Drug substances moisture sensitivity

Is the Drug Substance Moisture-Sensitive A moisture-sensitive compound can be degraded when exposed to moisture during the manufacturing process. In this case, do not select high-shear or low-shear wet granulation since the... 

The storage conditions and the length of the studies should be sufficient to cover storage, shipment, and subsequent use. Both drug substances and products should be evaluated under storage conditions that test for thermal stability (temperature effect) and moisture sensitivity (humidity tolerance). 

The drum provides protection from light and mechanical strength to protect the liner during shipment and handling. The majority of the protection from air and moisture is provided by the liner. Because LDPE is not a particularly good moisture barrier, a drug substance that is moisture sensitive may need additional protection. An alternative to a LDPE bag is a heat-sealable laminate bag with a comparatively low rate of water vapor transmission. 

Some excipients contain a certain amount of amorphous form such as spray-dried lactose,27 and others are hygroscopic, such as microcrystalline cellulose.28 These excipients will adsorb water, which causes a change in the micro-environment of the formulation. If the drug substance is moisture-sensitive, degradation may occur quickly. Therefore, consider both drug-excipient compatibility and excipient impurity profile in selecting excipients for low-dose drug products. 

If a drug substance is not moisture-sensitive and the dose strength ranges between 50 xg and 0.5 mg, consider wet granulation, fluid bed granulation, or multiparticulates by beads coating. The literature contains many successful examples.39 4... 

Fig. 15 Stability screening. Example of DSC purity results obtained for a drug substance sensitive to moisture. From the top to the bottom Initial sample (purity 99.9%), sample stored under humid conditions at 50°C (purity 99.7%), sample stored under humid conditions at 80°C (purity 99.1%).

Drug substance and carrier can be both in the glassy state. Total miscibility, partial miscibility, or total immiscibility has been observed. This type of system is very sensitive to temperature and moisture... 

The hygroscopicity of crospovidone (see Section 3.2.3.2) can be used to adsorb water in preparations that contain moisture-sensitive drugs, to improve their stability. It almost certainly also contributes to the efficacy of micronized/fine powder crospovidone as an active substance in the treatment of diarrhoea. 

Uses Pharmaceutical excipient, film-former for enteric coating of solid oral dosage forms, esp. for controlled release of drugs masks unpleasant tastes and odors barrier between incompat. active substances moisture barrier protecting against atmospheric humidity Features Effective barrier to gastric juice protects acid-sensitive drugs releases active at site of action... 

Dry compaction technique like roller compaction is experiencing renewed interest in the industry. There are a number of drug substances which are moisture sensitive and cannot be directly compressed. The roller compaction provides suitable alternative technology for processing these products. 

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