﻘﺮار‬. 6. ‫ﻏﻴﺮ ﻣﻨﺎﺳﺐ ﻟﻠﺒﻠﺪان اﻟﺪاﻓﺌﺔ‬. instability). ‫اﻟﻘﻮاﻋﺪ اﻟﺪﻫﻨﻴﺔ اﻷﺧﺮى ﺗﺸﻤﻞ اﻟﻘﻮاﻋﺪ اﻷﺧﺮى ﻫﺬه اﻟﻔﺌﺔ اﻟﻤﻨﺘﺠﺎت اﻟﺘﺠﺎ ﻳﺔ ﻣﺜﻞ‬: 7. ‫اﻟﺘﻜﻠﻔﺔ اﻟﻌﺎﻟﻴﺔ ﻧﺴﺒﻴﺎ‬. 6. Not suitable for warm countries. ‫ﻗﺎﻋﺪة دﻫﻨﻴﺔ )اﻟﺪﻫﻮن اﻟﺜﻼﺛﻴﺔ ﻣﻦ ﻳﻮت اﻟﻨﺨﻴﻞ وﻧﻮاة اﻟﻨﺨﻴﻞ وﺟﻮز اﻟﻬﻨﺪ ﻣﻊ أﺣﺎدي ﺳﺘﻴﺎرات اﻟﻐﻠﻴﺴﻴ ﻳﻞ اﻟﺬا اﻻﺳﺘﺤﻼب وﺳﺘﻴﺮات‬ ‫)اﻟﺒﻮ أوﻛﺴﻴﻞ‬. 7. Relatively high cost. (‫ﻗﻮاﻋﺪ وﻳﻜﻮ )اﻟﺪﻫﻮن اﻟﺜﻼﺛﻴﺔ اﻟﻤﺸﺘﻘﺔ ﻣﻦ ﻳﺖ ﺟﻮز اﻟﻬﻨﺪ‬ ‫ ﻣﻊ أﺟﺰاء ﻣﺘﻨﻮﻋﺔ ﻣﻦ اﻟﺠﻠﺴ ﻳﺪات‬18 ‫اﻟﻜ ﺑﻮن‬-12 ‫ﻗﻮاﻋﺪ وﻳﺘﺒﺴﻮل )ﺛﻼ اﻟﺠﻠﻴﺴ ﻳﺪات ﻣﻦ اﻷﺣﻤﺎض اﻟﺪﻫﻨﻴﺔ اﻟﻤﺸﺒﻌﺔ اﻟﻜ ﺑﻮن‬ Other fatty bases ‫)اﻟﺠﺰﺋﻴﺔ اﻟﻤﻘﺎﺑﻠﺔ‬ Other bases in this category include commercial products such as: Fattibase (triglycerides from palm, palm kernel, and coconut oils with self-emulsifying glyceryl monostearate and polyoxyl stearate), Wecobee bases (triglycerides derived from coconut oil) Witepsol bases (triglycerides of saturated fatty acids C12-C18 with varied portions of the corresponding partial glycerides). ‫ﻳﻤﻜﻦ ﺗﺤﻀﻴﺮ ﺗﺤﺎﻣﻴﻞ‬ Water-Soluble and Water-Miscible Bases ‫اﻟﺠﻴﻼﺗﻴﻦ اﻟﺠﻠﺴ ﻳﻦ ﻋﻦ ﻃ ﻳﻖ‬ 20) ‫ إذاﺑﺔ اﻟﺠﻴﻼﺗﻴﻦ اﻟﺤﺒﻴﺒﻲ‬The main members of this group are glycerinated gelatin and polyethylene %) (%70) ‫اﻟﺠﻠﺴ ﻳﻦ‬ ‫وإﺿﺎﻓﺔ اﻟﻤﺎء أو ﻣﺤﻠﻮل أو‬ glycols. ‫اﻟﻘﻮاﻋﺪ اﻟﻘﺎﺑﻠﺔ ﻟﻠﺬوﺑﺎن اﻟﻤﺎء واﻟﻘﻮاﻋﺪ اﻟﻘﺎﺑﻠﺔ ﻟﻼﻣﺘﺰاج ﺑﺎﻟﻤﺎء اﻷﻋﻀﺎء