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Journal articles on the topic 'Liquid Suppository'

Author: Grafiati

Published: 4 June 2025

Last updated: 23 June 2025

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1

Herasymova, I. V., H. B. Yurieva, T. H. Yarnykh, and D. V. Voronenko. "Research on the composition development of suppositories with echinacea and study of their stability." Ukrainian Journal of Military Medicine 3, no. 1 (2022): 67–74. http://dx.doi.org/10.46847/ujmm.2022.1(3)-067.

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The purpose of the work was to experimentally substantiate the composition and study the stability of extemporal suppositories with Echinacea, intended for use in complex therapy and prevention of genitourinary diseases. Materials and methods. The object of the study was samples of suppositories made by pouring using liquid Echinacea extract as an active pharmaceutical ingredient. Cocoa butter, Witepsol H15 and Witepsol W35 were used as suppository bases. The study was carried out using modern physicochemical, pharmaco-technological and microbiological methods. Results. On the basis of the carried out physicochemical and pharmaco-technological studies, it was found that in the manufacture of suppositories using liquid Echinacea extract, Cocoa butter or Witepsol can be used as a suppository bases. The main indicators of the quality of suppository samples were also studied: organoleptic characteristics, average weight, melting point, time of complete deformation, microbiological purity, meeting the requirements of the State Pharmacopoeia. Conclusions. As a result of the carried out physicochemical, pharmaco-technological and microbiological studies, a suppository base was selected for the creation of extemporal suppositories for the treatment and prevention of genitourinary diseases, the main quality indicators were established that meet the requirements of the State Pharmacopoeia of Ukraine, and the shelf life of the suppositories is 10 days.

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2

N. Al-Wiswasi, Noor, and Eman B.H. Al-Khedairy. "Formulation and in vitro Evaluation of In-situ Gelling Liquid Suppositories for Naproxen." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512) 17, no. 1 (2017): 31–38. http://dx.doi.org/10.31351/vol17iss1pp31-38.

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In-situ gelation is a process of gel formation at the site of application, in which a drug product formulation that exists as a liquid has been transformed into a gel upon contact with body fluids. As a drug delivery agent, the in-situ gel has an advantage of providing sustained release of the drug agent. In-situ gelling liquid suppositories using poloxamer 188 (26-30% W/W) as a suppository base with 10% W/W naproxen were prepared, the gelation temperature of these preparations were measured and they were all above the physiological temperature. Additives such as polyvinylpyrrolidin "PVP" ,hydroxylpropylmethylcellulose "HPMC", sodium alginate and sodium chloride were used in concentration ranging from (0.25-1%W/W) to modulate the gelation temperature and gel strength .The best preparation was obtained through using a combination of poloxamer 188, sodium alginate, naproxen and distilled water (29,0.5,10and 60.5 % W/W respectively)with gelation temperature of 33.6ÂºCÂ±0.2 and gel strength of 28Â±2 seconds. The release of drug from this preparation was sustained for about 12 hours and it was faster than conventional solid suppository (ProxenÂ® 500) and oral tablets (NaproxenÂ®500) using dialysis tubing method. Key words: - naproxen, in-situ gelation, liquid suppository, poloxamer188

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3

El-Kamel, Amal, and Mona El-Khatib. "Thermally Reversible In Situ Gelling Carbamazepine Liquid Suppository." Drug Delivery 13, no. 2 (2006): 143–48. http://dx.doi.org/10.1080/10717540500316003.

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4

Mishra, Preeti, Rajat Singh, Garima Kumari, Neha Kumari, and Amit Kumar Verma. "Formulation and Evaluation of Flax Herbal Suppositories." Journal of Drug Delivery and Therapeutics 12, no. 1 (2022): 19–22. http://dx.doi.org/10.22270/jddt.v12i1.5253.

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The rectal route has proven its worth in terms of achieving successful drug delivery both locally and systematically. The primary goal of this invention was to develop and evaluate Flax suppositories. To administer its herbal powder to internal sites, suppositories are placed directly into the rectum. A suppository comprises flax as a main active ingredient, administered through the rectal route, used as a laxative, and treatment of haemorrhoids and bacterial infections of the anus. For the formulation of the present invention, the suppository preferably comprises flax in an inert base, which may comprise any suitable inert pharmaceutical carrier. The base may optionally be any suitable inert base that is solid at room temperature. The flax may optionally comprise the liquid or gel form or a dry extract of the juice, or any other form of flax, all of which are collectively termed “flax extract”.  Keywords: Flax extract, suppository, Gelatin, Glycerine, Herbal suppositories.

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5

Yeo, Woo Hyun, Thiruganesh Ramasamy, Dong-Wuk Kim, et al. "Docetaxel-loaded thermosensitive liquid suppository: optimization of rheological properties." Archives of Pharmacal Research 36, no. 12 (2013): 1480–86. http://dx.doi.org/10.1007/s12272-013-0175-6.

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6

Pásztor, E., Á. Makó, G. Csóka, et al. "New formulation of in situ gelling Metolose-based liquid suppository." Drug Development and Industrial Pharmacy 37, no. 1 (2010): 1–7. http://dx.doi.org/10.3109/03639045.2010.489558.

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7

Choi, Han-Gon, Jae-Hee Jung, Jei-Man Ryu, Sung-June Yoon, Yu-Kyoung Oh, and Chong-Kook Kim. "Development of in situ-gelling and mucoadhesive acetaminophen liquid suppository." International Journal of Pharmaceutics 165, no. 1 (1998): 33–44. http://dx.doi.org/10.1016/s0378-5173(97)00386-4.

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8

Chul Soon, Yong, Choi Young-Kwon, Kim Yong-II, et al. "Physicochemical characterization andin vivo evaluation of thermosensitive diclofenac liquid suppository." Archives of Pharmacal Research 26, no. 2 (2003): 162–67. http://dx.doi.org/10.1007/bf02976664.

