دورية أكاديمية
Lipid-Gelucire based rectal delivery of ramipril prodrug exhibits significant lowering of intra-ocular pressure in normotensive rabbit: sustained structural relaxation release kinetics and IVIVC.
| العنوان: | Lipid-Gelucire based rectal delivery of ramipril prodrug exhibits significant lowering of intra-ocular pressure in normotensive rabbit: sustained structural relaxation release kinetics and IVIVC. |
|---|---|
| المؤلفون: | Nandi S; Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, India., Swain R; Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, India., Habibullah S; Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, India., Sahoo RN; Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, India., Nayak AK; Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, India., Mallick S; Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, India. |
| المصدر: | Pharmaceutical development and technology [Pharm Dev Technol] 2024 Jun; Vol. 29 (5), pp. 468-476. Date of Electronic Publication: 2024 May 02. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Informa Healthcare Country of Publication: England NLM ID: 9610932 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1097-9867 (Electronic) Linking ISSN: 10837450 NLM ISO Abbreviation: Pharm Dev Technol Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: London : Informa Healthcare Original Publication: Monticello, NY : Marcel Dekker, c1996- |
| مواضيع طبية MeSH: | Intraocular Pressure*/drug effects , Prodrugs*/administration & dosage , Prodrugs*/pharmacokinetics , Prodrugs*/pharmacology , Ramipril*/administration & dosage , Ramipril*/pharmacokinetics , Ramipril*/pharmacology , Administration, Rectal* , Delayed-Action Preparations*, Animals ; Rabbits ; Suppositories ; Male ; Biological Availability ; Antihypertensive Agents/administration & dosage ; Antihypertensive Agents/pharmacokinetics ; Antihypertensive Agents/pharmacology ; Lipids/chemistry ; Drug Liberation ; Administration, Oral ; Polyethylene Glycols |
| مستخلص: | Carboxylesterase enzymes convert a prodrug ramipril into the biologically active metabolite ramiprilat. It is prescribed for controlling ocular hypertension after oral administration. High concentrations of carboxylesterase enzymes in rectal and colon tissue can transform ramipril significantly to ramiprilat. Sustained rectal delivery of ramipril has been developed for intra-ocular pressure lowering effect using a normotensive rabbit model. Rectal suppositories have been formulated using a matrix base of HPMC K100-PEG 400-PEG 6000, incorporating varying amounts of Gelucire by the fusion moulding method. The presence of Gelucire in the suppository exhibited sustained structural relaxation-based release kinetics of RM compared to its absence. Intravenous and oral administration of ramipril has decreased IOP in the treated rabbit up to 90 and 360 min, respectively. Treated rabbits with suppositories have revealed decreased IOP for an extended period compared to the above. Formulation containing GEL 3% reduced intra-ocular pressure to 540 min, with the highest area under the decreased IOP curve. Compared to oral, the pharmacodynamic bioavailability of ramipril has been improved significantly using a sustained-release rectal suppository. A rectal suppository for sustained delivery of ramipril could be used to lower IOP significantly. |
| فهرسة مساهمة: | Keywords: Sustained rectal delivery; in vitro in vivo correlation (IVIVC); pharmacodynamic bioavailability; ramipril prodrug; structural relaxation kinetics |
| المشرفين على المادة: | 0 (Prodrugs) L35JN3I7SJ (Ramipril) 0 (Delayed-Action Preparations) 0 (Suppositories) 0 (Antihypertensive Agents) 121548-04-7 (gelucire 44-14) 0 (Lipids) 3WJQ0SDW1A (Polyethylene Glycols) |
| تواريخ الأحداث: | Date Created: 20240425 Date Completed: 20240620 Latest Revision: 20240620 |
| رمز التحديث: | 20240620 |
| DOI: | 10.1080/10837450.2024.2345807 |
| PMID: | 38662798 |
| قاعدة البيانات: | MEDLINE |
PDF full text from Publisher | تدمد: | 1097-9867 |
|---|---|
| DOI: | 10.1080/10837450.2024.2345807 |