اﻟﺮﺋﻴﺴﻴﻮن ﻫﺬه اﻟﻤﺠﻤﻮﻋﺔ ﻫﻢ اﻟﺠﻴﻼﺗﻴﻦ اﻟﻐﻠﻴﺴﻴ ﻳﻦ واﻟﺒﻮ إﻳﺜﻴﻠﻴﻦ ﺟﻼﻳﻜﻮل‬. (%10) ‫ﻣﻌﻠﻖ اﻟﺪواء‬. Glycerinated gelatin suppositories may be prepared by dissolving ‫ُﺗﺴﺘﺨﺪم ﻗﺎﻋﺪة اﻟﺠﻴﻼﺗﻴﻦ‬ ‫ اﻟﻐﻠﻴﺴﻴ ﻳﻨﻴﺔ أﻏﻠﺐ اﻷﺣﻴﺎن‬granular gelatin (20%) in glycerin (70%) and adding water or a solution or ‫ ﺗﺤﻀﻴﺮ اﻟﺘﺤﺎﻣﻴﻞ اﻟﻤﻬﺒﻠﻴﺔ‬، ً ‫ﻋﺎدة ﻣﺎ ﻳﻜﻮن اﻟﺘﺄﺛﻴﺮ‬ ‫ واﻟﺘﻲ‬suspension of the medication (10%). ‫اﻟﻤﻮﺿﻌﻲ اﻟﻤﻄﻮل ﻟﻠﻌﺎﻣﻞ‬ ‫اﻟﻄﺒﻲ ﻣﺮﻏﻮﺑًﺎ ﻓﻴﻪ‬. A glycerinated gelatin base is most frequently used in preparation of ‫ ﺗﻜﻮن ﻗﺎﻋﺪة اﻟﺠﻴﻼﺗﻴﻦ‬vaginal suppositories, with which prolonged local action of the medicinal ‫اﻟﻐﻠﻴﺴﻴ ﻳﻦ أﺑﻄﺄ اﻟﺘﻠﻴﻴﻦ‬ ‫ واﻻﺧﺘﻼط ﻣﻊ اﻟﺴﻮاﺋﻞ‬agent is usually desired. The glycerinated gelatin base is slower to soften ‫اﻟﻔﺴﻴﻮﻟﻮﺟﻴﺔ ﻣﻘﺎرﻧﺔ ﺑ ﺑﺪة‬ ً ‫إﻃﻼﻗﺎ‬ ‫ وﺑﺎﻟﺘﺎ ﺗﻮﻓﺮ‬،‫اﻟﻜﺎﻛﺎو‬ and mix with the physiologic fluids than is cocoa butter and therefore ‫أﺑﻄﺄ‬. provides a slower release. Glycerinated gelatin suppositories disadvantages ‫ﻋﻴﻮب ﺗﺤﺎﻣﻴﻞ اﻟﺠﻴﻼﺗﻴﻦ‬ ‫اﻟﺠﻠﺴ ﻳﻦ‬ A- Because glycerinated gelatin-based suppositories have a tendency to ‫ ﻷن اﻟﺘﺤﺎﻣﻴﻞ ذات اﻷﺳﺎس‬-‫أ‬ absorb moisture as a result of the hygroscopic nature of glycerin, ‫اﻟﺠﻴﻼﺗﻴﻨﻲ اﻟﻐﻠﻴﺴﻴ ﻳﻨﻲ ﺗﻤﻴﻞ‬ ‫إ اﻣﺘﺼﺎص اﻟﺮﻃﻮﺑﺔ ﻧﺘﻴﺠﺔ‬ they must be protected from atmospheric moisture to maintain