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9

Bassi, Anchal, Garima Sharma, Parneet Kaur Deol, Ratna Sudha Madempudi, and Indu Pal Kaur. "Preclinical Potential of Probiotic-Loaded Novel Gelatin–Oil Vaginal Suppositories: Efficacy, Stability, and Safety Studies." Gels 9, no. 3 (2023): 244. http://dx.doi.org/10.3390/gels9030244.

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The current study describes a suppository base composed of aqueous gelatin solution emulsifying oil globules with probiotic cells dispersed within. The favorable mechanical properties of gelatin to provide a solid gelled structure, and the tendency of its proteins to unravel into long strings that interlace when cooled, lead to a three-dimensional structure that can trap a lot of liquid, which was exploited herein to result in a promising suppository form. The latter maintained incorporated probiotic spores of Bacillus coagulans Unique IS-2 in a viable but non-germinating form, preventing spoilage during storage and imparting protection against the growth of any other contaminating organism (self-preserved formulation). The gelatin–oil–probiotic suppository showed uniformity in weight and probiotic content (23 ± 2.481 × 108 cfu) with favorable swelling (double) followed by erosion and complete dissolution within 6 h of administration, leading to the release of probiotic (within 45 min) from the matrix into simulated vaginal fluid. Microscopic images indicated presence of probiotics and oil globules enmeshed in the gelatin network. High viability (24.3 ± 0.46 × 108), germination upon application and a self-preserving nature were attributed to the optimum water activity (0.593 aw) of the developed composition. The retention of suppositories, germination of probiotics and their in vivo efficacy and safety in vulvovaginal candidiasis murine model are also reported.

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10

Choi, Han-Gon, Yu-Kyoung Oh, and Chong-Kook Kim. "In situ gelling and mucoadhesive liquid suppository containing acetaminophen: enhanced bioavailability." International Journal of Pharmaceutics 165, no. 1 (1998): 23–32. http://dx.doi.org/10.1016/s0378-5173(97)00385-2.

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11

Choi, Han-Gon, Mi-Kyung Lee, Moon-Hee Kim, and Chong-Kook Kim. "Effect of additives on the physicochemical properties of liquid suppository bases." International Journal of Pharmaceutics 190, no. 1 (1999): 13–19. http://dx.doi.org/10.1016/s0378-5173(99)00225-2.

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12

Yun, M. "Development of a thermo-reversible insulin liquid suppository with bioavailability enhancement." International Journal of Pharmaceutics 189, no. 2 (1999): 137–45. http://dx.doi.org/10.1016/s0378-5173(99)00227-6.

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13

Tyler, Theodore A., and Judith A. Genzale. "Liquid Chromatographic Determination of Miconazole Nitrate in Creams and Suppositories." Journal of AOAC INTERNATIONAL 72, no. 3 (1989): 442–44. http://dx.doi.org/10.1093/jaoac/72.3.442.

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Abstract A rapid method has been developed for the determination of miconazole nitrate in creams and suppositories. The sample is dissolved in ethanol, diluted in acetonitrile-water (1 + 1), and injected onto a C18 column. The mobile phase consists of 55% acetonitrile, a triethylammonium phosphate buffer, and an ion-pairing agent. The total run time is less than 4 min, and the active ingredient is determined using absorbance detection at 214 nm. The mean recovery of miconazole from spiked placebo samples was 99.7 ± 0.7% for the cream samples at the 2% level and 98.8 ± 0.3% for the suppository samples at the 4% level.

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14

Lv, Haixia, Suying Ma, Xiao Wang, and Xiaojun Shang. "Simultaneous Determination of Co-formulated Matrine and Secnidazole in Suppositories by Reverse Phase High Performance Liquid Chromatography." Tropical Journal of Pharmaceutical Research 12, no. 3 (2016): 413–18. http://dx.doi.org/10.4314/tjpr.v12i3.21.

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Purpose: To develop and validate a new, simple, sensitive and accurate high performance liquid chromatographic (HPLC) method for the simulataneous determination of matrine and secnidazole in suppositories.Methods: The method involved using a SinoChoom ODS-BP C18 column (5 ƒÊm, 4.6 mm ~ 200 mm) and mobile phase consisting of acetonitrile.triethylamine (0.05 %) in 0.025 mol/L KH2PO4 (20:80, v/v).The flow rate was 1 mL/min and detection was monitored at 210 and 311 nm for matrine and secnidazole, respectively. Total run time was 10 min and the column was maintained at 35 oC.Results: The excipients in the suppository did not interfere with the drug peaks. Matrine was eluted at a retention time (RT) of 4.30 min while linearity for the quantification of drug was obtained in the concentration range of 10.0 - 100.0 ƒÊg/mL (r2 = 0.9991). Secnidazole was eluted at a retention time (tr) of 6.69 min and linearity for the quantification of the drug was obtained in the concentration range of 10.0 - 150.0 ƒÊg/mL (r2 = 0.9993). Intra- and inter-day variations were < 1.0 % for both matrine andsecnidazole.Conclusion: The developed HPLC method was validated according to International Conference on Harmonisation (ICH) guidelines and proved to be suitable for the simultaneous determination of matrine and secnidazole in suppositories.Keywords: Matrine, Secnidazole, Suppository, HPLC, Assay

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15

ElSohly, Mahmoud A., Waseem Gul та Larry A. Walker. "Pharmacokinetics and Tolerability of Δ9-THC-Hemisuccinate in a Suppository Formulation as an Alternative to Capsules for the Systemic Delivery of Δ9-THC". Medical Cannabis and Cannabinoids 1, № 1 (2018): 44–53. http://dx.doi.org/10.1159/000489037.

