DISSOLUTION AND SOLUBILITY ENHANCEMENT STRATEGIES: CURRENT and NOVEL PROSPECTIVES

Abstract

The solubility is one of the important parameters to achieve the desired concentration of the drug in the systemic circulation in pharmacological response to be shown. The oral route is the most desirable and preferred method of administering therapeutic agents for their systemic effects, but the poor solubility of the drug is a major challenge for formulation scientist. Close to 40% of orally administered drugs suffer from formulation difficulties related to their water insolubility. Dissolution rate, absorption, distribution, and excretion of a moiety depend upon its solubility characteristics. Although several advantages associated with the oral route, the poorly soluble drugs suffer from slow dissolution and poor bioavailability. Based on solubility, drugs are classified into four classes of the BCS classification. Solubility challenges are faced in ClassII and Class IV of the BCS system this is important because most of the generic and NCE drugs come under class II drugs. The solubility behavior of drugs remains one of the most challenging aspects of formulation development. There are several methods available for solubility and dissolution enhancement of poorly water-soluble drugs. The aim of this clause is to distinguish the techniques of solubilization for the acquisition of effective absorption and improved bioavailability.

Enhancement of Dissolution Characteristics of Clopidogrel Bisulphate by Proniosomes

“…Enhancement of solubility is of critical concern in improving dissolution rate and bioavailability. Recently, different nanotechnology techniques have been used to increase the dissolution rate and bioavailability of many drugs [1,2].…”

Forced Degradation Study of Statins: A Review

“…There are several methods available to improve solubility, dissolution, and also bioavailability of drugs with poor solubility in water such as physical and chemical modifications, carrier system, micronization, etc. [10]. Formulation simvastatin nanoparticles with single emulsion diffusion method produce 50 % dose reduction without affecting its efficacy [11].…”

Formulation and Evaluation of Liquisolid Compacts of Lornoxicam

“…Finally, 5% w/w of crospovidone as a super disintegrant and 3% w/w PVP K-30 as a binder were added in the above powder blend. Table 1 denotes the key formulation characteristics of lornoxicam liquisolid compacts with different drug concentration and different excipient ratio respectively [8].…”