their ‫ﻃﺒﻴﻌﺔ اﻟﺠﻠﺴ ﻳﻦ اﻻﺳﺘﺮﻃﺎﺑﻴﺔ‬، ‫ﻓﻴﺠﺐ ﺣﻤﺎﻳﺘﻬﺎ ﻣﻦ اﻟﺮﻃﻮﺑﺔ‬ shape and consistency. ‫اﻟﺠﻮﻳﺔ ﻟﻠﺤﻔﺎظ ﻋ ﺷﻜﻠﻬﺎ‬ B- Due to hygroscopic nature, they may have a dehydrating effect and ‫وﺗﻤﺎﺳﻜﻬﺎ‬. ‫ ﺑﺴﺒﺐ ﻃﺒﻴﻌﺘﻬﺎ‬-‫ب‬ irritate the tissues upon insertion. The water in the formula for the ‫ ﻗﺪ ﻳﻜﻮن ﻟﻬﺎ ﺗﺄﺛﻴﺮ‬،‫اﻻﺳﺘﺮﻃﺎﺑﻴﺔ‬ ‫ﺗﺠﻔﻴﻒ وﺗﻬﻴﺞ اﻷﻧﺴﺠﺔ ﻋﻨﺪ‬ suppositories minimizes this action; however, if necessary, the ‫إدﺧﺎﻟﻬﺎ‬. ‫اﻟﻤﺎء اﻟﻤﻮﺟﻮد ﺗﺮﻛﻴﺒﺔ‬ suppositories may be moistened with water prior to insertion to ‫اﻟﺘﺤﺎﻣﻴﻞ ﻳﻘﻠﻞ ﻣﻦ ﻫﺬا اﻹﺟﺮاء‬. reduce the initial tendency of the base to draw water from the ‫ ﻳﻤﻜﻦ‬،‫ إذا ﻟﺰم اﻷﻣﺮ‬،‫وﻣﻊ ذﻟﻚ‬ ‫ﺗﺮﻃﻴﺐ اﻟﺘﺤﺎﻣﻴﻞ ﺑﺎﻟﻤﺎء ﻗﺒﻞ‬ mucous membranes and irritate the tissues. ‫اﻹدﺧﺎل ﻟﺘﻘﻠﻴﻞ اﻟﻤﻴﻞ اﻷو‬ ‫ﻟﻠﻘﺎﻋﺪة ﻟﺴﺤﺐ اﻟﻤﺎء ﻣﻦ‬ ‫اﻷﻏﺸﻴﺔ اﻟﻤﺨﺎﻃﻴﺔ وﺗﻬﻴﺞ‬ 33 ‫اﻷﻧﺴﺠﺔ‬.  ‫إﻳﺜﻴﻠﻴﻦ ﺟﻼﻳﻜﻮل‬ ‫اﻟﺒﻮ‬ ‫إﻳﺜﻴﻠﻴﻦ ﺟﻼﻳﻜﻮل ﻋﺒﺎرة ﻋﻦ ﺑﻮﻟﻴﻤﺮات ﻣﻦ أﻛﺴﻴﺪ اﻹﻳﺜﻴﻠﻴﻦ واﻟﻤﺎء ﻣﺤﻀﺮة ﺑﺄﻃﻮال ﺳﻼﺳﻞ ﻣﺨﺘﻠﻔﺔ وأوزان ﺟ ﻳﺌﻴﺔ وﺣﺎﻻت‬ ‫اﻟﺒﻮ‬ 8000‫ و‬،6000 ،4000 ،3350 ،1540 ،1500 ،1000 ،600 ،400 ،300 ‫إﻳﺜﻴﻠﻴﻦ ﺟﻼﻳﻜﻮل‬ ‫اﺳﺘﺨﺪاﻣﺎ ﻫﻮ اﻟﺒﻮ‬ ً ‫ واﻷﻛﺜﺮ‬،‫ﻓﻴ ﻳﺎﺋﻴﺔ‬. ‫إﻳﺜﻴﻠﻴﻦ‬ ‫ ﻳﻢﻛﻦ دﻣﺞ ﺗﻮﻟﻴﻔﺎت ﻣﺨﺘﻠﻔﺔ ﻣﻦ اﻟﺒﻮ‬.