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The objectives of this study were: (1) to assess the safety, tolerability, and pharmacokinetics of ascending doses of Δ9-tetrahydrocannabinol-hemisuccinate (THC-HS) after rectal administration as suppositories in male volunteers; and (2) to compare the pharmacokinetics of oral administration of Δ9-tetrahydrocannabinol (Δ9-THC) with an equivalent amount of Δ9-THC delivered as THC-HS via the suppository formulation. In support of the pharmacokinetic evaluations, an analytical method was developed and validated for the determination of Δ9-THC and for its major circulating metabolites 11-hydroxy-Δ9-tetrahydrocannabinol (11-OH-THC) and 11-nor-Δ9-tetrahydrocannabinol-9-carboxylic acid (THC-COOH) in human plasma. Δ9-THC, 11-OH-THC, and THC-COOH were extracted from plasma using solid phase extraction and analyzed by liquid chromatography-tandem mass spectrometry. The limits of detection and quantitation for all 3 analytes were 0.25 and 0.5 ng/mL, respectively. The method was validated over the range of 0.5–25 ng/mL. This method was used to quantify Δ9-THC and any THC-HS as Δ9-THC due to the inclusion of a hydrolysis step as part of the extraction procedure. Therefore, Δ9-THC measured was the total THC (free Δ9-THC plus Δ9-THC derived from THC-HS). The assay was reproducible for the measurement of all 3 analytes, with a variability of 7.2, 13.7, and 8.3%, respectively, at the 1 ng/mL level. The method was then used to assess the pharmacokinetics of Δ9-THC and metabolites from the suppository dosage form in doses equivalent to 1.25, 2.5, 5, 10, and 20 mg Δ9-THC per suppository as THC-HS. Systemic exposure to Δ9-THC, administered as THC-HS suppository, increased broadly dose proportionally. Systemic exposure and Cmax (obs) estimates for 11-OH-THC and THC-COOH generally increased subproportionally. The pharmacokinetic profiles of Δ9-THC and metabolites were also compared after oral administration of 10 mg Δ9-THC (as dronabinol capsules) and after administration of 10 mg equivalents of Δ9-THC as THC-HS in suppository form. Total systemic exposure to Δ9-THC was considerably higher following rectal administration of THC-HS than after oral administration. The Δ9-THC area under the plasma concentration versus time curve (AUC(0–∞)) for THC-HS was 2.44-fold higher (90% confidence interval: 1.78, 3.35) than for the capsule administration.

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16

Yong, Chul Soon, Yu-Kyoung Oh, Se Hyun Jung, et al. "Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol." European Journal of Pharmaceutical Sciences 23, no. 4-5 (2004): 347–53. http://dx.doi.org/10.1016/j.ejps.2004.08.008.

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17

Ban, Eunmi, and Chong-Kook Kim. "Design and evaluation of ondansetron liquid suppository for the treatment of emesis." Archives of Pharmacal Research 36, no. 5 (2013): 586–92. http://dx.doi.org/10.1007/s12272-013-0049-y.

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18

Welch, Ken, Ragnar Ek, and Maria Stromme. "Comparative Drug Release Measurements in Limited Amounts of Liquid: A Suppository Formulation Study." Current Drug Delivery 3, no. 3 (2006): 299–306. http://dx.doi.org/10.2174/156720106777731109.

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19

Kim, Chong-Kook, Sa-Won Lee, Han-Gon Choi, et al. "Trials of in situ-gelling and mucoadhesive acetaminophen liquid suppository in human subjects." International Journal of Pharmaceutics 174, no. 1-2 (1998): 201–7. http://dx.doi.org/10.1016/s0378-5173(98)00258-0.

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20

Lo, Yu-Li, Yijun Lin, and Hong-Ru Lin. "Evaluation of Epirubicin in Thermogelling and Bioadhesive Liquid and Solid Suppository Formulations for Rectal Administration." International Journal of Molecular Sciences 15, no. 1 (2013): 342–60. http://dx.doi.org/10.3390/ijms15010342.

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21

Ahmed, Haydar Mahmood, and Iman Sabah Jaafar. "Nefopam HCl in situ mucoadhesive liquid suppository, a potential drug delivery system to enhance bioavailability." F1000Research 14 (February 4, 2025): 160. https://doi.org/10.12688/f1000research.159557.1.

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Background Nefopam hydrochloride (NPH) is a non-narcotic analgesic that is severely affected by its extensive hepatic metabolism resulting in low oral bioavailability. This study aimed to develop NPH thermosensitive in situ gel to enhance its bioavailability by avoidance of first pass effect through rectal administration. Methods A cold method was employed to develop NPH thermosensitive rectal in situ gel utilizing various concentrations of poloxamer 407 (P 407) and poloxamer 188 (P188) alone or in mixture as thermosensitive polymers and hydroxypropyl methylcellulose K4M (HPMCK4M) as well as carboxymethyl cellulose (CMC) as mucoadhesive polymers. The achieved formulas were assessed for various in vitro constraints including: solution-gel temperature, gelation time, appearance, pH, gel strength, viscosity, in vitro drug release study. Furthermore, the optimized formula was evaluated for in vivo localization and permeability. Results The obtained outcomes demonstrated a direct correlation between solution-gelation temperatures and poloxamer 188 concentration as well as an inverse correlation with the concentration of both P407 and HPMCK4M. A direct correlation was perceived between the mucoadhesive forces and viscosity with HPMCK4M concentration. Additionally, an inverse correlation was observed between NPH released with HPMCK4M concentration. The optimal NPH gel formula (F8) (18% P407/2% P188 and 0.6%) presented a compatible pH value (7.2±0.35), an acceptable sol-gel T (35.4 °C), gel strength (39.54 ± 0.803), a mucoadhesion force of 6340.6 dyne/cm2 and sustained drug release of 85% at 8 hrs. Additionally it showed sufficient localization and a permeation flux of 0.0398 mg/cm2/h, and apparent permeability (Papp) of 1.99*10−3. Conclusions It was concluded that this drug delivery system may serve as a promising alternative to other dosage forms containing NPH, owing to avoidance of first-pass metabolism, enhanced bioavailability, non-invasiveness, and reduced adverse effects associated with other forms.

