Theophylline is a bronchodilator used in the treatment of asthma, it has a low molecular weight of 180.2. It is slightly acidic, when in a saturated solution of water and has a pKa of 8.81.
2. What are the implications of using the hydrate rather than the anhydrous form of theophylline (i) in formulation (manufacture of the tablet) and (ii) in biopharmaceutics (dissolution)? 20%
I. Manufacturing theophylline formulations come with challenges for both the anhydrous and hydrate. For the anhydrous form, a study showed that the wet granulation of theophylline anhydrous in conjunction with microcrystalline cellulose, led to the formation of the monohydrate form of the drug. This is significant because the monohydrate has slower dissolution than the anhydrous form of theophylline. Thus the method of manufacture is highly important as the study showed directly compressed pellets had better dissolution profiles. Also it shows the importance of the choice of excipients as pellets manufactured via wet granulation in the absence of microcrystalline cellulose showed similar release to that of directly anhydrous theophylline.
Theophylline monohydrate has a tendency to dehydrate during the drying process, it can do so at fairly cool temperatures of around 60⁰C. So this makes temperature an important factor in the manufacture of monohydrate as phase transition can occur.
II. A study conducted in 1992 found
The product was then suspended in 2 ml of water with a stir rod in a 50 ml Erlenmeyer flask and heated to boiling. Water was added in one milliliter increments until all the product was dissolved (18 ml added total). The saturated solution was allowed to slowly cool, and gradual white crystal formation was observed. Recrystallized product was collected once more by suction filtration with the Hirsch funnel once crystallization ceased. Collected product dried on a watch glass for a week, weighed 0.14 g (1.2 mmol), and the melting point was 139°-141°
According to an journal publication on the benefits of Theophylline “It is now apparent that patients taking theophylline may enjoy clinically important benefits in terms of functional status and quality of life, beyond simple bronchodiolation, as a result of theophylline's impact
This report concerns the acid-catalyzed hydration of norbornene to produce exo-norborneol. Such hydration reactions of alkenes typically occur under acidic conditions so that a strong enough electrophile is available in solution for the nucleophilic double bond on the alkene to successfully attack it. This is to say, that if this reaction is done in water, with the hydrogen as the electrophile, the O-H bond is too strong for the double bond to effectively attack the hydrogen and detach it. If instead H3O+ is available in acidic conditions, the extra proton attached to the molecule is the electrophile; this electrophile is strong enough for the reaction to proceed.
The mixture was transferred to an ice bath to crystallize the product, after which the product was collected by vacuum filtration on a Hirsch funnel, washing the flask with small aliquots of cold xylene and pouring the solution over the crystals, allowing the vacuum to thoroughly dry the product. Additional drying was achieved by transferring the product to filter paper and pressing the crystals to remove any excess moisture. The product was then weighed and a melting point determined. A comparative TLC was run in Hexanes:Ethyl Acetate solvent against maleic anhydride to verify the purity of the
The product was placed in a Craig tube and several drops of hot (100°C) solvent (50% water, 50% methanol, by volume) was added and heated until all of the crystals dissolved. The Craig tube was plugged and set in an Erlenmeyer flask to cool. Crystallization was induced once the mixture was at room temperature by scratching the inner wall of the tube. It was then placed into an ice bath for ten minutes until crystallization was complete. The tube was then
has a bioavailability that is linear until about 3mg at 40%. It then follows a nonlinear
A type of bronchodilator, aminophylline is a type of muscle relaxation medicine that helps lungs and chest circulate oxygen better. It is used to treat and prevent wheezing, restricted breathing and shortness of breath. The medicine is usually prescribed to those with bronchitis, asthma and lung diseases. As this medication requires a prescription, it is very important for a user to follow the instructions prescribed and take only at the times and the amount prescribed by his or her physician. Aminophylline can be in the form of liquid syrup, a pill or a cream. How this drug works is by making the lungs less sensitive to any allergens or foreign substances that may be inhaled, thus causing the muscles to relax in the chest and lungs and opening up the air passages so that breathing can be easier. It also increases the contractions in the diaphragm which aids better breathing patterns.