‫ﻣﺘﻮﺳﻂ اﻟﻮزن اﻟﺠ ﻳﺌﻲ ﻟﻜﻞ ﻣﻦ اﻟﺒﻮﻟﻴﻤﺮات‬ ‫وﺗﺸﻴﺮ اﻟﺘﺴﻤﻴﺎت اﻟﺮﻗﻤﻴﺔ إ‬ Polyethylene glycols (PEG) ‫ ﺑﺎﺳﺘﺨﺪام ﻧﻮﻋﻴﻦ أو أﻛﺜﺮ ﻣﻦ اﻷﻧﻮاع اﻟﻤﺨﺘﻠﻔﺔ ﻟﺘﺤﻘﻴﻖ ﻗﺎﻋﺪة ﺗﺤﻤﻴﻠﻴﺔ ﺑﺎﻟﻘﻮام واﻟﺨﺼﺎﺋﺺ اﻟﻤﻄﻠﻮﺑﺔ‬،‫ﺟﻼﻳﻜﻮل ﻋﻦ ﻃ ﻳﻖ اﻟﺪﻣﺞ‬. Polyethylene glycols are polymers of ethylene oxide and water prepared to various chain lengths, molecular weights, and physical states, the most commonly used being polyethylene glycol 300, 400, 600, 1,000, 1,500, 1,540, 3,350, 4,000, 6,000, and 8,000. The numeric designations refer to the average molecular weight of each of the polymers. Various combinations of these polyethylene glycols may be combined by fusion, using two or more of the various types to achieve a suppository base of the desired consistency and characteristics. PEG PEG Melting range Melting range 300 - 15°C 3350 54°C -58°C 400 4°C -8°C 4600 57°C -61°C 600 20°C -25°C 6000 56°C -63°C 1000 37°C -40°C 8000 60°C -63°C 1450 43°C -46°C ‫إﻳﺜﻴﻠﻴﻦ ﺟﻼﻳﻜﻮل‬ ‫ﺗﺤﺎﻣﻴﻞ اﻟﺒﻮ‬ ‫درﺟﺔ ﺣﺮارة‬ ‫ﻫﺬه ﻻ ﺗﺬوب‬ ‫اﻟﺠﺴﻢ ﺑﻞ ﺗﺬوب ﺑﺒﻂء‬ Polyethylene glycol suppositories ‫ ﻟﻴﺲ‬،‫ وﻟﺬﻟﻚ‬.‫ﺳﻮاﺋﻞ اﻟﺠﺴﻢ‬ ‫ﻣﻦ اﻟﻀﺮوري ﺻﻴﺎﻏﺔ اﻟﻘﺎﻋﺪة‬ PEG suppositories do not melt at body temperature but rather dissolve ‫ﻟﺘﺬوب درﺟﺔ ﺣﺮارة اﻟﺠﺴﻢ‬. ‫ﻣﻦ اﻟﻤﻤﻜﻦ ﺗﺤﻀﻴﺮ ﺗﺤﺎﻣﻴﻞ‬ slowly in the body's fluids. Therefore, the base need not be formulated to ‫ﻣﻦ ﻣﺨﺎﻟﻴﻂ اﻟﺒﻮ إﻳﺜﻴﻠﻴﻦ‬ melt at body temperature. ‫ﺟﻼﻳﻜﻮل ذات درﺟﺎت اﻧﺼﻬﺎر‬ ‫أﻋ ﺑﻜﺜﻴﺮ ﻣﻦ درﺟﺔ ﺣﺮارة‬ It is possible to prepare