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22

Lin, Hong-Ru, Chao-Chih Tseng, Yiu-Jiuan Lin, and Ming-Hung Ling. "A Novel In-Situ-Gelling Liquid Suppository for Site-Targeting Delivery of Anti-Colorectal Cancer Drugs." Journal of Biomaterials Science, Polymer Edition 23, no. 6 (2012): 807–22. http://dx.doi.org/10.1163/092050611x560861.

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23

Saleem, Aiman, Fakhar ud Din, Zakir Ali, et al. "Development and evaluation of regorafenib loaded liquid suppository for rectal delivery: In vitro, in vivo analyses." Journal of Drug Delivery Science and Technology 91 (January 2024): 105239. http://dx.doi.org/10.1016/j.jddst.2023.105239.

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24

Bialik, Maria, Marzena Kuras, Marcin Sobczak, and Ewa Oledzka. "Achievements in Thermosensitive Gelling Systems for Rectal Administration." International Journal of Molecular Sciences 22, no. 11 (2021): 5500. http://dx.doi.org/10.3390/ijms22115500.

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Rectal drug delivery is an effective alternative to oral and parenteral treatments. This route allows for both local and systemic drug therapy. Traditional rectal dosage formulations have historically been used for localised treatments, including laxatives, hemorrhoid therapy and antipyretics. However, this form of drug dosage often feels alien and uncomfortable to a patient, encouraging refusal. The limitations of conventional solid suppositories can be overcome by creating a thermosensitive liquid suppository. Unfortunately, there are currently only a few studies describing their use in therapy. However, recent trends indicate an increase in the development of this modern therapeutic system. This review introduces a novel rectal drug delivery system with the goal of summarising recent developments in thermosensitive liquid suppositories for analgesic, anticancer, antiemetic, antihypertensive, psychiatric, antiallergic, anaesthetic, antimalarial drugs and insulin. The report also presents the impact of various types of components and their concentration on the properties of this rectal dosage form. Further research into such formulations is certainly needed in order to meet the high demand for modern, efficient rectal gelling systems. Continued research and development in this field would undoubtedly further reveal the hidden potential of rectal drug delivery systems.

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Kim, Jin-Ki, Myung-Sun Kim, Jeong-Sook Park та Chong-Kook Kim. "Thermo-reversible flurbiprofen liquid suppository with HP-β-CD as a solubility enhancer: improvement of rectal bioavailability". Journal of Inclusion Phenomena and Macrocyclic Chemistry 64, № 3-4 (2009): 265–72. http://dx.doi.org/10.1007/s10847-009-9560-7.

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26

Dimitrova, Burya, Irini Doytchinova, and Margarita Zlatkova. "Reversed-phase high-performance liquid chromatography for evaluating the distribution of pharmaceutical substances in suppository base–phosphate buffer system." Journal of Pharmaceutical and Biomedical Analysis 23, no. 6 (2000): 955–64. http://dx.doi.org/10.1016/s0731-7085(00)00370-8.

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27

He, Wen, Yumin Du, Wenbing Dai, Yan Wu, and Mian Zhang. "Effects ofN-trimethyl chitosan chloride as an absorption enhancer on properties of insulin liquid suppository in vitro and in vivo." Journal of Applied Polymer Science 99, no. 3 (2005): 1140–46. http://dx.doi.org/10.1002/app.22317.

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28

Sirilun, Sasithorn, Bhagavathi Sundaram Sivamaruthi, Periyanaina Kesika, et al. "DEVELOPMENT AND STABILITY EVALUATION OF VAGINAL SUPPOSITORY CONTAINING GLYCYRRHIZA GLABRA L. FOR THE TREATMENT OF CANDIDA ALBICANS INFECTION." Asian Journal of Pharmaceutical and Clinical Research 11, no. 7 (2018): 205. http://dx.doi.org/10.22159/ajpcr.2018.v11i7.25927.

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Objective: The present study assessed the antioxidant activity, phytochemical content, and anti-Candida albicans property of ethanolic extract of Glycyrrhiza glabra L. (licorice). In addition, suppository formula (SF) was developed with licorice extract (LE), and the stability of SF was evaluated.Methods: The total phenolic and flavonoid content was measured by colorimetric methods. 2, 2′-azino-bis-3-ethylbenzthiazoline-6-sulfonic acid (ABTS), ferric reducing antioxidant power (FRAP), inhibition of lipid peroxidation (LPO), nitric oxide (NO), and superoxide (SO) radical scavenging assays were performed to evaluate antioxidant property. Antimicrobial activity was determined by plating method. The active principle was determined by high-performance liquid chromatography method.Results: The licorice sample was extracted with 95% ethanol, and 26.91±1.35% of yield was observed. The LE contains phenolic acids (167.70±3.18 mg gallic acid equivalent/g extract), flavonoids (162.53±9.95 mg quercetin equivalent/g extract), and glabridin (3.90±0.05 mg/g extract). LE exhibited the scavenging activity in terms of 810.53±25.37 μM of Trolox equivalent/mg of extract, 165.04±5.10 μM of FeSO4 equivalent/mg of extract, and 3750.35±1.25, 68.25±0.07, and 511±0.80 μM of Trolox equivalent/mg of extract in ABTS, FRAP, LPO, NO, and SO assays, respectively. About ≥62.50, ≥125, and ≥250 μg/mL of LE was recorded as minimal inhibitory concentration against C. albicans, Lactobacillus casei, and Lactobacillus acidophilus, respectively. The SF was formulated and the stability was evaluated. The activity and color of SFs did not differ on storage. Moreover, no spot formation was observed.Conclusion: The SF with LE could be the safe therapeutic strategy for the treatment of candida infection in vaginal region.

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Lebrat, Matthieu, Yassine Bouattour, Coralie Gaudet, et al. "Development and Stability of a New Formulation of Pentobarbital Suppositories for Paediatric Procedural Sedation." Pharmaceutics 15, no. 3 (2023): 755. http://dx.doi.org/10.3390/pharmaceutics15030755.