Based on these considerations, theophylline can be regarded as a useful altern-ative to other anti-inflammatory drugs for the chronic treatment of mild to mod-erate asthma. Theophylline should be used at lower doses to achieve plasmaconcentrations of 5–10 mg•, which will avoid the risk of side-effects.
Hence the present study was aimed to prepare mucoadhesive microspheres of sildenafil citrate using neem gum as bio compatible polymer and which would could prolong the release and enhance bioavailability of the
The hydrate prevention and control strategies may be implemented in isolation or in combination depending on the specific circumstance of the field, especially as it relates to practicability and economics [10] [A6]. The available different methods of hydrate inhibition are described briefly in this section.
Sustained release tablet formulation is a type of modified release system that gives initial release of dose to achieve therapeutic dose and followed by gradual release over an extended period of time. The main mechanism of sustained released systems is by releasing small amount of drug molecules over a period of time. There are three types of sustained release system. The first type is osmotic pump system. In this system, drug is concentrated at the core of tablets and the core is coated with semi-permeable membrane.
In present years, the interest in multiple-layered tablets as an oral controlled release System has increased. Multiple-layered tablets have some advantages Compared to conventional tablets. Commonly used to no chemical Incompatibilities of formulation components by physical separation. Release profiles of drug may depend on combining layers with different release patterns, and by combination of slow-release with immediate-release layers. Conte and Maggi have described an oral controlled-release tablet called Geomatrix, which is based on the
There are many types of vasodilators, but hydralazine will be the focus of this paper. Hydralazine is used to treat high blood pressure. High blood pressure is actually a very common condition but when it is not treated, it can cause damage to the brain, heart, blood vessels, kidneys and other vital organs of the body. Damage to these organs may cause heart disease, a heart attack, heart failure, stroke, kidney failure, loss of vision, and other problems (Hydralazine: MedlinePlus Drug Information. (n.d.). The patient should also be looking to make lifestyle changes and not just rely on only medication. These changes include eating a diet that is low in fat and salt, maintaining a healthy weight, and adding exercise into their daily lives (Hydralazine: MedlinePlus Drug Information. (n.d.).
Niosomes are the novel carrier systems which have the bilayer structure. Niosomes can deliver both hydrophilic and lipophilic drugs. But niosomes are unstable. There will be the aggregation, leakage, storage and stability problems. Proniosomes are the versatile preparations which are stable. These are the dried forms of niosomes. Zidovudine proniosomal gel was prepared of different formulation. The permeation studies were carried using rat abdominal skin. Higher percentage release was achieved using the Span 20 i.e., 97.55%±1.1. Effect of lecithin and effect of non-ionic surfactants was carried out. The higher percent entrapment efficiency was achieved to F1 formulation of about 74.70%. There was no effect of cholesterol concentration. As the lecithin concentration was increased the percent drug release also increase but only at a certain extend. At the certain limit surfactant concentration also increases the drug release. By using the proniosomes as carries the bioavailability of Zidovudine increases to 97%. The proniosomes after hydration was characterized using the light microscopy and scanning electron microscopy. Proniosomes are suitable delivery systems for many of the hydrophilic and lipophilic drugs.
Nowadays, there is an increasing demand on multifunctional excipients that replaces the need and use of multiple excipients. There are two ways that can fulfill this requirement, first, the development of new excipients with new chemical entity that has good properties including stability, flowability, compressibility, etc… and is compatible with other excipients in the formulation and with the Active Pharmaceutical Ingredient (API). The second way is to make new grades of exisiting excipient, or to modify it in a way that meets the needs of development. Excipient modifications can be categorized into chemical and physical modifications. The chemical modification deals with chemical reaction that add,