suppositories from PEG mixtures having melting ‫اﻟﺠﺴﻢ‬. ‫ﺗﺴﻤﺢ ﻫﺬه اﻟﺨﺎﺻﻴﺔ ﺑﺈﻃﻼق‬ points considerably higher than body temperature. ‫اﻟﺪواء ﺑﺸﻜﻞ أﺑﻄﺄ ﻣﻦ اﻟﻘﺎﻋﺪة‬ ‫ﺑﻤﺠﺮد إدﺧﺎل اﻟﺘﺤﻤﻴﻠﺔ‬، This property permits a slower release of the medication from the base once ‫وﺗﺴﻤﺢ ﺑﺘﺨ ﻳﻦ ﻫﺬه اﻟﺘﺤﺎﻣﻴﻞ‬ the suppository has been inserted, and permits convenient storage of these ‫ﺑﺸﻜﻞ ﻣﻨﺎﺳﺐ دون اﻟﺤﺎﺟﺔ إ‬ ‫اﻟﺘﺒ ﻳﺪ ودون ﺧﻄﺮ ﺗﻠﻴﻴﻨﻬﺎ‬ suppositories without need for refrigeration and without danger of their ‫ﺑﺸﻜﻞ ﻣﻔﺮط اﻟﻄﻘﺲ اﻟﺪا‬. softening excessively in warm weather. Further, their solid nature permits slow insertion without fear that they will melt in the fingertips (as cocoa butter suppositories sometimes do). Because they do not melt at body temperature but mix with mucous secretions upon dissolution, PEG-based suppositories do not leak from the orifice, as many cocoa butter-based suppositories. PEG suppositories that do not contain at least 20% water should be dipped in water just before use to avoid irritation of the mucous membranes after insertion. This procedure prevents moisture being drawn from the tissues ‫ ﻓﺈن ﻃﺒﻴﻌﺘﻬﺎ اﻟﺼﻠﺒﺔ ﺗﺴﻤﺢ ﺑﺈدﺧﺎﻟﻬﺎ ﺑﺸﻜﻞ ﺑﻄﻲء دون اﻟﺨﻮف ﻣﻦ ذوﺑﺎﻧﻬﺎ أﻃﺮاف‬،‫ﻋﻼوة ﻋ ذﻟﻚ‬ after insertion and the stinging sensation (ً‫اﻷﺻﺎﺑﻊ )ﻛﻤﺎ ﺗﻔﻌﻞ ﺗﺤﺎﻣﻴﻞ ﺑﺪة اﻟﻜﺎﻛﺎو أﺣﻴﺎﻧﺎ‬. ‫ ﻓﺈن اﻟﺘﺤﺎﻣﻴﻞ‬،‫درﺟﺔ ﺣﺮارة اﻟﺠﺴﻢ وﻟﻜﻨﻬﺎ ﺗﺨﺘﻠﻂ ﻣﻊ اﻹﻓﺮازات اﻟﻤﺨﺎﻃﻴﺔ ﻋﻨﺪ اﻟﺬوﺑﺎن‬ ‫ﻷﻧﻬﺎ ﻻ ﺗﺬوب‬ 34 ‫ ﻛﻤﺎ ﻫﻮ اﻟﺤﺎل ﻣﻊ اﻟﻌﺪﻳﺪ ﻣﻦ اﻟﺘﺤﺎﻣﻴﻞ اﻟﺘﻲ‬،‫إﻳﺜﻴﻠﻴﻦ ﺟﻼﻳﻜﻮل ﻻ ﺗﺘﺴﺮب ﻣﻦ اﻟﻔﺘﺤﺔ‬ ‫اﻟﻤﺼﻨﻮﻋﺔ ﻣﻦ اﻟﺒﻮ‬ ‫ﺑﺪة اﻟﻜﺎﻛﺎو‬ ‫ﺗﺤﺘﻮي ﻋ‬. ‫اﻟﻤﺎء ﻗﺒﻞ‬ ‫اﻷﻗﻞ‬ ‫ ﻣﺎء ﻋ‬%20 ‫إﻳﺜﻴﻠﻴﻦ ﺟﻼﻳﻜﻮل اﻟﺘﻲ ﻻ ﺗﺤﺘﻮي ﻋ‬ ‫ﻳﺠﺐ ﻏﻤﺲ ﺗﺤﺎﻣﻴﻞ اﻟﺒﻮ‬ ‫ ﻳﻤﻨﻊ ﻫﺬا اﻹﺟﺮاء ﺳﺤﺐ اﻟﺮﻃﻮﺑﺔ ﻣﻦ‬.‫اﻻﺳﺘﺨﺪام ﻣﺒﺎﺷﺮة ﻟﺘﺠﻨﺐ ﺗﻬﻴﺞ اﻷﻏﺸﻴﺔ اﻟﻤﺨﺎﻃﻴﺔ ﺑﻌﺪ إدﺧﺎﻟﻬﺎ‬ ‫اﻷﻧﺴﺠﺔ ﺑﻌﺪ إدﺧﺎﻟﻬﺎ واﻟﺸﻌﻮر ﺑﺎﻟﻮﺧﺰ‬  ‫ﻗﻮاﻋﺪ ﻣﺘﻨﻮﻋﺔ‬ ‫ وﻗﺪ ﺗﻜﻮن‬.‫اﻟﻤﺎء أو ﻗﺎﺑﻠﺔ ﻟﻼﻣﺘﺰاج ﺑﺎﻟﻤﺎء‬ ‫ﻣﺠﻤﻮﻋﺔ اﻟﻘﻮاﻋﺪ اﻟﻤﺘﻨﻮﻋﺔ ﻋﺒﺎرة ﻋﻦ ﻣﺨﺎﻟﻴﻂ ﻣﻦ ﻣﻮاد ﻳﺘﻴﺔ وﻣﻮاد ﻗﺎﺑﻠﺔ ﻟﻠﺬوﺑﺎن‬ ‫ﻫﺬه اﻟﻤﻮاد ﻣﺨﺎﻟﻴﻂ ﻛﻴﻤﻴﺎﺋﻴﺔ أو ﻓﻴ ﻳﺎﺋﻴﺔ‬. 1. 40 ‫ﺑﻮﻟﻴﻮﻛﺴﻴﻞ‬ Miscellaneous Bases ‫ وﻫﻮ ﻋﺎﻣﻞ‬،‫ﺳﺘﻴﺮات‬ The miscellaneous group of bases are mixtures of oleaginous and water- ‫ذو ﻧﺸﺎط ﺳﻄﺤﻲ‬ ‫ﻋﺪد ﻣﻦ‬ ‫ُﻳﺴﺘﺨﺪم‬ soluble or water-miscible materials. These materials may be chemical or ‫ﻗﻮاﻋﺪ اﻟﺘﺤﺎﻣﻴﻞ‬ ‫اﻟﺘﺠﺎ ﻳﺔ‬. physical mixtures. 40 ‫أوﻛﺴﻴﻞ‬ ‫ﺳﺘﻴﺮات ﻋﺒﺎرة ﻋﻦ‬ ‫ﺑﻮ‬ 1. Polyoxyl 40 stearate, a surface-active agent that is employed in a number ‫ﺧﻠﻴﻂ ﻣﻦ إﺳﺘﺮات‬ of commercial suppository bases. Polyoxyl 40 stearate is a mixture of the ‫أﺣﺎدي ﺳﺘﻴﺎرات‬ ‫ودﻳﺴﺘﻴﺮات ﻣﻦ‬ monostearate and distearate esters of mixed polyoxyethylene diols and the ‫أوﻛﺴﻲ‬ ‫ﺛﻨﺎﺋﻴ?