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Pentobarbital is a drug of choice to limit motion in children during paediatric procedural sedations (PPSs). However, despite the rectal route being preferred for infants and children, no pentobarbital suppositories are marketed, and therefore they must be prepared by compounding pharmacies. In this study, two suppository formulations of 30, 40, 50, and 60 mg of pentobarbital sodium were developed using hard-fat Witepsol® W25 either alone (formulation F1) or with oleic acid (formulation F2). The two formulations were subjected to the following tests described in the European Pharmacopoeia: uniformity of dosage units, softening time, resistance to rupture, and disintegration time. The stability of both formulations was also investigated for 41 weeks of storage at 5 ± 3 °C using a stability-indicating liquid chromatography method to quantify pentobarbital sodium and research breakdown product (BP). Although both formulae were compliant to uniformity of dosage, the results were in favour of a faster disintegration of F2 compared to F1 (−63%). On the other hand, F1 was found to be stable after 41 weeks of storage unlike F2 for which several new peaks were detected during the chromatographic analysis, suggesting a shorter stability of only 28 weeks. Both formulae still need to be clinically investigated to confirm their safety and efficiency for PPS.

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McEvoy, Eamon, Sheila Donegan, Joe Power, and Kevin Altria. "Optimisation and validation of a rapid and efficient microemulsion liquid chromatographic (MELC) method for the determination of paracetamol (acetaminophen) content in a suppository formulation." Journal of Pharmaceutical and Biomedical Analysis 44, no. 1 (2007): 137–43. http://dx.doi.org/10.1016/j.jpba.2007.02.025.

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31

Bezuglaya, Elena, Yurij Stolper, Nikolay Lyapunov, Igor Zinchenko, and Oleksii Liapunov. "Study of factors affecting some properties of hydrophilic suppository base." ScienceRise: Pharmaceutical Science, no. 5(45) (October 31, 2023): 4–15. http://dx.doi.org/10.15587/2519-4852.2023.286315.

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The aim. To study the effect of the composition of hydrophilic suppository bases on the physicochemical and osmotic properties of suppositories made from them. Materials and methods. The bases were studied with varying compositions of excipients. The microstructure of the bases was evaluated, and the disintegration time and resistance to rupture of suppositories made from them were determined. The kinetics of water absorption and solvent release were studied by dialysis. The content of propylene glycol (PG) and macrogol 400 (M400) in the receptor medium was determined by gas chromatography. The melted bases were studied by rotational viscometry. The electron paramagnetic resonance spectra of spin probes in hydrophilic solvents and bases were obtained; the type of spectrum, isotropic constant (AN), rotational correlation times (τ), and anisotropy parameter (ε) were determined. Results. The disintegration times and resistance to rupture of suppositories were determined depending on such factors as the content and grade of poloxamers, the ratio between high molecular weight macrogols and the mixed solvent PG-M400 (60 : 40 % m/m), the ratio of nonionic surfactant and cetostearyl alcohol (CSA) and their total content, water and hard fat content. The introduction of solid fat and a mixture of surfactants and CSA provides the uniform structure of the bases. The mass ratio between surfactants and CSA and their total content are important factors that provide acceptable resistance to rupture and disintegration times for suppositories and reduce water absorption and solvent release. As the temperature decreases from 45 °C to 20 °C, the bases transform from Newtonian liquids to solids. At that time, the microviscosity of the environment of the spin probes increased by about 5 times, but the parameters of their rotational diffusion in solid bases and the mixed solvent PG-M400 are comparable. This indicates the dissolved state of the spin probes in the bases and the absence of the formation of mixed associates from molecules of surfactant and CSA. Conclusions. By varying the composition of excipients, the properties of hydrophilic suppository bases can be controlled, significantly reducing their osmotic properties. The active substances in these bases may be in a dissolved state due to the high content of non-aqueous solvents

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Borko, Ye. A., I.V. Kovalevska, and T.P. Osolodchenko. "Determination of microbiological purity of rectal suppositories with diosmine and hesperidine." Annals of Mechnikov Institute, no. 2 (June 8, 2020): 9–12. https://doi.org/10.5281/zenodo.3885040.

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<strong>Introduction. </strong>The use of conservative methods of treatment, in terms of increasing the number of patients with anorectal diseases, is becoming increasingly important in modern realities. Proctological pathologies are becoming more characteristic for people of working age, and can affect not only the physical and mental health of an individual, but also the future reproductive state of the nation as a whole. , It is advisable to use dosage forms that will effect on several factors in the pathogenesis, while showing resorptive and local effects. As an example, of such a dosage form (DF) are rectal suppositories, which according to a complex of structural-mechanical and biopharmaceutical factors is the optimal DF for the release of active substances on the place of the pathological process. An important stage in the formulation of rectal suppositories it isn`t only the choice of active substances, but also quality control of ready-made DF. The SPhU of Ukraine regulates the quality indicator "microbiological purity" for suppositories as a critical stage of control, which means the necessity for a full range of studies to identify possible of microbial contamination in the DF. <strong>Material & Methods. </strong>We have selected 3 samples of rectal suppositories with diosmin and hesperidin for microbiological studies. In order to substantiate the stability during storage, we have proposed to use samples with different durations from the date of manufacture (1- just made; 2- 2 weeks storage; 3- 6 months storage). The testing of suppository samples for microbiological purity was carried out using with the Chistovich medium, blood agar-based soybean casein digest agar and Endo medium. As a preliminary preparation for the study of microbiological purity, tests were performing for compliance with the growth qualities of nutrient mediums. The definitions of microscopic study were carried out a microscopic method using a Konus Academi Microscope of Italian production with a DLT-Cam Basic 2MP camera. The test of microbiological purity was conducted with methods direct seeded on liquid nutrient mediums. The definitions of quantity of viable cells of microorganisms and fungus for methods of deep seeding have been conducting with adding sample in quantity 0.1 in agar medium.  <strong>Results & discussion. </strong>The results of the study of growth properties of nutrient mediums was shown, that all cultures of microorganisms met to the taxonomic designation of the strain. The obtained results have shown that after 14 days of incubation of suppositories samples on the Saburo medium - the fungus haven't growth. The results of researches samples with soybean casein digest broth and thyoglycollate medium in the quantity 1.0 and 0.1 haven`t shown the growth of microorganisms. Registration of growth of the microorganisms has been shown in research of samples in the quantity of 0.01. The microorganisms that have been detected during the studies by morphology of colonies and biological properties belong to the genus Bacillus sp. According to the research results by the method of direct seeding on cups the growth of fungus has been absented in all suppositories samples. <strong>Conclusion. </strong>Taking into account the obtained data we was indicated that viable fungal cells weren`t detected in the suppositories samples. The quantity of microorganisms was lower by 10<sup>3</sup> CFU/ml that meets the requirements of SPhU. Microorganisms that have been detected during the studies belong to the genus Bacillus sp. The strains of S. aureus, P. аeruginosa and representatives of the genus Enterobacteriacea sp. haven`t been detected. Suppositories samples that have been determinations on indicator of microbiological purity, meets the requirements of SPhU.

