Compounding capsules

Flavor characterization Flavor compounding Flavor enhancer Flavor-filled capsules Flavoring agent Flavoring agents... 

The encapsulation of herbicides has received much attention. Encapsulated alachlor is a high volume herbicide product generally sold as a Hquid formulation, although a dry granule version is also available. The capsules, produced by interfacial polymeri2ation (11), are reported to be spherical with a diameter of 2—15 p.m (75). Two thiocarbamate herbicides, EPTC and vemolate [1929-77-7], were encapsulated by interfacial polymeri2ation because they are volatile compounds. When appHed in unencapsulated form, they must be incorporated in the soil within two hours in order to provide effective weed control. When appHed as a microencapsulated formulation, the rate of volatili2ation is lower and soil incorporation can be delayed 24 hours (76). 

Several compounds such as BaZrS [12026-44-7], SrZrS [12143-75-8], and CaZrS [59087-48-8], have been made by reacting carbon disulfide with the corresponding zirconate at high temperature (141), whereas PbZrS [12510-11-1] was produced from the elements zirconium and sulfur plus lead sulfide sealed in a platinum capsule which was then pressurized and heated (142). Lithium zirconium disulfide [55964-34-6], LiZrS2, was also synthesized. Zirconium disulfide forms organometaUic intercalations with a series of low ionization (<6.2 eV)-sandwich compounds with parallel rings (143). 

Nitrite compounds are often known as poppers because of the popping noise produced when the capsules containing them are crushed between the fingers. Both amyl nitrite and butyl nitrite are yellowish liquids that evaporate at room temperature. These compounds are distributed under variety of names and are contained in a range of products, such as air fresheners. Iso-amyl nitrite is also available in the United States by prescription. Currently, the primary indication for isoamyl nitrite is for the treatment of cyanide poi-... 

Muramyl dipeptide derivatives have also been microencapsulated in lactide/glycolide copolymers for use alone as an immuno potentiator. L-lactide/glycolide copolymers were used to deliver MDP-B30, a lipophilic compound, from very small microspheres (less than 5 pm in diameter). The amount of MDP-B30 required for tumor growth inhibitory activity of mouse peritoneal macrophages was 2000 times less for the controlled release MDP-B30 microspheres than for the unen-capsulated drug (134). 

The sacrificial core approach entails depositing a coating on the surface of particles by either the controlled surface precipitation of inorganic molecular precursors from solution or by direct surface reactions [2,3,5,6,8,9,33-35,38], followed by removal of the core by thermal or chemical means. Using this approach, micron-size hollow capsules of yttrium compounds [2], silica spheres [38], and monodisperse hollow silica nanoparticles [3,35] have been generated. 

Plasma levels of diisopropyl methylphosphonate were measured in a single lactating Jersey cow after the sixth day of diisopropyl methylphosphonate oral administration (10 mg/kg/day) by gelatin capsule (Ivie 1980). For the first 5 days the cow was given unlabeled compound and fed hay ad libitum. The diisopropyl methylphosphonate administered on the 6th day was labeled with carbon 14. Based on measurements of label in the plasma, absorption in the cow paralleled that in rats and dogs, with the highest concentration detected in the plasma at 2 hours after administration. 

The study of diisopropyl methylphosphonate distribution in a lactating Jersey cow was the only study that used multiple doses of diisopropyl methylphosphonate (Ivie 1980). In this single cow, radioactivity was detected in the blood 2 hours after dosing with [14C]-radiolabeled compound but not in the tissues. The animal had received diisopropyl methylphosphonate in one gelatin capsule for 5 days before the radiolabeled dose was administered. If tissue uptake in the cow was similar to that in dogs, measurements made 2 hours after dosing may not have provided an opportunity to measure tissue uptake of label. After 24 hours, 0.1% of the administered label was found in the cow s milk (Ivie 1980). 

The development of the first effective analgesic drug, opium, was almost certainly adventitious, and occurred in prehistoric times. The use of the dried exudate from slitting the immature capsule of the opium poppy, Papaver somniferum, as an analgesic, sedative and euphoriant, has a long folkloric history. Isolation of the principal active component morphine (1) as a pure crystalline compound represented one of the early landmarks in organic chemistry. 

Provide either in vitro or in vivo assay results for representative compounds, describe how the in vitro or in vivo assay protocol is performed, and describe how and why the test results demonstrate that the tested compounds exhibit a useful pharmaceutical property. Ideally, provide and link in vitro assay results to in vivo assay results that in turn demonstrate that the claimed compounds can be used to treat or prevent a disease. Describe how to administer the application s compounds and intended administration recipients (e.g., humans), including dosage amounts and dosage forms (e.g., pills, tablets, capsules), possible ways of administering the dosage... 

Capsules are of two types hard and soft gelatin capsules. The present chapter will focus on the extemporaneous filling of hard gelatin capsules. Generally, the soft gelatin capsules are not compounded extemporaneously. Therefore, they are not discussed in this chapter. 

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