{"id":8935,"date":"2026-08-11T10:29:57","date_gmt":"2026-08-11T10:29:57","guid":{"rendered":"https:\/\/majistraleczacilari.org.tr\/?post_type=docs&p=3170"},"modified":"2026-08-21T12:33:36","modified_gmt":"2026-08-21T12:33:36","password":"","slug":"diazepam-rectal-gel","status":"publish","type":"docs","link":"https:\/\/majistraleczacilari.org.tr\/en\/dokumanlar\/ovule-suppository-rectal-gel\/diazepam-rectal-gel\/","title":{"rendered":"Diazepam Rectal Gel"},"content":{"rendered":"
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\"\"Dear Colleagues, I would like to draw attention once again to the importance of magistral compounding in delivering medications experiencing shortages and those defined as orphan drugs to patients.<\/p>\n

Diazepam is a psychotherapeutic substance belonging to the 1,4-benzodiazepine class that suppresses tension, agitation, and anxiety, while also possessing sedative and hypnotic properties. At higher doses, it also exhibits muscle relaxant and anticonvulsant properties. Highly effective in resolving epileptic seizures and preventing febrile convulsions, this medication is occasionally among the products experiencing shortages.<\/p>\n

It is possible to prepare this medication, which is included in American formulas (Allen\u2019s Compounded Formulations), in pharmacy laboratories. Diazepam rectal gel is used when diazepam needs to be administered via an alternative route. It can be used in nursing homes and care facilities when oral or parenteral routes are not suitable.<\/p>\n

\n

Drug dosage;<\/p>\n

Ages 2-5: 0.5mg \/ kg.<\/p>\n

Ages 6-11: 0.3 mg \/ kg.<\/p>\n

Ages 12 and older: 0.2 mg \/ kg.<\/p>\n

However, to reduce possible side effects, the dosage should be adjusted for elderly and debilitated patients. If necessary, a second dose may be administered 4-12 hours after the first dose. Not recommended during pregnancy.<\/p>\n

Formula:<\/strong><\/p>\n

Rp.<\/strong><\/p>\n

1-mg\/ml Diazepam Rectal Gel<\/strong><\/p>\n

Diazepam                                100 mg<\/p>\n

Methylcellulose 1500 mPa (cps)   2.5 g<\/p>\n

Methylparaben                         100 mg<\/p>\n

Glycerin                                      5 g<\/p>\n

Purified Water                      qs 100 ml<\/p>\n

Substances included in the formula:<\/strong><\/p>\n

Diazepam- Methyldiazepinone- Diazepamum [INN; IP3]- Ro-5-2807 [Roche, USA]:<\/strong><\/p>\n

Diazepam is a white or almost white to yellow, odorless or almost odorless, crystalline powder. According to the British Pharmacopoeia (BP), its solubilities are: very slightly soluble in water, soluble in alcohol, freely soluble in chloroform. According to the United States Pharmacopeia (USP), its solubilities are: 1:333 in water, 1:16 in alcohol, 1:2 in chloroform, and 1:39 in ether. According to the BP, the pH of its injectable solution ranges from 6.2 to 7.0, and according to the USP, from 6.2 to 6.9. According to the BP, the pH of its oral solution is between 4.7 and 5.4. Diazepam is a long-acting benzodiazepine derivative administered via oral and parenteral routes. Rectally administered diazepam is well absorbed, with a bioavailability of approximately 90%. Diazepam is widely distributed in the body. Its levels in the central nervous system are similar to those in plasma. Diazepam crosses the placenta and passes significantly into breast milk.<\/p>\n

Methylcellulose- Cellulose methyl ether- Cologel- Methyl ether cellulose:<\/strong><\/p>\n