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Klingmann, Viviane, Thibault Vallet, Juliane Münch, et al. "Dosage Forms Suitability in Pediatrics: Acceptability of Analgesics and Antipyretics in a German Hospital." Pharmaceutics 14, no. 2 (2022): 337. http://dx.doi.org/10.3390/pharmaceutics14020337.

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Although medicine acceptability is likely to have a significant impact on the patient’s adherence in pediatrics and therefore on therapy success, there is still little data even for common therapeutic areas. For analgesics/antipyretics, healthcare professionals face a wide variety of products and need knowledge to select the best adapted product for each patient. We investigated acceptability of those products most used at the University Children’s Hospital Düsseldorf, Germany. Based on 180 real-life observer reports of medicine intake, we used the acceptability reference framework to score acceptability of six distinct medicines. Both ibuprofen and paracetamol tablets, mainly used in adolescents, were positively accepted. This was not the case for the solution for injection of metamizole sodium. Regarding syrups, mainly used in children under 6 years of age, ibuprofen flavored with strawberry and provided with an oral syringe was positively accepted, while paracetamol flavored with orange and provided with a measuring cup was not. Suppository appeared to be an alternative to oral liquids in infants and toddlers with palatability and administration issues. Differences appeared to be driven by dosage forms and formulations. These findings improve knowledge on acceptability drivers and might help formulating and prescribing better medicines for children.

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Ramandeep, Kaur* Sandeep Kumar Ghanshyam Das Gupta. "PREPARATION AND EVALUATION OF IN SITU GELLING MICONAZOLE NITRATE LIQUID VAGINAL SUPPOSITORY." December 31, 2017. https://doi.org/10.5281/zenodo.2529311.

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The key purpose of this study was to prepare and evaluate of in situ gelling Miconazole nitrate liquid vaginal suppository for fungal infection. In situ gelation is a process of gel formulation at the site of application, in which a drug product formulation that exists as a liquid has been transformed into gel upon contact with body fluid or at body temperature. To solve the problem of conventional solid suppositories it would be desirable to develop a liquid suppository which forms a gel at body temperature with suitable gel strength not to be leaked out from vagina after administration and with a suitable bioadhesive force. The liquid vaginal suppository was prepared by cold method using as Poloxamer 407 & 188 as thermo reversible polymer and HPMC, Carbopol 934 and Sodium alginate as mucoadhesive polymer. Liquid suppository was prepared by different combinations of drug and excipients. Formulation was evaluated in terms of pH, Gelation temperature, Gel strength, Mucoadhesive property, Drug content estimation and in vitro drug release etc. Results indicated that HPMC based liquid suppository gave better gelation temperature than others and it was observed that the increased in concentration of HPMC shows decreased in gel strength, mucoadhesive property and drug release of formulation.

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Jiao, Yan, Shijing Xie, Abdul Baseer, and Fakhar Ud-din. "Rectal administration of Celecoxib liquid suppositories with enhanced bioavailability and safety in rats." Current Drug Delivery 19 (May 13, 2022). http://dx.doi.org/10.2174/1567201819666220513091015.

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Background: Celecoxib is broadly used for the treatment of rheumatoid arthritis, however its poor bioavailability and cytotoxicity in pure form has reduced its therapeutic efficacy. This study aims to develop celecoxib liquid suppositories with improved bioavailability and reduced toxicity. Methods: The celecoxib liquid suppositories were prepared by thoroughly mixing celecoxib, poloxamer 188 and poloxamer 407, and tween-20, respectively used as drug, polymers and surfactant, in triple distilled water using cold technique. The developed liquid suppositories were characterized in terms of their gelation temperature, gelation time, and gel strength. Moreover, the muco-adhesive force was determined for the suppositories. The release behavior of the liquid suppositories was investigated in distilled water and compared with drug suspension. Furthermore, pharmacokinetics and morphological studies were carried out in rats after rectal administration of the celecoxib liquid suppository compared with drug suspension. Results: Poloxamer 188 and Tween-20 concentrations have significantly reduced the gelation temperature and time, however, the gel strength and bio-adhesive force were significantly enhanced. The concentration of celecoxib has no significant effect on the properties of liquid suppositories. A significantly enhanced and potentially sustained drug release was observed from the celecoxib liquid suppositories as compared with the drug suspension. The optimized formulation was easy to administer rectally because it quickly forms gel upon insertion into the body due to a suitable gelation temperature of about 31.7 0C. After rectal administration in rats, the celecoxib liquid suppository gave a significantly increased pharmacokinetic profile including enhanced plasma concentration and 9.7 fold improved area under the curve (AUC) compared to the drug suspension. Additionally, the morphology study exhibited no toxicity to the rectal tissue, no signs of irritation, or injury after the application of suppository. However, severe rectal tissue toxicity and irritation was observed in the suspension treated rectum. Conclusions: t can be concluded that the liquid suppository system may significantly enhance the solubilization and bio-availability of sparingly water-soluble drugs as evident in the case of celecoxib with no toxicity at the site of application.

