Quantitative Evaluation of Effects of Drugs Concentrations and Densities on their Displacement Factors in Suppository Bases (original) (raw)
Related papers
The Pharma Innovation Journal, 2017
Paracetamol is available in various strengths as rectal suppositories, hence the need to evaluate the effects of drug-base ratio as a formulation variable on the physical and release properties of paracetamol suppositories formulated with a lipophilic base. Suppositories, each containing 60 mg to 500 mg of paracetamol in cocoa butter were prepared by fusion method using 1 g and 2 g capacity moulds. Physical and dissolution properties of the suppositories were determined by established methods. Quantitative effects of the drug-base ratio on physical and release properties of the suppositories were analysed using 2 factorial experimental designs. The independent and interaction coefficients of the two variables deviated from zero, indicating significant effects on the physical and release properties of the suppositories. While First-order release kinetics was observed for all the formulations, there was a significant change in the release rate constants with variation in the drug-base...
International Journal of Pharmaceutical Sciences, 2024
Suppositories are pharmaceutical dosage forms that hold a crucial place in the realm of drug delivery. Suppositories are the dosage form inserted into body cavity, mainly rectum and vagina to deliver the drug into the systemic circulation. Suppositories can be taken by patients who are unable to take medicine orally due to nausea and vomiting, and neurological disorder. Suppositories are used over other dosage form because it comes in different shapes and sizes. Suppositories are one of the very feasible modes of administration for medication. It can be prepared by using various bases like cocoa butter, PEG, and fatty base as main ingredients. It can be prepared by using hand rolling, compression molding, fusion molding, and automatic Mold method. Evaluation tests like Uniformity of weight, Content Uniformity test, Melting point determination test, General appearance test, Assay of active contents, Liquefaction time, Breaking test, Disintegration test, Dissolution test.
Effects of surfactant characteristics on drug availability from suppositories
Die Pharmazie, 2008
The addition of surfactants to suppository formulations is referred to in the scientific literature, but their effects on drug availability remain uncertain. Surfactants are reported to improve drug dispersion into hard fatty excipients, to increase the spreading of the melted suppository on the rectal mucosa leading to a greater contact surface, to reduce the viscosity of the molten mass and to reduce the pathway of drug particles to the interface. In the present study a systematic investigation based on tensiometric and rheological methods was carried out to evaluate the effects of nonionic surfactants with different HLBs (hydrophilic-lipophilic-balance) on drug availability and to clarify the possible mechanisms involved in the release process. The relationship between the melted suppositories and a membrane simulating the rectal barrier were investigated in the course of the in vitro release test by measuring their energy characteristics. At the same time, the potential influenc...
Tropical Journal of Natural Product Research, 2019
The World Health Organization (WHO) has recognized the use of rectal preparations for certain indications in children as an alternative to parenteral. However, challenges of stability in tropical countries have limited its application. Furthermore, adverse effects arise in the use of some excipients in infants and neonates. In this study, paediatric paracetamol suppositories using two plant-derived fats-shea butter and dika fat-and their combination as suppository bases in comparison with cocoa butter were formulated. Shea butter and dika fat were purified and characterised using acid, iodine and saponification values, refractive index and relative density. Paracetamol suppositories were formulated by fusion method and evaluated using appearance, weight uniformity, melting point range, solidification point, crushing strength, disintegration time and dissolution test. Physicochemical properties showed shea butter and dika fat as stable with minimal susceptibility to oxidation with melting point ranges of 32-35C and 37-39C respectively. Base mixtures yielded melting point ranges of 32-39C. The suppositories had crushing strengths 31 N and disintegration times ranged between 3-21 min. Paracetamol release from the single bases ranked cocoa butter >dika fat > shea butter. Paediatric paracetamol suppositories using these plant-derived fats compared well with cocoa butter. Paracetamol suppositories with mixtures of either shea butter or dika fat with cocoa butter had superior release properties compared to cocoa butter alone. Thus, could serve as an alternative to cocoa butter in the formulation of suppositories.
The objective of the current study was to explore the use of different suppository bases i.e. Cocoa butter and different grades of polyethylene glycol bases (4000 and 6000) and to observe the effect of plasticizers incorporated in the suppositories for the successful delivery of Zaltoprofen, an novel non steroidal anti inflammatory drug through rectal route of administration. Moreover, Zaltoprofen has tendency to cause gastric ulcer making it necessary to explore safer routes of its administration. Fusion method was used for the preparation of suppositories, which were further evaluated for their visual characteristics, physicochemical properties like dimensions, weight variation, liquefaction time, melting time, disintegration time, drug content and in-vitro release characteristics. Suppositories of PEG 4000 showed best drug release in vitro than other bases. Addition of plasticizer (PEG 400) at 30% concentration reduces the dissolution time in both grades of PEG suppositories.
Layered excipient suppositories: The possibility of modulating drug availability
International Journal of Pharmaceutics, 1997
The release rate of a drug dose from suppositories is affected by characteristics of the excipient (melting temperature and rate, viscosity at rectal temperature, hydro-lipophilic characteristics). Release kinetics from excipients commonly available do not always respond to clinical requirements, even after the introduction of auxiliary agents. Release curves which were differentiated and adaptable to therapeutic conditions were obtained by vehicling a drug in suppositories of two superimposed layers of lipophilic excipients with different characteristics and hence with a difference in drug availability. The two distinct excipient layers release the drug from these suppositories contemporaneously but independently. The amount of drug released in the time course is the sum of the single amounts individually released by the two suppository layers. By previously mixing the two excipients, release rate becomes uniform in the suppository body overall and is conditioned only by the assumed characteristics of the mixture. The release mechanism for superimposed layer suppositories is confirmed by the good agreement between experimental and calculated curves. By using a pair of excipients with different characteristics in superimposed layers between which the drug is distributed, it is possible to modulate drug release kinetics by regulating the reciprocal ratio between the two suppository fractions. © 1997 Elsevier Science B.V.
Formulation and Evaluation of Ibuprofen Suppositories
International Research Journal of Pharmacy, 2016
In this work suppositories containing Ibuprofen were prepared using water soluble bases (hydrous PEG and anhydrous PEG) and oil soluble bases (Suppocire AML, cacao butter, Witepsol E-75, Witepsol H-15, Novata DE-75, Suppocire AM, and Cacao butter). The prepared suppositories were evaluated for the parameters: weight variation, hardness, melting point, disintegration, melting point and drug content. In vitro drug release study was performed using USP type I apparatus in Sorensen's phosphate buffer pH 7.4 as dissolution media. Results showed that suppositories prepared using water soluble bases were within permissible range of all physical parameters. In vitro drug release from water soluble was greater than that from oil soluble bases. Suppocire AML, Cacao butter, Witepsol E-75 and Witepsol H-15 bases showed the highest values for the released ibuprofen among the tested bases. The lowest amount of drug released was observed with Novata DE-75 base. The study showed that the quality of suppositories is controlled by the type of base used.
The individual and interaction effects of type or nature of suppository base (N), concentration of surfactant (C), and storage (S) on the mechanical and release properties of chloroquine phosphate suppositories have been studied using a 2 3 factorial experimental design. Suppositories (1g) containing 100mg chloroquine phosphate each with or without 2%w/v Tween 20 as adjuvant, were prepared in Suppocire® AS2 and Witepsol® H15 bases. The mechanical properties of the suppositories were determined using crushing strength and dissolution properties were assessed using dissolution times (t 50 and t 80 -time for 50% and 80% drug release), and rates. The concentration of surfactant had the highest individual effect on the release properties of the suppository formulations while storage had the lowest effects. Thus, the type of suppository base and concentration of surfactant used in suppository formulations need to be carefully chosen in order to obtain suppositories of desired mechanical and drug release properties.
Evaluation of an acetic acid ester of monoglyceride as a suppository base with unique properties
AAPS PharmSciTech, 2001
The objective of this investigation was to evaluate an acetic acid ester of monoglycerides made from edible, fully hydrogenated palm oil (AC-70) as a suppository base and compare it with a commercially available semisynthetic base (Suppocire AI®). Benzocaine and miconazole were used as model drugs. Suppositories were prepared by the fusion method. The drug loads in the suppositories were kept at 2% to 5% (wt/wt). In vitro release of drug from the suppositories into Sorensen's phosphate buffer (pH 7.4) was studied using a US Pharmacopeia dissolution apparatus 1 and a spectrophotometer. The melting behavior of the bases and the physical state of the drug in the suppositories were studied using a differential scanning calorimeter (DSC). Powder x-ray diffractometry was used to study any possible polymorphic changes in the AC-70 base during formulation and storage. In vitro release studies revealed that the release of benzocaine from the AC-70 suppository was substantially slower than that of the commercial AI base. At a 2.5% (wt/wt) benzocaine load, the release of drug from the AC-70 suppositories was found to be linear. This slow and linear release was attributed to the physical property of the base, which forms liquid crystalline phases in the aqueous dissolution medium. The lyotropic liquid crystalline phase has the ability to incorporate drug into its structure and can control the release kinetics of the drug from such a system. The apparent pH of the release medium (water) was decreased by 1 to 1.5 pH units when the AC-70 base was used. The DSC studies revealed that the melting range of the AC-70 base is 36°C to 38°C, which is ideal for suppository formulations. The results of these studies support the possibility of using this new base for slow-release suppository formulations. This base may be of particular interest for a drug that requires an acidic environment to maintain its activity.
International Journal of Research in Pharmaceutical Sciences, 2020
The objective of this work is to (i) study the effect of variations in the proportions of four Macrogols on the pharmaco-technical characteristics of suppositories, (ii) de ine the optimal formula for a suppository with immediate effect; maximum disintegration and a minimum of hardness as de ined in the European Pharmacopoeia. The lattice design mixture has been proposed as an optimization technique, the formulation factors are presented by the proportions of PEG 400 (X1), PEG 600 (X2), PEG 4000 (X3) and PEG 6000 (X4) and the response variables are (i) the disintegration time (Y1) (ii) the hardness (Y2). The second-degree empirical model was postulated to model the variations of the two response variables using the least-squares method. The selected model explained about 67% and 84% of the variation for Y1 and Y2, respectively. All four factors had signi icant effects on the properties of the suppository. Interactions negatively affected both responses. The numerical desirability method gave the following optimal formula: PEG400 (28.71334 %); PEG600 (24.23773%), PEG4000 (35.00944%) and PEG6000 (12.03949%) for a disintegration of 25.839 (+/-2.3) min and hardness =2147.321 (+/-50) g.