Methylcellulose is a long-chain substituted cellulose derivative. It occurs as a white or yellowish-white, hygroscopic, odorless, fibrous powder or granules. It is practically insoluble in hot water, anhydrous alcohol, acetone, chloroform, ether, and toluene; it dissolves in cold water forming a colloidal dispersion. It also dissolves in glacial acetic acid and in equal volumes of an alcohol-chloroform mixture. The pH of its 1% aqueous solution is between 5.5 and 8.0. Methylcellulose solutions are stable at room temperature between pH 3 and 11. However, below pH 3, its viscosity decreases. When its solutions are heated, the viscosity decreases until gelation occurs. Methylcellulose has been reported to be incompatible with chlorocresol, mercuric chloride, resorcinol, tannic acid, silver nitrate, cetylpyridinium chloride, para-aminobenzoic acid, hydroxybenzoates, and phenol. The addition of high amounts of electrolytes to methylcellulose solutions causes an increase in the viscosity of the methylcellulose mucilage. However, at very high electrolyte concentrations, methylcellulose may precipitate completely.<\/p>\n

Methylcellulose is an excipient frequently used in oral and topical pharmaceutical preparations. In tablet formulations, low or medium viscosity grades are used as binders, and high viscosity grades are used as disintegrants. In sustained-release tablet formulations, it functions as a matrix material, a coating agent to mask the unpleasant taste of core tablets, or to protect core tablets from moisture prior to the sugar-coating process. Additionally, it is useful as a viscosity-increasing agent in suspension formulations and as an emulsifier in oil-containing formulations. In topically applied cream and gel type formulations, its high-viscosity grades are utilized as thickening agents.<\/p>\n

Methylparaben- Methyl hydroxybenzoate- Nipagin M- Methyl parahydroxybenzoate:<\/strong><\/p>\n

Methylparaben is widely used as an antimicrobial preservative in pharmaceutical formulations, cosmetic products, and foods. It is used alone or in combination with other parabens or other antimicrobial agents. It is the most frequently used preservative, especially in cosmetic products. Its antimicrobial activity decreases significantly in the presence of nonionic surfactants. The estimated acceptable daily maximum intake for methyl, ethyl, and propylparaben is reported as 10 mg per kg of body weight. Methylparaben occurs as colorless crystals or a white crystalline powder, odorless or with a faint characteristic odor. It is easily soluble in ethanol, methanol, ether, and propylene glycol; sparingly soluble in water; practically insoluble in liquid paraffin.<\/p>\n

Glycerin 98%- Glycerol [ASK; BP; DCF; FP; INN; P.Cx.79; Ph.Eur.]- Glycerolum anhydricum- Glycerol [ASK; BP; DCF; FP; INN; P.Cx.79; Ph.Eur.]- Wasserfreies Glycerol:<\/strong><\/p>\n

Glycerin is an excipient widely used for various purposes in pharmaceutical formulations and cosmetic products. It is used in oral, otic, ophthalmic, topical, and parenteral pharmaceutical formulations. While it is used for its moisturizing and emollient effects in topical pharmaceutical formulations, it mainly serves as a solvent in parenteral formulations. In oral formulations, it is used as an antimicrobial preservative, sweetening agent, and viscosity-increasing agent. It is a plasticizer for gelatin in soft gelatin capsules. It is also included in the composition of gelatin suppositories. Glycerin is a clear, colorless, sweet, hygroscopic, viscous liquid. It is miscible with water and alcohol; sparingly soluble in acetone; practically insoluble in chloroform, ether, fixed and volatile oils. Its aqueous solutions are neutral to litmus. According to the United States Pharmacopeia (USP), the pH of Glycerin Oral Solution, USP is between 5.5 and 7.5. Glycerin acquires explosive properties when combined with strong oxidizing agents such as potassium permanganate. Such mixtures must be strictly avoided. In the presence of light, it turns black when in contact with zinc oxide or basic bismuth nitrate. When glycerin contaminated with iron is used, mixtures containing phenol, salicylate, and tannin darken in color. It complexes with boric acid to form glyceroboric acid. The acidity of this compound is higher than that of boric acid.<\/p>\n

Purified Water- Purified water- Distilled water- Aqua purificata [IP3]- Gereinigtes Wasser [ASK]:<\/strong><\/p>\n