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"Rectal topical corticosteroid preparations." Drug and Therapeutics Bulletin 29, no. 17 (1991): 66–68. http://dx.doi.org/10.1136/dtb.29.17.66.

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Topical corticosteroid preparations have been the main treatment for attacks of mild to moderate proctitis and left-sided ulcerative colitis since the 1950s.1 This article reviews the liquid enema, foam and suppository formulations available.

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Peloquin, Charles A., Gordon T. James, Eileen McCarthy, and Marian Goble. "Pharmacokinetic Evaluation of Ethionamide Suppositories." Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy 11, no. 5 (1991). http://dx.doi.org/10.1002/j.1875-9114.1991.tb02645.x.

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The absorption and elimination of ethionamide (ETA) after oral tablets and rectal suppositories were determined in 12 healthy, adult male volunteers. A randomized, double‐blind, double‐dummy, crossover design was used. Treatments compared 250‐mg ETA tablets and a placebo suppository to a 500‐mg ETA suppository and two placebo tablets, given 7 days apart. Blood samples were collected at predetermined intervals for 12 hours after the dose. Serum concentrations of ETA were determined using high‐performance liquid chromatography. The area under the serum concentration‐time curve was used to compare the relative bioavailability of ETA from the two preparations. Relative bioavailability after rectal administration was 57.3% of that after oral administration. The maximum serum concentration after rectal administration was 33% of that after oral administration. Higher doses of ETA and serum concentration monitoring are recommended whenever the suppositories are used.

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J HASSON, KAHTAN, ESRAA G JABAR, and IHAB I ALKHALIFA. "EVALUATION OF INNOVATED FORMULA OF BISACODYL SUPPOSITORY FOLLOWING THE DISSOLUTION PROFILE AND STABILITY DATA USING DEVELOPED HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD." Asian Journal of Pharmaceutical and Clinical Research, February 3, 2020. http://dx.doi.org/10.22159/ajpcr.2020.v13i1.36222.

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Objective: Bisacodyl is a laxative drug used in the treatment of constipation, it is soluble in mineral acids, but it is practically insoluble in water. Therefore, it is very hard task to dissolve bisacodyl in alkaline medium so the objective of this study was the development of proper dissolution method for a new formulation of bisacodyl suppositories in a medium simulated to rectal region. Obviously, most of the bisacodyl suppositories preparation products will yield low percentages of dissolution in the alkaline medium of phosphate buffer pH 7.2. Methods: Preparation inclusion complex of bisacodyl with the solubilizing agent beta-cyclodextrin then incorporated in a suppository base. The quantitative analysis of bisacodyl in suppositories was carried by a developed and validated high-performance liquid chromatography method. Results and Discussion: The dissolution rates for the innovated formulation of bisacodyl complexed with beta-cyclodextrin suppositories were in average of 97.5% and the stored suppositories of this formulation maintained their specified physical and chemical properties along the real stability study. Conclusion: The application of the inclusion complexation technique of bisacodyl with beta-cyclodextrin in the production of suppositories enhances the dissolution rate and improves the stability of suppositories performance.

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SALMAN, Z. D., A. T. ALHAMDANY, and N. Z. YOUSIF. "An Innovative Mucoadhesive Thermosensitive In situ Gelling Liquid Suppository of Metoclopramide Hydrocloride for Treatment of Nausea and Vomiting Associated with Diseases." Indian Journal of Pharmaceutical Sciences 82, no. 4 (2020). http://dx.doi.org/10.36468/pharmaceutical-sciences.691.

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Kumudhavalli, M. V., Sangeetha S., S. Alexander, R. Shivananthan, B. S. Venkateswarlu, and M. Kumar. "Extraction and Quantification of Ano Rectal Formulation by UV-LC Techniques." Research Journal of Pharmacy and Technology, April 29, 2023, 1617–21. http://dx.doi.org/10.52711/0974-360x.2023.00264.

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Suppositories very popular formulations and are currently used therapeutically all over the world. Especially in pediatrics, where they can be used for the effective lowering of high fever accomplished with seizure. The choice of a suppository as the mode of drug delivery system in all cases even in infants when oral delivery is impossible, that is an unconscious or vomiting patient, or in the case of infants. Therefore, the quality control study of this dosage form with a modern instrumental analytical technique is highly desired. In consequence of the increased application of suppositories, there is a current demand for a rapid, effective analytical methods required for routine analysis. The literature search revealed that methods for the UV and high-performance liquid chromatography (HPLC) analysis of DZP are very rare.Thereforethe aim of the present research was to develop and validate a suitable general sample preparation and chromatography method for suppositories containing DZP. The primary method (I) is based on UV Spectroscopy. UV spectra of Diazepam are recorded. The secondary method is based on the Reverse phase HPLC method was developed. The UV detector was operated at 286nm. After method development the proposed method was validated as per ICH guidelines. The developed method was accurate and precise which shows the evident from the analytical data and recovery studies. The analytical results were in good and it complies with the label claims.

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Songprasertkul, P., R. Bosman, M. Mei, P. Treenate, and L. Millheiser. "(173) PERCEPTION OF MOISTURIZATION WITH USE OF A VAGINAL OVULE MOISTURIZER IN MENOPAUSAL WOMEN." Journal of Sexual Medicine 22, Supplement_1 (2025). https://doi.org/10.1093/jsxmed/qdaf068.150.

