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Excipient selection for sustained release formulations

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Sustained - release (SR) matrices are designed to release a drug slowly over an extended period of time. Formulations must be robust to ensure drug release over time and avoid dose-dumping. Innovator companies consider sustained-release oral dosage forms as a means to maximize drug efficacy, minimize the potential for adverse events, address clinical considerations such as dosing frequency, and respond to patient preference for simplified medication regimens for chronic disease. Key growth drivers in the rapidly expanding sector of sustained-release oral drug delivery include selection of excipients, enabling technologies, trends in patient preference and increasing physician comfort with the ability of prolonged drug release to deliver reliable blood levels. Excipients play a central role in the drug development process, in the formulation of sustained- release oral dosage forms and in their administration. The intended function of an excipient is to guarantee the required physico...

Capsule in capsule technology

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Capsule-in-capsule supplements are manufactured using specialty liquid-filled hard-capsule technology (LFHC). The capsule-in-capsule form allows for better release profiles that more precisely meet a customer’s target release. With liquid-filled hard-capsule technology, you have the option of immediate, extended, pulsed, or delayed release, unlike that of other forms. This allows for delivery of supplement or OTC compounds to two different regions of the GI tract, and even delivery to the colon with the addition of enteric coatings. This single oral dosage delivery system, which involves inserting a smaller pre-filled capsule containing either a liquid or semi-liquid formulation   into a larger liquid-filled capsule, offers numerous possibilities and a broad range of formulation and design options. New compounds in the pharmaceutical pipeline are increasingly complex and typically requires enabling technologies to address challenges such as solubility, permeability, stability,...

Proton Pump Inhibitors (PPI), H2 Blockers and antacids: A review

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  Medications for acid reflux, heartburn, and GERD (gastroesophageal reflux disease) come in three types: H2 blockers, proton pump inhibitors (PPIs), and antacids. They all work differently and are geared towards either prevention or quick relief. H2 blockers and proton pump inhibitors work better than antacids, but if you need something for very quick relief, antacids are an option. Antacids don’t do anything to prevent GERD (gastroesophageal reflux disease), but they can be used on demand for symptom relief. They are cheap and available over the counter.H2 blockers (histamine blockers) block one of the first stimuli for  acid production.  PPIs block the final step in the pathway of  acid secretion  in the stomach. In other words, the acid which has been produced (which may be reduced due to an H2 blocker) is prevented from arriving in the stomach. Of the three classes, antacids are the fastest acting. They start providing relief to the patient within five...

Solubility Enhancement Excipient

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  Introduction: Poorly soluble drugs are a major issue for the pharmaceutical industry. By using solubility enhancement excipients pharmaceutical formulators can increase the bioavailability of the API. Advanced solubility enhancement excipients can help companies bring products to market faster. Nowadays most of the drug substances are coming into the innovation pipeline with poor water solubility. Here, the influence of excipients will play a significant role to improve the dissolution of poorly aqueous soluble compounds. The drug substance needs to be dissolved in gastric fluids to get the better absorption and bioavailability of an orally administered drug. Dissolution is the rate-controlling stage for drugs which controls the rate and degree of absorption. Usually, poorly soluble oral administrated drugs show a slower dissolution rate, inconsistent and incomplete absorption which can lead to lower bioavailability. The low aqueous solubility of BCS class II and IV drugs is a ma...

Sustained Release Drug Delivery System: A Review

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Introduction: Presently pharmaceutical industries are focusing on development of sustained release formulations due to its inherent boons. Sustained release dosage forms are designed to release a drug at a predetermined rate by maintaining a constant drug level for a specific period of time. The basic rationale of sustained release drug delivery system optimizes the biopharmaceutical, pharmacokinetic and pharmacodynamics properties of a drug in such a way that its utility is maximized, side-effects are reduced and cure of the disease is achieved. Sustained release (SR) preparations are not new but several new modifications are being introduced. Rising number of patent expirations and soaring need for pediatric and geriatric dosage forms are providing a boost to the growth of the market. Growing awareness regarding added benefits provided by sustained release formulations is also stimulating the growth of the market.   SR has received most of the attention because of the fact that...