Distilled water is high-purity water prepared by the distillation of potable water and used as a solvent or vehicle in many pharmaceutical formulations. It is a clear and colorless liquid with no characteristic odor or taste. In pharmacy, water should be understood as distilled water. The shelf life of distilled water is limited. In any case, it must be boiled before use. Because additional specifications are required for water to be used in parenteral preparations, water for injection should be used for this purpose. Additionally, deionized water may also be used instead of distilled water in pharmaceutical preparations where its use is permitted, as it is cheaper and more easily obtained.<\/p>\n

Preparation of the formula:<\/strong><\/p>\n

The amount of each substance required for the total preparation is calculated. To obtain the equivalent of 100 mg of diazepam, the active substance is pulverized from a sufficient number of diazepam capsules. Methylcellulose and methylparaben are weighed. The calculated amounts of diazepam, methylcellulose, and methylparaben are thoroughly mixed. Glycerin is added to the mixture and triturated in a mortar until a homogeneous mixture is obtained. First, 10 ml of purified water is added and, after mixing thoroughly, the remainder of the water is added slowly to complete the formulation. If a more or less viscous gel is desired, the amount of methylcellulose in this formula can easily be modified. If suitable packaging cannot be obtained, it can be packaged in pre-measured volumes in plastic syringes. The expiration date is 6 months. Store at room temperature (15 to 30\u00baC), protected from light and moisture, and out of reach of children.<\/p>\n

Wishing you a good week\u2026<\/p>\n

References:<\/p>\n

1-Allen\u2019s Compounded Formulations<\/p>\n

2- RxMediaPharma\u00ae2018 Interactive Drug Information Resource<\/p>\n<\/div>\n

Specialist Pharmacist Ahmet Nezihi Pekcan
\nPekcan Pharmacy – Konya
\npekcanecz@gmail.com
\nTel: (332) 3520657http:\/\/www.majistralformul.com\/<\/a><\/p>\n<\/div>\n","protected":false},"excerpt":{"rendered":"

Dear Colleagues, I would like to draw attention once again to the importance of magistral compounding in delivering medications experiencing shortages and those defined as orphan drugs to patients. Diazepam […]<\/p>\n","protected":false},"author":1,"featured_media":3171,"comment_status":"open","ping_status":"closed","template":"","meta":{"_acf_changed":false,"footnotes":"","_members_access_role":[],"_members_access_error":""},"doc_category":[168],"doc_tag":[],"class_list":["post-8935","docs","type-docs","status-publish","has-post-thumbnail","hentry","doc_category-ovule-suppository-rectal-gel"],"acf":[],"year_month":"2026-09","word_count":1393,"total_views":"1","reactions":{"happy":"0","normal":"0","sad":"0"},"author_info":{"name":"m921a","author_nicename":"m921a","author_url":"https:\/\/majistraleczacilari.org.tr\/en\/author\/m921a\/"},"doc_category_info":[{"term_name":"Ovule - Suppository - Rectal Gel","term_url":"https:\/\/majistraleczacilari.org.tr\/en\/dokuman-kategori\/ovule-suppository-rectal-gel\/"}],"doc_tag_info":[],"knowledge_base_info":[],"knowledge_base_slug":[],"_links":{"self":[{"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/docs\/8935","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/docs"}],"about":[{"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/types\/docs"}],"author":[{"embeddable":true,"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/comments?post=8935"}],"version-history":[{"count":1,"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/docs\/8935\/revisions"}],"predecessor-version":[{"id":8937,"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/docs\/8935\/revisions\/8937"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/media\/3171"}],"wp:attachment":[{"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/media?parent=8935"}],"wp:term":[{"taxonomy":"doc_category","embeddable":true,"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/doc_category?post=8935"},{"taxonomy":"doc_tag","embeddable":true,"href":"https:\/\/majistraleczacilari.org.tr\/en\/wp-json\/wp\/v2\/doc_tag?post=8935"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}