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Abstract Introduction Menopause, an inevitable life stage, leaves women experiencing numerous symptoms. Vaginal dryness and discomfort are prevalent, being problematic during sexual intercourse and during day-to-day activities. Vaginal moisturizers are a key treatment option in the management of vaginal dryness and discomfort and enhance quality-of-life. To remain effective, they require consistent application several times per week. The volume of liquid applied into the vaginal canal with use of non-suppository moisturizers is often associated with leakage which can impact compliance. K-Y Liquibeads is a vaginal moisturiser in suppository format, held in an ovule that dissolves post-application, the released contents coat the vaginal mucosa, reducing friction and providing comfort. Objective To determine the duration of perceived moisturization in peri- and post-menopausal women using K-Y Liquibeads for daily comfort and during sexual intercourse. Secondly, to gather insight into product usage experience. Methods A consumer Home Use Test (HUT) of monadic design, assessing K-Y Liquibeads, was performed utilising the approach of ASTM standard E1958-22. Peri- and post-menopausal women were recruited and instructed to insert one ovule of K-Y Liquibeads on Day 1 and one ovule on Day 6. Self-administered questionnaires with either hedonic or Likert scale responses were collected to gain insights on user perception. Significance was set at 95% confidence interval (p = 0.05). Results A total of 300 women aged 43-65 years (225 postmenopausal, 75 perimenopausal) completed the study. Following both placements, K-Y Liquibeads were reported to provide a statistically significant feeling of moisturization at 24-, 48-, 72-, 84-hours. Ninety-eight percent (98%) of participants used the product applicator for insertion of the ovule into the vaginal canal, with a few participants (n = 3) preferring to use their finger. The majority of participants strongly agreed or agreed that K-Y Liquibeads provided a better sex experience with their partner, compared to when they did not use the product. Conclusions K-Y Liquibeads provided a statistically significant perception of moisturization for a duration of up to 84-hours (3.5 days), while also enhancing the sexual experience with their partner. These data suggest twice weekly product application provides moisturizing benefits. This consumer usage study shows promising functional benefits of the application of K-Y Liquibeads. Future studies could further evaluate K-Y Liquibeads as both a moisturizer and as a personal lubricant. Disclosure Yes, this is sponsored by industry/sponsor: Reckitt Benckiser Health Limited. Clarification: Industry initiated, executed and funded study. Any of the authors act as a consultant, employee or shareholder of an industry for: Reckitt Benckiser Health Limited.

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Vlachou, Marilena, Angeliki Siamidi, Anna Konstantinou, Panagoula Pavlou, and Ioannis Siamidis. "Modified release of acetaminophen from matrix tablet formulations: Influence of tablet geometry." Letters in Drug Design & Discovery 20 (October 17, 2022). http://dx.doi.org/10.2174/1570180820666221017162352.

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Background: Acetaminophen (APAP) or otherwise called paracetamol is a widely used over-the-counter, analgesic (common conditions treated include headaches, backache, toothache, muscle aches, arthritis, sore throat etc.) and antipyretic drug. It can be administered orally, in the form of a tablet (plain, effervescent, orodispersable, etc.) or liquid, rectally in the form of suppository or by injection (intravenously or intramuscularly). It is well absorbed orally with a plasma elimination half-life ranging from 1 to 4 h. The modified release oral formulation can prolong its therapeutic effects by maintaining APAP average plasma concentrations. Objective: In the context of this work, two APAP formulation tablets with different geometries were produced from standard pharmaceutical excipients, to investigate the role of altered tablet geometry in modified oral drug delivery. Methods: APAP tablets were prepared by direct compression, using hydroxypropyl methylcellulose (HPMC K15M), polyvinylpyrrolidone (PVP, MW: 55,000) and magnesium stearate, as ingredients. The release profiles were probed in aqueous dissolution media (pH 1.2 and 6.8), to simulate the conditions in the gastrointestinal tract, in a United States Pharmacopeia (USP) dissolution paddle apparatus II and analyzed using a ultraviolet (UV) spectrophotometer (λmax = 244 nm). Results: The results indicated that the tablets were within the acceptable range of all evaluation parameters (tablet dimensions, drug content, weight variation, and breaking force) as defined by the international standards stated in the US Pharmacopoeia. The dissolution results showed that the APAP’s release profile was controlled by the tablets’ different geometries and specifically the surface area (SA) and the surface area/volume (SA/V) ratio of the different tablets. The tablets with smaller SA/V ratios and SA showed slower drug release, indicative of a modified release motif. Conclusion: Altered tablet geometry plays an important role in APAP modified oral drug delivery.

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VENKATA RATNAM K, TIRUPATI REDDY G, and VENKATA RAJU RR. "The THERAPEUTIC IMPORTANCE OF GUMS IN FOLK MEDICINE FROM EASTERN GHATS, ANDHRA PRADESH." Asian Journal of Pharmaceutical and Clinical Research, May 31, 2019, 300–302. http://dx.doi.org/10.22159/ajpcr.2019.v12i7.33052.

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Objective: The objective of the present study is to collect ethnobotanical information of gums of medicinal plants from Eastern Ghats of Andhra Pradesh. Methods: Intensive ethnobotanical field trips were conducted in the forests of Eastern Ghats to collect firsthand information on therapeutic importance of gums used in folk medicine. Results: The present report deals with the therapeutic importance of gums in folk medicine used by local tribes inhabiting in and around the forests of Eastern Ghats of Andhra Pradesh. The results of the present study revealed that 21 crude drugs belong to 19 genera and 14 families of higher plants. The critical review of literature on crude drugs with reference to that of Eastern Ghats revealed that 13 crude drugs are hitherto not known to the science. 24 herbal formulations are commonly prepared by the local people to cure 14 human ailments. Out of 21 crude drugs reported in the present study, 10 crude drugs have pharmaceutical importance, namely drug delivery agents (Acacia), disintegrate in tablets (Sterculia), thickeners in oral liquids (Acacia and Mangifera), dilutents, binders, gelling agents in gels (Butea, Neem, and Moringa), and protective colloids in suspensions (Anogeissus) and bases in suppository. Conclusion: Natural gums of plant origin have multifarious pharmaceutical applications. In view of the potential crude drugs with promising therapeutic properties used by the tribal people, there is a need to take up the phytochemical and pharmacological investigations.

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