Oral powders formulation

The acute oral LD50 of dalapon for male rats is as high as 9,330 mg/kg, and for female rabbits is 3,860 mg/kg, suggesting that rabbits are more susceptible to the herbicide. The sodium salt of dalapon (in a dry powder formulation) to rabbit eyes produced pain and irritation, followed by severe conjunctivitis and comeal injury, which healed after several days. A 10% solution produced slight pain and conjunctivitis. Repeated or prolonged exposure to dalapon caused irritation to the mucous membrane linings of the mouth, nose, throat, lungs, and eyes. 

Each of the aforementioned techniques is capable of measuring powder that would be used in low-dose, solid oral dosage formulations. The technique must be compatible with the drug substance, and must be capable of producing the information that is needed. For example, if the particle size distribution is needed to ensure dose content uniformity, photon correlation spectroscopy can only provide an average particle size. In this instance, laser diffraction or image analysis would be more suitable techniques. Table 13.1 contains a comparison of the techniques that have been discussed. 

Some sterile powder formulations (these are predominantly, but not exclusively, antibiotics) may require sampling, mixing, milling, and subdivision activities similar to those found in oral powder manufacturing. The facilities and equipment utilized for these products is substantially different from that used for liquids, and the production area bears little resemblance to that utilized for liquids. These materials are received sterile and must be processed through sterilized equipment specifically intended for powder handling in a fully aseptic environment with ISO 5 protection over all open container activities. 

Powdered cellulose is widely used in oral pharmaceutical formulations and food products and is generally regarded as a nontoxic and nonirritant material. 

Poly(methylvinyl ether/maleic anhydride) and copolymers are widely used in a diverse range of topical and oral pharmaceutical formulations. These copolymers are generally regarded as nontoxic and nonirritant. Moreover, the dry powders and aqueous solutions are nonirritating with the exception of ES, MS, and A grades, which are irritating to the eye and may cause tissue damage. 

Oral paste and powder formulations of trimethoprim/sulfadiazine are approved for use in horses. An injectable suspension of trimethoprim/sulfadiazine (48%) is available for i.v. or i.m. administration to horses. Injections must be administered slowly i.v. to avoid collapse and i.m. 

Many oral solutions are intended for pediatric administration, of which oral solution formulations are a subset of a larger choice of formulation type such as suspension, syrup, powder or microcapsules for constitution to a suspension, powder for reconstitution to a solution or suspension, solid particles (powder, coated particles, extended release, enteric-coated granules, beads) in packets or capsules to be sprinkled on food, oral powders, and chewable tablets. The broader topic of pediatric formulation development is beyond the scope of this chapter, but this chapter will cover selected oral solutions for pediatric administration. 

Peak concentrations of didanosine are seen approximately 1 hour after oral administration of the chewable tablets or powder formulations and 2 hours after delayed-release capsules. The plasma elimination half-life of the parent drug is approximately 1.5 hours, but the estimated intracellular half-life of dideoxyadenosine 5 -triphosphate is substantially longer, 25 to 40 hours. As a result, didanosine can be administered once daily. Didanosine is excreted by both glomerular filtration and tubular secretion, and does not undergo metabolism to a significant degree. Drag doses therefore must be adjusted in patients with renal insnfficiency or renal failure. 

Didanosine is acid labile. To increase its absorption, some didanosine preparations (e.g. buffered tablets) have been formulated with antaeids. Additional concurrent antacids would not be expeeted to have any further clinically relevant effect on didanosine pharmaeokineties, although the US manufacturers of the oral powder for solution suggest that additional antacids may increase the adverse effects of the eomponents of this preparation (presumably both the antacid and didanosine components). 

Enhanced water solubility of dried products, which could foster the powder formulation process, as well as enhance oral assimilation of nutraceutical and pharmaceutical powdery products... 

Cachet Capsule Herbal tea Powder Formulation Preparation Solid dosage form Tablet Content uniformity Excipients Adapting oral dosage forms... 

The design of the formulation of capsules and oral powders and that of tablets are similar in some respects, but there are also some important differences. In this section, the general aspects of formulation design are discussed. 

Methadone is a potent synthetic opioid analgesic, structurally unrelated to any of the opium-derived alkaloids. It is a highly lipophilic, basic drug (pKa 9.2) available as a hydrochloride powder formulation that can be reconstituted for oral, rectal, or parenteral administration. Methadone was developed in Germany in 1942 as a synthetic substitute for morphine, and has been approved and widely employed for opioid detoxification maintenance as well as acute and chronic pain management. 

Zegerid is a combination product containing omeprazole 20 or 40 mg with sodium bicarbonate in immediate-release oral capsules and powder for oral suspension. It should be taken on an empty stomach at least 1 hour before a meal. Zegerid offers an alternative to the delayed-release capsules or the IV formulation in adult patients with nasogastric tubes. 

Preparation and administration of orai suspension - Take on an empty stomach 1 hour before a meal. The powder for oral suspension is supplied as unit-dose packets containing an immediate-release formulation of omeprazole. 

Proquin XR Proquin XR and other oral formulations of ciprofloxacin are not interchangeable. Proquin XR should be administered orally once daily for 3 days with a main meal of the day, preferably the evening meal. Proquin XR should be administered at least 4 hours before or 2 hours after antacids containing magnesium or aluminum, sucralfate, Videx (didanosine) chewable/buffered tablets or pediatric powder, metal cations such as iron, and multivitamin preparations containing zinc. Pragy/n XR tablets should be taken whole and never split, crushed, or chewed. 

Didanosine EC (Videx EC) - Didanosine EC has not been studied in pediatric patients. Please consult the complete prescribing information for didanosine buffered formulation and pediatric powder for oral solution for dosage and administration of didanosine to pediatric patients. 

The use of enzymes as digestive aids is only applied under specific medical circumstances. Some medical conditions (e.g. cystic fibrosis) can result in compromised digestive function due to insufficient production/secretion of endogenous digestive enzymes. Digestive enzyme preparations are often formulated in powder (particularly tablet) form, and are recommended to be taken orally immediately prior to or during meals. As the product never enters the blood... 

Amoxicillin is a close analogue to ampicillin that is also inactivated by -lactamases. The action and uses of amoxicillin are like those of ampicillin. Hence it is used against a wide variety of bacterial infections in farm animals including those of the gastrointestinal, respiratory, urinary, and mammary system. It is administered in the form of tablets, suspensions, powders, parenteral, and intramammary formulations at dosage rates of 10 mg/kg bw by the oral route and 7-15 mg/kg bw by the parenteral route. 

Residue depletion studies in cattle, swine, sheep, chickens, and turkeys given oral forms of oxytetracycline including feed premixes, soluble powders, and tablets showed that residues in all edible tissues, with the exception of kidney, were cleared of detectable amounts of oxytetracycline within 5 days postdose. Injectable forms of oxytetracycline yielded higher residue levels that persisted longer than the oral forms, while long-acting formulations of oxytetracycline required extended withdrawal periods (234). 

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